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US20030190376A1 - Anti-Aromatase composition - Google Patents

Anti-Aromatase composition Download PDF

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US20030190376A1
US20030190376A1 US10/342,582 US34258203A US2003190376A1 US 20030190376 A1 US20030190376 A1 US 20030190376A1 US 34258203 A US34258203 A US 34258203A US 2003190376 A1 US2003190376 A1 US 2003190376A1
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composition
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contain
aromatase
seed oil
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Michael Farley
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/42Cucurbitaceae (Cucumber family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/73Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • A61K36/736Prunus, e.g. plum, cherry, peach, apricot or almond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Definitions

  • This testosterone/estrone ratio will exert a powerful and considerable reactions to the emotional well being, as well as in sexual functions, libido, muscle mass and strength, energy, cardiovascular health, bone integrity and memory behavior.
  • testosterone/estrogen ratio is directly influenced by the aromitazation and bioavailable levels of several other hormones, including DHEA projesterone, androstenedione, estrone aldosterone, cortisol, estradiol and dihydrotestoasterone.
  • DHEA projesterone androstenedione
  • estrone aldosterone cortisol
  • estradiol estradiol
  • dihydrotestoasterone dihydrotestoasterone.
  • These hormones which directly effect testosterone and estrogen ratios also directly effect emotional well being, as well as sexual function, libido, muscle mass, fat to lean muscle ratios, strength, energy, cardiovascular health, osteoporosis, memory and cognitive function, as well as risk for breast cancer and benign prostate hypertrophy.
  • the present invention includes an anti-aromatase pharmaceutical or more specifically a nutraceutical composition in dose compound form comprising a formula in which each capsule or dose consists of:
  • Nettle root extract Uritica dioica 16:1 in the range of about 275 mg. to about 350 mg;
  • the present invention also relates to a totally new use of a male hormone panel aromatasition structure with an androgen pathway as depicted at Table I and II, also for breast cancer and other related treatments. TABLE I
  • Hormone Range Age Testosterone (Male) 70-135 20 yrs 60-110 20-30 yrs 50-80 31-40 yrs 40-70 41-50 yrs 35-65 51-60 yrs 20-55 61-70 yrs 15-45 70 yrs Dihydrotestosterone 22-72 30-39 yrs (Male) 52-123 40-49 yrs 51-107 50-59 yrs 39-89 60 yrs Androttenedione 100-150 (Male) 151-350 ⁇ close oversize brace ⁇ 15 yrs 351-450 (Female) 38-68 40-49 yrs 26-64 50-59 yrs 35-65 60 yrs
  • Tables I and II depict Aromatisation structure that are beneficial to the method of treatment of various ailments, for example, benign prostate hyperthrophy, some forms of breast cancer, and in the treatment of osteoporsis, etc.
  • the present invention relates to a totally new application of several naturally occurring aromatase inhibitors which interupt several stages in the presented hormone panel (Table I), which illustrates the currently accepted normal aromatization sequence.
  • This invention also incorporates for the first time, an inhibitor of sex hormone binding globulin which allows bioavailable hormone to remain active at target tissue sites for a longer period of time.
  • the present invention includes an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of:
  • Nettle root extract Uritica dioica 16:1 of about 300 mg;
  • this invention is an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of:
  • Nettle root extract Uritica dioica 16:1 of about 300 mg.
  • this invention resides in an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of:
  • Nettle root extract Urtica dioica ) 16:1 of about 300 mg.
  • the present invention is an anti-aromatase capsule or dose in compound form comprising a formula in the pharmaceutical or nutraceutical composition of which each capsule or dose consists of:
  • Nettle root extract Urtica dioica ) of about 300 mg.
  • the invention resides in a method of treatment utilizing a pharmaceutical composition consisting of a dosage or capsule constituted by an anti-aromatase pharmaceutical or nutraceutical composition in dose compound form comprising a formula in which each capsule or dose consists of:
  • Nettle root extract Urtica dioica 16:1 in the range of about 275 mg. to above 350 mg.;
  • the invention provides a method of treatment utilizing a pharmaceutical or nutraceutical composition consisting of a dosage or capsule constituted an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of:
  • Nettle root extract Uritica dioica 16:1 of about 300 mg.
  • the invention assists a method of treatment utilizing a pharmaceutical or nutraceutical composition consisting of a dosage or capsule constituting an anti-aromatase capsule or dose compound form in which the composition for the maintenance of testosterone/estrone ratios with the anti-aromatase composition being characterized by:
  • Nettle root extract Uritical dioica 16:1 of 275 mg. to above 350 mg.;
  • a method of treatment utilizing a specific nutraceutical or pharmaceutical anti-aromatase composition so as to maintain the testerone/estrone ratios said composition is characterized by:
  • Nettle root extract Uritica dioica ) of 300 mg.
  • the invention also includes a method of treatment utilizing a pharmaceutical or nutraceutical composition cosisting of a dosage or capsule constituting an anti-aromatase capsule or dose in compound form in which the composition consists of:
  • Nettle root extract Urtica dioica 16:1 of about 300 mg.
  • the invention furthermore includes a method of treatment utilizing a nutraceutical or a pharmaceutical composition consisting of a dosage or capsule constituted by an anti-aromatase capsule or dose in compound form comprising a formula in the composition of which each capsule or dose consists of:
  • Nettle root extract Urtica dioica ) of about 300 mg.
  • An anti-aromatase nutraceutical or pharmaceutical composition consisting of inc apsule or dose to contain:
  • Nettle root extract ( Urtica dioica ) 16:1 in the range of about 275 to 350 mg.
  • Pygeum Africanum Prunus africana bark extract standardized to contain at least 12 to 14% of total sterols in the range of about 20 to 40 mg.
  • This composition assists in the treatment of benign prostate hyperthropy and breast cancer etc.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Alternative & Traditional Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

