U.S. patent application number 11/023871 was filed with the patent office on 2005-05-19 for formulation for menopausal women.
Invention is credited to Hermelin, Marc S., Kirschner, Mitchell I., Levinson, R. Saul.
Application Number | 20050106266 11/023871 |
Document ID | / |
Family ID | 23618887 |
Filed Date | 2005-05-19 |
United States Patent
Application |
20050106266 |
Kind Code |
A1 |
Levinson, R. Saul ; et
al. |
May 19, 2005 |
Formulation for menopausal women
Abstract
The present disclosure relates to novel compositions which
provide improved nutritional support for premenopausal and
menopausal women and/or relief from systems associated with
menopause, as well as prophylactic effects, and methods for using
same.
Inventors: |
Levinson, R. Saul;
(Chesterfield, MO) ; Hermelin, Marc S.; (Glendale,
MO) ; Kirschner, Mitchell I.; (St. Louis,
MO) |
Correspondence
Address: |
BLACKWELL SANDERS PEPER MARTIN LLP
720 OLIVE STREET
SUITE 2400
ST. LOUIS
MO
63101
US
|
Family ID: |
23618887 |
Appl. No.: |
11/023871 |
Filed: |
December 22, 2004 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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11023871 |
Dec 22, 2004 |
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10131236 |
Apr 25, 2002 |
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10131236 |
Apr 25, 2002 |
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09409059 |
Sep 30, 1999 |
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6479545 |
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Current U.S.
Class: |
424/682 ;
514/560 |
Current CPC
Class: |
A61P 15/00 20180101;
A23L 33/15 20160801; A61K 45/06 20130101; A61P 1/10 20180101; A23L
33/12 20160801; A61P 15/12 20180101; A61P 25/02 20180101; A61P
21/00 20180101; A61P 25/20 20180101; A61P 3/02 20180101; A61P 5/34
20180101; A61P 25/24 20180101; A23L 33/16 20160801; A61P 29/02
20180101; A61P 19/02 20180101; A61P 9/00 20180101; Y10S 514/899
20130101; A61P 1/12 20180101; A23V 2002/00 20130101; A61P 1/08
20180101; A61P 5/30 20180101; A61P 25/22 20180101; A23V 2002/00
20130101; A23V 2250/211 20130101; A23V 2250/70 20130101; A23V
2250/156 20130101; A23V 2250/1868 20130101; A23V 2250/1874
20130101; A23V 2250/1872 20130101; A23V 2002/00 20130101; A23V
2250/71 20130101; A23V 2250/712 20130101; A23V 2250/708 20130101;
A23V 2250/704 20130101; A23V 2002/00 20130101; A23V 2250/1578
20130101; A23V 2250/1588 20130101; A23V 2250/1642 20130101; A23V
2250/1626 20130101; A23V 2002/00 20130101; A23V 2250/18 20130101;
A23V 2250/30 20130101; A23V 2250/704 20130101; A23V 2250/1592
20130101; A23V 2250/161 20130101; A23V 2250/1578 20130101; A23V
2200/224 20130101; A23V 2002/00 20130101; A23V 2200/224 20130101;
A23V 2250/5432 20130101 |
Class at
Publication: |
424/682 ;
514/560 |
International
Class: |
A61K 033/06; A61K
031/202 |
Claims
What is claimed is:
1. A composition for supplementing the diet, the composition
comprising: a. docosahexaenoic acid in an amount of from about 10
mg to about 1000 mg; and b. a calcium compound present in an amount
such that the ratio of docosahexaenoic acid to calcium compound is
from about 1:0.4 to 1:250.
2. A composition for administration to premenopausal and menopausal
women, the composition comprising: a. docosahexaenoic acid in an
amount of from about 10 mg to about 1000 mg; and b. a calcium
compound present in an amount such that the ratio of
docosahexaenoic acid to calcium compound is from about 1:0.4 to
1:250.
3. A method for providing nutritional supplementation to a
menopausal woman, which comprises: a. docosahexaenoic acid in an
amount of from about 10 mg to about 1000 mg; and b. a calcium
compound present in an amount such that the ratio of
docosahexaenoic acid to calcium compound is from about 1:0.4 to
1:250.
4. A method for providing nutritional supplementation to a
premenopausal woman, which comprises: a. docosahexaenoic acid in an
amount of from about 10 mg to about 1000 mg; and b. a calcium
compound present in an amount such that the ratio of
docosahexaenoic acid to calcium compound is from about 1:0.4 to
1:250.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation application of U.S.
patent application Ser. No. 10/131,236, filed Apr. 25, 2002; said
application being a continuation of U.S. patent application Ser.
No. 09/409,059, filed Sep. 30, 1999 now issued as U.S. Pat. No.
6,479,545, the entire contents of which are hereby incorporated by
reference in their entirety.
BACKGROUND OF THE INVENTION
[0002] The present invention is directed to novel compositions for
use by premenopausal women and menopausal women for the purpose of
providing improved nutritional support and/or relief from the
symptoms of menopause, as well as to methods for using same.
[0003] Menopause, the transition from the reproductive stage to the
non-reproductive stage of a woman's life, is characterized
primarily by the cessation of menstruation. However, menopause has
come to signify much more than simply the loss of reproductive
capability, as it is also associated with a number of acute and
chronic conditions. Menopausal syndrome consists of a number of
varying and often highly distressing symptoms resulting from
hormonal imbalance and nutritional deficiency in the female
body.
[0004] Hot flashes and sweating secondary to vasomotor instability
affect 75% of women. Psychologic and emotional symptoms of fatigue,
insomnia, irritability and nervousness are common. Lack of sleep
due to disturbance by recurring hot flashes contributes to fatigue
and irritability. Dizziness, parenthesis and cardiac symptoms of
palpitations and tachycardia may also occur; the incidence of heart
disease increases. Other common symptoms include nausea,
constipation, diarrhea, arthralgia and myalgia. The Merck Manual,
1793 (16.sup.th Ed. 1992).
[0005] Menopause is also characterized by osteoporosis, or loss of
bone density, resulting in increased bone fractures and vertebral
column collapse. Bone loss begins around age 35. This loss
accelerates during menopause, which generally occurs around age 45
to 55. Bone mass losses average 1-2% each year after menopause.
Primary sites are the vertebrae, which show anterior collapse
resulting in stooping and backache, the hips and the wrist. The
Merck Manual 1793(16.sup.th Ed. 1992). Osteoporosis develops over
decades and is related to peak bone mass, as well as to the degree
of bone loss.
[0006] Estrogen replacement therapy has been used to relieve the
symptoms of menopause. The Merck Manual 1793(16.sup.th Ed. 1992).
However, estrogen therapy is not without its limitations. In some
instances the side effects of estrogen therapy can be quite severe.
These side effects include increased risk of certain cancers, such
as breast cancer. Estrogen has also been implicated in certain
endometrial cancers. Although treatments with progestin have been
shown to counter these adverse side effects, postmenopausal women
treated with such an estrogen-progestin regimen frequently
experience undesirable uterine bleeding. Further, hormone therapy
alone is insufficient to meet the varied and heightened nutritional
requirements of a woman during this phase in her life. Adequate
nutritional intake is also necessary.
[0007] Appropriate nutritional intake is increasingly important to
menopausal women. For example, adequate calcium intake prevents
osteoporosis. Moreover, certain vitamins and minerals enhance
calcium absorption and utilization. However, while vitamin and
mineral supplements providing calcium for women is known in the
art, conventional supplements fail to meet other nutritional
requirements of menopausal women. Specifically, conventional
supplements lack certain fatty acids which are especially useful to
treat symptoms of fatigue or tiredness commonly experienced by a
woman undergoing menopause. Fatty acids are essential in supporting
life's activities as the body derives most of its energy from
triglycerides, a molecule of glycerol with three fatty acids.
Linoleic acid and linolenic acid, in particular, are two fatty
acids which are indispensable to body functions. The inclusion of
these two fatty acids in nutritional supplements is of particular
significance because they are not produced by the body and must be
supplied through food. However, conventional nutritional
supplements fail to include these two fatty acids.
[0008] The use of fatty acids in various forms and for various
purposes has been previously disclosed. Horrobin et al. disclose a
method of prevention or treatment of endometriosis wherein
effective amounts of one or both gamma-linolenic acid and/or
dihomo-gamma-linolenic acid are administered to women.
