Note : Les descriptions sont présentées dans la langue officielle dans laquelle elles ont été soumises.
CA 2959004 2017-02-24
Composition for Improving Cognitive Function
FIELD
The invention relates to a composition to improve cognitive function and
use thereof.
BACKGROUND
Caffeine may be consumed to enhance wakefulness and cognitive
performance, typically by ingesting beverages that include caffeine, such as
coffee. A deficiency of such a caffeine source is the lack of complementary
ingredients to assist with reducing negative side-effects of caffeine
consumption
such as anxiety, jitteriness, and headache.
Traditional stimulants that improve cognitive performance act on
neurotransmission mechanisms in the brain. One common mechanism includes
the release of neurotransmitters involved in motivation, attention, and
learning,
such as dopamine, norepinephrine, and serotonin. Such traditional stimulants
are not designed to replenish these neurotransmitters once they are released
and degraded in the brain.
Currently available ingestible products that are marketed as boosting
cognitive performance, such as Brainergy (EVO-X Health Products (USA))
similarly lack effective ingredients or sufficient amounts of effective
ingredients
to contribute in replenishing neurotransmitters.
SUMMARY
An aspect of the invention provides a composition comprising L-tyrosine,
caffeine, L-theanine, Rhodiola rosea extract, pyridoxine hydrochloride (HCL),
and 5-hydroxytryptophan (5-HTP). In some embodiments, the dosage amount
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of L-tyrosine is about 200 to about 1000 mg. In some embodiments, the dosage
amount of caffeine is about 50 to about 250 mg. In some embodiments, the
dosage amount of L-theanine is about 50 to about 400 mg. In some
embodiments, the dosage amount of Rhodiola rosea extract is about 20 to
about 200 mg. In some embodiments, the Rhodiola rosea extract comprises
about 3% salidroside. In some embodiments, the dosage amount of pyridoxine
HCI is about 10 to about 50 mg. In some embodiments, the dosage amount of
5-HTP is about 5 to about 50 mg. In some embodiments, the composition is
orally-administered. In certain embodiments, the composition is in capsule
form. In other embodiments, the composition is in powder form. In other.
embodiments, the composition is in liquid form. In other embodiments, the
composition is a dietary supplement. In other embodiments, the composition is
included in food or drink.
In one embodiment, the composition comprises 500 mg of L-tyrosine,
200 mg of caffeine, 160 mg of L-theanine, 80 mg of Rhodiola rosea extract, 40
mg of pyridoxine HCL, and 20 mg of 5-HTP.
In another aspect, the invention provides use of the composition of the
above embodiments for improving cognitive performance.
Another aspect of the invention provides a method of improving
cognitive performance comprising ingesting the composition of the above
embodiments.
Another aspect of the invention provides a composition for enhancing
cognitive function comprising L-tyrosine, caffeine, L-theanine, Rhodiola rosea
extract, pyridoxine HCL, and 5-HTP.
DETAILED DESCRIPTION OF EMBODIMENTS
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There is a need for a stimulant that provides caffeine together with
ingredients that alleviate caffeine's negative side effects as well as
ingredients
that provide the body with what it needs to replenish neurotransmitters.
One aspect of the invention relates to a composition that stimulates the
brain to improve cognitive performance, provides building blocks for the body
to
replenish neurotransmitters, and diminishes, reduces, or eliminates negative
side effects of caffeine consumption. Examples of enhancing cognitive
performance include increasing wakefulness and/or mental acuity. Examples of
negative side effects include jitteriness, anxiety, headache, and other
undesired
effects that are associated with caffeine intake. Through a combination of
ingredients, the composition described herein enhances cognitive performance
and diminishes, reduces, or eliminates such negative side effects in a user.
The
term "user" refers to a subject that ingests the composition. The embodiments
are intended primarily, but not exclusively, for use with human subjects.
Thus,
provided herein are compositions for consumption that may be used to provide
desired effects of enhancing cognitive performance and replenishing
neurotransmitters, and inhibiting undesired effects of caffeine.
As used herein, the term "dose" refers to a recommended ingestion
amount for a subject that is of average mass (e.g., 50-100 kg). For a subject
whose body mass falls outside of the average range, ingestion amounts may be
adjusted accordingly.
