Tanaproget compositions containing ethinyl estradiol

• US 20060280800A1
• Filed: 06/07/2006
• Published: 12/14/2006
• Est. Priority Date: 06/09/2005
• Status: Abandoned Application

• Current Assignee: Wyeth LLC (Pfizer Inc.)
• Original Assignee: Wyeth (Pfizer Inc.)
• Inventors: Ali, Zafar, Chatlapalli, Ramarao, Hasan, Shamim, Ghorab, Mohamed, Nagi, Arwinder
• Application Number:
  US11/448,965
• Publication Number:
  US 20060280800A1
• Time in Patent Office: Days
• US Class Current: 424/489
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/536 ortho- or peri-condensed with carbocyclic ring systems
• CPC Class Codes: A61K 31/538 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 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1682 Processes
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/24 : of the sex hormones

Abstract

Compositions containing micronized tanaproget, or a pharmaceutically acceptable salt thereof, and ethinyl estradiol and methods of preparing the same are provided. Also provided are kits containing the compositions, methods of contraception and hormone replacement therapy including administering a composition containing micronized tanaproget and ethinyl estradiol.

Claims

1. A pharmaceutical composition comprising an effective amount of micronized tanaproget, or a pharmaceutically acceptable salt thereof, and an effective amount of ethinyl estradiol.

2. The composition according to claim 1, wherein said tanaproget comprises about 0.1% to about 1% wt/wt of said composition.

3. The composition according to claim 2, wherein said tanaproget comprises about 0.17% to about 0.53% wt/wt of said composition.

4. The composition according to claim 2, wherein said tanaproget comprises about 0.17% wt/wt of said composition.

5. The composition according to claim 2, wherein said tanaproget comprises about 0.35% wt/wt of said composition.

6. The composition according to claim 2, wherein said tanaproget comprises about 0.52% wt/wt of said composition.

7. The composition according to claim 1, wherein said ethinyl estradiol comprises about 0.03 to about 0.05% wt/wt of said composition.

8. The composition according to claim 7, wherein said ethinyl estradiol comprises about 0.035% wt/wt of said composition.

9. The composition according to claim 1, wherein said ethinyl estradiol is a 2% triturate in lactose.

10. The composition according to claim 9, wherein said ethinyl estradiol 2% triturate in lactose comprises about 1.75% of said composition.

11. The composition according to claim 1, further comprising microcrystalline cellulose, anhydrous lactose, croscarmellose sodium, and magnesium stearate

12. The composition according to claim 11, wherein said microcrystalline cellulose comprises about 30 to about 56% wt/wt of said composition.

13. The composition according to claim 11, wherein said anhydrous lactose comprises about 30 to about 56% wt/wt of said composition

14. The composition according to claim 11, wherein said croscarmellose sodium comprises about 2 to about 6% wt/wt of said composition.

15. The composition according to claim 11, wherein said magnesium stearate comprises about 0.25 to about 0.5% wt/wt of said composition.

16. The composition according to claim 11, comprising about 0.175% wt/wt of micronized tanaproget, or a pharmaceutically acceptable salt thereof, about 0.035% wt/wt of ethinyl estradiol, about 54.5% wt/wt of microcrystalline cellulose, about 37.3% wt/wt of anhydrous lactose, about 6% wt/wt of croscarmellose sodium, and about 0.25% wt/wt of magnesium stearate.

17. The composition according to claim 1, comprising about 0.35% wt/wt of micronized tanaproget, or a pharmaceutically acceptable salt thereof, about 0.035% wt/wt of ethinyl estradiol, about 54.4% wt/wt of microcrystalline cellulose, about 37.2% wt/wt of anhydrous lactose, about 6% wt/wt of croscarmellose sodium, and about 0.25% wt/wt of magnesium stearate.

18. The composition according to claim 11, comprising about 0.525% wt/wt of micronized tanaproget, or a pharmaceutically acceptable salt thereof, about 0.035% wt/wt of ethinyl estradiol, about 54.3% wt/wt of microcrystalline cellulose, about 37.1% wt/wt/ of anhydrous lactose, about 6% wt/wt of croscarmellose sodium, and about 0.25% wt/wt of magnesium stearate.

29. A method of contraception comprising administering to a female of child bearing age a composition of claim 1.

30. A method of hormone replacement therapy comprising administering to a female in need thereof a composition of claim 1.

19. A process for preparing an oral composition comprising micronized tanaproget, or a pharmaceutically acceptable salt thereof, comprising:

(a) mixing said micronized tanaproget, or a pharmaceutically acceptable salt thereof, and ethinyl estradiol; and

(b) granulating the product of step (a).

20. The process according to claim 19, wherein step (a) further comprises microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, and magnesium stearate.

21. The process according to claim 19, wherein said composition is compacted and compressed into a tablet suitable for oral administration.

22. The process according to claim 21, wherein said tablet is encapsulated in a capsule.

23. A pharmaceutical kit comprising a daily dosage unit of said tablet of claim 21.

24. A pharmaceutical kit comprising a daily dosage unit of said capsule of claim 22.

25. A pharmaceutically useful kit which comprises:

(a) a first phase of 14 to 21 daily dosage units of a formulation comprising tanaproget and ethinyl estradiol; and

(b) a second phase of 0 to 7 daily dosage units of an orally and pharmaceutically acceptable placebo;

wherein the total number of the daily dosage units is 28.

26. The kit according to claim 25, further comprising an antiprogestin.

27. The kit according to claim 25, wherein said formulation comprises about 100 μ

g, 200 μ

g, or 300 μ

g of tanaproget.

28. The kit according to claim 25, wherein said formulation comprises about 20 μ

g of ethinyl estradiol.