Specifically, the fatty acids may be administered in the form of
the acid itself or as an ester, amide, salt or any other functional
derivative capable of being converted to the acid within the body
and may be from natural or synthetic sources.
[0009] Maxson et al., U.S. Pat. No. 4,900,734, disclose a
pharmaceutical composition containing estradiol and progesterone
for oral administration. Specifically, the pharmaceutical
composition comprises estradiol dissolved in an oil vehicle
containing a suspension of micronized progesterone. Further, the
oil vehicle is high in glycerides of polyunsaturated fatty acids.
Specifically, linoleic and linolenic acids are disclosed as
particularly effective polyunsaturated fatty acids. The combined
administration of these steroids is disclosed as being useful for
replacement hormone therapy in the treatment of menopausal
women.
[0010] Cohen, U.S. Pat. No. 4,945,103, discloses a method for
treating women who suffer from premenstrual syndrome (PMS) which
comprise administration of melatonin in sufficient doses to relieve
symptoms associated with PMS. Specifically, Cohen discloses that
progestogen can be administered in combination with melatonin.
Further, melatonin can administered to women orally, parenterally
or in the form of an implant. Cohen specifically discloses that PMS
may be linked to a nutritional deficiency in either vitamin
B-complex, especially vitamin B6 (pyroxidine), or essential fatty
acids, especially linolenic acid.
[0011] Horrobin, U.S. Pat. No. 5,380,757, discloses a method of
treatment of vulvar dystrophy and/or vaginal dryness, which
medicament comprises gamma-linolenic (GIA) and/or
dihomo-gamma-linolenic acid (DGIA), optionally in association with
other essential fatty acids of the n-6 or n-3 series. Horrobin
discloses that deficiency of linoleic acid in the diet may produce
atrophy and hyperkeratosis of the skin.
[0012] Miyamoto et al., U.S. Pat. No. 5,461,170, disclose a
glyceride preparation having a branched saturated fatty acid and/or
myristic acid residues for use in liquid oils and/or solid
cosmetics of the same. Specifically, Miyamoto et al. disclose a
polyol fatty-acid ester having mixed acid group produced by
reacting a partial ester of a polyol and a branched fatty acid with
a straight chain fatty acid or a lower alcohol ester thereof in the
presence of a lipase. The obtained glyceride mixture contains a
large amount of diglyceride having a branched, saturated fatty acid
group, and a straight chain, fatty acid group. The reference does
not specifically disclose either linoleic or linolenic acid and/or
menopause.
[0013] Sultenfuss, U.S. Pat. No. 5,514,382, discloses a daily
vitamin and mineral supplement for women comprising vitamin A,
beta-carotene, niacin, riboflavin, pantothenic acid, pyridoxine,
cyanocobalamin, biotin, paraminobenzoic acid, inositol, choline,
calcium, chromium, copper, iodine, iron, magnesium, manganese,
molybdenum, selenium, zinc, and bioflavonoid. For women over 40
years of age, iron is optionally included.
[0014] Shylankevich, U.S. Pat. No. 5,569,459, discloses
compositions containing various vitamins, minerals and herbal
extracts that can be used for alleviation of premenstrual syndrome,
menopausal disorders, and stimulating estrogen production.
Specifically, the invention relates to such pharmaceutical
compositions and dietary supplements that contain natural soybean
phytoestrogens of the isoflavone group.
[0015] Vitamins For Women disclose a Calcium/Vitamin/Mineral
supplement program for women over forty. Specifically, the "over
forty" formula discloses a composition containing ingredients which
come in day and/or night formulas that "assure better utilization
and absorption." Physician's Desk Reference for Nonprescription
Drugs, (9.sup.th Ed., 1988) 718.
[0016] However, the previously disclosed formulations are deficient
for various reasons. In particular, none of the previously
disclosed formulations contain critical components, such as
essential fatty acids or calcium, in amounts specifically tailored
to meet the needs of premenopausal and menopausal women. Moreover,
the previously disclosed formulations fail to disclose the
significance of the proportion of the various components to one
another. Therefore, there is a need for formulations specifically
tailored to meet the needs of menopausal women. Further, there is a
need for drug delivery regimens which are specifically adapted to
meet the needs of premenopausal and menopausal women.
SUMMARY OF THE INVENTION
[0017] The compositions of the present inventive subject matter
overcome the deficiencies of currently-available nutritional
supplements by providing formulations and drug delivery regimens
which are specifically tailored for women just prior to, during and
after the period of menopause. The present compositions contain a
novel combination of various components, such as fatty acids, in
critical ratios and amounts, optionally in combination with various
vitamins and minerals.
[0018] One embodiment of the present inventive, subject matter is a
composition for administration to a menopausal woman, which
comprises:
[0019] an essential fatty acid compound selected from the group
consisting of a linoleic acid compound, a linolenic acid compound,
a docosahexaenoic acid compound, an omega-3 fatty acid compound, an
omega-2 fatty acid compound, a derivative thereof and a combination
thereof in an amount of about 10 mg to about 1,000 mg;
[0020] a calcium compound or derivative thereof in an amount of
about 400 mg to about 2500 mg;
[0021] a folic acid compound or derivative thereof in an amount of
about 0.4 mg to about 5.0 mg; and,
[0022] wherein the weight ratio of the essential fatty acid
compound to the calcium compound or derivative thereof is about
1:0.4 to 250 in a single or multiple dosage unit.
[0023] Another embodiment of the present inventive subject matter
is a composition for administration to a menopausal woman, which
comprises:
[0024] a first fatty acid compound selected from the group
consisting of a linoleic acid compound, a derivative thereof and a
combination thereof in an amount of about 10 mg to about 1,000
mg;
[0025] a second fatty acid compound selected from the group
consisting of a linolenic acid compound, a derivative thereof and
combinations thereof in an amount of about 10 mg to about 1,000
mg;
[0026] a third fatty acid compound selected from the group
consisting of a docosahexaenoic acid compound, an omega-3 fatty
acid, an omega-2 fatty acid, a derivative thereof and a combination
thereof in an amount of about 10 mg to about 1,000 mg;
[0027] a calcium compound or derivative thereof in an amount of
about 400 mg to about 2500 mg;
[0028] a folic acid compound or derivative thereof in an amount of
about 0.4 mg to about 5.0 mg;
[0029] wherein the weight ratio of the sum of the amounts of said
first and second fatty acid compounds to the amount of said third
fatty acid compound is about 1:0.5 to 1.5; and
[0030] wherein the weight ratio of the sum of the amounts of said
first, second and third fatty acid compounds to the amount of said
calcium compound or derivative thereof is about 1:0.4 to 50.
[0031] A further embodiment of the present inventive subject matter
is a composition for administration to a menopausal woman, which
comprises:
[0032] a first fatty acid compound selected from the group
consisting of a linoleic acid compound, a derivative thereof and a
combination thereof in an amount of about 10 mg to about 1,000
mg;
[0033] a second fatty acid compound selected from the group
consisting of a linolenic acid compound, a derivative thereof and
combinations thereof in an amount of about 10 mg to about 1,000
mg;
[0034] a third fatty acid compound selected from the group
consisting of a docosahexaenoic acid compound, an omega-3 fatty
acid, and omega-2 fatty acid, a derivative thereof and a
combination thereof in an amount of about 10 mg to about 1,000
mg;
[0035] a calcium compound or derivative thereof in an amount of
about 400 mg to about 2500 mg;
[0036] a vitamin C compound or derivative thereof in an amount of
about 25 mg to about 500 mg;
[0037] a vitamin E compound or derivative thereof in an amount of
about 10 mg to about 500 mg;
[0038] wherein the weight ratio of the sum of the amounts of said
first and second fatty acid compounds to the amount of said third
fatty acid compound is about 1:0.5 to 1.5; and
[0039] wherein the weight ratio of the sum of the amounts of said
first, second and third fatty acid compounds to the amount of said
calcium compound or derivative thereof is about 1:0.4 to 50.
