Note: Descriptions are shown in the official language in which they were submitted.
_
ANAEROBIC ANTIOXIDANT COMPOSITION
TECHNICAL FIELD
[0001] The disclosure relates generally to antioxidant compositions
and particularly relates
to anaerobic antioxidant compositions for improving free radical levels in a
user.
BACKGROUND
[0002] The disclosure relates to compositions, methods, and systems
for improving free
radical levels in a user and for the treatment of oxidative stress in a user.
Oxidative stress is
responsible for numerous conditions and diseases and can cause extensive
damage to cells,
proteins, and DNA (Deoxyribonucleic Acid). The compositions, methods, and
systems disclosed
herein mitigate oxidative stress and lower the levels of dangerous free
radicals in a body.
[0003] Bodies are constantly under attack from oxidative stress.
Oxygen molecules include
two oxygen atoms that are bonded together with a covalent bond. These two
bonded oxygen
atoms can split into two separate oxygen atoms that each have one unpaired
electron. Unpaired
electrons are very unstable and will immediately seek out other unpaired
electrons to form a
stable pair of electrons. These unpaired electrons are referred to as "free
radicals" and can be
responsible for causing extensive damage to a body. When oxygen atoms have a
free radical, i.e.
an unpaired electron, the oxygen atom can cause oxidative stress in a body.
[0004] Free radicals are associated with numerous human diseases,
including cancer,
atherosclerosis, Alzheimer's disease, Parkinson's disease, and many others.
Free radicals have a
link to aging symptoms, and in fact aging has been defined as a gradual
accumulation of free-
radical damage. Substances that generate free radicals can be found in food,
medicines, water,
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and air. Some substances that are known for having high quantities of free
radicals include fried
foods, alcohol, tobacco, pesticides, and air pollutants. Additionally, free
radicals are the natural
byproducts of chemical processes that take place in the body. Thus, the
accumulation of free
radicals in inevitable and it is important to mitigate the damage caused by
free radicals and
oxidative stress.
[0005] When a free radical is formed, a chain reaction can occur that can
lead to broken cell
membranes which can then alter what enters and exits a cell. The chain
reaction may change the
structure of a lipid, protein, or DNA strand. The damaged cells can mutate and
turn into
cancerous cells. The cascading damage initiated by a free radical can change
DNA code that is
then replicated by the body with the incorrect DNA sequence. Because free
radicals can cause
extensive damage to a body, it is desirable to reduce free radical levels in a
body and thereby
mitigate the damage caused by free radicals.
[0006] Oxidative stress occurs where there are too many free radicals and
too much cellular
damage caused by free radicals. Oxidative stress is associated with damage of
proteins, lipids,
and nucleic acids. Oxidative stress can play a role in the development of
numerous conditions,
including macular degeneration, cardiovascular disease, certain cancers,
emphysema,
alcoholism, Alzheimer's disease, Parkinson's disease, ulcers, inflammatory
diseases, arthritis,
lupus, and others. Some symptoms of oxidative stress include fatigue,
headaches, noise
sensitivity, memory loss and brain fog, muscle and joint pain, wrinkles,
vision trouble, and
decreased immunity. It is therefore desirable to reduce or eliminate oxidative
stress in a body.
[0007] In light of the foregoing, the disclosure provides compositions,
methods, and systems
for improving free radical levels in a body and for treating oxidative stress.
The compositions,
methods, and systems of the disclosure are also applicable in the treatment
and support of the
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body's natural detoxification process and/or the treatment or support of the
body's natural
defense systems for combatting viruses, bacteria, heavy metal toxicity,
radiation, certain
medications, the process of aging, and others.
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..
BRIEF DESCRIPTION OF THE DRAWINGS
[0009] Non-limiting and non-exhaustive implementations of the
disclosure are described
with reference to the following figures, wherein like reference numerals refer
to like parts
throughout the various views unless otherwise specified. Advantages of the
disclosure will
become better understood with respect to the following description and
accompanying drawing
where:
[0010] FIG. 1 illustrates the chemical structure of reduced
glutathione (GSH) according to
one implementation consistent with the teachings and principles of the
disclosure;
[0011] FIG. 2 illustrates the chemical oxidation reaction of reduced
glutathione (GSH) to
oxidized glutathione (GSSG) according to one implementation consistent with
the teachings and
principles of the disclosure;
[0012] FIG. 3 illustrates a structure of a liposome and a lipid
bilayer according to one
implementation consistent with the teachings and principles of the disclosure;
[0013] FIG. 4 illustrates a standard curve for reduced glutathione
resulting from a short-term
analysis of a clinical example consistent with the teachings and principles of
the disclosure;
[0014] FIG. 5 illustrates a standard curve for reduced glutathione
resulting from a long-term
analysis of a clinical example consistent with the teachings and principles of
the disclosure;
[0015] FIG. 6 illustrates concentrations of reduced glutathione
resulting from a short-term
analysis of a clinical example consistent with the teachings and principles of
the disclosure;
[0016] FIG. 7 illustrates concentrations of oxidized glutathione
resulting from a short-term
analysis of a clinical example consistent with the teachings and principles of
the disclosure;
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[0017] FIG. 8 illustrates ratios of reduced glutathione to oxidized
glutathione resulting from
a short-term analysis of a clinical example consistent with the teachings and
principles of the
disclosure;
[0018] FIG. 9 illustrates concentrations of reduced glutathione resulting
from a long-term
analysis of a clinical example consistent with the teachings and principles of
the disclosure;
[0019] FIG. 10 illustrates concentrations of oxidized glutathione resulting
from a long-term
analysis of a clinical example consistent with the teachings and principles of
the disclosure;
[0020] FIG. 11 illustrates ratios of reduced glutathione to oxidized
glutathione resulting
from a long-term analysis of a clinical example consistent with the teachings
and principles of
the disclosure;
[0021] FIG. 12 illustrates ratios of reduced glutathione to oxidized
glutathione resulting
from a long-term analysis versus the baseline analysis of a clinical example
consistent with the
teachings and principles of the disclosure;
[0022] FIG. 13 illustrates a schematic flow chart diagram of a method of
improving free
radical levels in a user consistent with the teachings and principles of the
disclosure; and
[0023] FIG. 14 illustrates a schematic flow chart diagram of a method of
improving free
radical levels in a user consistent with the teachings and principles of the
disclosure.
CA 3041914 2019-04-30
DETAILED DESCRIPTION
[0025] Disclosed herein are compositions, methods, and systems for
improving free radical
levels in a body and/or for alleviating oxidative stress in a body. The
compositions, methods, and
systems disclosed herein can reduce and alleviate the damage caused by free
radicals. An
embodiment of the disclosure is a composition including an antioxidant and a
deoxygenated
water solvent. The composition is such that the antioxidant remains in a
reduced state. The
composition may be microencapsulated and may further be packaged in an airless
container that
is configured to maintain an anaerobic environment. The composition may be
provided for
topical, oral, intravenous, intramuscular administration, and/or inhalant
administration.
[0026] An embodiment of the disclosure is a composition including reduced
glutathione and
a deoxygenated water solvent. The composition is such that the reduced
glutathione remains in
its reduced state and does not oxidize to form a more stable form of
glutathione. The
composition may be microencapsulated in a phospholipid liposomal structure or
some other
microencapsulation structure. The composition may be packaged in an airless
dispenser that is
configured to maintain an anaerobic environment.
[0027] The composition disclosed herein demonstrates unexpectedly good
results for
improving free radical levels in a body, alleviating oxidative stress in a
body, and for treating or
alleviating symptoms of multiple conditions and diseases. The composition
disclosed herein
demonstrates unexpectedly good results for treating burns, including
alleviating pain associated
with burns and for healing burns. The composition disclosed herein
demonstrates unexpectedly
good results for treating shingles and post herpetic neuralgia. The
composition disclosed herein
demonstrates unexpectedly good results for treating Herpes Type 1 and Type 2.
The composition
disclosed herein demonstrates unexpectedly good result for treating tardive
dyskinesia. The
6
CA 3041914 2019-04-30
composition disclosed herein demonstrates unexpectedly good results for
treating or alleviating
symptoms associated with the Epstein Barr Virus.
[0028] Free radicals can cause extensive damage to a body and persistent
free radical
damage can lead to oxidative stress. Free radicals are atoms or molecules that
are highly reactive
with other cellular structures. Free radicals include an unpaired electron
that is highly unstable.
