Claims for Patent: 4,616,006

Summary for Patent: 4,616,006

Title:	Triphasic oral contraceptive
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 17.alpha.-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.
Inventor(s):	Pasquale; Samuel A. (Basking Ridge, NJ)
Assignee:	Ortho Pharmaceutical Corporation (Raritan, NJ)
Application Number:	06/744,189
Patent Claims:	1. 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 17.alpha.-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 17.alpha.-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 17.alpha.-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. 2. The unit according to claim 1 wherein the dosage units are in the form of tablets. 3. The unit according to claim 1 wherein the estrogen is selected from 17.alpha.-ethinylestradiol, estrone, estradiol and estriol. 4. The unit according to claim 2 wherein the estrogen is 17.alpha.-ethinylestradiol. 5. The unit according to claim 1 wherein the progestogen is selected from D-norgestrel, norethindrone, progesterone and D-17.beta.-acetoxy-13.beta.-ethyl-17.alpha.-ethinyl-gon-4-en-3-one oxime. 6. The unit according to claim 5 wherein the progestogen is norethindrone. 7. The unit according to claim 5 wherein the progestogen is D-17.beta.-acetoxy-13.beta.-ethyl-17.alpha.-ethinyl-gon-4-en-3-one oxime. 8. A composition according to claim 1 wherein the estrogen daily dosage in all three phases is equivalent to 0.035 mg of 17.alpha.-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. 9. A composition according to claim 1 wherein the estrogen daily dosage in all three phases is equivalent to 0.035 mg of 17.alpha.-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. 10. 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 17.alpha.-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 17.alpha.-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 17.alpha.-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.