[0040] An even further embodiment of the present inventive subject
matter is a composition for administration to a menopausal woman,
which comprises:
[0041] a first fatty acid compound selected from the group
consisting of a linoleic acid compound, a derivative thereof and a
combination thereof in an amount of about 10 mg to about 1,000
mg;
[0042] a second fatty acid compound selected from the group
consisting of a linolenic acid compound, a derivative thereof and
combinations thereof in an amount of about 10 mg to about 1,000
mg;
[0043] a third fatty acid compound selected from the group
consisting of a docosahexaenoic acid compound, an omega-3 fatty
acid, an omega-2 fatty acid, a derivative thereof and a combination
thereof in an amount of about 10 mg to about 1,000 mg;
[0044] a calcium compound or derivative thereof in an amount of
about 400 mg to about 2500 mg;
[0045] a folic acid compound or derivative thereof in an amount of
about 0.4 mg to about 5.0 mg;
[0046] a vitamin C compound or derivative thereof in an amount of
about 25 mg to about 500 mg;
[0047] a vitamin E compound or derivative thereof in an amount of
about 10 mg to about 500 mg;
[0048] a vitamin A compound or derivative thereof in an amount of
about 2,500 IU to about 6,500 IU;
[0049] wherein the weight ratio of the sum of the amounts of said
first and second fatty acid compounds to the amount of said third
fatty acid compound is about 1:0.5 to 1.5; and;
[0050] wherein the weight ratio of the sum of said first, second
and third fatty acid compounds to the amount of said calcium
compound or derivative thereof is about 1:0.4 to 50.
[0051] Another embodiment of the present inventive subject matter
is a composition for administration to a menopausal woman, which
comprises:
[0052] a first fatty acid compound selected from the group
consisting of a linoleic acid compound, a derivative thereof and a
combination thereof in an amount of about 10 mg to about 1,000
mg;
[0053] a second fatty acid compound selected from the group
consisting of a linolenic acid compound, a derivative thereof and
combinations thereof in an amount of about 10 mg to about 1,000
mg;
[0054] a third fatty acid compound selected from the group
consisting of a docosahexaenoic acid compound, an omega-3 fatty
acid, an omega-2 fatty acid, a derivative thereof and a combination
thereof in an amount of about 10 mg to about 1,000 mg;
[0055] a calcium compound or derivative thereof in an amount of
about 400 mg to about 2500 mg;
[0056] a folic acid compound or derivative thereof in an amount of
about 0.4 mg to about 5.0 mg;
[0057] a vitamin C compound or ester derivative thereof in an
amount of about 25 mg to about 500 mg;
[0058] a vitamin E compound or derivative thereof in an amount of
about 10 mg to about 500 mg;
[0059] a vitamin B6 compound or derivative thereof in an amount of
about 10 mg to about 50 mg;
[0060] a vitamin B12 compound or derivative thereof in an amount of
about 25 mcg to about 75 mcg;
[0061] a vitamin D compound or derivative thereof in an amount of
about 200 IU to about 625 IU;
[0062] wherein the weight ratio of the sum of the amounts of said
first and second fatty acid compounds to the amount of said third
fatty acid compound is about 1:0.5 to 1.5, and
[0063] wherein the weight ratio of the sum of the amounts of said
first, second and third fatty acid compounds to the amount of said
calcium compound or derivative thereof is about 1:0.4 to 50.
[0064] Yet another embodiment of the present inventive subject
matter is a composition for administration to a menopausal woman,
which comprises:
[0065] a biologically active substance for treating symptoms of
menopause;
[0066] a calcium compound or derivative thereof in an amount of
about 400 mg to about 2500 mg;
[0067] a folic acid compound or derivative thereof in an amount of
about 0.4 mg to about 5.0 mg.
[0068] A further embodiment of the present inventive subject matter
is a drug delivery regimen, which comprises:
[0069] a first dosage form comprising a first biologically active
substance to be administered to a menopausal woman at a
predetermined time period;
[0070] a second dosage form comprising a second biologically active
substance to be administered to the menopausal woman simultaneously
with said fist dosage form;
[0071] wherein said first biologically active substance and said
second biologically active substance are incompatible
substances.
[0072] An additional embodiment of the present inventive subject
matter is a method for providing nutritional supplementation to a
menopausal woman, which comprises: administering an essential fatty
acid compound to the woman during the period commencing at the
onset of menopause, said essential fatty acid compound being
selected from the group consisting of a linoleic acid compound, a
linolenic acid compound, a docosahexaenoic acid compound, an
omega-3 fatty acid compound, an omega-2 fatty acid compound, a
derivative thereof and a combination thereof;
[0073] administering about 400 mg co about 2500 mg of a calcium
compound or derivative thereof to the woman during the period
commencing at the onset of menopause;
[0074] administering about 0.4 mg to about 5.0 mg of a folic acid
compound or derivative thereof to the woman during the period
commencing at the onset of menopause; and
[0075] wherein the weight ratio of the essential fatty acid
compound to the calcium compound or derivative thereof is about
1:0.4 to 250.
[0076] Another embodiment of the present inventive subject matter
is a method for providing nutritional supplementation to a
menopausal woman, which comprises:
[0077] administering a first fatty acid compound to the woman
during a period commencing at the onset of menopause, said first
fatty acid compound being selected from the group consisting of a
linoleic acid compound, a derivative thereof and a combination
thereof;
[0078] administering a second fatty acid compound to said woman
during the period commencing at the onset of menopause, said second
fatty acid compound being selected from the group consisting of a
linolenic acid compound, a derivative thereof and a combination
thereof;
[0079] administering a third fatty acid compound to said woman
during the period commencing at the onset of menopause, said third,
fatty acid compound being selected from the group consisting of a
docosahexaenoic acid compound, an omega-3 fatty acid, an omega-2
fatty acid, a derivative thereof and a combination thereof, and
said third fatty acid compound being provided to the woman together
with said first and second fatty acid compounds;
[0080] administering about 400 mg to about 2500 mg of a calcium
compound or derivative thereof to said woman;
[0081] wherein the weight ratio of the sum of the amounts of said
first and second fatty acid compounds to the amount of said third
fatty acid compound is about 1:0.5 to 1.5; and
[0082] wherein the weight ratio of the sum of the amounts of said
first, second and third fatty acid compound to the amount of said
calcium compound or derivative thereof is about 1:0.4 to 50.
[0083] Yet another embodiment of the present inventive subject
matter is a method for providing nutritional supplementation to a
menopausal woman while reducing symptoms associated with menopause,
which comprises:
[0084] administering a first fatty acid compound to the woman
during a period commencing at the onset of menopause, said first
fatty acid compound being selected from the group consisting of a
linoleic acid compound, a derivative thereof and a combination
thereof;
[0085] administering a second fatty acid compound to said woman
during the period commencing at the onset of menopause, said second
fatty acid compound being selected from the group consisting of a
linolenic acid compound, a derivative thereof and a combination
thereof;
[0086] administering a third fatty acid compound to said woman
during the period commencing at the onset of menopause, said third
fatty acid compound being selected from the group consisting of a
docosahexaenoic acid compound, an omega-3 fatty acid, an omega-2
fatty acid, a derivative thereof and a combination thereof, and
said third fatty acid compound being provided to the woman together
with said first and second fatty acid compounds;
[0087] administering about 400 mg to 2500 mg of a calcium compound
or derivative thereof to said woman;
[0088] administering a therapeutic substance to said woman;
[0089] wherein the weight ratio of the sum of the amounts of said
first and second fatty acid compounds to the amount of said third
fatty acid compound is about 1:0.5 to 1.5; and
[0090] wherein the weight ratio of the sum of said first, second
and third fatty acid compound to the amount of said calcium
compound or derivative thereof is about 1:0.4 to 50.
[0091] A further embodiment is a method for delaying the onset of
menopause, which comprises: administering an essential fatty acid
to a woman prior to menopause, said fatty acid being selected from
the group consisting of a linoleic acid compound, a linolenic acid
compound, a docosahexaenoic acid compound, an omega-3 fatty acid
compound, an omega-2 fatty acid compound, a derivative thereof and
a combination thereof; wherein said essential fatty acid is
administered in an amount sufficient to delay the onset of
menopause.
[0092] A still further embodiment is a method for providing,
nutritional supplementation to a menopausal woman while reducing
symptoms associated with menopause, which comprises:
[0093] administering a fatty acid compound to the woman during a
period commencing at the onset of menopause, said fatty acid
compound being selected from the group consisting of a linoleic
acid compound, a linolenic acid compound, a docosahexaenoic acid
compound, an omega-3 fatty acid, an omega-2 fatty acid, a
derivative thereof and a combination thereof;
[0094] administering about 400 mg to 2500 mg of a calcium compound
or derivative thereof to said woman;
[0095] and administering a non-nutritional active to said
woman.
