Note: Descriptions are shown in the official language in which they were submitted.
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NUTRITIONAL OR DIETARY SUPPLEMENT
COMPOSITION AND METHODS FOR USING SAME
FOR TREATING VISUAL ACUITY LOSS
BACKGROUND
I . The Field of the Invention
This invention relates to nutritional or dietary supplement compositions that
promote
retinal health through the prevention, stabilization, reversal,
and/ortreatment ofvisual acuity
loss in people with certain ocular diseases or susceptible to the same. More
specifically, the
present invention relates to nutritional or dietary supplement compositions
that decrease the
loss of visual acuity by reducing the risk of developing late stage or
advanced age-related
macular degeneration.
2. The Background Art
Age-related macular degeneration (AMD) is a disease that causes progressive
damage
to the macula. The macula is the central part of the retina that allows a
person to see sharply
the fine details of an image. When the macula degenerates, people experience
blurring or
darkness in the center of their vision.
Macular degeneration leads to loss of central vision that is usually needed
for
activities requiring fine vision such as reading, driving and recognizing the
faces of others.
The words on a page may look blurred or straight lines may seem distorted.
Often objects
in the central vision look distorted and dim, and colors look faded. As the
disease becomes
worse, more light is typically needed to read or perform simple everyday
tasks. Over time
if not treated, the blurred spot in the center of vision gradually gets larger
and darker.
Whereas in later stages of AMD, a patient may not be able to recognize faces
until a person
is close up to them.
Peripheral, or side, vision is usually retained in macular degeneration,
whereas
blindness does not generally occur even in advanced/end-stage macular
degeneration.
However, central vision loss impairs proficiency in performing most activities
ofdaily living
and can therefore make it more difficult for people to live their lives
independently.
As appreciated, AMD is a single disease, but it can take two different forms:
(1) dry
(atrophic macular degeneration) and (2) wet (neovascular/exudative macular
degeneration).
Dry macular degeneration is the more common form of the disease and accounts
for
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approximately ninety percent (90%) of all of the cases of AMD. The classic
lesion in dry
macular degeneration is geographic atrophy. Geographic atrophy of the macula
causes
severe central visual loss. One of the most common early signs of dry AMD is
drusen.
Drusen are yellow deposits under the retina and are often found in people over
the age of 60.
Drusen alone do not usually cause vision loss. In fact, scientist are unclear
about the
connection between drusen and AMD. The do know, however, that an. increase in
the size
or number of drusen raises a person's risk of developing either advanced dry
AMD or wet
AMD.
Dry AMD has three stages, all of which may occur in one or both eyes. The
first
stage is characterized as early AMD where the patient has either several small
drusen or a
few medium-sized drusen. AT this stage, there are typically no symptoms and no
vision loss.
Stage two is generally known as intermediate AMD which includes those persons
that have
either many medium-sized drusen or one or more large drusen. Some of these
people see a
blurred spot in the center of their vision and more light is typically needed
for reading and
other tasks. Lastly, is the third stage which is classified as advanced dry
AMD. Advanced
dry AMD include those people having a breakdown of light-sensitive cells and
supporting
tissue in the central retinal area. This breakdown can cause a blurred spot in
the center of
their vision. Over time, the blurred spot may get bigger and darker, thereby
taking away
more of their central vision and. making it difficult to read or recognize
faces at a distance.
There is no treatment, laser or other, that can halt or reverse the relentless
progression of dry macular degeneration related vision loss. Once dry AMD
reaches the
advanced stages, no form of treatment can prevent vision loss. However,
treatment can delay
and possible prevent intermediate AMD from progressing to the advanced stage
in which
vision loss occurs. On such treatment was found from a study that was
conducted testing a
combination of vitamins, antioxidants, and zinc which resulted in slowing the
progression
of the disease.
In particular, this study was the first randomized placebo-controlled clinical
trial
evaluating vitamin supplementation for AMD and was titled the Age-Related Eye
Disease
Study (AREDS). AREDS enrolled patients between 1992 and 1998. The study's
results
were published in 2001 and suggested that oral supplementation with high-dose
antioxidants
(Vitamins C and E and beta-carotene), as well as zinc, reduced the risk of
vision loss in
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patients with AM.D_ Copper was added to the AREDS formulation to prevent
copper
deficiency anemia, a condition associated with high levels of zinc intake. The
recommended
supplement derived from AREDS consisted of. 500 milligrams of Vitamin C, 400
international units (IU) of beta-carotene, 80 milligrams of zinc and 2
milligrams of copper.