Free radicals are natural byproducts of ongoing biochemical reactions in the
body, including
ordinary metabolic processes and immune system responses. Free radical-
generating substances
can be found in food, drugs, medicines, air, and water. Such substances
include fried foods,
alcohol, tobacco, pesticides, air pollutants, and many more. Free radicals can
cause damage to
parts of cells such as proteins, DNA, and cell membranes by stealing electrons
through a process
referred to as oxidation. The unpaired electron in a free radical is highly
unstable and "steals" an
electron from another molecule to perform a much more stable electron pair.
When free radicals
oxidize important components of a cell, those components lose the ability to
function normally
and the accumulation of such damage can cause a cell to die. Numerous studies
indicate that
increased production of free radicals causes or accelerates nerve cell injury
and leads to disease.
[0029] Antioxidants, also known as "free radical scavengers," are compounds
that either
reduce the formation of free radicals or reach with and neutralize free
radicals. Antioxidants
often work by donating an electron to the free radical before the free radical
can oxidize other
cell components. Once the electrons of the free radical are paired, the free
radical is stabilized
and becomes nontoxic. Therapy aimed at increasing the availability of
antioxidants in cells can
be effective in preventing or slowing the course of diseases.
[0030] The compositions, methods, and systems disclosed herein provide
unexpectedly
effective means for reducing the levels of free radicals in a body. When the
levels of free radicals
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in a body are reduced, oxidative stress and many other conditions can be
treated or alleviated.
The compositions, methods, and systems disclosed herein provide unexpectedly
good results for
maintaining reduced glutathione in a reduced state such that the reduced
glutathione can serve as
an effective scavenger of free radicals.
[0031] The disclosure further extends to the anaerobic manufacture,
packaging, and delivery
of therapeutic amounts of bio-effective reduced glutathione (GSH). In the
following description
of the disclosure, reference is made to the accompanying drawings, which form
a part hereof,
and in which is shown by way of illustration specific implementations in which
the disclosure
may be practiced. It is understood that other implementations may be utilized,
and structural
changes may be made without departing from the scope of the disclosure.
[0032] In describing and claiming the subject matter of the disclosure, the
following
terminology will be used in accordance with the definitions set out below.
[0033] As used herein, the terms "comprising," "including," "containing,"
"characterized
by," and grammatical equivalents thereof are inclusive or open-ended terms
that do not exclude
additional, unrecited elements or method steps.
[0034] As used herein, the phrase "consisting of' and grammatical
equivalents thereof
exclude any element, step, or ingredient not specified in the claim.
[0035] As used herein, the phrase "consisting essentially of' and
grammatical equivalents
thereof limit the scope of a claim to the specified ingredients, materials or
steps and those that do
not materially affect the basic and novel characteristic or characteristics of
the claimed
disclosure.
[0036] As used herein, "effective amount" means an amount of an ingredient
or a
component of the product that is nontoxic, but sufficient to provide the
desired effect and
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performance at a reasonable benefit/risk ratio attending any dietary
supplement or product. For
example, an effective amount of a vitamin or mineral is an amount sufficient
to prevent a
deficiency thereof and to reduce the incidence of some adverse effects.
[0037] Unless defined otherwise, all technical and scientific terms used
herein have the
same meanings as commonly understood by one of ordinary skill in the art to
which this
disclosure pertains and belongs.
[0038] Oxidative stress, or high levels of free radicals in the body, is
responsible for
numerous health issues and is virtually impossible to avoid. Oxidative stress
reflects an
imbalance between the systemic manifestation of reactive oxygen species and
the body's ability
to readily detoxify the reactive intermediates or repair the resulting damage.
Disturbances in the
body's normal redox state of cells can cause toxic effects through the
production of peroxides
and free radicals that damage all components of a cell, including proteins,
lipids, and DNA.
Oxidative stress from oxidative metabolism causes base damage as well as
strand breaks in
DNA. Further, some reactive oxidative species act as cellular messengers in
redox signaling.
Thus, oxidative stress may cause disruptions in the body's normal mechanisms
of cellular
signaling. In humans, oxidative stress is thought to be involved in the
development of attention
deficit hyperactivity disorder, cancer, Parkinson's disease, Lafora disease,
Alzheimer's disease,
atherosclerosis, heart failure, myocardial infarction, fragile X syndrome,
sickle-cell disease, licen
planus, vitiligo, autism, infection, chronic fatigue syndrome, and depression,
among other.
[0039] Chemically, oxidative stress is associated with increased production
of oxidizing
species or a significant decrease in the effectiveness of antioxidant
defenses, such as glutathione.
Reduced glutathione (GSH) is often referred to as the body's master
antioxidant. Glutathione is
composed of three amino acids, including cysteine, glycine, and glutamine, and
glutathione can
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CA 3041914 2019-04-30
_
be found in virtually every cell of the body. The highest concentration of
glutathione is typically
found in the liver where it serves a critical function in the body's natural
detoxification process.
This natural detoxification process is important for treating oxidative stress
in the body and
avoiding the production of damaging peroxides and free radicals.
[0040] Glutathione is an important component of the body's natural
defense system.
Glutathione can be depleted by compositions or processes that are associated
with free-radical
damage, including for example, viruses, bacteria, heavy metal toxicity,
radiation, certain
medications, and the process of aging. The depletion of glutathione is
associated with lower
immune function, increased vulnerability to infection, and a reduction in the
liver's ability to
detoxify the body. As the generation of free radicals exceeds the body's
ability to neutralize and
eliminate them, oxidative stress occurs. A primary function of glutathione is
to alleviate
oxidative stress.
[0041] Reduced glutathione is under tight homeostatic control both
intracellularly and
extracellularly. A dynamic balance is maintained between the synthesis of
reduced glutathione,
its recycling from oxidized glutathione, and its utilization.
[0042] Reduced glutathione is utilized as a cofactor by multiple
peroxidase enzymes to
detoxify peroxides that are generated by oxygen radical attack on biological
molecules. Reduced
glutathione is further utilized as a cofactor by transhydrogenases to reduce
oxidized centers on
DNA, proteins, and other biomolecules. Reduced glutathione is further utilized
as a cofactor by
glutathione S-transferases (hereinafter "GST") to conjugate reduced
glutathione with
endogenous substances (e.g. estrogens), exogenous electrophiles (e.g. arene
oxides, unsaturated
carbonyls, and organic halides), and diverse xenobiotics. Low GST activity may
increase risk for
disease, and paradoxically, some reduced glutathione conjugates can also be
toxic.
CA 3041914 2019-04-30
_
[0043] Reduced glutathione can be depleted by direct attack by free
radicals and other
oxidative agents. The homeostatic glutathione redox cycle attempts to keep
reduced glutathione
repleted as it is being consumed. Amounts available from foods are limited
(less than 150
mg/day), and oxidative depletion can outpace synthesis.
[0044] The liver is the largest reservoir of reduced glutathione.
The parenchymal cells
synthesize reduced glutathione for P450 conjugation and numerous other
metabolic
requirements, then export reduced glutathione as a systemic source of SH-
reducing power.
Reduced glutathione is carried in the bile to the intestinal luminal
compartment. Epithelial tissues
of the kidney tubules, intestinal lining, and lungs have substantial P450
activity and a modest
capacity to export reduced glutathione.
[0045] Equivalents of reduced glutathione circulate in the blood
predominately as cystine
(i.e., the oxidized and more stable form of cysteine.) Cells import cystine
from the blood,
reconvert it to cysteine, and form it to synthesize reduced glutathione.
Conversely, inside the
cell, reduced glutathione assists in re-reducing oxidized forms of other
antioxidants such as
ascorb ate and alpha-tocopherol.
[0046] Reduced glutathione is an important cell protectant; it
directly quenches reactive
hydroxyl free radicals, other oxygen-centered free radicals, and radical
centers on DNA and
other biomolecules. Reduced glutathione is a primary protectant of the skin,
lens, cornea, and
retina against radiation damage and other biochemical foundations of P450
detoxification in the
liver, kidneys, lungs, intestinal, epithelia, and other organs.
[0047] Reduced glutathione is the essential cofactor for many
enzymes that require thiol-
reducing equivalents, and it helps keep redox-sensitive active sites on
enzymes in the necessary
reduced state. Higher-order thiol cell systems, the metallothioneins,
thioredoxins, and other
11
CA 3041914 2019-04-30
redox regulator proteins are ultimately regulated by the levels of reduced
glutathione, and the
ration of reduced glutathione to oxidized glutathione. The balance of reduced
and oxidized
glutathione is crucial to homeostasis in the body, to stabilizing the cellular
biomolecular
spectrum, and to facilitating cellular performance and survival. Reduced
glutathione and its
metabolites interface with energetics and neurotransmitter syntheses through
several prominent
metabolic pathways. Reduced glutathione availability down-regulates the pro-
inflammatory
potential of leukotrienes and other eicosanoids. Recently discovered S-nitroso
metabolites,
generated in vivo from reduced glutathione and nitric oxide (NO), further
diversify the impact of
reduced glutathione on the body's metabolism.