An anti-aromatase nutraceutical or pharmaceutical composition, consisting of a capsule or dose to contain
Nettle root extract (Urtica dioica) 16:1 in the range of about 275 to 350 mg.
Pumpkin seed oil (Cucubita pepo) in the range of about 150 to 205 mg.
Pygeum Africanum (Prunus africana) bark extract standardized to contain at least 12 to 15% of total sterols in the range of about 20 to 40 mg. and
Chrysin in the range of 475 to 550 mg.
This composition assists in the treatment of benign prostate hyperthropy and breast cancer, etc. and also a method of utilizing the composition.

Description

  • This is a Divisional Application of patent application Ser. No. 09/921,018, filing date of Jun. 21, 2001.[0001]
  • It is known, that throughout life of a mammal or a human being, testosterone/estrone ratios do have a considerable effect on mammal or human life. [0002]
  • This testosterone/estrone ratio will exert a powerful and considerable reactions to the emotional well being, as well as in sexual functions, libido, muscle mass and strength, energy, cardiovascular health, bone integrity and memory behavior. [0003]
  • It is advantageous that testosterone/estrogen ratio is directly influenced by the aromitazation and bioavailable levels of several other hormones, including DHEA projesterone, androstenedione, estrone aldosterone, cortisol, estradiol and dihydrotestoasterone. These hormones which directly effect testosterone and estrogen ratios, also directly effect emotional well being, as well as sexual function, libido, muscle mass, fat to lean muscle ratios, strength, energy, cardiovascular health, osteoporosis, memory and cognitive function, as well as risk for breast cancer and benign prostate hypertrophy. [0004]
  • It is well established, that as a human being ages, these testosterone/estrone ratios adjust and change with age, with increasing formation levels of estrone and a proportional decrease in the formation of testosterone. [0005]
  • It is known from the specification of U.S. Pat. No. 4,598,072 to Schweibert et. al dated Jul. 1, 1986 to provide for an aromatase inhibitor and an antiandrogen which generally is applicable for the treatment of prostatic hyperglania, incorporated herein by reference only. [0006]
  • Furthermore, it is known from the specification of U.S. Pat. No. 5,972,921 to Santti et. al dated Oct. 26, 1999 in the use of an aromatase inhibitor administered for the specific treatment for men for detrusor wrethral dyssynergia. This is incorporated herein for reference only. [0007]
  • It is also known from the specification of U.S. Pat. No. 5,861,389 to Radlmaier et.al dated Jan. 19, 1999 for specific treatment of only androgen deficiency in men using selective aromatase inhibitors. This is incorporated herein for reference only.[0008]
  • The present invention includes an anti-aromatase pharmaceutical or more specifically a nutraceutical composition in dose compound form comprising a formula in which each capsule or dose consists of: [0009]
  • a. Nettle root extract ([0010] Uritica dioica) 16:1 in the range of about 275 mg. to about 350 mg;
  • b. Pumpkin seed oil ([0011] cucubita pepo) in the range of about 150 mg. to about 205 mg.;
  • c. Pygeum Africanum ([0012] prunus africana) bark extract standardized to contain about 12 to 14% of total sterols in the range of about 20 mg. to about 40 mg; and
  • d. Chrysin in the range of about 475 mg. to about 550 mg. [0013]
  • However, the present invention also relates to a totally new use of a male hormone panel aromatasition structure with an androgen pathway as depicted at Table I and II, also for breast cancer and other related treatments. [0014]
    TABLE I
    Figure US20030190376A1-20031009-C00001
  • [0015]
    TABLE II
    Normal Range of Hormone Values