[0096] Another embodiment is a method for reducing the possibility
of premature menopause, which comprises: administering an essential
fatty acid to a woman prior to menopause, said fatty acid being
selected from the group consisting of a linoleic acid compound, a
linolenic acid compound, a docosahexaenoic acid compound, an
omega-3 fatty acid compound, an omega-2 fatty acid compound, a
derivative thereof and a combination thereof, wherein said
essential fatty acid is administered in an amount sufficient to
reduce the risk of premature menopause.
[0097] An additional embodiment is a method for providing
nutritional supplementation to a premenopausal woman or a
menopausal woman, which comprises: administering to the
premenopausal woman or menopausal woman a biologically active
substance for treating symptoms of menopause; administering to the
premenopausal woman or menopausal woman a calcium compound or
derivative thereof in an amount of 400 mg to about 2500, and
administering to the premenopausal woman or menopausal woman a
folic acid compound or derivative thereof in an amount of about 0.4
mg to about 5.0 mg.
DETAILED DESCRIPTION OF THE INVENTION
[0098] As used herein, "menopausal woman" refers to any woman who
has experienced ovarian failure. The ovarian failure can be
measured by blood tests for low estrogen levels (estradiol) or
elevated gonadotropin levels (follicle stimulating hormone). When
menopause occurs it remains for the life of the woman. The term
"menopause" also encompasses the postmenopause or the
postmenopausal period. The term "menopause" also encompasses
natural menopause and artificial menopause.
[0099] "Premenopausal woman" refers to any woman during the period
commencing five years prior to onset of menopause.
[0100] "Nutritional status" refers to the levels of vitamins,
minerals and other nutrients which will be available for use by the
menopausal woman.
[0101] "Nutritional status" refers to the presence or absence of
any nutrient deficiency, or in other words, the extent to which
physiological nutrient demands are being satisfied such that
deficiency is avoided.
[0102] "Optimize neurological development" refers to attainment of
the highest degree of neurological development possible through
natural processes without the use of any unnatural substances or
procedures, such as drugs, surgery and the like.
[0103] "Biologically active substance" refers to any substance or
substances comprising a drug, active therapeutic substance,
metabolite, medicament, vitamin, or mineral, any substance used for
treatment, prevention, diagnosis, cure or mitigation of disease or
illness, any substance which affects anatomical structure or
physiological function, or any substance which alters the impact of
external influences on an animal, or metabolite thereof, and as
used herein, encompasses the terms "active substance", "therapeutic
substance", "agent", "active agent", "drug", "medication",
"medicine", "medicant", and other such similar terms.
[0104] "Non-nutritional active" refers to any substance or
substances comprising a drug, active therapeutic substance,
metabolite, or medicament, or any other substance used for
treatment, prevention, diagnosis, cure or mitigation of disease or
illness, any substance which affects anatomical structure or
physiological function, or any substance which alters the impact of
external influences on an animal, or metabolite thereof and as used
herein, that is not a vitamin, mineral, or any other nutritional
compound or compositions.
[0105] "Specific physiological needs" refers to the unique
requirements for certain levels of certain nutrients by one class
of persons, such as menopausal women, premenopausal women,
postmenopausal women, etc., as distinguished from other
classes.
[0106] "Biologically-acceptable" refers to being safe for human
consumption.
[0107] "Storage-incompatible substances" refers to substances that
may not be formulated together in a single dosage unit or stored
together in direct contact because the substances will interact in
a negative manner and also substances that cannot be formulated
together in a single dosage unit because the sum total of the
dosage amounts of the substances would result in a single dosage
unit which is too large to be swallowed. The term also refers to
substances which may be stored in direct contact, however, one of
the substances is preferably formulated in a dosage form which is
either not preferred or incompatible with the other substance.
Storage-incompatibility also refers to two or more substances
wherein at least one substance is a prescription substance and at
least one substance is a non-prescription substance.
[0108] "Storage-incompatibility refers to the state that exists
between storage-incompatible substances, as defined above.
[0109] The compositions of the present inventive subject matter
provide several specific new and unexpected benefits. First, the
formulations ensure that menopausal women are provided with
adequate energy during the period of menopause. Secondly, the
formulations allow the menopausal women to maintain the adequate
fatty acid stores for both her future use. Thirdly, the fatty acids
optimize the neurological maintenance of the menopausal women.
Fourthly, when administered just prior to menopause, the present
compositions prepare women for the increased physiological demands
and stresses to be placed upon their bodies. Additionally, the
present compositions provide nutritional supplementation to women
during the early stage of menopause known as premenopause.
[0110] Finally, the present compositions help minimize the risk of
menopause related disorders and symptoms resulting from such
disorders.
[0111] The present inventive subject matter is based, in part, on
the discovery that when compositions having certain fatty acids, in
certain amounts and proportions to one another, are administered to
women just prior to, during and after menopause, the women will
achieve optimal nutritional supplementation. In particular,
supplementing a menopausal woman's diet with the formulations
described below for a period commencing when symptoms of menopause
are actually experienced, or preferably just prior to when
menopause would generally be expected, will ensure that the woman
has adequate essential fatty acids for present and future use. The
fatty acid supplement may also further contain vitamins and
minerals to confer added health benefits to the menopausal woman.
In addition to benefiting humans, the present invention can also
benefit non-human mammals. The composition of the present invention
could be administered to a mammal in animal feed, pill form, or
other appropriate dosage forms to such mammals.
[0112] Without being limited by theory, the present compositions
stimulate or play a vital role in one or more natural biological
pathways. For example, the arachidonic acid cascade may play a
significant role in the support and maintenance of a menopausal
woman's health. Specifically, in the arachidonic acid cascade,
linoleic acid is converted first to gamma-linolenic acid and then
to further metabolites such as dihomo-gamma-linolenic acid and
arachidonic acid which are precursors of 1 and 2 series
prostaglandin respectively, as shown in the outline below: 1
[0113] The present composition may contain an essential fatty acid
compound. The fatty acid compound may be a linoleic acid compound,
derivatives thereof or any combination of linoleic acid and/or
linoleic acid derivatives. The fatty acid compound may be a
linolenic acid compound, derivatives thereof and/or an combinations
of linolenic acid and/or linoleic acid derivatives. The fatty acid
compound may also be a docosahexaepoic acid compound, an omega-3
fatty acid compound, an omega-2 fatty acid compound, derivatives
thereof or combinations thereof. The fatty acid may further be a
combination of any of the above discussed fatty acids.
[0114] Preferably, the fatty acid compound is present in the
composition in an amount ranging from about 10 mg to 1,000 mg. More
preferably, the fatty acid compound is present in the composition
in an amount ranging from about 15 mg to 200 mg, independently of
the other fatty acid compounds. Even more preferably, the fatty
acid compounds is present in the composition in an amount ranging
from about 20 mg to about 100 mg, independently of the other fatty
acid compounds. Most preferably, the fatty acid compound is present
in the composition in an amount ranging from about 25 mg to 50 mg,
independently of the other fatty acid compounds.
[0115] Three fatty acid compounds may be present in the present
composition in critical proportions to one another. Preferably, the
weight ratio of the sum of the amounts of said first and second
fatty acid compounds to the amount of said third fatty acid
compound is about 1:0.5 to 1.5. More preferably, the weight ratio
of the sum of the amounts of said first and second fatty acid
compound is about 1:0.7 to 1.3. Even more preferably, the weight
ratio of the sum of the amounts of said to the amount of said third
fatty acid compound is about 1:0.9 to 1.2. Most preferably, the
weight ratio of the sum of the amounts of said first and second
fatty acid compounds to the amount of said third fatty acid
compound is about 1:0.9 to 1.1.
[0116] The compositions of the present invention may incorporate
any compound that can react with an essential fatty acid to form a
biochemically active compound. Preferably, the compound is a
compound which fulfills a nutritional need, for example, without
limitation, sphingomyelin, myelin derivatives thereof and
combinations thereof.
[0117] Particular classes of fatty acid compound derivatives used
in the present invention, include, without limitation, phospholipid
esters of linoleic acid, ethers of linoleic acid, sterolderivatives
of linoleic acid, phospholipid esters of linolenic acid, ethers of
linolenic acid, sterolderivatives of linolenic acid and
combinations thereof.
[0118] Non-limiting exemplary fatty acid compounds used in the
present invention, include, without limitation, phosphatidal
choline esters of linoleic acid, phosphatidal ester of linoleic
acid, phosphatidal choline esters of linolenic acid, sipolsterol
ester of linolenic acid, and combinations thereof.