[0048] According to the present disclosure, a reduced glutathione
supplement may be
manufactured in an anaerobic environment using one or more non-reactive gasses
to ensure the
maintenance of the reduced form, rather than the oxidized form, of
glutathione. Additionally, de-
oxygenated water may be used during the manufacturing process and as a carrier
for the
supplement. By using de-oxygenated water, very little of the oxygen is
available in the water to
convert the reduced glutathione to oxidized glutathione.
[0049] In an embodiment of the disclosure, a composition for reducing
oxidative stress
and/or improving free radical levels in a user is disclosed. The composition
includes an effective
amount of reduced glutathione for reducing oxidative stress in the user, and a
deoxygenated
water solvent. In an embodiment, the composition is encapsulated in an aqueous
solution. In an
embodiment, the composition is packaged in an airless dispenser configured to
maintain an
anaerobic environment.
[0050] In a further embodiment of the disclosure, a method of reducing
oxidative stress in a
user is disclosed. The method includes providing a composition to the user,
wherein the
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_
composition comprises an effective amount of reduced glutathione for reducing
oxidative stress
in the user and a deoxygenated water solvent. In an embodiment, the
composition is encapsulated
in a phospholipid liposome structure and the composition is packaged in an
airless dispenser
configured to maintain an anaerobic environment.
[0051] In a further embodiment of the disclosure, a method for
manufacturing a composition
for reducing oxidative stress in a user is disclosed. The method includes
mixing reduced
glutathione powder and deoxygenated water in an anaerobic environment to form
a reduced
glutathione solution. The method includes packaging the reduced glutathione
solution in an
airless dispenser in an anaerobic environment such that the reduced
glutathione is not
substantially exposed to an oxygen source from manufacture to dispensing.
[0052] In an embodiment of the disclosure, reduced glutathione is
dissolved in a
deoxygenated water solvent. The deoxygenated water solvent has had dissolved
oxygen (02)
gasses removed from the water. Various techniques for removing dissolved
oxygen from water
are known in the art, including for example, boiling water at atmospheric
pressure, boiling water
at reduced pressure, purging water with nitrogen gas (N2), and sonication of
the water under
reduced pressure. Additionally, water deoxygenation may be performed by bio
reactive
processes including, for example, yeast-based bio reactive processes. In an
embodiment, highly
pure deoxygenated water is utilized in combination with other components of
the composition
disclosed herein.
[0053] Referring now to the figures, FIG. 1 illustrates the
chemical structure 100 of reduced
glutathione. As illustrated, reduced glutathione comprises glutamic acid 102,
cysteine 104, and
glycine 106. Reduced glutathione (GSH) is a linear tripeptide of L-glutamine,
L-cysteine, and
glycine. Reduced glutathione is technically referred to as N-L-gamma-glutamyl-
cysteinyl glycine
13
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or L-glutathione. The molecule includes a sulfhydryl (SH) group on the
cysteinyl portion that
accounts for its strong electron-donating character that enables glutathione
to be effective in
reducing oxidative stress in the body. Glutathione is oxidized as an electron
is lost, and two such
molecules (with a lost electron) become linked or dimerized by a disulfide
bridge. The dimerized
molecules form glutathione disulfide or oxidized glutathione (GSSG). The
linkage is reversible
upon re-reduction.
[0054] The synthesis of reduced glutathione includes two closely linked and
enzymatically-
controlled reactions that utilize adenosine triphosphate (ATP). First,
cysteine and glutamate are
combined by gamma-glutamyl cysteinyl synthetase. Second, reduced glutathione
synthetase
combines gamma-glutamylcysteine with glycine to generate reduced glutathione.
As the levels of
reduced glutathione rise, the processes are self-limited against further
production of reduced
glutathione. Otherwise, cysteine availability is usually rate-limiting.
Fasting, protein-energy
malnutrition, and other dietary amino acid deficiencies limit the synthesis of
reduced glutathione.
The recycling of reduced glutathione is catalyzed by glutathione disulfide
reductase, which uses
reducing equivalents from nicotinamide adenine dinucleotide phosphate (NADPH)
to reconvert
oxidized glutathione to glutathione disulfide. The reducing power of ascorbate
helps conserve
systemic reduced glutathione.
[0055] FIG. 2 illustrates the oxidation reaction 200 of reduced glutathione
(GSH) 202 to
oxidized glutathione (GSSG) 208. The reaction 200 produces two electrons and
two protons as
illustrated at 206.
[0056] In an embodiment of the disclosure, a composition is provided to a
user. The
composition includes 99.9% purity reduced glutathione powder. The reduced
glutathione powder
is solubilized in a deoxygenated water solvent and encapsulated in a plant-
based phospholipid
14
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liposome structure. The composition includes an effective amount of stevia,
natural lemon
essential oil, and natural peppermint essential for improving the overall
flavor of the composition
for human oral consumption. In an embodiment, the composition includes from
about 525 mg to
about 575 mg of reduced glutathione per 4 g of solution.
[0057] In an embodiment, the resulting liquid composition is packaged in an
airless
dispenser that is configured to maintain the composition in an anaerobic
environment. As such,
the airless dispenser protects the reduced glutathione from degradation and
conversion to
oxidized glutathione. Applicant recognizes that previous purported supplements
including
reduced glutathione suffer from a sulfur smell due to the strong oxidation of
reduced glutathione.
As such, the airless dispenser extends the effective shelf-life of the reduced
glutathione in the
present disclosure by substantially eliminating contact of the reduced
glutathione with oxygen,
even after first use of the composition. Applicant recognizes that other forms
of packaging and
delivery result in the reduced glutathione making contact with oxygen and thus
rapidly degrading
and oxidizing into oxidized glutathione, even if a successful manufacture of
reduced glutathione
is initially achieved.
[0058] FIG. 3 illustrates a liposome structure 300 for microencapsulation
of the composition
of the disclosure. A composition including reduced glutathione and a
deoxygenated water
solvent may be microencapsulated in a liposome structure 300. In an
embodiment, the reduced
glutathione and deoxygenated water solvent are microencapsulated in a plant-
based phospholipid
liposome.
[0059] The liposome structure 300 includes a lipid bilayer 312. The lipid
bilayer 312 is
formed of two layers of lipids having opposite orientations. A lipid is a
naturally occurring
compound that is insoluble in polar solvents such as water. A lipid is
insoluble in water due to a
CA 3041914 2019-04-30
long hydrophobic hydrocarbon chain. The hydrophobic chain may be saturated or
unsaturated.
Lipids further include a glycerol molecule bonded to the long hydrophobic
hydrocarbon chain.
Depending on the type of lipid, the lipid may further include other molecules
such as a phosphate
group. The lipid bilayer 312 includes a first layer of lipids each having a
first head group 302 and
a first tail group 304. The lipid bilayer 312 includes a second layer of
lipids each having a second
head group 308 and a second tail group 306. As shown in the liposome structure
300 and the
lipid bilayer 312, the first layer of lipids and the second layer of lipids
are oriented in opposite
directions. This orientation of the lipids is promoted by the natural water
insolubility of the long
hydrophobic hydrocarbon chains. When lipids are disposed in water, the lipids
can form the
liposome structure 300 because the long hydrophobic hydrocarbon chains are
insoluble in water
but the head groups are water-soluble. The water-soluble head groups can form
a layer that is
facing an aqueous solution both outside and inside the liposome structure 300.
By contrast, the
long hydrophobic hydrocarbon chains face into the middle of the lipid bilayer
312 and away
from the aqueous solution located outside and inside the liposome structure
300.
[0060] The lipid bilayer 312 in the liposome structure 300 forms a core
310. Other
molecules or substances can be disposed within the core 310 of the liposome
structure 300. In an
embodiment, the composition is disposed within the core 310. The reduced
glutathione and/or
deoxygenated water solvent may be disposed within the core 310 such that the
reduced
glutathione and/or deoxygenated water solvent is microencapsulated by the
liposome structure
300.
[0061] In an embodiment, the composition includes reduced glutathione
present in the
composition from 5% to 20% by weight of the total composition. The composition
further
includes a deoxygenated water solvent. The composition is encapsulated by any
suitable means.
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_
_
The composition may be encapsulated by way of "microencapsulation" with
biopolymers,
polysaccharides, hydrocolloids, or gums, and the composition may specifically
be encapsulated
in a liposome structure. Further, the composition may be encapsulated in a
hard-shelled capsule
and/or a soft-shelled capsule.