Specifically, AREDS found that people at high risk of developing advanced
stages
of AMD lowered their risk by about 25% when treated with a high-dose
combination of
Vitamin C, Vitamin E, beta-carotene and zinc. AREDS further demonstrated that
treatment
with zinc in combination with the high-dose antioxidants reduced the risk of
progression to
advanced AMD in susceptible individuals by 25%. In addition, among those most
at risk of
developing advanced AMD, inclusive of people with intermediate AMD or advanced
AMD
in one eye but not the other, the nutrients reduced the risk of vision loss
caused by advanced
AMD by almost a 20% reduction. (AREDS Report No. 8, Arch Ophthalmon. 2001;
119(10):1417-1436.)
Wet macular degeneration form of AMD is less common, but more severe than the
dry form. Wet macular degeneration accounts for approximately ten percent
(10%) of all
AMD. This form of the disease is characterized by choroidal neovascularization
(CNV), the
development of abnormal blood vessels beneath the retinal pigment epithelium
layer of the
retina. As the blood vessels grow abnormally, they can leak blood and fluid
which can
eventually cause scarring to the retina and damage to the macula. resulting in
a profound loss
of central vision.
Although there is no cure for wet AMD, treatments may include: (1) laser
surgery
(i.e., laser photocoagulation) where a small beam of light destroys the
abnormal blood
vessels; (2) photodynamic therapy involving a light activated drug that is
injected into the
patient's body to destroy leaking blood vessels; and (3) special medications
that slow the
formation of new blood vessels in the eye (anti-angiogenesis, anti-VEGF
therapy), such as
bevacizumab (Avastin ) and ranibizumab (Lucentis ), may be injected into the
eye to
stabilize or improve vision.
The exact cause of AMD is not known, but there are a number of risk factors
that may
plan a role. For example, it has been found that the same things that seem to
put a person at
risk for heart disease and stroke also put that person at risk for AMD. These
risk factors may
include high blood pressure, high cholesterol, obesity, smoking and low levels
of nutrient
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and minerals such as zinc and vitamins. It has also been determined that
people of the
Caucasian race and of the female gender display a greater likelihood of having
AMD. A
person's genetic makeup may also be a factor, such as a person having a
variant of the
complement factor H (CFH) gene is more likely to develop AMD. Correspondingly,
the
CFH gene variant may be responsible for about half of the approximately
fifteen million
cases of macular degeneration in the United States. It has been surmised that
the odds of
developing macular degeneration are increased by about 2.5 to 5.5 times if a
person has the
CFH gene variant.
In most cases, early detection and treatment of both dry and wet macular
degeneration
can help a patient delay or possibly prevent intermediate AMD from progressing
to the
advanced stage, in which central vision may be lost. Moreover, lifestyle
factors such as
eating a healthy diet that is high in fruits and vegetables and low in animal
fat, exercising
regularly, maintaining a healthy weight and not smoking can potentially aid in
the prevention
of macular degeneration. As noted above, the AREDS study found that people at
high risk
of developing advanced stages of AMD lowered their risk by about 25% when
being treated
with a high-dose combination of Vitamin C, Vitamin E, beta-carotene and zinc.
Thus, what
is needed is a nutritional or dietary supplement composition that is more
efficacious than the
composition used in the AREDS study which more effectively decreases visual
acuity loss
in people with certain ocular diseases, namely AMD.
SUMMARY OF THE INVENTION
The present invention provides systems and methods for administering
nutritional or
dietary supplement compositions to a patient for preventing, stabilizing,
reversing, and/or
treating visual acuity loss, namely, reducing the risk of developing advanced
stages of AMD.