[0119] The present composition contains a calcium compound,
derivatives thereof or any combination of calcium compound and
derivatives thereof. Preferably, the calcium is present in the
composition in an amount ranging from about 400 mg to about 2,500
mg. More preferably, the calcium is present in the composition in
an amount ranging from about 600 mg to about 1,800 mg. Even more
preferably, the calcium is present in the composition in an amount
ranging from about 800 mg to about 1,600 mg. Most preferably, the
calcium is present in the composition in an amount ranging, from
about 1,000 mg to about 1,400 mg.
[0120] The proportion of total fatty acids to total calcium content
in the present inventions is a critical feature.
[0121] Where three fatty acid compounds are present, preferably,
the weight ratio of the sum of the amounts of the first, second and
third fatty acid compounds to the amount of said calcium compound
or derivative thereof is about 1:0.4 to 50. More preferably, the
weight ratio of the sum of the amounts of the first, second and
third fatty acid compounds to the amount of said calcium compound
or derivative thereof is about 1:4 to 20. Even more preferably, the
weight ratio of the sum of the amounts of the first, second and
third fatty acid compounds' to the amount of said calcium compound
or derivative thereof is about 1:7 to 15. Most preferably, the
weight ratio of the sum of the amounts of the first, second and
third fatty acid compounds to the amount of said calcium compound
or derivative thereof is about 1:10 to 14.
[0122] The fatty acids of the present inventive subject matter may
be used as such or as biologically acceptable and physiologically
equivalent derivatives as, for example, detailed later herein.
Reference to any of the fatty acids including reference in the
claims is to be taken as including reference to the acids when in
the form of such derivatives. Equivalence is demonstrated by entry
into the biosynthetic pathways of the body as evidence by effects
corresponding to those of the acids themselves or their natural
glyceride esters. Thus, indirect identification of useful
derivatives is by their having the valuable effect in the body of
the fatty acid itself, but conversion, for example, of
gamma-linolenic acid to dihomo-gamma-linolenic acid and on to
arachidonic acid can be shown directly by gas chromatographic
analysis of concentrations in blood, body fat, or other tissue by
standard techniques, well known to persons of ordinary skill in the
art to which the present inventive subject matter pertains.
[0123] Derivatives of linoleic acid, as used in the present
inventive subject matter, include, without limitation, salts of
linoleic acid, alkaline salts of linoleic acid, esters of linoleic
acid and combinations thereof. Derivatives of linolenic acid, as
used in the present inventive subject matter, include, without
limitation, salts of linolenic acid, alkaline salts of linolenic
acid, esters of linolenic acid and combinations thereof. The salts
and alkaline salts herein refer to those regularly used organic or
inorganic salts which are acceptable for pharmaceutical use.
Non-limiting exemplary linolenic acids include gamma-linoleic acid
and dihomo-gamma-linolenic acid.
[0124] The fatty acids of the present inventive subject matter may
be from any source, including, without limitation, natural or
synthetic oils, fats, waxes or combinations thereof. Moreover, the
fatty acids herein may be derived, without limitation, from
non-hydrogenated oils, partially hydrogenated oils, fully
hydrogenated oils or combinations thereof. Non-limiting exemplary
sources of fatty acids include seed oil, fish or marine oil, canola
oil, vegetable oil, safflower oil, sunflower oil, nasturtium seed
oil, mustard seed oil, olive oil, sesame oil, soybean oil, corn
oil, peanut oil, cottonseed oil, rice bran oil, babassu nut oil,
palm oil, low erucic rapeseed oil, palm kernel oil, lupin oil,
coconut oil, flaxseed oil, evening primrose oil, jojoba, tallow,
beef tallow, butter, chicken fat, lard, dairy butterfat, shea
butter or combinations thereof. Specific non-limiting exemplary,
fish or marine oil sources include shellfish oil, tuna oil, mackrel
oil, salmon oil, menhaden, anchovy, herring, trout, sardines or
combinations thereof. Preferably, the source of the fatty acids is
fish or marine oil, soybean oil or flaxseed oil.
[0125] Calcium compounds include, but are not limited to, any of
the well known calcium supplements, such as calcium carbonate,
calcium sulfate, calcium oxide, calcium hydroxide, calcium apatite,
calcium citrate-malate, bone meal, oyster shell, calcium gluconate,
calcium lactate, calcium phosphate, calcium levulinate, and the
like. Derivatives of calcium compounds, as used herein, include,
without limitation, salts of calcium, alkaline salts of calcium,
esters of calcium, and combinations thereof. The salts and alkaline
salts herein refer to those regularly used organic or inorganic
salts which are acceptable for pharmaceutical use. The calcium of
the present composition may be from any source, without
limitation.
[0126] Folic acid is also incorporated into the composition of the
present inventive subject matter. Preferably, folic acid is present
in an amount ranging from about 0.4 mg to about 5.0 mg. More
preferably, folic acid is present in an amount ranging from about
0.6 mg to about 1.3 mg. Even more preferably, folic acid is present
in an amount ranging from about 0.8 mg to about 1.2 mg. Most
preferably, folic acid is present in an amount ranging from about
0.9 mg to about 1.1 mg.
[0127] The present composition may optionally contain additional
vitamins and biologically-acceptable minerals. Non-limiting
exemplary vitamins and biologically acceptable minerals and their
derivatives thereof for inclusion in the present compositions
include vitamin A, B vitamins, vitamin C, vitamin D, vitamin E,
vitamin K, iron, calcium, magnesium, potassium, copper, chromium,
zinc, molybdenum, iodine, boron, selenium, manganese, bioflavonoid,
derivatives thereof or combinations thereof. These vitamins and
minerals may be from any source or combination of sources, without
limitation. Non-limiting exemplary B vitamins include, without
limitation; thiamine, niacinamide, pyridoxine, riboflavin,
cyanocobalamin, biotin, pantothenic acid or combinations thereof.
Other nutritionally active compounds may also be present, including
without limitation, fiber, carbohydrates, fats, proteins, amino
acids, derivatives thereof and combinations thereof.
[0128] When vitamin C is present in the composition of the present
inventive subject matter, it is preferably present in an amount
ranging from about 10 mg to about 600 mg. More preferably, the
vitamin C is present in an amount ranging from about 25 mg to about
500 mg. Even more preferably, the vitamin C is present in an
immediate release form in an amount ranging from about 25 mg to
about 50 mg. Most preferably, the vitamin C is present in a
controlled release form in an amount ranging from about 250 mg to
about 500 mg.
[0129] When vitamin E is present in the composition of the present
inventive subject matter, it is preferably present in an amount
ranging from about 5 mg to about 500 mg. More preferably, the
vitamin E is present in an amount ranging from about 10 mg to about
400 mg. Even more preferably, the vitamin E is present in a
controlled release form in an amount ranging from about 250 mg to
about 400 mg. Most preferably, the vitamin E is present in an
immediate release form in an amount ranging from about 10 mg to
about 50 mg.
[0130] Vitamin B6 may also be present in the composition of the
present inventive subject matter. Vitamin B6 is preferably present
in an amount ranging from about 5 mg to about 200 mg. More
preferably, vitamin B6 is present in an amount ranging from about
10 mg to about 50 mg. Even more preferably, vitamin B6 is present
in an amount ranging from 15 mg to about 40 mg: Most preferably,
vitamin B6 is present in a controlled release form in an amount
ranging from 20 mg to about 30 mg.
[0131] Vitamin B12 may also be incorporated into the present
composition. Preferably, the vitamin B12 is present in an amount
ranging from about 25 mcg to about 75 mcg. More preferably, the
vitamin B12 is present in an amount ranging from about 35 mcg to
about 65 mcg. Even more preferably, the vitamin B12 is present in
an amount ranging from about 40 mcg to about 60 mcg. Most
preferably, the vitamin B12 is present in an amount ranging from
about 45 mcg to about 55 mcg.
[0132] Vitamin D may also be incorporated into the present
composition. Preferably, vitamin D is present in an amount ranging
from about 200 IU to about 625 IU. More preferably, vitamin D is
present in an amount ranging from about 300 IU to about 500 IU.
Even more preferably, vitamin D is present in an amount ranging
from about 350 IU to about 450 IU. Most preferably, vitamin D is
present in an amount, ranging from about 375 IU to about 425
IU.
