U.S. patent application number 09/789150 was filed with the patent office on 2001-10-25 for composition and method for reducing serum cholesterol levels.
Invention is credited to Sorkin, Harlan Lee JR..
Application Number | 20010034338 09/789150 |
Document ID | / |
Family ID | 23563407 |
Filed Date | 2001-10-25 |
United States Patent
Application |
20010034338 |
Kind Code |
A1 |
Sorkin, Harlan Lee JR. |
October 25, 2001 |
Composition and method for reducing serum cholesterol levels
Abstract
A composition and method for reducing serum cholesterol in
humans and animals is provided. The method comprises administering
phytosterol and policosanol which together produce a synergistic
effect in lowering serum cholesterol levels. Preferably the
administered composition includes about 3.2:1 parts by weight of
phytosterol and policosanol.
Inventors: |
Sorkin, Harlan Lee JR.;
(Champaign, IL) |
Correspondence
Address: |
Cummings & Lockwood
Granite Square
700 State Street
P.O. Box 1960
New Haven
CT
06509-1960
US
|
Family ID: |
23563407 |
Appl. No.: |
09/789150 |
Filed: |
February 20, 2001 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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09789150 |
Feb 20, 2001 |
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09395524 |
Sep 14, 1999 |
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6197832 |
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Current U.S.
Class: |
514/171 ;
514/729 |
Current CPC
Class: |
A61K 36/899 20130101;
A61K 45/06 20130101; A61K 2300/00 20130101; A61K 2300/00 20130101;
A61K 31/575 20130101; A61K 36/899 20130101; A61K 31/575
20130101 |
Class at
Publication: |
514/171 ;
514/729 |
International
Class: |
A61K 031/575; A61K
031/045 |
Claims
I claim:
1. A composition for reducing serum cholesterol levels in humans
and animals, said composition comprising: from about 5% to about
75% by weight of phytosterol, from about 1% to about 60% by weight
of policosanol, and from 0% to about 65% by weight of
pharmaceutically acceptable formulation aids.
2. The composition of claim 1, wherein the composition comprises
from about 10% to about 60% by weight of phytosterol, and from
about 3% to about 46% by weight of policosanol.
3. The composition of claim 1, wherein the composition comprises
about 3.2:1 parts by weight of phytosterol and policosanol.
4. The composition of claim 1, wherein the formulation aids
comprise diluents, stabilizers, binders, buffers, lubricants,
coating agents, preservatives, emulsifiers, and suspension
agents.
5. A method for reducing serum cholesterol levels in humans and
animals by administering to at least one of a human and an animal
from about 5% to about 75% by weight of phytosterol, from about 1%
to about 60% by weight of policosanol, and from 0% to about 65% by
weight of pharmaceutically acceptable formulation aids.
6. The method of claim 5, further comprising administering a
mixture including from about 10% to about 60% by weight of
phytosterol, and from about 3% to about 46% by weight of
policosanol.
7. The method of claim 5, further comprising administering about
3.2:1 parts by weight of phytosterol and policosanol.
8. The method of claim 5, further comprising administering
formulation aids selected from the group including diluents,
stabilizers, binders, buffers, lubricants, coating agents,
preservatives, emulsifiers and suspension agents.
Description
[0001] This application is a continuation of application Ser. No.
09/395,524 filed on Sep. 14, 1999.
FIELD OF THE INVENTION
[0002] The present invention relates generally to compositions and
methods for reducing serum cholesterol levels and, more
particularly, to a composition and method for lowering serum
cholesterol by administering policosanols and phytosterols.
BACKGROUND OF THE INVENTION
[0003] Elevated serum cholesterol levels (>200 mg/dL) have been
indicated as a major risk factor for heart disease, the leading
cause of death among Americans. As a result, experts have
recommended that those individuals at high risk decrease serum
cholesterol levels through dietary changes, a program of physical
exercise, and lifestyle changes. It is recommended that the intake
of saturated fat and dietary cholesterol be strictly limited and
that soluble fiber consumption be increased. Strictly limiting the
intake of saturated fat and cholesterol does not, itself, present a
risk to proper health and nutrition. Even where saturated fat and
cholesterol are severely restricted from the diet, the liver
remains able to synthesize sufficient quantities of cholesterol to
perform necessary bodily functions.