    Figure US20030190376A1-20031009-P00899
    Hormone Range Age
    Testosterone (Male)  70-135 20 yrs
     60-110 20-30 yrs
    50-80 31-40 yrs
    40-70 41-50 yrs
    35-65 51-60 yrs
    20-55 61-70 yrs
    15-45 70 yrs
    Dihydrotestosterone 22-72 30-39 yrs
    (Male)  52-123 40-49 yrs
     51-107 50-59 yrs
    39-89 60 yrs
    Androttenedione 100-150
    (Male) 151-350 {close oversize brace} 15 yrs
    351-450
    Figure US20030190376A1-20031009-P00899
    (Female)
    38-68 40-49 yrs
    26-64 50-59 yrs
    35-65 60 yrs
  • Both Tables I and II depict Aromatisation structure that are beneficial to the method of treatment of various ailments, for example, benign prostate hyperthrophy, some forms of breast cancer, and in the treatment of osteoporsis, etc. [0016]
  • Specifically, the present invention relates to a totally new application of several naturally occurring aromatase inhibitors which interupt several stages in the presented hormone panel (Table I), which illustrates the currently accepted normal aromatization sequence. This invention also incorporates for the first time, an inhibitor of sex hormone binding globulin which allows bioavailable hormone to remain active at target tissue sites for a longer period of time. [0017]
  • Suitably, the present invention includes an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of: [0018]
  • a. Nettle root extract ([0019] Uritica dioica) 16:1 of about 300 mg;
  • b. Pumpkin seed oil ([0020] Cucubita pepo) in the range of about 150 mg. to about 205 mg.;
  • c. Pygeum Africanum ([0021] Prunus africana) bark extract standardized to contain about 12 to 14% of total sterols in the range of about 20 mg. to about 40 mg.; and
  • d. Chrysin in the range of about 475 mg. to about 550 mg. [0022]
  • Conveniently, this invention is an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of: [0023]
  • a. Pumpkin seed oil ([0024] Cucubita pepo) of about 175 mg;
  • b. Nettle root extract ([0025] Uritica dioica) 16:1 of about 300 mg.;
  • c. Pygeum Africanum ([0026] Prunus africana) bark extract standardized to contain 12 to 14% of total sterols in the range of about 20 mg. to about 40 mg; and
  • d. Chrysin in the range of about 475 mg. to about 550 mg. [0027]
  • Advantageously, this invention resides in an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of: [0028]
  • a. Pygeum Africanum ([0029] Prunus africana) bark extract standardized to contain 13% total sterols and about 25 mg.;
  • b. Pumpkin seed oil ([0030] Cucubita pepo) of about 175 mg.;
  • c. Nettle root extract ([0031] Urtica dioica) 16:1 of about 300 mg.; and
  • d. Chrysin in the range of about 475 mg. to about 550 mg. [0032]
  • Moreover, the present invention is an anti-aromatase capsule or dose in compound form comprising a formula in the pharmaceutical or nutraceutical composition of which each capsule or dose consists of: [0033]
  • a. Chrysin of about 500 mg.; [0034]
  • b. Nettle root extract ([0035] Urtica dioica) of about 300 mg.;
  • c. Pumpkin seed oil ([0036] Cucubita pepo) of about 175 mg.; and
  • d. Pygeum Africanum ([0037] Prunus africana) bark extract standardized to contain 13% total sterols and about 25 mg.
  • In addition, the invention resides in a method of treatment utilizing a pharmaceutical composition consisting of a dosage or capsule constituted by an anti-aromatase pharmaceutical or nutraceutical composition in dose compound form comprising a formula in which each capsule or dose consists of: [0038]
  • a. Nettle root extract ([0039] Urtica dioica) 16:1 in the range of about 275 mg. to above 350 mg.;
  • b. Pumpkin seed oil ([0040] Cucubita pepo) in the range of about 150 mg. to about 205 mg.;
  • c. Pygeum Africanum ([0041] Prunus africana) bark extract standardized to contain 12 to 14% of total sterols in the range of about 20 mg. to about 40 mg.; and