[0133] Vitamin A may also be incorporated into the present
composition. Preferably, vitamin A is present in the composition in
an amount ranging from about 2,500 IU to about 6,500 IU. More
preferably, vitamin A is present in the composition in an amount
ranging from about 4,000 IU to about 6,000 IU. Even more
preferably, vitamin A is present in the composition in an amount
ranging from about 4,500 IU to about 5,500 IU. Most preferably,
vitamin A is present in the composition in an amount ranging from
about 4,750 IU to about 5,250 IU.
[0134] Magnesium, when present, is preferably in the composition of
the present inventive subject matter in an amount ranging from
about 25 mg to about 400 mg. More preferably, magnesium is present
in the composition of the present inventive subject matter in an
immediate release form in an amount ranging from about 25 mg to
about 100 mg. Even more preferably, magnesium is present in the
composition of the present inventive subject matter in a controlled
release form in an amount ranging from about 100 mg to about 400
mg. Acceptable magnesium compounds which may be incorporated into
the present inventive subject matter include, but are not limited
to, magnesium stearate, magnesium carbonate, magnesium oxids,
magnesium hydroxide and magnesium sulfate.
[0135] The composition of the present inventive subject matter may
also include one or more biologically active substances or
therapeutic substances, including, without limitation, hormones,
steroids, fiber, estrogens, progestins, sedative-hypnotics,
barbiturates, benzodiazepines, antidepressants, tranquilizers,
sedatives, osteoporotics, anti-platelets, aminobisphosphonates,
herbals, herbal derivatives, plant derivatives, phyto-chemical
derivatives and combinations thereof.
[0136] If the non-nutritional active is a hormone, the hormone is
administered in a dosage amount ranging from about 0.15 mg to about
11.25 mg. If the non-nutritional active is an osteoporotic, the
osteoporotic is administered in a dosage amount ranging from about
2.5 mg to about 60 mg.
[0137] Non-limiting exemplary therapeutic substances include,
medroxyprogesterone acetate, megestrol acetate, clonidine,
norethindrone acetate, ethinyl estradiol, conjugated estrogen,
natural estrogen, synthetic estrogen, estradiol, progesterone,
clomiphene, clomiphene citrate, zuclomiphene, zuclomiphene citrate,
enclomiphene, enclomiphene citrate, aspirin, calcitonin,
alendronate, etidronate, pamidronate, clodronate, tiludronate,
residronate, ibandronate and combinations thereof.
[0138] Non-limiting exemplary herbals and herbal derivatives
include agrimony, alfalfa, aloe vera, amaranth, angelica, anise,
barberry, basil; bayberry; bee pollen, birch, bistort, blackberry,
black cohosh, black walnut, blessed thistle, blue cohosh, blue
vervain, boneset, borage, buchu, buckthorn, bugleweed, burdpock,
capsicum, cayenne, caraway, cascara sagrada, catnip, celery,
centaury, chamomile chaparral, chickweed, chicory, chinchona,
cloves, coltsfoot, comfrey, cornsilk, couch grass, cramp bark,
culver's root, cyani, cornflower, damiana, dandelion, devils claw,
dong quai, echinacea, elecampane, ephedra, eucalyptus, evening
primrose, eyebright, false unicorn, fennel, fenugreek, figwort,
flaxseed, garlic, gentian, ginger, ginseng, golden seal, gotu kola,
gum weed, hawthorn, hops, horehound, horseradish, horsetail,
hoshouwu, hydrangea, hyssop, iceland moss, irish moss, jojoba,
juniper, kelp, lady's slipper, lemon grass, licorice, lobelia,
mandrake, marigold, marjoram, marshmallow, mistletoe, mullein,
mustard, myrrh, nettle, oatstraw, oregon grape, papaya, parsley,
passion flower, peach, pennyroyal, peppermint, periwinkle,
plantain, pleurisy root, pokeweed, prickly ash, psyllium, quassia,
queen of the meadow, red clover, red raspberry, redmond clay,
rhubarb, rose hips, rosemary, rue, safflower, saffron, sage, St.
Johnswort, sarsaparilla, sassafras, saw palmetto, scullcap, senega,
senna, shepherd's purse, slippery elm, spearmint, spikenard,
squawvine, stillingia, strawberry, taheebo, thyme, uva ursi,
valerian, violet, watercress, white oak cherry, wild lettuce, wild
yam, willow, wintergreen, witch hazel, wood betony, wormwood,
yarrow, yellow dock, yerba santa, yucca and combinations thereof.
Herbal derivatives, used herein, refers to herbal extracts, and
substances derived from plants and plant parts, such as leaves,
flowers and roots, without limitation. Preferably, the herbal or
herbal derivative is black cohosh, licorice, false unicorn,
siberian ginseng, sarsaparilla, squaw vine, blessed thistle and
combinations thereof.
[0139] Various additives may be incorporated into the present
composition. Optional additives of the present composition include,
without limitation, starches, sugars, fats, antioxidants, amino
acids, proteins, nucleic acids, electrolytes, derivatives thereof
or combinations thereof.
[0140] Non-limiting exemplary amino acids of the present inventive
subject matter include histidine, isoleucine, leucine, lysine,
methionine, phenylalanine, threonine, tryptophan, valine, alanine,
arginine; asparagine, aspartic acid, cysteine, glutamic acid,
glutamine, glycine, proline, serine, tyrosine, derivatives thereof,
and combinations thereof. Preferably, the amino acid present is
leucine, isoleucine, valine, derivatives thereof or combinations
thereof.
[0141] The compositions, methods and drug delivery regimens of the
present inventive subject matter may facilitate the simultaneous
administration of storage-incompatible substances, particularly
storage incompatible substances tailored to the needs of
premenopausal and menopausal women. Storage-incompatible substances
may be any substances that may not be formulated together in a
single dosage unit or stored together in direct contact because the
substances will interact in a negative manner and also substances
that cannot be formulated together in a single dosage unit because
the sum total of the dosage amounts of the substances would result
in a single dosage unit which is too large to be swallowed.
Storage-incompatible substances also include those substances which
may be stored in direct contact, however, one of the substances is
preferably formulated in a dosage form which is either not
preferred or incompatible with he other substance. The
storage-incompatible substances may include any
storage-incompatible substances, without limitation.
[0142] For example, the storage incompatible substances may be
hydrophobic compounds and hydrophilic compounds, olefinic compounds
and non-olefinic compounds, pH sensitive and non-pH sensitive
compounds, substances requiring an anhydrous environment and
substances requiring a non-anhydrous environment, acidic drugs and
basic drugs, effervescent tablets and high water content drugs or
dosage forms, gelatin capsules and aldehydes, quaternary ammonium
compounds and anionic substances or any combination of the
above.
[0143] Storage incompatible substances also include substances that
cannot be formulated together in a single dosage unit because the
sum total of the dosage amounts of the substances results in a
single dosage unit too large to swallow. The compositions, methods
and drug delivery regimens of the present inventive subject matter
address this problem by separating the large dosage into multiple
doses small enough to swallow comfortably, while keeping all of the
substances and doses together in one package.
[0144] Non-limiting exemplary storage incompatible substances
include without limitation, ascorbic acid and aluminum hydroxide,
ascorbic acid and sodium bicarbonate, citric acid and sodium
carbonate, folic acid and calcium-carbonate; activated charcoal and
amyl nitrate, gelatin capsules and formaldehyde, gelatine capsules
and gluteraldehyde, konicin chloride and soap, etylpyridinium
chloride and sodium stearate, omega fatty acids and combinations
thereof.
[0145] It is also possible in the nutritional composition of the
present inventive subject matter for the dosage form to combine any
forms of release well known to persons of ordinary skill in the
art. These include, without limitation, immediate release, extended
release, pulse release, variable release, controlled release, timed
release, sustained release, delayed release, long acting, and
combinations thereof. The ability to obtain immediate release,
extended release, pulse release, variable release, controlled
release, timed release, sustained release, delayed release, long
acting characteristics and combinations thereof is performed using
well known procedures and techniques available to the ordinary
artisan. Each of these specific techniques or procedures for
obtaining the release characteristics does not constitute an
inventive aspect of this inventive subject matter all of which
procedures are well known to those of ordinary skill in the art. As
used herein, a "controlled release form" means any form having at
least one component formulated for controlled release. As used
herein, "immediate release form" means any form having all its
components formulated for immediate release.
