METHOD AND PHARMACEUTICAL COMPOSITION FOR OBTAINING THE PLASMATIC PROGESTERONE LEVELS REQUIRED FOR DIFFERENT THERAPEUTIC INDICATIONS

• US 20110104289A1
• Filed: 04/14/2008
• Published: 05/05/2011
• Est. Priority Date: 04/14/2008
• Status: Abandoned Application

• Current Assignee: POSI Visionary Solutions LLP
• Original Assignee: POSI Visionary Solutions LLP
• Inventors: Savoir Vilboeuf, John Claude, Martinez de Leon, Juan Ramon, De Gyves Lopez Lena, Aurelio
• Application Number:
  US12/937,779
• Publication Number:
  US 20110104289A1
• Time in Patent Office: Days
• US Class Current: 424/489
• 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: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/04 for inducing labour or abortion; Uterotonics
• CPC Class Codes: A61P 15/06 Antiabortive agents; Labour repressants
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 15/18 Feminine contraceptives

Abstract

The invention relates to the development of a method and pharmaceutical compositions for obtaining plasmatic progesterone levels in humans and for maintaining a plasmatic progesterone concentration between 42 and 3.5 ng/mL for eight days as well as maximum plasmatic concentrations (Cmax) between 12 and 42 ng/mL, sufficient for use in different therapeutic options that require said progesterone concentrations.

Claims

1. A method for maintaining sustained plasma progesterone concentrations in humans between 42 and 3.5 ng/mL during 8 days and maximum plasma concentrations (Cmax) between 12 and 42 ng/mL sufficient for application in different therapeutic options requiring said progesterone concentrations.

2. The method according to claim 1, being sufficient to maintain progesterone plasma concentrations between 13 and 3.5 ng/mL from administration of a single 100 mg progesterone injection in the form of an injectable suspension.

3. The method according to claim 2, wherein application is in secondary amenorrhea, dysfunctional uterine hemorrhage, premenstrual syndrome, progesterone replacement in ovariectomized women.

4. The method according to claim 1, wherein progesterone plasma concentrations are maintained between 20 and 7 ng/mL from administration of a single 200 mg progesterone injection in the form of an injectable suspension.

5. The method according to claim 1, wherein progesterone plasma concentrations are maintained between 26 and 8 ng/mL from 200 mg multiple progesterone injection in the form of injectable suspension.

6. The method according to claim 4, wherein application is luteal phase complement in assisted reproduction procedures, threatened abortion and prevention of relapsing abortion by luteal insufficiency, premature labor, endometriosis, endometrial hyperplasia and hirsutism, in secondary amenorrhea, dysfunctional uterine hemorrhage and premenstrual syndrome when higher progesterone levels are required.

7. The method according to claim 1, for maintaining progesterone plasma concentrations between 42 and 13 ng/mL from administering multiple 300 mg injections of progesterone in the form of an injectable suspension.

8. The method according to claim 7, wherein application is a luteal phase complement in assisted reproduction procedures, threatened abortion and prevention of relapsing abortion by luteal insufficiency, premature labor, endometriosis, endometrial hyperplasia and hirsutism, in secondary amenorrhea, dysfunctional uterine hemorrhage and premenstrual syndrome when higher levels of progesterone are required.

9. The method according to claim 1, obtained from an injectable aqueous suspension of progesterone particles.

10. The method according to claim 9, obtained from a single injection or sole dose from an injectable aqueous suspension of spherical shape progesterone particles.

11. The method according to claim 9, obtained from multiples injections or multiple doses of an injectable aqueous suspension of spherical shape progesterone particles.

12. The method according to claim 9, obtained from an injectable aqueous suspension of progesterone particles without a defined geometric shape.

13. The method according to claim 12, obtained from a single injection or sole dose of an injectable aqueous suspension of progesterone particles without a defined geometric shape.

14. The method according to claim 12, obtained from repeated injections of an injectable aqueous suspension of progesterone particles without a defined geometric shape.

15. The method according to claim 1, obtained from an injectable suspension.

16. Injectable pharmaceutical composition for single injection of spherical shape progesterone particles.

17. Pharmaceutical composition according to claim 16, wherein progesterone particle shape lacks of a defined geometric shape.

18. Pharmaceutical composition according to claim 16, wherein progesterone particles not having a defined geometric shape are crystals which may be injected in the shape of injectable aqueous suspension.

19. Use of a pharmaceutical composition according to claim 16, for treatment of secondary amenorrhea, dysfunctional uterine hemorrhage, premenstrual syndrome (when higher progesterone concentrations are required), progesterone replacement in ovariectomized women, luteal phase complement in assisted reproduction procedures, threatened abortion and relapsing abortion prevention by luteal insufficiency, premature labor, endometriosis, endometrial hyperplasia, hirsutism, and others.

20. Injectable aqueous suspension of spherical shape progesterone particles.

21. Injectable aqueous suspension of progesterone crystals without a defined geometric shape.