Certain embodiments of the systems and methods of the present invention
comprise
administering a nutritional or dietary supplement composition effective for
preventing,
stabilizing, reversing, and/or treating visual acuity loss, wherein the
composition comprises
an effective amount of Vitamin C, Vitamin E, Vitamin B61 folate, Vitamin B121
zinc, and
copper. In some embodiments, an effective amount of thiamin, riboflavin,
niacin, biotin,
pantothenic acid, lutein, and/or zeaxanthin may be added into the administered
formulation
of the composition. As contemplated herein, the effective amount of the
constituents
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comprising the administered nutritional or dietary supplement composition may
be delivered
by means of a tablet, granules, microgranules, powders, or liquids.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
It will be readily understood that the components of the present invention, as
generally described herein, could be modified, arranged and designed in a wide
variety of
different formulas. Thus, the following more detailed description of the
embodiments of the
composition and systems and methods of the present invention is not intended
to limit the
scope of the invention. The scope of the invention is as broad as claimed
herein.
As discussed above, the AREDS study demonstrated that people at high risk of
developing advanced stages of visual acuity loss, namely AMD, lowered their
risk by about
25% when being treated with a high-dose combination of Vitamin C (as ascorbic
acid),
Vitamin E (d-alpha tocopheryl), beta-carotene, zinc (as zinc oxide) and copper
(as copper
oxide). Since the results of the AREDS study were released in the late 90's,
it has been found
that after an average of four years of supplementation of the combination of
beta carotene
and Vitamin A, this combination actually had no benefit and possibly had an
adverse effect
on the incidence of lung cancer and cardiovascular diseases. Such that, the
mortality rate was
seventeen percent (17%) higher in the active-treatment group than in the
placebo group.
(Omenn et al., Effects of a Combination of Beta Carotene and Vitamin A on Lung
Cancer
and Cardiovascular Disease, New England Journal of Medicine, May 2, 1996.)
In view of the increase in mortality rate associated with the combination of
beta
carotene and Vitamin A, there are significant reasons to believe that oral
supplementation
with lutei.n and zeaxanthin (dietary carotenoids that do not have Vitamin A
activity) is
superior to the use of beta-carotene for the prevention of AMD. Most
significantly, lutein
and zeaxanthin are the only major dietary carotenoids found in the macula. The
concentration of these xanthophylls within the macula varies with the amount
in an
individual's diet and, therefore, is easily modifiable with nutritional or
dietary
supplementation. Lutein and zeaxanthin also have been found to protect against
light
damage by being very efficient absorbers of blue light, which has the most
energy in the
visible spectrum and is the most damaging. In addition, these carotenoids are
good anti-
oxidants and scavenge reactive oxygen molecules like the antioxidant vitamins
In select
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embodiments of the nutritional or dietary supplement composition of the
present invention,
an effective amount of lutein in the range of between about 5 mg and about 25
mg can be
found. In certain embodiment of the compositions of the present invention an
effective
amount of zeaxanthin in the range of between about I mg and about 4 mg can be
found. In
some embodiments an effective amount of lutein comprises 10 mg and an
effective amount
of zeaxanthin comprises 2 mg.
Additionally, in clinical studies it has also been shown that high dosage (>
400
IU/dosage) of Vitamin E supplements may increase all-cause mortality and
should therefore
be avoided. (Miller, Ill et al., Meta-Analysis: High Dosage Vitamin E
Supplementation May
Increase All-Cause Mortality, ww,acnnn.ais,ort)content/1.4211./37.abstract.)
Whereas, the
form of Vitamin E supplements receiving the most market exposure in
pharmaceutical
preparations is all-rac-a-tocopheryl acetate (3) which is synthetically
derived. In nature,
eight substances have been found to have Vitamin E activity, namely, alpha,
beta, gamma
and delta tocopherol and alpha, beta, gamma and delta tocotrienol. Contrary to
the use of
Vitamin E (d-alpha tocopheryl) as used in the AREDS study, it has been found
that
tocotrienols posses powerful antioxidant, anticancer and cholesterol lowering
properties.
(Laboratory of Molecular Medicine, Ohio State University Medical Center: 12
Jan. 2006.)
Thus, current findings point towards tocotrienol as a potent neuroprotective
form of natural
Vitamin E. In select embodiments of the nutritional or dietary supplement
composition of
the present invention, Vitamin E (as natural d-alpha) tocopheryl succinate
with mixed d-
alpha, d-beta, d-gamma, d-delta-tocopherols and tocotrienols) can be found in
the range of
200 mg - 800 mg. In certain embodiments, an effective amount of Vitamin E (as
natural d-
alpha) tocopheryl succinate with mixed d-alpha, d-beta, d-gamma, d-delta-
tocopherols and
tocotrienols) comprises 400 mg.