In some embodiments, the composition is provided in capsule form for
oral consumption (i.e., ingestion). In other embodiments, the composition is
provided in a powder form, and may be added to food or drink for ingestion. In
some embodiments, the composition is formulated as a dietary supplement. In
some embodiments, the supplement is provided in a liquid form for ingestion as
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drops, or in measured portions (e.g., mL or spoonfuls). In some embodiments,
the composition may be applied transdermally. In some embodiments, the
composition may be added to food for ingestion by eating. In some
embodiments, the composition may be added to a liquid for ingestion by
drinking.
The composition is a stimulant because one of its ingredients is caffeine.
Caffeine increases wakefulness and cognitive function, but may cause side
effects which are undesirable, including anxiety and headache. Caffeine is
known to antagonize adenosine receptors in the brain. Adenosine causes
sedation and relaxation when it acts upon its receptors. Caffeine prevents
this
action and thereby suppresses relaxation and sedation, and causes alertness
and wakefulness. This inhibition of adenosine can influence the dopamine,
serotonin, acetylcholine, and adrenaline systems.
Certain neurotransmitters are involved in motivation, attention, and
learning. Examples of such neurotransmitters include dopamine,
norepinephrine, and serotonin. Neurotransmitters may be recycled by re-uptake
mechanisms, but there are many mechanisms at play. Monoamine oxidase is
an enzyme in the brain that breaks down neurotransmitters while they are in
the
synaptic cleft, and thereby prevents re-uptake. This process is so significant
that a class of neurologic drugs, namely monoamine oxidase inhibitors (MA01s),
inhibit this pathway specifically to increase levels of neurotransmitters. The
composition described herein provides resources to counter this degradation,
by
including the building blocks for neurotransmitters. Such building blocks
include
precursors for neurotransmitters such as dopamine, norepinephrine, and
serotonin. Thus by providing these precursors, neurotransmitters that have
been depleted due to stress or cognitive load may be replenished. The
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amounts of such precursors in the composition are set to avoid adverse effects
such as, for example, upset stomach or-headache.
In the composition described herein, caffeine is paired with ingredients
that reduce its undesirable properties and ingredients that are mood
enhancers,
meaning that they maintain a healthy mood balance specifically during
prolonged cognitive exertion. The dosage amount of caffeine in the composition
is between about 50 and about 250 mg. In certain embodiments, the dosage
amount is 200 mg. The following ingredients are included in the composition
together with caffeine: L-tyrosine, L-theanine, Rhodiola rosea extract,
pyridoxine HCL, and 5-HTP. One or more other ingredient, such as a suitable
carrier, excipient, vehicle, flavouring agent, stabilizer, etc., as generally
known
in the art, may also be included in the composition.
L-tyrosine, which is the amino acid precursor to several
neurotransmitters, including dopamine and norepinephrine, is able to cross the
blood-brain-barrier, so it is able to enter the brain from an oral dose. In
contrast
to the composition described herein, many products and formulations use an
acetylated version of L-tyrosine, N-acetyl-L-tyrosine (NALT), often due to its
improved solubility. Unlike L-tyrosine, however, NALT has been shown by
numerous studies to be incapable of effectively crossing the blood-brain
barrier,
and to have no significant impact on cognitive processes (Magnusson, I., et
aL,
(1989) Metabolism 38(10): 957-961). The dosage amount of L-tyrosine in the
composition is between about 200 and about 1000 mg. In certain
embodiments, the dosage amount is 500 mg.
L-theanine acts to reduce anxiety, diminish severity and frequency of
headache, and attenuate increases in blood pressure that result from stress
and/or caffeine consumption (Yoto, A. et aL, (2012) J. Physiol. Anthropol.
31(1):
28). L-theanine is an amino acid that is not common in the human diet. L-
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theanine is structurally similar to L-glutamine and the neurotransmitters that
are
produced from it (e.g., GABA and glutamate). L-theanine is known to reach the
brain and act in the brain following an oral dose. L-theanine induces
relaxation
without sedation, and is also implicated in reducing the perception of stress
and
5 slightly improving attention. L-theanine is useful in attenuating the
"edge," or
overstimulation, of stimulants such as caffeine. A combination of L-theanine
with caffeine has been shown through several studies in healthy humans to be
synergistic in promoting cognition and attention (Kahathuduwa C.N., et al.,
(2016) Nutr. Neurosci. (On-line) 1-9; Haskell C.F., et al. (2008) Biol.
Psychol.