[0062] In an embodiment where the composition is encapsulated in a
capsule, the capsule
may be manufactured from an aqueous solution of gelling agents such as animal
protein or plant
polysaccharides or their derivatives such as carrageenans and modified forms
of starch and
cellulose. Other ingredients may be added to the capsules including
plasticizers such as glycerin
or sorbitol to decrease the capsule's hardness. Additionally, ingredients such
as coloring agents,
preservatives, disintegrants, lubricants, and/or surface treatments may be
added. In an
implementation, the composition is encapsulated in a soft-shelled capsule such
as a single-piece
gel encapsulation. A soft-shelled capsule can be an effective delivery system
for oral drugs and
especially for poorly soluble drugs. The soft-shelled capsule may include
liquid ingredients that
increase solubility or permeability of the composition. In an implementation,
the composition is
encapsulated in a hard-shelled capsule such as a two-piece gel encapsulation.
The hard-shelled
capsule can be an effective delivery system for oral drugs and especially for
powdered drugs.
[0063] In an embodiment where the composition is encapsulated by way
of
microencapsulation, the reduced glutathione and/or deoxygenated water solvent
is surrounded by
a coating that promotes a slow release of the reduced glutathione into the
body of the user.
Microencapsulation is a process in which small particles or droplets are
surrounded by a coating
to produce a small capsule. In the present disclosure, microencapsulation may
be employed to
enclose reduced glutathione inside a micrometric wall made of a hard of soft
soluble film. The
microencapsulation of reduced glutathione can promote the slow release of
reduced glutathione
17
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and prevent the degradation of oxidation of the highly unstable reduced
glutathione. A
microcapsule is a small sphere with a uniform or mostly uniform wall around
it, and the wall
may be referred to as a shell, coating, membrane, or capsule. The microcapsule
may have a
diameters between a few micrometers and a few millimeters. The wall of the
microcapsule may
be formed of lipids or polymers. Example coating materials for the wall of the
microcapsule
include ethyl cellulose, polyvinyl alcohol, gelatin, and sodium alginate. In
various embodiments,
the composition is microencapsulated by way of pan coating, centrifugal
extrusion, vibrational
nozzle, spray-drying, ionotropic gelation, coacervation-phase separation,
interfacial
polycondensation, interfacial cross-linking, in situ polymerization, and/or
matrix polymerization.
[0064]
The composition may be microencapsulated with various different materials. The
composition may be microencapsulated with a plant-based material. Some plant-
based
carbohydrate polymers that are suitable for microencapsulation include starch,
polysaccharide,
cellulose, plant exudates such as gum Arabic, um karaya, and mesquite gum, and
plant extracts
such as galactomannans and soluble soybean. Some plant-based proteins that are
suitable for
microencapsulation include gluten and isolates such as pea or soy. Some plant-
based lipids that
are suitable for microencapsulation include fatty acids, alcohols, glycerides,
waxes, and
phospholipids. The composition may be microencapsulated with a marine-based
material. Some
marine-based carbohydrate polymers suitable for microencapsulation include
carrageenan and
alginate. The composition may be microencapsulated with a microbial or animal-
based material.
Some microbial or animal-based carbohydrate polymers that are suitable for
microencapsulation
include xanthan, gellan, dextran, and chitosan. Some microbial or animal-based
proteins that are
suitable for microencapsulation include caseins, whey proteins, and gelatin.
Some microbial or
18
CA 3041914 2019-04-30
_
animal-based lipids that are suitable for microencapsulation include fatty
acids, alcohols,
glycerides, waxes, and phospholipids.
[0065] In an embodiment, the composition is microencapsulated with a
lipid. Lipids exhibit
general insolubility in water and include molecules and substances of large
diversity and
structural variety such as oils, fats, waxes, and phospholipids. The
composition may particularly
be microencapsulated with a phospholipid. Phospholipids include two long chain
fatty acids and
a hydroxyl group. Numerous species of phospholipids are possible by variation
of the different
head groups and fatty acyl substitution at the first and second position of
the glycerol backbone.
Phospholipids may form a liposome structure that encapsulates the reduced
glutathione and/or
deoxygenated water solvent of the present disclosure. The liposome structure
forms an aqueous
interior that is separated by one or more phospholipid bilayers from the
aqueous exterior. The
manufacturing techniques used, and the intensity of mixing employed will
govern the size of the
liposome structure.
[0066] The microencapsulated composition that includes reduced
glutathione and
deoxygenated water solvent shows unexpectedly good results for maintaining
reduced
glutathione in the highly unstable reduced form. When the reduced glutathione
remains reduced,
the reduced glutathione remains effective for scavenging free radicals in the
user's body and
thereby "neutralizing" the free radicals or rendering them non-toxic in the
body. Further, the
microencapsulated composition demonstrates unexpectedly good results for
promoting the slow
release of reduced glutathione into the body such that the reduced glutathione
is used effectively
and is not immediately oxidized.
19
CA 3041914 2019-04-30
_
Clinical Example Testing The Bio-Effectiveness Of The Composition
[0067] In one study conducted to test the effectiveness of a
composition comprising reduced
glutathione as disclosed above, the bio-effectiveness and availability of
reduced glutathione in
the body was greatly enhanced compared with purported GSH supplements known in
the art.
The composition provided unexpectedly good results given that purported GSH
supplements
known in the art in fact fail to deliver reduced glutathione to the user.
[0068] In one clinical study, a composition including reduced
glutathione in a deoxygenated
water solvent was provided to a user. The composition was encapsulated in a
phospholipid
liposome structure and packaged and delivered from an airless dispenser. The
composition
included 550+2 mg of reduced glutathione per 4 g of solution. The composition
was provided to
three human volunteers as a liquid-based oral supplement, and it was provided
to one human
volunteer as a liquid-based topical treatment to be applied topically. The
human serum levels of
reduced glutathione and oxidized glutathione were sampled initially before
ingestion to establish
a baseline level, and the serum levels were again sampled three times over
eight hours after
ingestion or application of the composition. The participants continued to
take the composition
once every morning at least thirty minutes before meals for four weeks. The
serum levels of the
participants were sampled once each week during the four-week study period to
collect data for
long-term effects of the composition.
[0069] Each participant experienced a short-term increase in serum
levels of reduced
glutathione equal to at least a 30% increase in the presence of reduced
glutathione in the serum.
Each participant experienced a long-term progressive reduction of oxidized
glutathione equal to
at least a 30% reduction in the presence of oxidized glutathione in the serum.
As discussed
previously, the ratio of reduced glutathione to oxidized glutathione is an
important and well-
CA 3041914 2019-04-30
understood marker for cellular oxidative stress. The results of the clinical
example indicate that
the composition was bioavailable unlike other pill and capsule delivery forms
of purported GSH
supplements. Further, the composition provided long-term reduction in systemic
cellular
oxidative stress in each of the participants.
[0070]
In the above-referenced study, four persons agreed to participate. The
participants
included one male and one female ranging in age from 23 to 83 years of age.
The participants
were assigned a number from #1 to #4 as follows: (1) 61-year-old female, (2)
55-year-old male,
(3) 23-year-old female, and (4) 83-year-old female. Each of the participants
was permitted to
each the morning of the first serum collection but refrained from taking
antioxidant dietary
supplements during the course of the four-week study period. The participants'
blood was
collected for baseline measurements at approximately 8:00 AM by intravenous
puncture. The
serum was extracted, processed, and frozen for later analysis. After the
collection of the baseline
serum sample, the participants immediately consumed the composition by
dispensing 4 mL of
the liquid composition into their mouth and swishing for 15-20 seconds before
swallowing. The
participants refrained from drinking for 15 minutes afterward. The participant
who used the
product topically applied approximately the same amount of the composition
onto the abdomen
and soft areas under the arms. Samples of the participants' blood were against
collected at 2
hours, 6 hours, and 8 hours after the first collection. The participants
consumed the composition
one time per day in the morning for a four-week period. The participants'
blood was collected
each week at exactly seven-day intervals for four weeks at approximately 10:00
AM. The
participants were instructed to consume the composition four hours prior to
collection. The
serum was extracted, processed, and frozen for later analysis. All serum
samples were assayed
within thirty days of collection.
21
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Analysis of the Serum Samples.
[0071] The serum samples were analyzed to determine the levels of reduced
glutathione and
oxidized glutathione. The serum samples were analyzed using the BioVision
(Milpitas, CA)
Glutathione Fluorometric Assay Kit (GSH, GSSG, and Total) k264. Wasatch
Scientific
Laboratories in Murray, Utah, USA was contracted to perform the assay using
the BioVision
fluorometric kit and method. Whole blood samples were collected and
immediately centrifuged
to separate the serum from the red blood cells and heavier components.
