US4425339A
Expired / Lapsed
US
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Treatment of menopausal symptoms
Assignee: Syntex Pharmaceuticals International Ltd
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Filing: 1981-04-09
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Granted: 1984-01-10
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Expires: 2001-04-09
Abstract
Abstract A method for treating menopausal symptoms and a pharmaceutical package for effecting the method are disclosed. The method comprises a three phase sequence of estrogen and progestogen administration and an additional drug-free fourth phase during at least one menstrual cycle as follows: (a) as phase one, 0.2 mg to 1.5 mg of estrone, (or of other natural estrogen in an amount sufficient to result in an effect equivalent to the selected amount of estrone within the aforegiven range) for 4-9 days, followed by (b) as phase two, 0.2 mg to 1.5 mg of estrone, (or of other natural estrogen in an amount sufficient to result in an effect equivalent to the selected amount of estrone within the aforegiven range), plus 0.2 to 1.5 mg of norethisterone (or of other styptic progestogen, in an amount sufficient to result in an effect equivalent to the selected amount of norethisterone within the aforegiven range); with the proviso that the dosage levels of estrogen and progestogen be approximately equal (as defined in terms of estrone and nonethisterone above); for 6-11 days, followed by (c) as phase three, twice the dosage of estrogen and twice the dosage of progestogen used in phase two, for at least 6 days, or for an arbitrarily selected greater number of days to a maximum of 90 days; followed by (d) as phase four, no therapeutically active dosage, i.e., either no treatment or a placebo, for 6-8 days.
Inventors
- 👤 Alan G. Pitchford
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 00:19
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/56; A61K31/565
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
175 words
A method for treating menopausal symptoms in the female human, which method comprises administering to a subject in need of such treatment, a daily sequence of unit dosages over a repeating cycle, which dosage sequence comprises: (a) administering, as phase one, for a period of 4-9 days, a natural estrogen in daily dosages corresponding in estrogenic activity to about 0.2-1.5 mg of estrone, followed by (b) administering, as phase two, for a period of 6-11 days, daily dosages of a combination of a natural estrogen and a styptic progestogen, wherein the amounts of estrogen and progestogen are approximately equal by weight and correspond in estrogenic activity to about 0.2-1.5 mg of estrone, and in progestogenic activity to about 0.2-1.5 mg of norethisterone, followed by (c) administering, as phase three, for a period of 6-90 days, a combination of a natural estrogen and a styptic progestogen in daily dosages twice those administered in phase two, followed by (d) administering, as phase four, no therapeutically active dosage, i.e., either no treatment or a placebo, for 6-8 days.
Claim 2
Independent Claim
175 words
A method for treating menopausal symptoms in the female human, which method comprises administering to a subject in need of such treatment, a daily sequence of unit dosages over a repeating cycle, which dosage sequence comprises: (a) administering, as phase one, for a period of 4-9 days, a natural estrogen in daily dosages corresponding in estrogenic activity to about 0.2-1.5 mg of estrone, followed by (b) administering, as phase two, for a period of 6-11 days, daily dosages of a combination of a natural estrogen and a styptic progestogen, wherein the amounts of estrogen and progestogen are approximately equal by weight and correspond in estrogenic activity to about 0.2-1.5 mg of estrone, and in progestogenic activity to about 0.2-1.5 mg of norethisterone, followed by (c) administering, as phase three, for a period of 6-90 days, a combination of a natural estrogen and a styptic progestogen in daily dosages twice those administered in phase two, followed by (d) administering, as phase four, no therapeutically active dosage, i.e., either no treatment or a placebo, for 6-8 days.
Claim 3
Dependent Claim
38 words
The method of claim 1 wherein the period specified in (a) is 5 days; the period specified in (b) is 7 days; the period specified in (c) is 9 days; the period specified in (d) is 7 days.
Claim 4
Dependent Claim
95 words
The method of claim 2, wherein: the dosage in (a) of natural estrogen corresponds in estrogenic activity to about 0.4-0.6 mg of estrone; the dosages in (b) of natural estrogen and styptic progestogen correspond in estrogenic activity to about 0.4-0.6 mg of estrone, and in progestogenic activity to about 0.4-0.6 mg of norethisterone; the dosages in (c) of natural estrogen and styptic progestogen are each twice the amount of the corresponding hormone in (b), and correspond in estrogenic activity to about 0.8-1.2 mg of estrone, and in progestogenic activity to about 0.8-1.2 mg of norethisterone.
Claim 5
Dependent Claim
95 words
The method of claim 2, wherein: the dosage in (a) of natural estrogen corresponds in estrogenic activity to about 0.9-1.1 mg of estrone; the dosages in (b) of natural estrogen and styptic progestogen correspond in estrogenic activity to about 0.9-1.1. mg of estrone, and in progestogenic activity to about 0.9-1.1 mg of norethisterone; the dosages in (c) of natural estrogen and styptic progestogen are each twice the amount of the corresponding hormone in (b) and correspond in estrogenic activity to about 1.8-2.2 mg of estrone, and in progestogenic activity to about 1.8-2.2 mg of norethisterone.