Other clinical studies that have been conducted concluded with data from a
large
cohort of women at risk of cardiovascular disease indicating that daily
supplementation with
folic acid, pyridoxine and cyanocobalamin may reduce the risk of AMD. The
results, based
on an average of 7.3 years of treatment and follow-up of women at increased
risk of
cardiovascular disease, found that those assigned to active treatment had a
statistically
significant thirty-five percent (35%) to forty percent (40%) decreased risk
ofAMD. (Christen
et al., FolicAcid, Pyridoxine, and Cyanocobalamin Combination Treatment andAge-
Related
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Macular Degeneration in Women: The Women's Antioxidant and Folic Acid
Cardiovascular
Study, American Medical Association, 2009.) Selected embodiments of the
nutritional or
dietary supplement composition of the present invention comprise an effective
amount of
folate (as folic acid) in the range of between about 500 mcg and about 1,500
mcg. In certain
embodiments, an effective amount of folate (as folic acid) comprises 1,000
meg.
As appreciated, the B Vitamins work synergistically. Meaning, a deficiency in
one
often indicates a deficiency in another. While they should always be taken
together, two to
three times more of one B Vitamin can be taken for a particular disorder.
(James F. Balch,
Prescription for Natural Healing, Penguin Putnam Inc., 2000, pgs. 15-16.)
Correspondingly,
certain embodiments of the nutritional or dietary supplement composition of
the present
invention incorporate an effective amount of Vitamin B6 (as pyridoxine HCI)
and Vitamin
B12 (ascyanocaobalamin). In selected embodiments, an effective amount of
Vitamin Bfi may
be in the range ofbetween about 40 mg and about 60 mg and an effective amount
of Vitamin
B12 may be in the range of between about 500 mcg and about 1,500 meg. In
certain
embodiments of the nutritional or dietary supplement composition of the
present invention,
an effective amount of Vitamin B. comprises 50 mg and an effective amount of
Vitamin Bt2
comprises 1,000 mcg.
It has also been found that Vitamin D which may protect against AMD. In
selected
embodiments of the nutritional or dietary supplement composition of the
present invention,
an effective amount of pantothenic acid (as D-calcium pantothenate) may be
found in the
range of between about 25 mg and about 75 mg. In certain embodiments of the
nutritional
or dietary supplement composition of the present invention, an effective
amount of
pantothenic acid (as D-calcium pantothenate) may comprise 50 mg.
The following examples will illustrate several embodiments of the present
invention
in further detail. It will be readily understood that the nutritional or
dietary supplement
composition of the present invention, as generally described and illustrated
in the Examples
herein, could be synthesized in a variety of formulations and dosage forms.
Thus, the
following more detailed description of the embodiments of the methods,
formulations and
compositions of the present invention, as represented in the Examples are not
intended to
limit the scope of the invention, as claimed, but it is merely representative
of various
contemplated embodiments of the present invention.
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EXAMPLE I
A formulation of one embodiment of the nutritional or dietary supplement of
the
present invention is set forth as:
Amount per serving
Vitamin C (as ascorbic acid) 400 mg - 500 mg
Vitamin E (as natural d-alpha- 200 mg - 800 mg
tocopheryl succinate with
mixed d-alpha, d-beta, d-
gamma and d-delta-
tocopherols and tocotrienols)
Thiamin (as thiamin mononitrate) 25 mg - 75 mg
Riboflavin 25 mg - 75 mg
Niacin (as niacinamide) 25 mg - 75 mg
Vitamin B6 (as pyridoxine HCI) 40 mg - 60 mg
Folate (as folic acid) 500 mcg - 1,500 mcg
Vitamin B12 (As cyanocabalmin) 500 mcg - 1,500 mcg
Biotin 25 mg - 75 mg
Pantothenic acid (as D-calcium 25 mg - 75 mg
pantothenate)
Zinc (as zinc oxide) 50 mg - 100 mg
Copper (as copper gluconate) 1 mg - 4mg
In selected embodiments, the dosage size is two tablets per serving. In
certain embodiments
of the present invention, a method for preventing, stabilizing, treating,
and/or preventing
ocular neovascularization in a subject having or at risk for ocular
neovascularization
comprises the administering to the subject an effective amount of the
composition of
Example I.