[0004] More recently, experts have begun to examine the individual
components of the lipid profile, in addition to the total
cholesterol level (TC). While an elevated TC is a risk factor, the
levels of the various forms of cholesterol which make up TC may
also be risk factors. Elevated low-density lipoprotein (LDL) is a
cause for concern, as these loosely packed lipoproteins are more
likely to lodge within the cardiovascular system leading to the
formation of plaque. Low levels of high-density lipoproteins (HDL)
are an additional risk factor, as they serve to sweep artery
clogging cholesterol from the blood stream. A better indication of
risk appears to be the ratio of TC:HDL.
[0005] A number of nutritional factors have been shown to improve
serum cholesterol levels. For example, the use of phytosterols has
been well documented in human clinical trials and in animal studies
to lower serum cholesterol levels. This cholesterol lowering effect
has been attributed to interference with the absorption of dietary
cholesterol. Phytosterols, being structurally similar to
cholesterol, competitively bind with cholesterol sterol receptor
sites, thus preventing cholesterol uptake. Unlike their cholesterol
counterparts, phytosterols are very poorly absorbed, and some are
not absorbed at all. Therefore, phytosterols do not contribute to
an increase in serum cholesterol levels. In addition to competing
for receptor sites, phytosterols also compete for the enzyme
cholesterol esterase. This enzyme is required by cholesterol for
its breakdown to components which may be absorbed through the
microvilli which line the wall of the small intestine. Thus,
phytosterols also impede the enzymatic breakdown and intestinal
absorption of cholesterol, which further reduces serum cholesterol
levels.
[0006] Plant derived long-chained aliphatic alcohols have also been
documented to reduce serum cholesterol levels in experimental
models, healthy humans and in type II hypercholesterolemic
patients. These aliphatic alcohols, collectively known as
policosanol, have been employed in the treatment of elevated serum
cholesterol levels in only the past five years, but policosanol has
shown much promise, as reported in a number of published human
clinical trials. The mechanism of action has not yet been
elucidated, but policosanol's effectiveness is attributed to its
influence on the bio-synthesis of cholesterol within the liver.
This accounts for the ability of policosanol not only to decrease
total cholesterol, but also to decrease LDL serum levels and
increase HDL levels.
SUMMARY OF THE INVENTION
[0007] The present invention provides a composition for reducing
serum cholesterol levels in humans and animals, and a method for
reducing serum cholesterol levels in humans and animals by
administering the composition. The composition comprises from about
5% to about 75% by weight of phytosterol, and from about 1% to
about 60% by weight of policosanol. The composition further
comprises from 0% to about 65% by weight of pharmaceutically
acceptable formulation aids, such as diluents, stabilizers,
binders, buffers, lubricants, coating agents, preservatives,
emulsifiers and suspension agents.
[0008] In a preferred embodiment, the composition comprises from
about 10% to about 60% by weight of phytosterol, and from about 3%
to about 46% by weight of policosanol. In the most preferred
embodiment of the invention, the composition comprises about 3.2:1
parts by weight of phytosterol and policosanol.
DETAILED DESCRIPTION OF THE INVENTION
[0009] As noted previously, policosanol is a mixture of
high-molecular weight aliphatic alcohols. These alcohols occur
naturally in wax form and are characterized by fatty alcohol chains
ranging from 20 to 39 carbon atoms in length. The major component
of policosanol are the aliphatic alcohols octacosanol and
triacontanol. Policosanol is isolated from a number of different
plant sources, including sugar cane wax and rice bran wax. The
policosanol used in the preferred embodiment of the invention is
obtained from rice bran wax and has the formulation set forth below
in Table I. This material is sold under the name "Rice Bran Wax"
and is available from Traco Labs, Inc. It should be understood,
however, that the invention is not limited in this regard and that
policosanol commonly available from other naturally occurring
sources may be utilized.
