Note: Descriptions are shown in the official language in which they were submitted.
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NUTRITIONAL DRINK
FIELD OF THE INVENTION
[0002] This invention relates to nutritional supplements. More particularly,
the invention
relates to compositions and methods for supplementing the diet for improving
health and
preventing disease.
BACKGROUND
[0003] Chronically elevated blood levels of cholesterol lead to cardiovascular
disease as
the cholesterol finds its way into the walls of blood vessels and damages
them. This ultimately
results in symptoms of chronic arterial insufficiency such as angina and
claudication on the one
hand, and acute vascular insufficiency, such as heart attack and stroke on the
other.
[0004] Over $120 billion dollars is spent on direct and indirect costs
associated with
cardiovascular disease annually in the United States alone. Cardiovascular
disease incidence
increases with serum LDL cholesterol in a log linear fashion and more
importantly declines with
treatment-induced reduction of serum LDL cholesterol.
[0005] Conventional therapy for elevated blood cholesterol levels takes the
form of four
classes of FDA approved medications: statins, bioresins, fibrates, and niacin.
[0006] Of these, statins are the most widely used with greater than $20
billion in annual
sales; however, all the classes, including statins, have side effects and at
higher doses, that are
necessary to achieve targets, result in side effects that limit their utility.
This is especially so of
niacin and statins.
[0007] Recently, it has been appreciated that in attempting to lower
cholesterol, two or
more drugs with different mechanisms of action can lower toxicity and produce
synergy in the
cholesterol lowering effect. Vytorin, a recently introduced combination of
Zetia and Simvastatin,
CA 02717157 2010-10-07
has been shown to decrease cholesterol absorption and synthesis and reduce
cholesterol better
than the sum of the expected reduction of either drug alone. This is explained
by a phenomenon I
refer to as "escape homeostasis." When one pathway to cholesterol elevation is
blocked, an
alternative pathway is often enhanced by the body, so that the overall
cholesterol levels are
maintained. There is, thus, a built-in or automatic drug resistance that can
only be overcome with
multiple active agents working simultaneous at different sites. It is
noteworthy that evidence
exists that even homeopathic, previously felt sub-therapeutic amounts of
biologically active
cholesterol lowering compounds can exert powerful efficacy with minimal side
effects when
combined with other agents that work by alternative pathways.
SUMMARY
[0008] The invention is based on the development of a cholesterol lowering
beverage that
utilizes multiple mechanisms and sites of action to reduce cholesterol and
also has ingredients
that reduce toxicity, increase the rate of metabolism both on a general and a
cellular level and,
finally stimulate compliance by causing a sense mild euphoria and well-being,
as well as
enhancing metabolism.
[0009] Accordingly, in one aspect, the invention features a nutritional
beverage that
includes water and at least two active ingredients selected from among the
following: niacin, a
phytosterol component, red yeast rice, coenzyme Q10, L-carnitine, and ascorbic
acid.
[0010] In another aspect, the invention features the beverage being
administered to a
human subject twice daily in two servings.
[0011] In another aspect, the invention features the two daily servings being
stored in a
single container.
[0012] In another aspect, the invention features each serving of the beverage
including
about 5 to 100 mg of niacin.
[0013] In another aspect, the invention features each serving of the beverage
including
about 500 to 1,500 mg of the phytosterol component.
[0014] In another aspect, the invention features each serving of the beverage
including
about 300 to 1,500 mg of red yeast rice.
[0015] In another aspect, the invention features each serving of the beverage
including
about 50 to 250 mg of L-carnitine.
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[0016] In another aspect, the invention features each serving of the beverage
including
about 300 to 1,200 mg of ascorbic acid.
[0017] In another aspect, the invention features each serving of the beverage
including
about 10 to 200 mg of coenzyme Q10.
[0018] In another aspect, the invention features each serving of the beverage
including
less than about 50 mg of niacin.
