US3957982A
Expired / Lapsed
US
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Method for contraception by the application of combination-type sequential preparations
Assignee: Bayer Pharma AG
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Filing: 1974-12-23
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Granted: 1976-05-18
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Expires: 1994-12-23
Abstract
Abstract Method of contraception in which an estrogen and a progestagen are orally administered daily for 21 days, the first 4-6 days at a low contraceptively effective daily dose, the next 4-6 days at a daily estrogen dose 1-2 times and a daily progestrogen dose 1-1.5 times that of the first 4-6 days, and for the next 9-11 days at a daily estrogen dose from that of the first 4-6 days to that of the next 4-6 days and a daily progestogen dose higher than either prior daily dose, up to 3 times that of the initial dose, followed by 7 days without hormone administration.
Inventors
- 👤 Ursula Lachnit-Fixson
- 👤 Alan G. Pitchford
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 00:48
CPC Classifications
A; A61; A61K; A61K45/00; A61K45/06
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
156 words
A method of contraception which comprises administering for 21 successive days to a female of child-bearing age a combination of an estrogen and a progestogen, for the first 4-6 days in a low but contraceptively effective daily dosage corresponding in estrogenic activity to 0.020-0.050 mg. of 17α-ethinylestradiol and in progestogenic activity to 0.050-0.125 mg. of d-norgestrel; for the next 4-6 days, at an estrogen daily dosage from 1-2 times the initial daily low dosage and at a progestogen daily dosage of from 1-1.5 times the dosage of the first 4-6 days; and for the next 9-11 days, at a daily estrogen dosage of from the initial daily dosage to the subsequent daily dosage and at a progestogen daily dosage higher than the previous daily dosages of up to 3 times that of the first daily dosage and corresponding in progestogenic activity to 0.100-0.250 mg. of d-norgestrel, followed by about 7 days without progestogen and estrogen administration.
Claim 2
Independent Claim
156 words
A method of contraception which comprises administering for 21 successive days to a female of child-bearing age a combination of an estrogen and a progestogen, for the first 4-6 days in a low but contraceptively effective daily dosage corresponding in estrogenic activity to 0.020-0.050 mg. of 17α-ethinylestradiol and in progestogenic activity to 0.050-0.125 mg. of d-norgestrel; for the next 4-6 days, at an estrogen daily dosage from 1-2 times the initial daily low dosage and at a progestogen daily dosage of from 1-1.5 times the dosage of the first 4-6 days; and for the next 9-11 days, at a daily estrogen dosage of from the initial daily dosage to the subsequent daily dosage and at a progestogen daily dosage higher than the previous daily dosages of up to 3 times that of the first daily dosage and corresponding in progestogenic activity to 0.100-0.250 mg. of d-norgestrel, followed by about 7 days without progestogen and estrogen administration.
Claim 3
Dependent Claim
14 words
A method according to claim 1 wherein the estrogen and progestogen are administered orally.
Claim 4
Dependent Claim
15 words
A method according to claim 1 wherein the estrogen and progestogen are administered in admixture.
Claim 5
Dependent Claim
51 words
A method according to claim 1 wherein the first combination of estrogen and progestogen is administered for 6 days, the second combination of estrogen and progestogen is administered for 5 days, the third combination of estrogen and progestogen is administered for 10 days and a placebo is administered for 7 days.
Claim 6
Dependent Claim
18 words
A method according to claim 1 wherein in at least one of the stages the estrogen is 17α-ethinylestradiol.
Claim 7
Dependent Claim
15 words
A method according to claim 5 wherein the estrogen in all three stages is 17α-ethinylestradiol.
Claim 8
Dependent Claim
18 words
A method according to claim 1 wherein in at least one of the stages the progestogen is d-norgestrel.
Claim 9
Dependent Claim
15 words
A method according to claim 7 wherein the progestogen in all three stages is d-norgestrel.
Claim 10
Dependent Claim
22 words
A method according to claim 1 wherein in at least one of the stages the progestogen is cyproterone acetate or 17α-ethinyl-19-nortestosterone acetate.
Claim 11
Dependent Claim
28 words
A method according to claim 1 wherein in all three stages the progestogen is d-norgestrel and the estrogen is 17α-ethinyl-19-nortestosterone acetate and they are administered orally in admixture.
