Administration of non-oral androgenic steroids to women

Details Administration of non-oral androgenic steroids to women Administration of non-oral androgenic steroids to women

2000-06-09

2003-06-24

Pryor, Alton N (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

C514S169000, C514S170000, C514S172000, C514S177000, C514S178000, C514S182000

Reexamination Certificate

active

06583129

ABSTRACT:

THE FIELD OF THE INVENTION
This invention broadly relates to the administration of androgens to women. Accordingly, this invention covers the fields of pharmaceutical sciences and medicine.
BACKGROUND OF THE INVENTION
It is known that a functional level of androgenic hormones in females promotes sexual health and activity, feelings of well being, maximizes muscle mass and function, and inhibits bone loss. Further, a functional level of androgenic hormones may promote cardiovascular and coronary health, decrease breast tenderness, decrease vasomotor instability, modulate immune function, enhance certain cognitive abilities, improve urogential health, reduce estrogen supplementation related side effects, and provide direct neuroprotective effects.
The attainment of functional levels of androgenic hormones in women, such as testosterone, may be influenced by the serum concentrations of sex hormone binding globulin (SHBG). SHBG is a protein produced by the liver that binds sex hormones such as testosterone and estradiol in the blood. The SHBG-bound sex hormones are generally “non-functional”, i.e., unavailable to exert biological action at sex hormone receptors in target tissues and/or undergo clearance from the blood.
Use of oral estrogens raises serum levels of SHBG. SHBG levels are also elevated in various conditions, e.g., hyperthyroidism and pregnancy, and by certain other medications, e.g., anti-convulsants. Elevated SHBG levels alter the levels of androgenic hormones and the doses needed to achieve functional levels.
The present invention provides methods, compositions, and kits to achieve functional levels of androgenic steroids in women with elevated SHBG levels and thus improve their health.
SUMMARY OF THE INVENTION
Accordingly, the present invention provides a method and kit for improving health in a woman who has an elevated or substantially elevated level of sex hormone binding globulin (SHBG). Additionally, the present invention provides a method and kit for improving health in a woman receiving oral estrogen supplementation. Further, the present invention provides a method and kit for improving health in a woman in need of oral estrogen supplementation.
In one aspect, such methods include non-orally administering an androgenic steroid, in an amount sufficient to provide a therapeutic effect in the presence of elevated, or substantially elevated SHBG levels. In another aspect, such methods include non-orally administering an androgenic steroid, in an amount sufficient to provide a therapeutic effect in the presence of an oral estrogen administration. In yet another aspect, such methods include co-administering an effective amount of an orally administered estrogen and an amount of a non-orally administered androgenic steroid which is sufficient to provide a therapeutic effect in the presence of oral estrogen administration.
Examples of specific androgenic steroids which may be utilized include but are not limited to: testosterone, methyltestosterone, androstenedione, adrenosterone, dehydroepiandrosterone, oxymetholone, fluoxymesterone, methandrostenolone, testolactone, pregnenolone, 17&agr;-methylnortestosterone, norethandrolone, dihydrotestosterone, danazol, oxymetholone, androsterone, nandrolone, stanozolol, ethylestrenol, oxandrolone, bolasterone and mesterolone, testosterone propionate, testosterone cypionate, testosterone phenylacetate, and testosterone enanthate, testosterone acetate, testosterone buciclate, testosterone heptanoate, testosterone decanoate, testosterone caprate, testosterone isocaprate, isomers and derivatives thereof, and a combination thereof.
The amount of androgenic steroid to be administered may be measured according to several different parameters. In one aspect, the amount of androgenic steroid administered may be an amount sufficient to achieve a therapeutic effect equivalent to a total testosterone serum level of from about 15 to about 1000 ng/dl. In another aspect of the present invention, the amount of androgenic steroid administered may be an amount sufficient to achieve a therapeutic effect equivalent to a free testosterone serum level of from about 0.5 to about 30 pg/ml. In a further aspect of the present invention, the amount of androgenic steroid administered may be an amount sufficient to achieve a therapeutic effect equivalent to a bioavailable testosterone serum level of from about 1 to about 70 ng/dl. In yet another aspect of the present invention, the amount of androgenic steroid administered may be an amount sufficient to achieve a therapeutic effect equivalent to a testosterone dosage of at least about 50 mcg/day.
Examples of specific estrogens which may be utilized in connection with the method of the present invention include but are not limited to: 17&bgr;-estradiol, 17&agr;-estradiol, conjugated equine estrogen, esterified estrogen, micronized estradiol, sodium estrogen sulfate, ethinyl estradiol, estrone, tibolone, selective estrogen receptor modulators (SERM's), phytoestrogens, isomers and derivatives thereof, and a combination thereof. In one aspect of the invention, the amount of estrogen administered may be a dosage sufficient to achieve a therapeutic effect equivalent to a conjugated equine estrogen dosage of about 0.2 to about 3.0 mg/day.
Various forms of non-oral administration of androgen may be employed in accordance with the methods of the present invention, including but not limited to: topical administration, or parenteral administration, or a combination thereof. In one aspect, the forms of topical administration include without limitation, transdermal, or transmucosal, or sublingual, or a combination thereof. In another aspect, the parentarel forms of administration include without limitation, intramuscular injection, or subcutaneous implantation, or a combination thereof.
A progestin may be coadministered with the androgenic steroid and the estrogen, when desired. In one aspect, the progestin administration may be an amount sufficient to provide endometrial safety during oral estrogen administration. In another aspect, the progestin administration may be an amount sufficient to provide effective contraception.
There are many indicators of the improved health which may occur as a result of the method of the present invention. Of particular note, without limitation thereto, are the restoration, enhancement, improvement, or prevention of characteristics such as: sexual desire, frequency of sexual activity, stimulation to sexual organs, ability to achieve orgasm, pleasure in sexual activity, vital energy, sense of well-being, mood and sense of emotional well being, shyness, cognitive abilities, muscle mass and function, body composition, bone mineral density, skin and hair condition, pubic hair, urogenital atrophy, vaginal dryness, dry eyes, health in autoimmune conditions, vasomotor instability, breast tenderness, symptoms of premenstrual syndrome, and a combination thereof.


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