Claim 6
Dependent Claim
14 words
The method of claim 3 or claim 4 wherein the natural estrogen is estrone.
Claim 7
Dependent Claim
13 words
The method of claim 3 or claim 4 wherein the progestrogen is norethisterone.
Claim 8
Dependent Claim
19 words
The method of claim 3 or claim 4 wherein the natural estrogen is estrone and the progestogen is norethisterone.
Claim 9
Dependent Claim
151 words
A pharmaceutical composition for treating menopausal symptoms in the human female which comprises: (a) 4-6 dosage units each containing, in admixture with a pharmaceutically acceptable excipient, a natural estrogen in an amount corresponding in estrogenic activity to about 0.2 mg to 1.5 mg of estrone; and (b) 6-11 dosage units, each containing, in admixture with a pharmaceutically acceptable excipient, a combination of a natural estrogen and a styptic progestogen, wherein the amounts of estrogen and progestogen are approximately equal by weight and correspond in estrogenic activity to about 0.2 to 1.5 mg of estrone, and in progestogenic activity to about 0.2 to 1.5 mg of norethisterone; and (c) 6-90 dosage units each containing, in admixture with a pharmaceutically acceptable excipient, twice the amount of estrone and twice the amount of progestogen as in (b); and optionally (d) 6-8 dosage units containing no estrogen or progestogen but only a pharmaceutically acceptable placebo.
Claim 10
Dependent Claim
151 words
A pharmaceutical composition for treating menopausal symptoms in the human female which comprises: (a) 4-6 dosage units each containing, in admixture with a pharmaceutically acceptable excipient, a natural estrogen in an amount corresponding in estrogenic activity to about 0.2 mg to 1.5 mg of estrone; and (b) 6-11 dosage units, each containing, in admixture with a pharmaceutically acceptable excipient, a combination of a natural estrogen and a styptic progestogen, wherein the amounts of estrogen and progestogen are approximately equal by weight and correspond in estrogenic activity to about 0.2 to 1.5 mg of estrone, and in progestogenic activity to about 0.2 to 1.5 mg of norethisterone; and (c) 6-90 dosage units each containing, in admixture with a pharmaceutically acceptable excipient, twice the amount of estrone and twice the amount of progestogen as in (b); and optionally (d) 6-8 dosage units containing no estrogen or progestogen but only a pharmaceutically acceptable placebo.
Claim 11
Dependent Claim
43 words
The pharmaceutical composition of claim 8, wherein the number of dosage units in (a) is 5; the number of dosage units in (b) is 7; the number of dosage units in (c) is 9; the number of dosage units in (d) is 7.
Claim 12
Dependent Claim
96 words
The pharmaceutical composition of claim 8, wherein the dosage in (a) of natural estrogen corresponds in estrogenic activity to about 0.4-0.6 mg of estrone; the dosages in (b) of natural estrogen and styptic progestogen correspond in estrogenic activity to about 0.4-0.6 mg of estrone and in progestogenic activity to about 0.4-0.6 mg of norethisterone; the dosages in (c) of natural estrogen and styptic progestogen are each twice the amount of the corresponding hormone in (b) and correspond in estrogenic activity to about 0.8-1.2 mg of estrone and in progestogenic activity to about 0.8-1.2 mg of norethisterone.
Claim 13
Dependent Claim
96 words
The pharmaceutical composition of claim 8, wherein the dosage in (a) of natural estrogen corresponds in estrogenic activity to about 0.9-1.1 mg of estrone; the dosages in (b) of natural estrogen and styptic progestogen correspond in estrogenic activity to about 0.9-1.1 mg of estrone and in progestogenic activity to about 0.9-1.1 mg of norethisterone, the dosages in (c) of natural estrogen and styptic progestogen are each twice the amount of the corresponding hormone in (b) and correspond in estrogenic activity to about 1.8-2.2 mg of estrone and in progestogenic activity to about 1.8-2.2 mg of norethisterone.
Claim 14
Dependent Claim
14 words
The pharmaceutical composition of claim 10 or 11, wherein the natural estrogen is estrone.
Claim 15
Dependent Claim
14 words
The pharmaceutical composition of claim 10 or 11, wherein the styptic progestogen is norethisterone.
Claim 16
Dependent Claim
20 words
The pharmaceutical composition of claim 10 or 11, wherein the natural estrogen is estrone and the styptic progestogen is norethisterone.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-01-09 | 1987-07-11 | 1988-01-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-01-09 | 1991-07-11 | 1992-01-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-01-09 | 1995-07-11 | 1996-01-10 | $7700.00 | Window Closed / Lapsed |