Approximately 120 pL
of serum was added to 40 pL of an ice-cold perchloric acid PCA buffer in a 1
mL aliquot. The
solution was vortexed and stored on ice for five minutes. The solution was
centrifuged at 13,000
G for two minutes, and the supernatant was collected and frozen at -60degC.
[0072] FIG. 5 illustrates a standard curve for reduced glutathione for the
short-term analysis.
The standard curve for reduced glutathione and oxidized glutathione were
created, and then the
prepared serum samples were tested at two dilutions to determine the optimal
dilution for the
best dynamic resolution of the assay. The samples were processed and assayed
in duplicate pairs
at the chosen dilution. The results of each pair were reviewed and compared
for repeatability and
best-fit samples were used. FIG. 4 illustrates a mass of reduced glutathione
(GSH) in nanograms
on the x-axis plotted against the relative fluorescence units (RFU) on the y-
axis.
[0073] FIG. 5 illustrates a standard curve for reduced glutathione for the
long-term analysis.
The standard curve for reduced glutathione and oxidized glutathione were
created, and then the
prepared serum samples were tested at two dilutions to determine the optimal
dilution for the
best dynamic resolution of the assay. The samples were processed and assayed
in duplicate pairs
at the chosen dilution. The results of each pair were reviewed and compared
for repeatability and
best-fit samples were used. FIG. 4 illustrates a mass of reduced glutathione
(GSH) in nanograms
22
CA 3041914 2019-04-30
on the x-axis plotted against the relative fluorescence units (RFU) on the y-
axis. The results of
the assay were compiled and displayed in tabular and graphical form. In
addition, ratiometric
results of reduced glutathione (GSH) and oxidized glutathione (GSSG) were
created for each
sample.
[0074] FIG. 6 illustrates concentrations of reduced glutathione for each of
the four
aforementioned participants for the short-term analysis. FIG. 6 illustrates
concentrations in
lig ImL for each of four possible serum draws for each of the four
participants. Draw one is the
baseline draw. Draw two was taken at the baseline plus four hours. Draw three
was taken at the
baseline plus six hours. Draw four was taken at the baseline plus eight hours.
As illustrated in
FIG. 6, all participants in the short-term analysis experienced an increase in
serum levels of
reduced glutathione. The increase concentration of reduced glutathione
appeared to peak at
approximately six to eight hours after ingestion. The increase in reduced
glutathione was on
average 30% above baseline levels. Participant one, a female, applied the
composition topically
and experienced elevated serum levels of reduced glutathione.
[0075] FIG. 7 illustrates concentrations of oxidized glutathione for each
of the four
aforementioned participants for the short-term analysis. FIG. 7 illustrates
concentrations in
mg ImL for each of four possible serum draws for each of the four
participants. Draw one is the
baseline draw. Draw two was taken at the baseline plus four hours. Draw three
was taken at the
baseline plus six hours. Draw four was taken at the baseline plus eight hours.
Participant one, a
female, applied the composition topically and experienced elevated serum
levels of reduced
glutathione. As illustrated in FIG. 7, concentrations of oxidized glutathione
appeared to respond
differently for each participant. The most significant change in levels of
oxidized glutathione was
an almost 50% reduction in participant one who applied the composition
topically. In
23
CA 3041914 2019-04-30
participants three and four, the levels of oxidized glutathione on average
reduced slightly from
baseline.
[0076] FIG. 8 illustrates the ratios of reduced glutathione to oxidized
glutathione for each of
the participants for the short-term analysis. As illustrated in FIG. 8, the
composition provided a
short-term antioxidant benefit to each of the participants. The
reduced/oxidized glutathione ratio
is an accepted standard to measure cellular oxidative stress. This study
illustrates the redox ratio
trend over time. After ingestion, each participant experienced an increase in
the redox ration
compared to the baseline, even eight hours after consuming or applying the
composition.
[0077] FIG. 9 illustrates concentrations of reduced glutathione for each of
the four
aforementioned participants for the long-term analysis. FIG. 9 illustrates
concentrations in
pn/mL for each of three weekly serum draws for each of the four participants.
Draw one (not
shown due to laboratory error) was taken at 10:00 AM exactly one week after
ingestion or
application of the composition. Draw two occurred at 10:00 AM two weeks after
ingestion or
application of the composition. Draw three occurred at 10:00 AM exactly three
weeks after
ingestion or application of the composition. Draw four occurred at 10:00 AM
exactly four weeks
after ingestion or application of the composition. The human serum samples
were assayed for
concentrations of reduced and oxidized glutathione. Participant one, a female,
applied the
composition topically and participants two, three, and four ingested orally a
liquid-based
composition.
[0078] As illustrated in FIG. 9, the participants' serum levels of reduced
glutathione show
mixed results. Participants one and three demonstrates levels of reduced
glutathione that are very
close to the baseline levels without significant increase. Participants two
and four demonstrated
long-term increase in levels of reduced glutathione equal to approximately 20-
22%. The long-
24
CA 3041914 2019-04-30
term serum levels of reduced glutathione when viewed alone showed positive
results in
participants two and four.
[0079] FIG. 10 illustrates concentrations of oxidized glutathione for each
of the four
aforementioned participants for the long-term analysis. FIG. 10 illustrates
concentrations in
lig ImL for each of three weekly serum draws for each of the four
participants. Draw one (not
shown due to laboratory error) was taken at 10:00 AM exactly one week after
ingestion or
application of the composition. Draw two occurred at 10:00 AM two weeks after
ingestion or
application of the composition. Draw three occurred at 10:00 AM exactly three
weeks after
ingestion or application of the composition. Draw four occurred at 10:00 AM
exactly four weeks
after ingestion or application of the composition. The human serum samples
were assayed for
concentrations of reduced and oxidized glutathione. Participant one, a female,
applied the
composition topically and participants two, three, and four ingested orally a
liquid-based
composition.
[0080] As illustrated in FIG. 10, each of the four participants experienced
a significant
decrease in long-term concentrations of oxidized glutathione (GSSG). As
discussed previously,
reduced glutathione is oxidized inside cells and converted to oxidized
glutathione according to
the reaction 200 illustrated in FIG. 2. A portion of the oxidized glutathione
is shuttled out of the
cells and into the intracellular space and into the blood. When the ratio of
reduced/oxidized
glutathione is calculated, a true reduction is cellular oxidation is evidence.
[0081] FIG. 11 illustrates the ratios of reduced glutathione to oxidized
glutathione for each
of the four aforementioned participants for the long-term analysis. As
illustrated in FIG. 11, each
of the participants experienced a sustained and cumulative decrease in
oxidative stress. The
reduced/oxidized glutathione redox ratio increased for all participants over
the four weeks of
CA 3041914 2019-04-30
ingesting or applying the composition. Applicant notes that participant three
and participant four
represent a wide age and health gap, where one is a 23-year-old healthy female
and the other is
an 83-year old female with health issues due to age. The composition had a
positive long-term
effect in both the young participant and the older participant, where the
older participant
experienced a greater rise in the redox ratio. The data further shows that
participant one
experienced a redox benefit, even by applying the product topically. Applicant
notes that
participant one only applied about one-third of the dose compared to the oral
participants, not
following specific dosing instructions. The results for all participants
clearly demonstrates the
benefits of the novel composition comprising reduced glutathione that is
disclosed herein.
[0082] FIG. 12 illustrates the ratios of reduced glutathione to oxidized
glutathione for each
of the participants for the long-term analysis versus the baseline analysis.
FIG. 12 illustrates a
comparison of the change in redox over time as a result of supplementation
with the composition
disclosed herein. As illustrated in FIG. 12, all participants experienced a
net average increase
above baseline redox ratios, with participant two (55-year-old male) and
participant four (83-
year-old female) experiencing the greatest increase. Applicant notes that it
is anticipated that
participant one (61-year-old female) would have experienced a greater result
if the dosage
requirements for topical application were followed more consistently.
[0083] The effects of the novel composition comprising reduced glutathione
that is
disclosed herein indicate a bioavailability of reduced glutathione and its
short-term and long-
term benefits in the human body as indicated in the serum concentrations of
reduced glutathione
(GSH) and oxidized glutathione (GSSG). All participants experienced a
noticeable increase in
GSH/GSSG redox ratio indicating a true reduction in cellular oxidative stress,
with the older
26
CA 3041914 2019-04-30
participants (age 55-83) experiencing higher ratios. This is consistent with
the assumption that
older participants have a greater amount of cellular oxidative stress to be
reduced.