  • d. Chrysin in the range of about 475 mg. to about 550 mg. [0042]
  • Also, the invention provides a method of treatment utilizing a pharmaceutical or nutraceutical composition consisting of a dosage or capsule constituted an anti-aromatase capsule or dose in compound form in which the pharmaceutical or nutraceutical composition consists of: [0043]
  • a. Nettle root extract ([0044] Uritica dioica) 16:1 of about 300 mg.;
  • b. Pumpkin seed oil ([0045] Cucubita pepo) in the range of about 150 mg. to about 205 mg.;
  • c. Pygeum Africanum ([0046] Prunus africana) bark extract standardized to contain about 12 to 14% of total sterols in the range of about 20 mg. to about 40 mg.; and
  • d. Chrysin in the range of about 475 mg. to about 550 mg. [0047]
  • Furthermore, the invention assists a method of treatment utilizing a pharmaceutical or nutraceutical composition consisting of a dosage or capsule constituting an anti-aromatase capsule or dose compound form in which the composition for the maintenance of testosterone/estrone ratios with the anti-aromatase composition being characterized by: [0048]
  • a. Nettle root extract ([0049] Uritical dioica) 16:1 of 275 mg. to above 350 mg.;
  • b. Pumpkin seed oil ([0050] Cucubita pepo) of 150 mg. to about 205 mg.;
  • c. Pygeum Africanum ([0051] Prunus africana) bark extract standardized to contain about 12 to 14% of total sterols of 20 mg. to about 40 mg.; and
  • d. Chrysin of 475 mg. to 550 mg. [0052]
  • Advantageously, a method of treatment utilizing a specific nutraceutical or pharmaceutical anti-aromatase composition so as to maintain the testerone/estrone ratios, said composition is characterized by: [0053]
  • a. Chrysin of 500 mg.; [0054]
  • b. Nettle root extract ([0055] Uritica dioica) of 300 mg.;
  • c. Pumpkin seed oil ([0056] Cucubita pepo) of 175 mg.; and
  • d. Pygeum Africanum ([0057] Prunus africana) bark extract standardized to contain 13% total sterols and 25 mg.
  • The invention also includes a method of treatment utilizing a pharmaceutical or nutraceutical composition cosisting of a dosage or capsule constituting an anti-aromatase capsule or dose in compound form in which the composition consists of: [0058]
  • a. Pygeum Africanum ([0059] Prunus africana) bark extract standardized to contain 13Λ total sterols and about 25 mg.;
  • b. Pumpkin seed oil ([0060] Cucubita pepo) of about 175 mg.;
  • c. Nettle root extract ([0061] Urtica dioica) 16:1 of about 300 mg.; and
  • d. Chrysin in the range of about 475 mg. to about 550 mg. [0062]
  • The invention furthermore includes a method of treatment utilizing a nutraceutical or a pharmaceutical composition consisting of a dosage or capsule constituted by an anti-aromatase capsule or dose in compound form comprising a formula in the composition of which each capsule or dose consists of: [0063]
  • a. Chyrsin of about 500 mg.; [0064]
  • b. Nettle root extract ([0065] Urtica dioica) of about 300 mg.;
  • c. Pumpkin seed oil ([0066] Cucubita pepo) of about 175 mg.; and
  • d. Pygeum Africanum ([0067] Prunus africana) bark extract stadardized to contain 13% total sterols and about 25 mg.
  • An anti-aromatase nutraceutical or pharmaceutical composition, consisting of inc apsule or dose to contain: [0068]
  • Nettle root extract ([0069] Urtica dioica) 16:1 in the range of about 275 to 350 mg.
  • Pumpkin seed oil ([0070] Cucubita pepo) in the range of about 150 to 205 mg.
  • Pygeum Africanum ([0071] Prunus africana) bark extract standardized to contain at least 12 to 14% of total sterols in the range of about 20 to 40 mg. and
  • Chrysin in the range of 475 to 550 mg. [0072]
  • This composition assists in the treatment of benign prostate hyperthropy and breast cancer etc. [0073]

