Cyclic progestin regimens and kits

• US 20060009428A1
• Filed: 07/06/2005
• Published: 01/12/2006
• Est. Priority Date: 07/07/2004
• Status: Abandoned Application

• Current Assignee: Wyeth LLC (Pfizer Inc.)
• Original Assignee: Wyeth (Pfizer Inc.)
• Inventors: Grubb, Gary Sondermann, Constantine, Ginger Dale
• Application Number:
  US11/174,592
• Publication Number:
  US 20060009428A1
• Time in Patent Office: Days
• US Class Current: 514/170
• CPC Class Codes: A61K 31/5355 Non-condensed oxazines and containing further heterocyclic rings
• CPC Class Codes: A61K 31/536 ortho- or peri-condensed with carbocyclic ring systems
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 5/34 Gestagens

Abstract

A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen.

Claims

1. A method of contraception in a female of child bearing age which comprises administering over a period of 28 consecutive days:

(a) a first phase in which from 21 to 27 daily dosage units of an active agent are administered, each daily dosage unit containing an effective amount of an active agent consisting of at least one progestin; and

(b) a second phase of from 1 to 7 days wherein no effective amount of an active agent is administered.

2. The method according to claim 1, wherein the progestin is selected from the group consisting of 17-hydroxy progesterone esters, 19-nor-17-hydroxy progesterone esters, 17α

-ethinyltestosterone and derivatives thereof, 17α

-ethinyl-19-nor-testosterone and derivatives thereof, norethindrone, norethindrone acetate, ethynodiol diacetate, dydrogesterone, medroxy-progesterone acetate, norethynodrel, allylestrenol, lynoestrenol, fuingestanol acetate, medrogestone, norgestrienone, dimethiderome, ethisterone, cyproterone acetate, levonorgestrel, dl-norgestrel, d-17α

-acetoxy-13β

-ethyl-17α

-a-ethinyl-gon-4-en-3-one oxime, cyproterone acetate, gestodene, desogestrel, etonorgestrel, norgestimate, norelgestromin, chlormadione, dienogest, and drospirenone.

3. The method according to claim 1, wherein from 1 to 7 daily dosage units of a pharmaceutically acceptable placebo are delivered in the second phase.

4. The method according to claim 1, which comprises:

a) a first phase of 21 daily dosage units; and

b) a second phase of 7 daily dosage units of an orally and pharmaceutically acceptable placebo.

5. The method according to claim 1, which comprises:

a) a first phase of 23 daily dosage units; and

b) a second phase of 5 daily dosage units of an orally and pharmaceutically acceptable placebo.

6. The method according to claim 1, which comprises:

a) a first phase of 25 daily dosage units; and

b) a second phase of 3 daily dosage units of an orally and pharmaceutically acceptable placebo.

7. The method according to claim 1, which comprises:

a) a first phase of 27 daily dosage units; and

b) a second phase of 1 daily dosage units of an orally and pharmaceutically acceptable placebo.

8. The method according to claim 1, wherein the progestin is 5-(4,4-Dimethyl-2-thioxo-1,4-dihydro-2H-benzo[d] [1,3]oxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile.

9. A method of contraception in a female of child bearing age which comprises administering over a period of 28 consecutive days:

(a) a first phase in which from 21 to 27 daily dosage units of an active agent are administered, each daily dosage unit containing an effective amount of an active agent consisting of a progestin of the formula;

(b) a second phase of from 1 to 7 days wherein no effective amount of an active agent is administered.

10. A pharmaceutically useful kit adapted for daily oral administration, which comprises:

(a) 21 to 27 daily dosage units of an active agent, each daily dosage unit containing an effective amount of an active agent consisting of at least one progestin; and

(b) one or more packages for said daily dosage units.

11. The pharmaceutically useful kit according to claim 10, wherein the progestin is selected from the group consisting of 17-hydroxy progesterone esters, 19-nor-17-hydroxy progesterone esters, 17α

-ethinyltestosterone and derivatives thereof, 17α

-ethinyl-19-nor-testosterone and derivatives thereof, norethindrone, norethindrone acetate, ethynodiol diacetate, dydrogesterone, medroxy-progesterone acetate, norethynodrel, allylestrenol, lynoestrenol, fuingestanol acetate, medrogestone, norgestrienone, dimethiderome, ethisterone, cyproterone acetate, levonorgestrel, dl-norgestrel, d-17α

-acetoxy-13β

-ethyl-17α

-a-ethinyl-gon-4-en-3-one oxime, cyproterone acetate, gestodene, desogestrel, etonorgestrel, norgestimate, norelgestromin, chlormadione, dienogest, and drospirenone.

12. The pharmaceutically useful kit according to claim 10, further comprising from 1 to 7 daily dosage units of a pharmaceutically acceptable placebo.

13. The pharmaceutically useful kit adapted for daily oral administration according to claim 10, which comprises:

a) 21 daily dosage units of an active agent; and

b) 7 daily dosage units of an orally and pharmaceutically acceptable placebo.

14. The pharmaceutically useful kit adapted for daily oral administration according to claim 10, which comprises:

a) 23 daily dosage units of an active agent; and

b) 5 daily dosage units of an orally and pharmaceutically acceptable placebo.

15. The pharmaceutically useful kit adapted for daily oral administration according to claim 10, which comprises:

a) 25 daily dosage units of an active agent; and

b) 3 daily dosage units of an orally and pharmaceutically acceptable placebo.

16. The pharmaceutically useful kit adapted for daily oral administration according to claim 10, which comprises:

a) 27 daily dosage units of an active agent; and

b) 1 daily dosage units of an orally and pharmaceutically acceptable placebo.

17. The pharmaceutically useful kit according to claim 10, wherein said daily dosage units are in the form of tablets.

18. The pharmaceutically useful kit according to claim 10, wherein said daily dosage units are in the form of a topical cream or gel.

19. The pharmaceutically useful kit according to claim 10, wherein said daily dosage units are delivered via a sustained release delivery system selected from among a transdermal, transmucosal or transvaginal drug delivery system.

20. The kit according to claim 10, wherein the progestin is 5-(4,4-Dimethyl-2-thioxo-1,4-dihydro-2H-benzo[d] [1,3]oxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile.

21. A pharmaceutically useful kit adapted for daily oral administration, which comprises:

(a) 21 to 27 daily dosage units of an active agent, each daily dosage unit containing an effective amount of an active agent consisting of at least one progestin of the formula;

(b) one or more packages for said daily dosage units.