[0084] The results of the clinical example demonstrate conclusively that
the composition
disclosed herein is effectively delivering reduced glutathione. The
composition includes reduced
glutathione and a deoxygenated water solvent. The composition is manufactured
and packaged in
an anaerobic environment, in stark contrast with previous supplements known in
the art that
purport to deliver reduced glutathione but instead deliver oxidized
glutathione. The careful
maintenance of an anaerobic condition, as disclosed herein, provides the
unexpected result
(given all prior failures) of a composition that genuinely comprises reduced
glutathione. The
composition disclosed herein provides increased levels of reduced glutathione,
reduced cellular
oxidative stress, and provides all the appurtenant benefits.
[0085] It should be appreciated that in various embodiments, dosage amounts
may be
adjusted depending on the effect on any given individual, as well as the
biometrics of that
individual. For example, a larger person may require a higher dosage than a
smaller person.
Similarly, a person suffering from an acute condition may benefit from a
higher dose for a time
until the condition is controlled, at which point a lower dose may provide
sufficient management
over time.
Clinical Example For Treatment Of Skin Burns
[0086] In one embodiment, the composition is provided for the treatment of
burns and for
burn pain relief and healing. In a study, the composition was applied
topically to greater than 200
patients experiencing severe pain caused by first, second, or third degree
burns. The patients
reported complete pain resolution within minutes of topical application of the
composition.
Additionally, the patients reported rapid healing of the burn.
27
CA 3041914 2019-04-30
Clinical Example For Treatment Of Shingles And Postherpetic Neuralgia
[0087]
In one embodiment, the composition is provided for the treatment of shingles
and
postherpetic neuralgia (PHN). In a study, the composition is provided to 103
patients for the
treatment of shingles and/or PHN. Each of the greater than 103 patients
participating in the study was
over the age of 70 years and experienced active shingles lesions and neuralgia
for at least three years.
The composition was applied topically to each of the 103 patients. Of the 103
patients, 98% reported
pain resolution within 34 minutes. The remaining 2% reported pain resolution
within two days. In the
study, there was zero incidence of Post Herpatic Neuralgia after the
composition was topically
applied.
Clinical Example For The Treatment Of Herpes Type 1 And Type 2
[0088]
In one embodiment, the composition is provided for the treatment of Herpes
Type 1
and/or Type 2. In a study, the composition is topically applied to patients
with Type 1 or Type 2
Herpetic lesions. Each of the patients reported pain relief and resolution of
herpetic symptoms. In the
study, for patients that experienced a reoccurrence of a herpetic lesion, the
composition was reapplied
and the patient experienced quick resolution of the pain and other symptoms.
[0089]
In a study, the composition is topically applied for the treatment of cold
stores. The
study includes 12 patients that have experienced cold sores and report the
sensation that a cold sore
lesion will appear. In the study, the composition is topically applied to the
area where the patient
reports the cold sore lesion will appear. For each of the 12 patients, the
cold sore lesion never
blossomed and never appeared.
Clinical Example For The Treatment Of Tardive Dyskinesia
[0090]
In one embodiment, the composition is provided for the treatment of tardive
dyskinesia.
In a study, the composition is topically applied over the course of six weeks.
In the study, the
28
CA 3041914 2019-04-30
composition is topically applied to two patients. Each of the two patients
experienced complete
resolution of the tardive dyskinesia. In the study, each of the two patients
had been wheelchair and
bed bound for at least ten years. Upon receiving topical application of the
composition over the
course of six weeks, each of the two patients was able to walk, eat, drink,
and converse. The patients
admitted to having been aware of all they had experienced over the course of
the ten years they
suffered from tardive dyskinesia.
Clinical Example For The Treatment Of Diabetic Neuropathy
[0091] In one embodiment, the composition is provided for the treatment of
diabetic neuropathy.
In a study, the composition is topically applied to greater than one-hundred
patients. In the study,
approximately 5 mL of the composition is rubbed topically on the foot and/or
leg of each of the
greater than one-hundred patients. In the study, the patients reported
experiencing complete pain
relief after about four hours. In the study, the patients reported complete
permanent relief after
receiving treatment for 3-6 months.
Clinical Example For The Treatment Of Symptoms Associated With The Epstein
Barr Virus
[0092] In one embodiment, the composition is provided for the treatment of
symptoms
associated with the Epstein Barr Virus (EBV). In a study, the composition is
provided for oral
consumption to 25 patients. In the study, each of the 25 patients reported
that symptoms resolved in
3-5 days after the oral dose of the composition. In the study, the composition
was provided to the
patients at a dosage of approximately 1100 mg per day.
[0093] In one embodiment, the composition may be provided for the treatment
of cellular
oxidative stress. When the composition is provided for the treatment of
cellular oxidative stress, it
may be ingested orally or administered topically. Applicant notes that in
further embodiments the
29
CA 3041914 2019-04-30
composition may be administered intravenously or intramuscularly, or in a
tablet or powder form
without departing from the scope of the disclosure.
[0094] In one embodiment, the composition is provided for the treatment of
acute levels of free
radicals in the body. In such an embodiment, the composition may be prepared
for immediate
intravenous or intramuscular administration. The composition may further or
alternatively be
provided for oral ingestion or topical application. In such an embodiment, the
composition may be
provided for regular administration after acute levels of free radicals in the
body have been treated
and reduced to safe levels.
[0095] In one embodiment, the composition is provided for the treatment of
acetaminophen
overdose. The molecule known as N-acetylcysteine (hereinafter "NAC") is known
in the art for
the treatment of acetaminophen overdose. Pharmaceutical NAC is primarily used
in medical
settings for respiratory conditions, to manage acetaminophen overdose, and to
prevent radio-
contrast-induced nephropathy. However, the half-life of NAC is approximately
5.6 hours, and
30% of NAC is renally excreted by the body. Orally administered or inhaled NAC
is associated
with drowsiness, stomatitis, clamminess, rhinorrhea, and hemoptysis, and NAC
is a category B
pregnancy risk. In contrast with NAC, where the half-life is extremely short
and the molecule is
unstable, the shelf-life of the composition disclosed herein is at least one
year. Therefore, the
composition disclosed herein provides an alternative to NAC that is shelf-
stable for an extended
period and demonstrates high viability and efficacy.
[0096] Referring now to FIG. 13, a schematic block diagram of a method 1300
for
improving free radical levels in a user is illustrated. The method 1300 begins
and a composition
is provided to a user at 1302. The composition includes an antioxidant in a
reduced state and a
CA 3041914 2019-04-30
deoxygenated water solvent. The composition is such that the antioxidant
remains in its reduced
state.
[0097] FIG. 14 is a schematic block diagram of a method 1400 for improving
free radical
levels in a user. The method 1400 begins and a composition is provided to a
user at 1402. The
composition includes reduced glutathione present in the composition from 5% to
20% by weight
of the total composition. The composition includes a deoxygenated water
solvent. The
composition includes an effective amount of one or more preservatives. The
composition
includes an effective amount of one or more natural flavoring components for
improving an
overall flavor of the composition. The composition is microencapsulated. The
composition is
packaged in an airless dispenser configured to maintain an anaerobic
environment.
[0098] In one embodiment, a 99.9% purity reduced glutathione powder is
solubilized in
deoxygenated water and encapsulated in a plant-based phospholipid liposome
structure. In the
embodiment, the composition includes from about 8% to about 14% by weight
reduced
glutathione. The composition includes from about 4% to about 11% by weight
sunflower lecithin.
The composition includes from about 0.2% to about 0.6% by weight lemon
essential oil. The
composition includes from about 0.1% to about 0.5% peppermint essential oil.
The composition
includes from about 0.01% to about 0.25% stevia extract. The composition
includes sodium
benzoate and potassium sorbate.
[0099] In an embodiment of the disclosure, the composition includes highly
pure L-
glutathione reduced. In an embodiment of the disclosure, the reduced
glutathione comprises a
purity from about 98% to about 99.9% purity. In an embodiment, the purity is
from about 90% to
about 99.9% purity. In an embodiment, the purity is from about 95% to about
99.9% purity. In an
embodiment, the purity is from about 99.0% to about 99.9% purity. It should be
appreciated that
31
CA 3041914 2019-04-30
various ranges of purity may be extracted from any of the aforementioned
ranges as if those
ranges were disclosed explicitly.
[0100] In an embodiment of the disclosure, the composition includes
sunflower lecithin.
Lecithin is a fat found in a plurality of food products. Sunflower lecithin is
a phospholipid
comprising phosphatidylcholine, phosphatidylinositol,
phosphatidylethanolamine, and omega-6
linoleic acid. Sunflower lecithin is associated with processing fats and
supporting cell
membranes. In an embodiment of the disclosure, the sunflower lecithin is
provided for
encapsulating the composition and protecting the reduced glutathione
component.
[0101] In an embodiment of the disclosure, the composition includes lemon
essential oil.