[0019] In another aspect, the invention features the phytosterol component
including at
least one phytosterol ester.
[0020] In another aspect, the invention features the beverage including at
least three
active ingredients selected from among the following: niacin, a phytosterol
component, red yeast
rice, coenzyme Q 10, L-carnitine, and ascorbic acid.
[0021] In another aspect, the invention features the beverage including at
least four active
ingredients selected from among the following: niacin, a phytosterol
component, red yeast rice,
coenzyme Q 10, L-carnitine, and ascorbic acid.
[0022] In another aspect, the invention features the beverage including at
least five active
ingredients selected from among the following: niacin, a phytosterol
component, red yeast rice,
coenzyme Q10, L-carnitine, and ascorbic acid.
[0023] In another aspect, the invention features the beverage including
niacin, a
phytosterol component, red yeast rice, coenzyme Q10, L-carnitine, and ascorbic
acid.
[0024] In another aspect, the invention features the beverage including
maltodextrin.
[0025] In another aspect, the invention features the beverage including two
daily
servings. Each serving can include as ingredients water, about 5 to 50 mg of
niacin, about 500 to
1,500 mg of at least one phytosterol ester, about 300 to 1,500 mg of red yeast
rice, about 10 to
200 mg of coenzyme Q10, about 50 to 250 mg of L-carnitine, and about 300 to
1,200 mg of
ascorbic acid.
[0026] In another aspect, the invention features two servings of the beverage
being
packaged in a container.
[0027] In another aspect, the invention features the beverage including water,
about 50 to
200 mg of niacin, about 1,400 to 4,000 mg of a phytosterol component, about
1,200 to 4,800 mg
of red yeast rice, about 20 to 400 mg of coenzyme Q10, about 400 to 2,000 mg
of L-carnitine,
and about 200 to 4,000 mg of ascorbic acid.
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[0028] The invention also features a method that includes the step of
administering to a
subject for at least 7 days a beverage comprising water and at least two
active ingredients
selected from among the following: niacin, a phytosterol component, red yeast
rice, coenzyme
Q 10, L-camitine, and ascorbic acid.
[0029] In another aspect, the method also features the step of administering
the beverage
to the subject twice daily.
[0030] The invention also features a composition for reducing blood
cholesterol. The
composition includes niacin, a phytosterol component, red yeast rice, coenzyme
Q10, L-
carnitine, and ascorbic acid.
[0031] Unless otherwise defined, all technical terms used herein have the same
meaning
as commonly understood by one of ordinary skill in the art to which this
invention belongs.
Although methods and materials similar or equivalent to those described herein
can be used in
the practice or testing of the present invention, suitable methods and
materials are described
below. All publications, patent applications, patents and other references
mentioned herein are
incorporated by reference in their entirety. In the case of conflict, the
present specification,
including definitions will control.
DETAILED DESCRIPTION
[0032] The invention provides an aqueous composition of ingredients and
dietary
supplements to yield a cholesterol lowering drink. The composition is
typically contained within
a two-serving container such as a can or bottle and includes water and a
combination of at least
two of niacin, a phytosterol component, red yeast rice, coenzyme Q10, L-
carnitine, and ascorbic
acid in amount effective to reduce serum cholesterol levels in a subject who
drinks the
composition on a regular basis (e.g., once a day, twice a day, every two days,
or every three
days).
[0033] The active ingredients are preferably included at a concentration
effective to
reduce a subject's serum cholesterol by at least 10% (e.g., at least 20, 30,
40, or 50%) when
included in combination with each other and administered to the subject on a
regular basis (e.g.,
twice a day or once a day for at least 2, 3, 4, 5, 6, 12, or 24 weeks). In an
exemplary
embodiment, the composition can be administered twice daily to the subject in
the form of and as
part of a beverage, e.g., as a nutritional drink.