Claim 12
Dependent Claim
49 words
A method according to claim 9 wherein 0.040 - 0.090 mg., 0.050 - 0.125 mg. and 0.100 - 0.250 mg., respectively, of d-norgestrel and 0.020 - 0.050 mg., 0.030 - 0.050 mg. and 0.025 - 0.050 mg., respectively, of 17α-ethinylestradiol are administered in the first, second and third stages.
Claim 13
Dependent Claim
200 words
The three-stage oral contraceptive composition comprising 21 separate dosage units, adapted for successive daily oral ingestion, consisting essentially of: as the first stage, 4-6 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen and a progestogen at low but contraceptively effective respective dosages corresponding in activity to 0.020-0.050 mg. of 17α-ethinyl-estradiol and in progestogenic activity to 0.050-0.125 mg. of d-norgestrel followed by, as the second stage, 4-6 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a dosage from the same to twice the dosage of the first stage, and a progestogen at a dosage from 1-1.5 times the dosage of the first stage, followed by, as the third stage, 9-11 dosage units containing, in admixture with pharmaceutically acceptable carrier, a combination of an estrogen at a dosage from that of the first stage to that of the second stage, and a progestogen at a higher dosage than the first and second stages up to three times that of the first stage and corresponding in progestogenic activity to 0.100-0.250 mg. of d-norgestrel, optionally followed by, as the fourth stage, 7 dosage units free of estrogen and progestogen.
Claim 14
Dependent Claim
200 words
The three-stage oral contraceptive composition comprising 21 separate dosage units, adapted for successive daily oral ingestion, consisting essentially of: as the first stage, 4-6 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen and a progestogen at low but contraceptively effective respective dosages corresponding in activity to 0.020-0.050 mg. of 17α-ethinyl-estradiol and in progestogenic activity to 0.050-0.125 mg. of d-norgestrel followed by, as the second stage, 4-6 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a dosage from the same to twice the dosage of the first stage, and a progestogen at a dosage from 1-1.5 times the dosage of the first stage, followed by, as the third stage, 9-11 dosage units containing, in admixture with pharmaceutically acceptable carrier, a combination of an estrogen at a dosage from that of the first stage to that of the second stage, and a progestogen at a higher dosage than the first and second stages up to three times that of the first stage and corresponding in progestogenic activity to 0.100-0.250 mg. of d-norgestrel, optionally followed by, as the fourth stage, 7 dosage units free of estrogen and progestogen.
Claim 15
Dependent Claim
16 words
A composition according to claim 12 wherein the dosage units are in the form of tablets.
Claim 16
Dependent Claim
18 words
A composition according to claim 12 wherein in at least one of the stages the estrogen is 17α-ethinylestradiol.
Claim 17
Dependent Claim
15 words
A composition according to claim 14 wherein the estrogen in all three stages is 17α-ethinylestradiol.
Claim 18
Dependent Claim
18 words
A composition according to claim 12 wherein in at least one of the stages the progestogen is d-norgestrel.
Claim 19
Dependent Claim
15 words
A composition according to claim 16 wherein the progestogen in all three stages is d-norgestrel.
Claim 20
Dependent Claim
22 words
A composition according to claim 12 wherein in at least one of the stages the progestogen is cyproterone acetate or 17α-ethinyl-19-nortestosterone acetate.
Claim 21
Dependent Claim
21 words
A composition according to claim 12 wherein in all three stages the progestogen is d-norgestrel and the estrogen is 17α-ethinyl-19-nortestosterone acetate.
Claim 22
Dependent Claim
48 words
A composition according to claim 19 wherein 0.040 - 0.090 mg., 0.050 - 0.125 mg. and 0.100 - 0.250 mg., respectively, of d-norgestrel and 0.020 - 0.050 mg., 0.030 - 0.050 mg. and 0.025 - 0.050 mg., respectively, of 17α-ethinylestradiol and in the first, second and third stages.
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) | 1979-05-18 | 1979-11-17 | 1980-05-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-05-18 | 1983-11-17 | 1984-05-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-05-18 | 1987-11-17 | 1988-05-18 | $7700.00 | Window Closed / Lapsed |