Lemon essential oil may be provided to improve an overall flavor of the
composition. As
disclosed, oxidized glutathione provides a sulfur smell that may be pungent or
off-putting to a
user. Additionally, the composition of the present disclosure may oxidize with
oxygen in the air
when the composition is being ingested, and the oxidized may cause the
composition to become
unpalatable to the user immediately before the user ingests the composition.
The lemon essential
oil may be provided to counteract the sulfur smell of the oxidized glutathione
and increase the
flavor of the composition.
[0102] In an embodiment of the disclosure, the composition includes
peppermint essential
oil. As discussed previously with respect to the lemon essential oil, the
peppermint essential oil
may be provided to improve the overall flavor of the composition and mask a
sulfur smell arising
from the oxidation of the reduced glutathione.
[0103] In an embodiment of the disclosure, the composition includes stevia
extract. As
discussed previously with respect to the lemon essential oil and/or the
peppermint essential oil,
32
CA 3041914 2019-04-30
=
the stevia extract may be provided to improve the overall flavor of the
composition and mask a
sulfur smell arising from the oxidation of the reduced glutathione.
[0104] In an embodiment of the disclosure, the composition includes
sodium benzoate.
Sodium has a chemical formula of NaC7H502. Sodium benzoate is known as a food
preservative
and has an E number of E211. Sodium benzoate is the sodium salt of benzoic
acid and exists in
the form when dissolved in water. As a food additive, sodium benzoate is
bacteriostatic and
fungistatic under acidic condition. Sodium benzoate is included in the
composition as a
preservative in an embodiment of the disclosure.
[0105] In an embodiment of the disclosure, the composition includes
potassium sorbate.
Potassium sorbate has a chemical formula of CH3CH=CH-CH=CH-0O2K. Potassium
sorbate is
a known food preservative and has an E number of E202. Potassium sorbate is
known for
inhibiting molds and yeasts in a variety of foods and liquids. Potassium
sorbate is included in the
composition as a preservative in an embodiment of the disclosure.
Examples
[0106] Chart 1 below shows an example embodiment of the
composition. Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
Chart 1:
Component Weight Percent Total
Composition
L-glutathione reduced 14.00
Sunflower lecithin 10.50
Lemon essential oil 0.40
Peppermint essential oil 0.25
33
CA 3041914 2019-04-30
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
[0107] Chart 2 below shows an example embodiment of the composition.
Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
Chart 2:
Component Weight Percent Total Composition
L-glutathione reduced 10.00
Sunflower lecithin 10.50
Lemon essential oil 0.40
Peppermint essential oil 0.25
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
[0108] Chart 3 below shows an example embodiment of the composition.
Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
34
CA 3041914 2019-04-30
Chart 3:
Component Weight Percent Total Composition
L-glutathione reduced 8.00
Sunflower lecithin 10.50
Lemon essential oil 0.40
Peppermint essential oil 0.25
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
[0109] Chart 4 below shows an example embodiment of the
composition. Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
Chart 4:
Component Weight Percent Total Composition
L-glutathione reduced 14.00
Sunflower lecithin 4.00
Lemon essential oil 0.40
Peppermint essential oil 0.25
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
CA 3041914 2019-04-30
[0110] Chart 5 below shows an example embodiment of the composition.
Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
Chart 5:
Component Weight Percent Total Composition
L-glutathione reduced 14.00
Sunflower lecithin 11.00
Lemon essential oil 0.40
Peppermint essential oil 0.25
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
[0111] Chart 6 below shows an example embodiment of the composition.
Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
Chart 6:
Component Weight Percent Total Composition
L-glutathione reduced 14.00
Sunflower lecithin 10.50
Lemon essential oil 0.20
Peppermint essential oil 0.25
36
CA 3041914 2019-04-30
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
[0112] Chart 7 below shows an example embodiment of the composition.
Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
Chart 7:
Component Weight Percent Total Composition
L-glutathione reduced 14.00
Sunflower lecithin 10.50
Lemon essential oil 0.60
Peppermint essential oil 0.25
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
[0113] Chart 8 below shows an example embodiment of the composition.
Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
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Chart 8:
Component Weight Percent Total Composition
L-glutathione reduced 14.00
Sunflower lecithin 10.50
Lemon essential oil 0.40
Peppermint essential oil 0.10
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
[0114] Chart 9 below shows an example embodiment of the
composition. Components were
dissolved in deoxygenated water and encapsulated in a plant-based phospholipid
liposome
structure. The composition was packaged and stored in an airless dispenser.
Chart 9:
Component Weight Percent Total Composition
L-glutathione reduced 14.00
Sunflower lecithin 10.50
Lemon essential oil 0.40
Peppermint essential oil 0.50
Sodium benzoate 0.10
Potassium sorbate 0.10
Stevia extract 0.10
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_
[0115] Example 1 is a composition for reducing oxidative stress in
a user. The composition
includes an effective amount of reduced glutathione for reducing oxidative
stress in the user, and
deoxygenated water solvent.
[0116] Example 2 is a composition as in Example 1, wherein the
composition is
encapsulated in a phospholipid liposome structure.
[0117] Example 3 is a composition as in any of Examples 1-2,
wherein the composition is
packaged in an airless dispenser configured to maintain an anaerobic
environment.
[0118] Example 4 is a composition as in any of Examples 1-3,
wherein the reduced
glutathione comprises from about 8% to about 14% by weight of the total
composition.
[0119] Example 5 is a composition as in any of Examples 1-4,
wherein the composition
comprises from about 500 mg to about 600 mg reduced glutathione per 4 g of the
composition.
[0120] Example 6 is a composition as in any of Examples 1-5,
wherein the reduced
glutathione comprises a purity from about 98% to about 99.9% purity.
[0121] Example 7 is a composition as in any of Examples 1-6,
further comprising an
effective amount of sodium benzoate for preserving the composition.
[0122] Example 8 is a composition as in any of Examples 1-7,
further comprising an
effective amount of potassium sorbate for preserving the composition.
[0123] Example 9 is a composition as in any of Examples 1-8,
further comprising an
effective amount of natural flavoring comprising one or more of: lemon
essential oil, peppermint
essential oil, and stevia extract.
[0124] Example 10 is a composition as in any of Examples 1-9,
wherein the composition is
prepared for liquid oral consumption.
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[0125] Example 11 is a composition as in any of Examples 1-10, wherein the
composition is
prepared for topical application.
[0126] Example 12 is a composition as in any of Examples 1-11, wherein the
composition is
prepared for intravenous or intramuscular administration.
[0127] Example 13 is a composition as in any of Examples 1-12, wherein the
reduced
glutathione comprises from about 4 g to about 20 g per 100 mL of the
deoxygenated water
solvent.
[0128] Example 14 is a method of reducing oxidative stress in a user. The
method includes
providing a composition to the user, wherein the composition includes an
effective amount of
reduced glutathione for reducing oxidative stress in the user, and a
deoxygenated water solvent.
[0129] Example 15 is a method as in Example 14, wherein the composition is
encapsulated
in a phospholipid liposome structure.
[0130] Example 16 is a method as in any of Example 14-15, wherein the
composition is
packaged in an airless dispenser configured to maintain an anaerobic
environment.
[0131] Example 17 is a method as in any of Example 14-16, wherein the
reduced
glutathione comprises from about 8% to about 14% by weight of the total
composition.
[0132] Example 18 is a method as in any of Example 14-17, wherein the
composition
comprises from about 500 mg to about 600 mg reduced glutathione per 4 g of the
composition.
[0133] Example 19 is a method as in any of Example 14-18, wherein the
reduced
glutathione comprises a purity from about 98% to about 99.9% purity.
[0134] Example 20 is a method as in any of Example 14-19, wherein the
reduced
glutathione comprises a purity from about 99.0% to about 99.9% purity.
CA 3041914 2019-04-30
[0135] Example 21 is a method as in any of Example 14-20, wherein the
composition
further comprises an effective amount of sodium benzoate for preserving the
composition.
[0136] Example 22 is a method as in any of Example 14-21, wherein the
composition
further comprises an effective amount of potassium sorbate for preserving the
composition.
[0137] Example 23 is a method as in any of Example 14-22, wherein the
composition
further comprises an effective amount of natural flavoring for improving an
overall flavor of the
composition, wherein the natural flavoring comprises one or more of: lemon
essential oil,
peppermint essential oil, and stevia extract.
[0138] Example 24 is a method as in any of Example 14-23, wherein the
composition is
provided to the user for liquid oral consumption.
[0139] Example 25 is a method as in any of Example 14-24, wherein the
composition is
provided to the user for topical administration.
[0140] Example 26 is a method as in any of Example 14-25, wherein the
composition is
provided to the user for intravenous or intramuscular administration.