[0146] Any biologically-acceptable dosage form well known to
persons of ordinary skill in the art, and combinations thereof, are
contemplated by the inventive subject matter. Examples of such
dosage forms include, without limitation, chewable tablets, quick
dissolve tablets, effervescent tablets, reconstitutable powders,
elixirs, liquids, solutions, suspensions, emulsions, tablets,
multi-layer tablets, bi-layer tablets, capsules, soft gelatin
capsules, hard gelatin capsules, caplets, lozenges, chewable
lozenges, beads, powders, granules, particles, microparticles,
dispersible granules, cachets, douches, suppositories, creams,
topicals, inhalants, aerosol inhalants, patches, particle
inhalants, implants, depot implants, ingestibles, injectables,
infusions, health bars, confections, animal feeds, cereals,
yogurts, cereal coatings, foods, nutritive foods, functional foods
and combinations thereof. The preparation of the above dosage forms
are well known to persons of ordinary skill in the art.
[0147] The following procedures represent, without limitation,
acceptable methods of preparing formulations falling within the
scope of the inventive subject matter. For example, animal feed may
be made by methods well known to persons of ordinary skill in the
art. Animal feeds may be prepared by mixing the formulation with
binding ingredients to form a plastic mass. The mass is then
extruded under high pressure to form tubular (or "spaghetti-like")
structures that are cut to pellet size and dried.
[0148] Quick dissolve tablets may be prepared, for example, without
limitation, by mixing the formulation with agents such as sugars
and cellulose derivatives, which promote dissolution or
disintegration of the resultant tablet after oral administration,
usually within 30 seconds.
[0149] Cereal coatings may be prepared, for example, without
limitation, by passing the cereal formulation, after it has been
formed into pellets, flakes, or other geometric shapes, under a
precision spray coating device to deposit a film of active
ingredients, plus excipients onto the surface of the formed
elements. The units thus treated are then dried to form a cereal
coating.
[0150] For example, health bars may be prepared, without
limitation, by mixing the formulation plus excipients (e.g.,
binders, fillers, flavors, colors, etc.) to a plastic mass
consistency. The mass is then either extended or molded to form
"candy bar" shapes that are then dried or allowed to solidify to
form the final product.
[0151] Soft gel or soft gelatin capsules may be prepared; for
example, without limitation, by dispersing the formulation in an
appropriate vehicle (vegetable oils are commonly used) to form a
high viscosity mixture. This mixture is then encapsulated with a
gelatin based film using technology and machinery known to those in
the soft gel industry. The industrial units so formed are then
dried to constant weight.
[0152] Chewable tablets, for example, without limitation, may be
prepared by mixing the formulations with excipients designed to
form a relatively soft, flavored, tablet dosage form that is
intended to be chewed rather than swallowed. Conventional tablet
machinery and procedures, that is both direct compression and
granulation, i.e., or slugging, before compression, can be
utilized. Those individuals involved in pharmaceutical solid dosage
form production are well versed in the processes and the machinery
used as the chewable dosage form is a very common dosage form in
the pharmaceutical industry.
[0153] Film coated tablets, for example, without limitation, may be
prepared by coating tablets using techniques such as rotating pan
coating methods or air suspension methods to deposit a contiguous
film layer on a tablet. This procedure is often done to improve the
aesthetic appearance of tablets, but may also be done to improve
the swallowing of tablets, or to mask an obnoxious odor or taste,
or to improve the usual properties of an unsightly uncoated
tablet.
[0154] Compressed tablets, for example, without limitation, may be
prepared by mixing the formulation with excipients intended to add
binding qualities to disintegration qualities. The mixture is
either directly compressed or granulated then compressed using
methods and machinery quite well known to those in the industry.
The resultant compressed tablet dosage units are then packaged
according to market need, i.e., unit dose, rolls, bulk bottles,
blister packs, etc.
[0155] The present inventive subject matter contemplates
nutritional compositions formulated for administration by any
route, including without limitation, oral, buccal, sublinqual,
rectal, parenteral, topical, inhalational, injectable and
transdermal. The physicochemical properties of nutritional
compositions, their formulations, and the routes of administration
are important in absorption. Absorption refers to the process of
nutritional composition movement from the site of administration
toward the systemic circulation. Most orally administered
nutritional compositions are in the form of tablets or capsules
primarily for convenience, economy, stability, and patient
acceptance. They must disintegrate and dissolve before absorption
can occur. Using the present inventive subject matter with any of
the above routes of administration or dosage forms is performed
using well known procedures and techniques available to the
ordinary skilled artisan.
[0156] The present inventive subject matter contemplates the use of
biologically-acceptable carriers which may be prepared from a wide
range of materials. Without being limited thereto, such materials
include diluents, binders and adhesives, lubricants, plasticizers,
disintegrants, colorants, bulking substances, flavorings,
sweeteners and miscellaneous materials such as buffers and
adsorbents in order to prepare a particular medicated
composition.
[0157] Binders may be selected from a wide range of materials such
as hydroxypropylmethylcellulose, ethylcellulose, or other suitable
cellulose derivatives, povidone, acrylic and methacrylic acid
co-polymers, pharmaceutical glaze, gums, milk derivatives, such as
whey, starches, and derivatives, as well as other conventional
binders well known to persons skilled in the art. Exemplary
non-limiting solvents are water, ethanol, isopropyl alcohol,
methylene chloride or mixtures and combinations thereof. Exemplary
non-limiting bulking substances include sugar, lactose, gelatin,
starch, and silicon dioxide.
[0158] The plasticizers used in the dissolution modifying system
are preferably previously dissolved in an organic solvent and added
in solution form. Preferred plasticizers may be selected from the
group consisting of diethyl phthalate, diethyl sebacate, triethyl,
citrate, cronotic acid, propylene glycol, butyl phthalate, dibutyl
sebacate, caster oil and mixtures thereof, without limitation. As
is evident, the plasticizers may be hydrophobic as well as
hydrophilic in nature. Water-insoluble hydrophobic substances, such
as diethyl phthalate, diethyl sebacate and caster oil are used to
delay the release of water-soluble vitamins, such as vitamin B6 and
vitamin C. In contrast, hydrophilic plasticizers are used when
water-insoluble vitamins are employed which aid in dissolving the
encapsulated film, making channels in the surface, which aid in
nutritional composition release.
[0159] The composition of the present inventive subject matter may
be administered in a partial, i.e., fractional dose, one or more
times during a 24 hour period, a single dose during a 24 hour
period of time, a double dose during a 24 hour period of time, or
more than a double dose during a 24 hour period of time.
Fractional, double or other multiple doses may be taken
simultaneously or at different times during the 24 hour period. The
doses may be uneven doses with regard to one another or with regard
to the individual components at different administration times. For
example, without limitation, the amount of calcium in a morning
dose is different from the amount of calcium in an evening
dose.
[0160] The compositions of the present invention are intended for
use by humans and other mammals. The dosages are adjusted according
to body weight and thus may be set forth herein on a per body
weight basis. For example, if the formula specifies a range of
about 10-1000 mg for a 55 kg individual; that range would be
adjusted for a 35 kg individual to about 6.3-63 mg (e.g., the lower
range limit=(35 kg/55 kg)*10 mg=6.3 mg). Decimal amounts may be
rounded to the nearest whole number. In the above manner the
present compositions may thus be adapted to be suitable for any
individual, including any mammal, regardless of its size.
[0161] The present composition is adapted to meet the specific
physiological needs of a menopausal woman. For example, the
formulations may focus on special nutritional needs of a menopausal
woman that are not generally or adequately addressed in nutritional
dietary supplements, such as essential fatty acids, without
limitation. The iron and calcium, when present, are provided in
amounts to optimize nutritional benefit to the menopausal woman,
while minimizing unpleasant side effects which may accompany overly
large doses. The formulation can be further tailored based upon the
specific needs, genetic predispositions or identified deficiencies
of individual women, on either a generalized or case by case basis
for greater specificity. Further, the composition may be
specifically adapted for treating conditions associated with
menopause or to maximize neurological maintenance of a menopausal
woman. The composition may also be adapted for inhibiting loss in
bone mass and preventing deficiency of essential acids in
menopausal women. Moreover, the present composition can be used as
one component of a prescribed therapy.
[0162] The composition of the inventive subject matter may be
provided in a blister pack or other such pharmaceutical package,
without limitation. Further, the compositions of the present
inventive subject matter may further include or be accompanied by
indicia allowing women to identify the compositions as products for
menopausal women. The indicia may further additionally include an
indication of the above specified time periods for using said
compositions.