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[0034] Niacin lowers cholesterol by inhibiting lipoprotein formation or
release in the
liver. Phytosterols lower cholesterol by competing for absorption in the
intestines. Red Yeast
Rice is a dietary supplement and coloring agent that has been used in Chinese
food and
medicines for centuries. It decreases synthesis and absorption of cholesterol,
produces red
coloration which stimulates appetite, compliance, and metabolism. On a
cellular level, L-
carnitine and coenzyme Q 10 enhance transport of fatty acids to the
mitochondria and enhance
the burning of fatty acids respectively. L-carnitine can also cause a mild
sense of euphoria, a
beneficial effect that may result in greater compliances with the preparation
containing it.
Ascorbic acid changes the constitution of bile to decrease cholesterol
absorption and inhibit the
HMG-CoA reductase pathway, the rate-limiting step in cholesterol biosynthesis.
[0035] In an exemplary embodiment, the phytosterol component can include one
or more
phytosterol esters.
[0036] In one embodiment, the beverage can include 6.9 g of a composition in
an 8-
ounce serving. The beverage can be packaged in a bottle or other container
that contains two
servings. The composition can include the following ingredients in each 8-
ounce serving: about
12.5 mg of niacin (niacinamide), about 500 mg of vitamin C (ascorbic acid),
about 150 mg of L-
carnitine (L-carnitine-L-tartrate), about 25 mg of coenzyme Q 10, about 660 mg
of phytosterol
esters, and q.s. maltodextrin. Servings of the beverage can be consumed twice
daily, for
example, one serving in the morning and one serving at night.
[0037] In another embodiment, the beverage can include 8.2 g of a composition
in an 8-
ounce serving. The beverage can be packaged in a bottle or other container
that contains two
servings. The composition can include the following ingredients in each 8-
ounce serving: about
600 mg of red yeast rice powder, about 12.5 mg of niacin (niacinamide), about
500 mg of
vitamin C (ascorbic acid), about 150 mg of L-carnitine (L-carnitine-L-
tartrate), about 25 mg of
coenzyme Q10, about 660 mg of phytosterol esters, and q.s. maltodextrin.
Servings of the
beverage can be consumed twice daily, for example, one serving in the morning
and one serving
at night.
[0038] Although 8-ounce servings are described herein, the serving size can be
different
as long as the amounts of each ingredient remain consistent. For example, each
serving can be 6,
7, 7.5, 8.5, 9, 10, 12, 13, 14, or 16 ounces.
[0039] Each serving of the composition can include niacin in the amounts of
about 4.5, 5,
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6, 6.1, 6.5, 6.6, 6.9, 7, 7.5, 8, 9, 9.9, 10, 10.1, 10.5, 11, 11.5, 11.9, 12,
12.1, 12.5, 12.6, 12.9, 13,
15, 19, 20, 25, 30, 40, 50, 60, 70, 75, 80, 90, 99, 100, 101, or 110 mg or
more. In exemplary
embodiments, each serving of the composition can contain less than about 50 mg
of niacin. In
one exemplary embodiment, each serving of the composition can contain about
12.5 mg of
niacin.
[0040] Each serving of the composition can include phytosterol esters in the
amounts of
about 300, 400, 500, 550, 600, 625, 640, 649, 651, 660, 675, 700, 800, 900,
1,000, 1,250, 1,320,
1,500, 1,800, 1,900, 1,950, 1,999, 2,000, 2,001, 2,050, or 2,100 mg or more.
In exemplary
embodiments, each serving of the composition can contain about 660 mg of
phytosterol esters.
[0041] Each serving of the composition can include coenzyme Q in the amounts
of about
8, 9, 10, 13, 15, 17, 19, 20, 22.5, 24, 24.5, 24.9, 25, 25.1, 25.5, 26, 27,
27.5, 28, 29, 30, 35, 40,
45, 50, 55, 75, 90, 100, 150, 200, 250, or 300 mg or more. In exemplary
embodiments, each
serving of the composition can contain about 25 mg of coenzyme Q.