[0141] Example 27 is a method as in any of Example 14-26, wherein the
reduced
glutathione comprises from about 4 g to about 20 g per 100 mL of the
deoxygenated water
solvent.
[0142] Example 28 is a method as in any of Example 14-27, wherein the
composition is
provided to the user for short-term treatment of cellular oxidative stress.
[0143] Example 29 is a method as in any of Example 14-28, wherein the
composition
increases blood-serum levels of reduced glutathione in the user by at least
25%.
[0144] Example 30 is a method as in any of Example 14-29, wherein the
composition is
provided for long-term treatment of cellular oxidative stress.
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[0145] Example 31 is a composition. The composition includes an antioxidant
in a reduced
state and a deoxygenated water solvent. The composition is such that the
antioxidant remains in
its reduced state.
[0146] Example 32 is a composition as in Example 31, wherein the
composition is
microencapsulated.
[0147] Example 33 is a composition as in any of Examples 31-32, wherein the
composition
is packaged in an airless dispenser configured to maintain an anaerobic
environment.
[0148] Example 34 is a composition as in any of Examples 31-33, wherein the
antioxidant is
reduced glutathione and wherein the reduced glutathione comprises from 8% to
14% by weight
of the total composition.
[0149] Example 35 is a composition as in any of Examples 31-34, wherein the
composition
is microencapsulated in a liposome structure.
[0150] Example 36 is a composition as in any of Examples 31-35, wherein the
composition
is microencapsulated in a gelatin composition.
[0151] Example 37 is a composition as in any of Examples 31-36, wherein the
antioxidant is
reduced glutathione, and wherein the reduced glutathione comprises a purity
from 98% to 99.9%
purity in its dry state.
[0152] Example 38 is a composition as in any of Examples 31-37, further
comprising an
effective amount of one or more preservatives selected from a list comprising:
potassium sorbate,
sodium benzoate, sorbic acid, benzoic acid, natural benzyl alcohol, erythorbic
acid, sodium
erythorbate, ferrous gluconate, methyl paraben, potassium benzoate, rosemary
extract, and
sodium citrate.
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..
[0153] Example 39 is a composition as in any of Examples 31-38,
further comprising an
effective amount of one or more natural flavoring components for improving an
overall flavor of
the composition selected from a list comprising: lemon essential oil,
peppermint essential oil,
monk fruit extract, agave, honey, natural cane sugar, glucose, fruit
concentrate, natural fruit
powder, spearmint essential oil, wintergreen essential oil, orange essential
oil, tangerine essential
oil, lavender essential oil, and stevia extract.
[0154] Example 40 is a composition as in any of Examples 31-39,
wherein the antioxidant is
reduced glutathione and wherein the composition comprises from 4 g to 20 g
reduced glutathione
per 100 mL of the deoxygenated water solvent.
[0155] Example 41 is a composition as in any of Examples 31-40,
wherein the composition
is provided for reducing oxidative stress in a user.
[0156] Example 42 is a composition as in any of Examples 31-41,
wherein the composition
is provided for improving free radical levels in a user.
[0157] Example 43 is a composition as in any of Examples 31-42,
wherein the composition
is provided for the treatment of skin burns.
[0158] Example 44 is a composition as in any of Examples 31-43,
wherein the composition
is provided for treatment of shingles.
[0159] Example 45 is a composition as in any of Examples 31-44,
wherein the composition
is provided for treatment of Herpes Type 1 and/or Herpes Type 2.
[0160] Example 46 is a composition as in any of Examples 31-45,
wherein the composition
is provided for treatment of tardive dyskinesia.
[0161] Example 47 is a composition as in any of Examples 31-46,
wherein the composition
is provided for treatment of diabetic neuropathy.
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[0162] Example 48 is a composition as in any of Examples 31-47, wherein the
composition
is provided for treatment of symptoms associated with Epstein Barr Virus.
[0163] Example 49 is a composition as in any of Examples 31-58, wherein the
composition
is prepared for administration with an inhaler.
[0164] Example 50 is a composition as in any of Examples 31-59, wherein the
composition
is prepared for topical administration.
[0165] Example 51 is a composition as in any of Examples 31-50, wherein the
composition
is prepared for intravenous administration.
[0166] Example 52 is a composition as in any of Examples 31-51, wherein the
composition
is prepared for intramuscular or subcutaneous administration.
[0167] Example 53 is a composition as in any of Examples 31-52, wherein the
composition
is prepared for liquid oral consumption.
[0168] Example 54 is a composition as in any of Examples 31-53, wherein the
antioxidant is
reduced glutathione.
[0169] According to one or more embodiments of the disclosure, a
composition may include
a combination of all or some, but not all, of the following ingredients:
[0170] (a) L-glutathione reduced;
[0171] (b) deoxygenated water;
[0172] (c) sunflower lecithin;
[0173] (d) lemon essential oil;
[0174] (e) peppermint essential oil;
[0175] (f) sodium benzoate;
[0176] (g) potassium sorbate; and/or
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[0177] (h) stevia extract.
[0178] Other embodiments of the composition may comprise, for example,
concentrations
of L-glutathione reduced as follows:
[0179] (al) from 5% to 20% by weight the total composition;
[0180] (a2) from 6% to 19% by weight the total composition;
[0181] (a3) from 7% to 18% by weight the total composition;
[0182] (a4) from 8% to 17% by weight the total composition;
[0183] (a5) from 8% to 16% by weight the total composition;
[0184] (a6) from 8% to 15% by weight the total composition;
[0185] (a7) from 8% to 14% by weight the total composition;
[0186] (a8) from 8% to 13% by weight the total composition;
[0187] (a9) from 9% to 14% by weight the total composition;
[0188] (al 0) from 10% to 14% by weight the total composition;
[0189] (all) from 9% to 13% by weight the total composition;
[0190] (a12) from 10% to 12% by weight the total composition;
[0191] (a13) from 10% to 11% by weight the total composition.
[0192] With respect to ingredient (c) noted above for example, the amount
of sunflower
lecithin that may be included in the final composition is based on a percent
by weight of the total
weight of the final composition described herein. The composition may comprise
ingredient (c)
for example, in concentrations as follows:
[0193] (c1) from 1% to 20% by weight the total composition;
[0194] (c2) from 2% to 19% by weight the total composition;
[0195] (c3) from 3% to 18% by weight the total composition;
CA 3041914 2019-04-30
[0196] (c4) from 4% to 17% by weight the total composition;
[0197] (c5) from 4% to 16% by weight the total composition;
[0198] (c6) from 4% to 15% by weight the total composition;
[0199] (c7) from 4% to 14% by weight the total composition;
[0200] (c8) from 4% to 13% by weight the total composition;
[0201] (c9) from 4% to 12% by weight the total composition;
[0202] (c10) from 4% to 11% by weight the total composition;
[0203] (c11) from 5% to 10% by weight the total composition;
[0204] (c12) from 6% to 9% by weight the total composition;
[0205] (c13) from 6% to 8% by weight the total composition.
[0206] The foregoing percentages, concentrations, and ratios are presented
by example only
and are not intended to be exhaustive or to limit the disclosure to the
precise percentages,
concentrations, and ratios disclosed. It should be appreciated that each value
that falls within a
disclosed range is disclosed as if it were individually disclosed as set forth
herein. For example, a
range indicating a weight percent from about 8% to about 14% additionally
includes ranges
beginning or ending with all values within that range, including for example a
range beginning at
8.1%, 8.2%, 8.3%, and so forth.
[0207] Also, according to one or more non-limiting embodiments of the
disclosure, any of
the concentrations for ingredients (a) or (c), for example, as listed above,
may indicate the
concentration for any of ingredients (b) and (d) thru (h), as listed above.
For example, an
embodiment of the disclosure may comprise, for example, (a7) from 8% to 14% by
weigh the
total composition of L-glutathione reduced, and equal parts by weight of lemon
essential oil and
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peppermint essential oil. For example, the composition may comprise all, or
any combination of
but not all, of the ingredients (a) thru (h).
[0208] The foregoing description has been presented for the purposes of
illustration and
description. It is not intended to be exhaustive or to limit the disclosure to
the precise form
disclosed. Many modifications and variations are possible in light of the
above teaching. Further,
it should be noted that any or all the aforementioned alternate
implementations might be used in
any combination desired to form additional hybrid implementations of the
disclosure.
[0209] Further, although specific implementations of the disclosure have
been described and
illustrated, the disclosure is not to be limited to the specific forms or
arrangements of parts so
described and illustrated. The scope of the disclosure is to be defined by the
claims appended
hereto, any future claims submitted here and in different applications, and
their equivalents.
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