10 77(2):113-22; Giesbrecht T. et a/. (2010) Nutr Neurosci. 13(6):283-90;
and
Owen G.N. et al. (2008) Nutr. Neurosci. 11(4):193-8). The dosage amount of L-
theanine in the composition is between about 50 and about 400 mg. In certain
embodiments, the dosage amount is 160 mg.
Extracts obtained from the herb Rhodiola rosea have been shown to
15 reduce effects of stress and fatigue and improve cognition in fatigued
individuals
and people with a high workload (Khanum, F., et al., (2005) Comprehensive
Reviews in Food Science and Food Safety 4: 55-62). Rhodiola rosea extract
has been shown to reliably reduce symptoms of stress in persons fatigued from
non-exercise related stressors (Shevstov, V. A., et al., Phytomedicine 10
20 (2003): 95-105). Rhodiola rosea extracts are typically standardized for
rosavin
and/or salidroside content (Khanum, F., et al., (2005) Comprehensive Reviews
in Food Science and Food Safety 4: 55-62). Research shows that rosavins
have little therapeutic benefit, and that salidroside is the key agent
responsible
for the health benefits. The Rhodiola rosea extract used in the composition
25 described herein is standardized to 3% salidroside. The dosage amount of
Rhodiola rosea extract in the composition is between about 20 and about 200
mg. In certain embodiments, the dosage amount is 80 mg.
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Pyridoxine HCL aids conversion of precursors to active
neurotransmitters. Pyridoxine is a form of vitamin B6, which is converted by
cells to pyridoxal phosphate (PLP). The requirement of pyridoxine in the
central
nervous system (CNS) is 100-fold greater than in the peripheral organs
(Yarlagadda, A., et al., (2007) Psychiatry (Edgmont) 4(8): 58-60). In humans,
an
exogenous source of vitamin B6 is required for amino acid metabolism. PLP is
critical for many cellular processes in the human body. Specifically, this
molecule is used by enzymes to convert neurotransmitter precursors into the
active neurotransmitter. For example, L-Dopa decarboxylase converts L-Dopa
into dopamine, and this enzyme is dependent on PLP. The dosage amount of
pyridoxine HCL in the composition is between about 10 and about 50 mg. In
certain embodiments, the dosage amount is 40 mg.
5-HTP is a clinically-effective precursor to the neurotransmitter serotonin
(Birdsall, T.C. (1998) Alternative Medicine Review 3(4): 271-280). 5-HTP acts
to improve the mood of a subject by increasing serotonin synthesis in the
brain.
Serotonin is one of the principal neurotransmitters involved in healthy mood
balance and feelings of joy. High doses of 5-HTP are often used as a sleep
aid,
as serotonin is subsequently converted into melatonin, which is known to have
sedative properties. Low doses of 5-HTP are therefore included in the dietary
supplement to minimize any potential sedating effects. The dosage amount of
5-HTP in the composition is between about 5 and about 50 mg. In certain
embodiments, the dosage amount is 20 mg.
Although not essential, the composition may preferably be consumed on
an empty stomach. This is because certain dietary protein could compete with
uptake of the amino acids (e.g., L-tyrosine) in the composition (Wurtman, R.
J.,
et al., (1981) Pharmacological Reviews 32(4): 315-335. Thus, efficacy of the
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composition may be maximized by consumption of the composition on an empty
stomach.
Exemplary dosage amounts for ingredients of the composition are
presented in Table 1. For example, such dosage amounts may be provided in a
single capsule or in two or more capsules. The dosages were developed in
consideration of potential adverse effects (e.g., sedation) that have been
reported at higher doses of certain ingredients (e.g., 5-HTP and/or L-
theanine),
and also considering synergies between ingredients (such as caffeine and L-
theanine) (Giesbrecht, T., et al., (2010) Nutritional Neuroscience 13(6)), 283-
290
While the invention has been described with reference to the examples
provided, it is to be understood that the invention is not limited by this
description. To the contrary, the invention is intended to cover various
modifications and equivalent arrangements included within the spirit and scope
of the appended claims.
All cited publications are herein incorporated by reference in their
entirety to the same extent as if each individual publication was specifically
and
individually indicated to be incorporated by reference in its entirety.
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Table 1. An ingredient list for an embodiment of the composition
Ingredient Dosage Range per Suggested Amount per
dose (mg) dose (mg)
L-tyrosine 200-1000 500
caffeine 50-250 200
L-theanine 50-400 160
Rhodiola rosea extract 20-200 80
pyridoxine HCL 10-50 40
-5-HTP 5-50 20
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