[0042] Each serving of the composition can include L-carnitine in the amounts
of about
90, 95, 100, 110, 115, 125, 135, 140, 145, 149, 149.1, 149.9, 150, 150.1,
150.5, 151, 153, 155,
160, 170, 175, 180, 190, 200, 250, 300, 400, or 500 mg or more. In exemplary
embodiments,
each serving of the composition can contain about 75-150 mg of L-carnitine. In
one exemplary
embodiment, each serving of the composition can contain about 150 mg of L-
carnitine.
[0043] Each serving of the composition can include ascorbic acid in the
amounts of about
50, 100, 200, 250, 300, 400, 450, 475, 490, 499, 499.1, 500, 500.1, 500.5,
501, 510, 520, 535,
550, 600, 625, 640, 649, 651, 660, 675, 700, 800, 900, 1,000, 1,500, or 2,000
mg or more. In
exemplary embodiments, each serving of the composition can contain about 500
mg of ascorbic
acid.
[0044] Each serving of the composition can include red yeast rice in the
amounts of
about 300, 400, 500, 550, 575, 590, 595, 599, 599.1, 599.9, 600, 600.1, 600.5,
601, 610, 620,
625, 640, 650, 660, 675, 700, 800, 900, 1,000, 1,250, 1,500, 1,800, 1,900,
1,950, 1,999, 2,000,
2,001, 2,050, 2,100, or 2,400 mg or more. In exemplary embodiments, each
serving of the
composition can contain about 600 mg of red yeast rice.
[0045] The composition can also feature maltodextrin making up the remainder
of any
6.9 g, 8.2 g, or other amount of the composition premixture before the
addition of water to create
the beverage. The beverage may also contain artificial or natural flavorings
and colorings.
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Example 1
[0046] A beverage for administration twice daily to a human subject can
include two
servings stored in a container such as, for example, a bottle. Each serving of
the beverage can
include water (100-500 ml) and 6.9 g of the composition. The composition can
include as
ingredients phytosterol esters (about 660 mg), niacin (less than about 50 mg),
coenzyme Q 10
(about 25 mg), ascorbic acid (about 500 mg), L-carnitine (about 75-150 mg),
and maltodextrin
(q.s.).
Example 2
[0047] A beverage for administration twice daily can include two servings
stored in a
container such as, for example, a bottle or can. Each serving of the beverage
can include water
(about 100 to 500 ml) and 8.2 g of the composition. As ingredients, the
composition can feature
phytosterol esters (about 660 mg), niacin (less than about 50 mg), red yeast
rice (about 600 mg),
coenzyme Q10 (about 25 mg), ascorbic acid (about 500 mg), L-camitine (about 75-
150 mg), and
maltodextrin (q.s.).
[0048] In an exemplary method of the invention, the composition can be
administered to
a human subject at least twice daily in the form of a beverage or nutritional
drink. The two daily
doses of the beverage can be contained within a single container such as, for
example, a bottle or
can. In another embodiment, each serving of the beverage can be packaged in a
separate bottle
or container. The beverage can be administered twice daily for at least 7
days. The beverage can
include water and at least two active ingredients selected from among the
following: niacin, a
phytosterol component, red yeast rice, coenzyme Q 10, L-carnitine, and
ascorbic acid.
[0049] In another method of the invention, the composition may be administered
at an
interval different than twice daily, e.g., once, three times, or four times
daily.
[0050] In still another method of the invention, the composition can be
administered to a
human subject to reduce the subject's blood cholesterol levels.
Other Embodiments
[0051] It is to be understood that while the invention has been described in
conjunction
with the detailed description thereof, the foregoing description is intended
to illustrate and not
limit the scope of the invention, which is defined by the scope of the
appended claims. Other
aspects, advantages, and modifications are within the scope of the following
claims.
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