US4616006A
Expired / Lapsed
US
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Triphasic oral contraceptive
Assignee: Ortho Pharmaceutical Corp
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Filing: 1985-06-13
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Granted: 1986-10-07
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Expires: 2005-06-13
Abstract
Abstract A method of contraception in which an estrogen and a progestogen are administered daily in a three phase sequence for 21 days is disclosed. In the first phase a combination of an estrogen and a progestogen in a low but contraceptively effective daily dosage corresponding in estrogenic activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone is administered for 5-8 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.25-1.0 mg of norethindrone for 7-11 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.35-2.0 mg of norethindrone for 3-7 days; followed by 6-8 days without administering either an estrogen or a progestogen.
Inventors
- 👤 Samuel A. Pasquale
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 11:15
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/56; A61K31/565
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
172 words
A triphasic oral contraceptive unit consisting of 21 separate dosage units, adapted for successive daily oral administration comprising: 7 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen and a progestogen at contraceptively effective dosages corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone as the first phase; followed by 7 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.25-1.0 mg of norethindrone as the second phase; followed by 7 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.35-2.0 mg of norethindrone as the third phase, and optionally containing 7 dosage units free of estrogen and progestogen; provided that the estrogen daily dosage is the same in all three phases.
Claim 2
Dependent Claim
172 words
A triphasic oral contraceptive unit consisting of 21 separate dosage units, adapted for successive daily oral administration comprising: 7 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen and a progestogen at contraceptively effective dosages corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone as the first phase; followed by 7 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.25-1.0 mg of norethindrone as the second phase; followed by 7 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.35-2.0 mg of norethindrone as the third phase, and optionally containing 7 dosage units free of estrogen and progestogen; provided that the estrogen daily dosage is the same in all three phases.
Claim 3
Dependent Claim
16 words
The unit according to claim 1 wherein the dosage units are in the form of tablets.
Claim 4
Dependent Claim
17 words
The unit according to claim 1 wherein the estrogen is selected from 17α-ethinylestradiol, estrone, estradiol and estriol.
Claim 5
Dependent Claim
11 words
The unit according to claim 2 wherein the estrogen is 17α-ethinylestradiol.
Claim 6
Dependent Claim
18 words
The unit according to claim 1 wherein the progestogen is selected from D-norgestrel, norethindrone, progesterone and D-17β-acetoxy-13β-ethyl-17α-ethinyl-gon-4-en-3-one oxime.
Claim 7
Dependent Claim
11 words
The unit according to claim 5 wherein the progestogen is norethindrone.
Claim 8
Dependent Claim
12 words
The unit according to claim 5 wherein the progestogen is D-17β-acetoxy-13β-ethyl-17α-ethinyl-gon-4-en-3-one oxime.
Claim 9
Dependent Claim
55 words
A composition according to claim 1 wherein the estrogen daily dosage in all three phases is equivalent to 0.035 mg of 17α-ethinylestradiol; and the progestogen daily dosage is equivalent to 0.50 mg of norethindrone in the first phase, 0.75 mg of norethindrone in the second phase and 1.0 mg of norethindrone in the third phase.
Claim 10
Dependent Claim
55 words
A composition according to claim 1 wherein the estrogen daily dosage in all three phases is equivalent to 0.035 mg of 17α-ethinylestradiol; and the progestogen daily dosage is equivalent to 0.180 mg of norgestimate in the first phase, 0.215 mg of norgestimate in the second phase and 0.250 mg of norgestimate in the third phase.
Claim 11
Dependent Claim
172 words
A triphasic oral contraceptive unit consisting of 21 separate dosage units, adapted for successive daily oral administration comprising: 5-8 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen and a progestogen at contraceptively effective dosages corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone as the first phase; followed by 7-11 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.25-1.0 mg of norethindrone as the second phase; followed by 3-7 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.35-2.0 mg of norethindrone as the third phase, and optionally containing 6-8 dosage units free of estrogen and progestogen; provided that the estrogen daily dosage is the same in all three phases.
Claim 12
Dependent Claim
172 words
A triphasic oral contraceptive unit consisting of 21 separate dosage units, adapted for successive daily oral administration comprising: 5-8 dosage units containing, in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen and a progestogen at contraceptively effective dosages corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone as the first phase; followed by 7-11 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding in activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.25-1.0 mg of norethindrone as the second phase; followed by 3-7 dosage units containing in admixture with a pharmaceutically acceptable carrier, a combination of an estrogen at a contraceptively effective dosage corresponding to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.35-2.0 mg of norethindrone as the third phase, and optionally containing 6-8 dosage units free of estrogen and progestogen; provided that the estrogen daily dosage is the same in all three phases.
References Cited (Backward Citations)
US4530839A
Cited
US4544554A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-10-06 | 1990-04-07 | 1990-10-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-10-06 | 1994-04-07 | 1994-10-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-10-06 | 1998-04-07 | 1998-10-07 | $7700.00 | Window Closed / Lapsed |