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EXAMPLE 11
A formulation of one embodiment of the nutritional or dietary supplement of
the
present invention is set forth as:
Amount per serving
Vitamin C (as ascorbic acid) 400 mg - 500 mg
Vitamin E (as natural d-alpha- 200 mg - 800 mg
tocopheryl succinate with
mixed d-alpha, d-beta, d-
gamma and d-delta-
tocopherols and tocotrienols)
Thiamin (as thiamin mononitrate) 25 mg - 75 mg
Riboflavin 25 mg -75 mg
Niacin (as niacinamide) 25 mg - 75 mg
Vitamin B. (as pyridoxine IICI) 40 mg - 60 mg
Folate (as folic acid) 500 mcg - 1,500 mcg
Vitamin B12 (as cyanocabalmin) 500 mcg - 1,500 mcg
Biotin 25 mg - 75 mg
Pantothenic acid (as D-calcium 25 mg - 75 mg
pantothenate)
Zinc (as zinc oxide) 50 mg - 100 mg
Copper (as copper gluconate) 1 mg - 4mg
Lutein 5 mg - 25 mg
Zeaxanthin 1 mg - 4mg
In selected embodiments, the dosage size is two tablets per serving. In
certain embodiments
of the present invention, a method for preventing, stabilizing, treating,
and/or preventing
ocular neovascularization in a subject having or at risk for ocular
neovascularization
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comprises the administering to the subject an effective amount of the
composition of
Example H.
EXAMPLE III
A formulation of one embodiment of the nutritional or dietary supplement of
the
present invention is set forth as:
Amount per serving % Daily Value
Vitamin C (as ascorbic acid) 500 mg 833%
Vitamin E (as natural d-alpha- 400 Mg 1,333%
tocopheryl succinate with
mixed d-alpha, d-beta, d-
gamma and d-delta-
tocopherols and tocotrienols)
Thiamin (as thiamin mononitrate) 50 mg 3,333%
Riboflavin 50 mg 2,941%
Niacin (as niacinamide) 50 mg 250%
Vitamin B6 (as pyridoxine HCl) 50 mg 2,500%
Folate (as folic acid) 1,000 mcg 250%
Vitamin B12 (As cyanocabalmin) 1,000 mcg 16,667%
Biotin 50 mg 17%
Pantothenic acid (as D-calcium 50 mg 500%
pantothenate)
Zinc (as zinc oxide) 50 mg 333%
Copper (as copper gluconate) 2 mg 100%
In selected embodiments, the dosage size is two tablets per serving. In
certain embodiments
of the present invention, a method for preventing, stabilizing, treating,
and/or preventing
ocular neovascularization in a subject having or at risk for ocular
neovascularization
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comprises the administering to the subject an effective amount of the
composition of
Example III.
EXAMPLE IV
A formulation of one embodiment of the nutritional or dietary supplement of
the
present invention is set forth as:
Amount per serving % Daily
Vitamin C (as ascorbic acid) 500 mg 833%
Vitamin E (as natural d-alpha- 400 Mg 1,333%
tocopheryl succinate with
mixed d-alpha, d-beta, d-
gamma and d-delta-
tocopherols and tocotrienols)
Thiamin (as thiamin mononitrate) 50 mg 3,333%
Riboflavin 50 mg 2,941%
Niacin (as niacinamide) 50 mg 250%
Vitamin. B6 (as pyridoxine HC1) 50 mg 2,500%
Folate (as folic acid) 1,000 meg 250%
Vitamin B12 (As cyanocabalmin) 1,000 mcg 16,667%
Biotin 50 mg 17%
Pantothenic acid (as D-calcium 50 mg 500%
pantothenate)
Zinc (as zinc oxide) 50 mg 333%
Copper (as copper gluconate) 2 mg 100%
Lutein 10 mg
Zeaxanthin 2 mg
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In selected embodiments, the dosage size is two tablets per serving. In
certain embodiments
of the present invention, a method for preventing, stabilizing, treating,
and/or preventing
ocular neovascularization in a subject having or at risk for ocular
neovascularization
comprises the administering to the subject an effective amount of the
composition of
Example IV.
The present invention may be embodied in other specific forms without
departing
from its fundamental functions or essential characteristics. The described
embodiments are
to be considered in all respects only as illustrative, and not restrictive.
All changes which
come within the meaning and range of equivalency of the illustrative
embodiments are to be
embraced within their scope.