1TABLE I Rice Bran Wax typical long-chain aliphatic alcohol
profile: Carbon Fatty Alcohol Composition (%) C.sub.22OH Docosanol
(Behenyl Alcohol) 0.36 C.sub.24OH Tetracosanol (Lignoceryl Alcohol)
3.21 C.sub.26OH Hexacosanol (Cerotyl Alcohol) 2.93 C.sub.28OH
Octacosanol (Montanyl Alcohol) 5.59 C.sub.30OH Triacontanol
(Melissyl Alcohol) 8.35 C.sub.32OH Dotriacontanol 4.64 C.sub.34OH
Tetratriacontanol 2.22 C.sub.36OH Hexatriacontanol .50 Total
policosanols 23-33%
[0010] Phytosterols are also mixtures of long-chained aliphatic
alcohols in a wax form. They are naturally occurring in many common
vegetable food products. The particular phytosterol used in the
preferred embodiment of the invention is derived from vegetable oil
and has the formulation set forth in Table II. This material is
sold under the trademark "CHOLESTATIN" and is available from Traco
Labs, Inc. Again, however, it should be understood that the
invention is not limited to this particular phytosterol product,
and that any number of other commonly available phytosterols can be
used.
2TABLE II Phytosterol composition: Total sterols 88% Min. Assay
Specification B-Sitosterol 43% Min. campesterol 25% Min.
stigmasterol 15% Min.
[0011] As noted previously, phytosterol and policosanol lower serum
cholesterol links by two independent and unrelated mechanisms of
action. However, both compounds together are expected to have a
synergistic effect on lowering serum cholesterol. As previously
mentioned, phytosterols impede the enzymatic breakdown and
intestinal absorption of cholesterol, which reduces serum
cholesterol levels. Policosanol acts directly on the cholesterol
synthesis pathway itself, thereby inhibiting the bio-synthesis of
cholesterol from saturated fat. However, both compounds together
are expected to have a synergistic effect on lowering serum
cholesterol levels. Thus, the combination of both phytosterol and
policosanol into a single composition is expected to provide a more
effective treatment for elevated serum cholesterol than would be
expected from the additive effect of both components.
[0012] Examples of compositions made according to the invention is
set forth below:
EXAMPLE 1
[0013]
3 tablet formula: ingredient amt/cap function "CHOLESTATIN" (Min.
88% phytosterols) 250 mg active "Rice Bran Wax" (23-33%
policosanols) 250 mg active Calcium phosphate 261.7 mg base
Cellulose 49.4 mg tablet coating agent Stearic acid 23.8 mg
lubricant Magnesium stearate 6.8 mg lubricant Silicon dioxide 9.4
mg diluent
EXAMPLE 2
[0014]
4 Soft gelatin capsule formulation: ingredient amt/cag function
"CHOLESTATIN" (Min. 88% 250 mg active phytosterols) "Rice Bran Wax"
(23-33% policosanols) 250 mg active Medium Chain Triglycerides 700
mg diluent/emulssifying suspending agent
[0015] Previous clinical and toxicological testing of policosanol
and phytosterol has shown that the tolerance of both components is
good. Significantly larger doses of both waxes are readily
tolerated. Occasional GI irritation might be expected at extremely
high doses, far greater than the normal dosage range. In the event
such irritation should occur, it would be expected to be minimal,
and would not pose any risk to health.
[0016] Toxicology performed on the 50% phytosterol/50% rice bran
wax composition has proven that the composition is non-toxic at an
oral dose of 5000 mg/kg of body weight in Sprague-Dawley rats.
Accordingly, oral dosages in humans of up to a maximum dosage of
1500 mg administered three times per day is considered
appropriate.
[0017] While preferred embodiments have been shown and described,
various modifications and substitutions may be made without
departing from the spirit and scope of the invention. Accordingly,
it is to be understood that the present invention has been
described by way of example and not by limitation.
* * * * *