Claims (5)

1. A method of treatment utilizing a pharmaceutical or nutraceutical anti-aromatase composition for the maintenance of testostrone/estrone ratioos said anti-aromatase composition is characterized by:
a. Nettle root extract (Uritica dioica) 16:1 of 275 to above 350 mg.;
b. Pumpkin seed oil (Cucubita pepo) of 150 mg. to about 205 mg.;
c. Pygeum Africanum (Prunus africana) bark extract standardized to contain about 12 to 14% of total sterols of 20 mg. to about 40 mg.; and
d. Chrysin of 475 mg. to 550 mg.
2. A method of treatment as claimed in claim 1, wherein the composition consists of:
a. Nettle root extract (Uritica dioica) 16:1 of 300 mg.;
b. Pumpkin seed oil (Cucubita pepo) of 150 mg. to 205 mg.;
c. Pygeum Africanum (Prunus africana) bark extract standarized to contain about 12 to 14% of total sterols of 20 mg. to 40 mg.; and
d. Chrysin of 475 mg. to 550 mg.
3. A method of treatment as claimed in claim 1, wherein the composition comprising:
a. Pumpkin seed oil (Cucubita pepo) of 175 mg.;
b. Nettle root extract (Uritica dioica) 16:1 of 300 mg.;
c. Pygeum Africanum (Prunus africana) bark extract standardized to contain 12 to 14% of total sterols of 20 mg. to 40 mg.; and
d. Chrysin of 475 mg. to 550 mg.
4. A method of treatment utilizing a composition as claimed in claim 1, wherein the composition comprising:
a. Pygeum Africanum (Prunus africana) bark extract standardized to contain 13% total sterols and 25 mg.;
b. Pumpkin seed oil (Cucubita pepo) of 175 mg.;
c. Nettle root extract (Uritica dioica) 16:1 of 300 mg.; and
d. Chrysin in the range of about 475 mg. to 550 mg.
5. A method of treatment utilizing a nutraceutical or pharmaceutical anti-aromatase composition for the maintenance of testerone/estrone ratios, said composition comprising:
a. Chyrsin of 500 mg.;
b. Nettle root extract (Uritica dioica) of 300 mg.;
c. Pumpkin seed oil (Cucubita pepo) of 175 mg.; and
d. Pygeum Africanum (Prunus africana) bark extract standardized to contain 13% total sterols and 25 mg.
US10/342,582 2001-06-21 2003-01-13 Anti-Aromatase composition Abandoned US20030190376A1 (en)

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