[0163] For example, without limitation, the indicia may be time
indicia indicating a specific or general time of day for
administration of the composition, or the indicia may be a day
indicia indicating a day of the week for administration of the
composition.
[0164] The composition of the present invention may be used prior
to and during menopause. Use of the compositions may commence at
the onset of menopause. The composition of the present inventive
subject matter is preferably administered during a period
commencing no later than the appearance of the first symptoms
associated with menopause and continuing throughout a woman's life.
More preferably, the composition is administered during a period of
time commencing just prior to menopause or just prior to any
symptoms of menopause. The phrases "just prior to menopause" and
"prior to any symptoms of menopause" are intended herein to include
commencement of administration of compositions approximately one
month to five years prior to an age generally identified with
initiation of menopause.
[0165] Preferably, the commencement of administration of the
composition is when the woman is thirty five to fifty years of age.
More preferably, the commencement of administration is one month
prior to the woman turning forty years of age. Even more
preferably, the commencement of administration is one year prior to
the woman turning forty years of age. Most preferably, the
commencement of administration five years prior to the woman
turning forty years of age.
[0166] The present inventive subject matter includes a method for
providing nutritional supplementation to a menopausal woman. The
methods include administration of the present composition to women
during a critical period. The critical period of administration is
the period commencing just prior to menopause and continuing
through the postmenopausal period of a woman's life.
[0167] The method of the present inventive subject matter may
prevent or at least minimize fatty acid deficiency in menopausal
women. The present method may also be used to prevent or treat
symptoms associated with menopause. Further, the present method may
inhibit the loss in bone mass commonly experienced by menopausal
women. The present method may delay onset or menopause and/or
reduce possibility of premature menopause.
[0168] The present methods may be carried out alone or in
conjunction with a therapeutic therapy or regimen, without
limitation. The therapeutic therapy or regimen may be for treating
symptoms associated with menopause or may be entirely unrelated to
menopause. For example, without limitation, the present method may
be incorporated as part of hormonal or estrogen therapy, or in
combination with dietary manipulation.
[0169] The foregoing is considered as illustrative only of the
principles of the inventive subject matter. Further, since numerous
modifications and changes will readily occur to those skilled in
the art, it is not desired to limit the inventive subject matter to
the exact construction and operation shown and described, and
accordingly all suitable modifications and equivalents may be
resorted to, falling within the scope of the inventive subject
matter.
[0170] The following examples are illustrative of preferred
embodiments of the inventive subject matter and are not to be
construed as limiting the inventive subject matter thereto. All
percentages are based on the percent by weight of the final
delivery system or formulation prepared unless otherwise indicated
and all totals equal 100% by weight.
EXAMPLES
Example 1
[0171] The following formulations are used to prepare compositions
for administration to premenopausal and menopausal women:
1 Component Dose Units Vitamin A (Beta Carotene) 5,000 I.U. Vitamin
D 400 I.U. Vitamin E 400 I.U. Vitamin C 100 I.U. Vitamin B1 20 mg.
Vitamin B2 20 mg. Vitamin B6 25 mg. Vitamin B12 50 mcg. Vitamin B3
100 mg. Folic Acid 1.0 mg. Calcium Carbonate 1,200 mg. Copper 2 mg.
Zinc 15 mg. Selenium 65 mcg. DHA/Linolenic/Linoleic Acid 50/25/25
mg.
[0172] It would be anticipated that upon administration of the
above composition, an average normal menopausal woman would
be-expected to have reduced incidence of nutritional deficiency and
reduced menopausal-related symptoms or disorders when compared to
an average normal menopausal woman following a conventional
nutritional regimen.
Example 2
[0173] The following compositions are for administration to
premenopausal women and menopausal women in accordance with the
regimen indicated below:
2 Regimen Component Dose First Morning Calcium Carbonate 350 mg
Tablet (orange): B Complex 55 mg Second Morning Calcium Carbonate
350 mg Tablet (white): Vitamin A 3,000 IU Vitamin C 100 IU Vitamin
D 400 IU Selenium 65 mcg Zinc 15 mg Cooper 2 mg Evening Tablet
Calcium Carbonate 350 mg B Complex 110 mg Vitamin A 2,000 IU Folic
Acid 1 mg Evening Capsule Vitamin E 400 IU DHA 50 mg Linolenic Acid
25 mg Linoleic Acid 25 mg Calcium Carbonate 150 mg
[0174] It would be anticipated than upon following the above
regimen, an average normal menopausal woman would be expected to
have reduced incidence of nutritional deficiency and reduced
menopausal-related symptoms or disorders when compared to an
average normal menopausal woman following a conventional
nutritional regimen.
Example 3
[0175] A soft gelatin supplement in accordance with the
compositions of Examples 1 and 2 above, may be prepared, by first
combining mineral oil and soybean oil in a first vessel and
blending it to form a uniform oil mixture, heating the oil mixture
to 45 degrees Celsius, and then adding propylene glycol. In a
second vessel preheated to 70 degrees Celsius, yellow beeswax and
soybean oil are added and blended until a uniform wax mixture is
formed. The wax mixture is cooled to 35 degrees Celsius and then
added to the oil mixture. To this combined oil and wax mixture,
folic acid, vitamin B.sub.6, iron, magnesium, and calcium are then
added and blended together to form a uniform biologically active
mixture. The mixture is then cooled to 30 degrees Celsius to form a
viscous biologically active core composition, after which time the
composition is ready for encapsulation in a soft gelatin shell.
[0176] A soft gelatin shell is prepared by heating purified water
in a suitable vessel and then adding gelatin. This water gelatin
mixture is mixed until the gelatin is fully dissolved, and then
glycerin, preservatives, one or more flavors, and one or more
colorants are added. This gelatin mixture is blended well and
cooled. The shells are then filled with the core composition and
formed in accordance with soft gelatin techniques commonly used and
well known to persons of skill in the art.
Example 4
[0177] The following compositions are for administration to
premenopausal women and menopausal women in accordance with the
regimen indicated below:
3 Regimen Component Dose First Morning Calcium Carbonate 350 mg
Tablet (orange): B Complex 55 mg Second Morning Calcium Carbonate
350 mg Tablet (white: Vitamin A 3,000 IU Vitamin C 100 IU Vitamin D
400 IU Selenium 65 mcg Zinc 15 mg Cooper 2 mg Evening Tablet
Calcium Carbonate 350 mg B Complex 110 mg Vitamin A 2,000 IU Folic
Acid 1 mg Evening Capsule Vitamin E 400 IU DHA 50 mg Linolenic Acid
25 mg Linoleic Acid 25 mg Calcium Carbonate 150 mg Evening Tablet
Alendronate 10 mg
[0178] It would be anticipated that upon following the above
regimen, an average normal menopausal woman would be expected to
have reduced incidence of nutritional deficiency and reduced
menopausal-related symptoms or disorders when compared to an
average normal menopausal woman following a conventional
nutritional regimen.
Example 5
[0179] The following compositions are for administration to
premenopausal women and menopausal women in accordance with the
regimen indicated below:
4 Regimen Component Dose First Morning Calcium Carbonate 350 mg
Tablet (orange): B Complex 55 mg Second Morning Calcium Carbonate
350 mg Tablet (white: Vitamin A 3,000 IU Vitamin C 100 IU Vitamin D
400 IU Selenium 65 mcg Zinc 15 mg Cooper 2 mg Evening Tablet
Calcium Carbonate 350 mg B Complex 110 mg Vitamin A 2,000 IU Folic
Acid 1 mg Evening Capsule Vitamin E 400 IU DHA 50 mg Linolenic Acid
25 mg Linoleic Acid 25 mg Calcium Carbonate 150 mg Evening Tablet
PREMPRO .TM. 2.5 mg conjugated estrogens 2.5 mg progesterone
[0180] It would be anticipated that upon following the above
regimen, an average normal menopausal woman would be expected to
have reduced incidence of nutritional deficiency and reduced
menopausal-related symptoms or disorders when compared to an
average normal menopausal woman following a conventional
nutritional regimen.
[0181] The inventive subject matter being thus described, it will
be apparent that the same may be varied in many ways. Such
variations are not to be regarded as a departure from the spirit
and scope of the inventive subject matter, and all such
modifications are intended to be within the scope of the appended
claims.
* * * * *