PHARMACEUTICAL COMPOSITION BASED ON MICRONIZED PROGESTERONE, PREPARATION METHOD AND USES THEREOF

• US 20110135719A1
• Filed: 11/01/2010
• Published: 06/09/2011
• Est. Priority Date: 11/13/2001
• Status: Abandoned Application

• Current Assignee: Besins Healthcare Luxemborg SARL (Besins Healthcare, Inc.)
• Original Assignee: Besins Manufacturing Belgium
• Inventors: Besse, Jerome, Besins, Antoine
• Application Number:
  US12/916,795
• Publication Number:
  US 20110135719A1
• Time in Patent Office: Days
• US Class Current: 424/451
• 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 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/685 one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
• CPC Class Codes: A61K 36/28 Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• CPC Class Codes: A61K 36/63 Oleaceae (Olive family), e.g. jasmine, lilac or ash tree
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/06 Antiabortive agents; Labour repressants
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61P 5/32 Antioestrogens
• CPC Class Codes: A61P 5/34 Gestagens

Abstract

The present invention relates to a pharmaceutical composition comprising micronized progesterone, soya bean lecithin, and at least one oil selected from the group consisting of sunflower oil, olive oil, sesame see oil, colza oil, almond oil, to the method for the preparation thereof and to the uses thereof for treating a physiological condition linked to insufficiency of progesterone secretion.

Claims

1-10. -10. (canceled)

11. A pharmaceutical composition comprising micronized progesterone, soy bean lecithin, and at least one oil selected from the group consisting of sesame oil, colza oil, and almond oil.

12. The pharmaceutical composition of claim 11, wherein the oil is sesame oil.

13. The pharmaceutical composition of claim 11, wherein the oil is colza oil.

14. The pharmaceutical composition of claim 11, wherein the oil is almond oil.

15. The pharmaceutical composition of claim 11, wherein at least about 80% of the particles of said micronized progesterone are characterized by a particle size of between 1 and 15 μ

m, as measured in the composition.

16. The pharmaceutical composition according to claim 11, wherein at least 50% of the particles of said micronized progesterone have a particle size of between 1 and 10 μ

m, as measured in the composition.

17. The pharmaceutical composition according to claim 11, wherein at least 25% of the particles of said micronized progesterone have a particle size of between 1 and 5 μ

m, as measured in the composition.

18. The pharmaceutical composition according to claim 11, wherein the progesterone/oil ratio is between 0.15/1 and 3/1.

19. The pharmaceutical composition according to claim 11, wherein the soy bean lecithin/oil ratio is between 0.005/1 and 0.3/1.

20. The pharmaceutical composition according to claim 11, wherein the progesterone/oil ratio is between 0.25/1 and 2/1.

21. The pharmaceutical composition according to claim 11, wherein the progesterone/oil ratio is between 0.40/1 and 1/1.

22. The pharmaceutical composition according to claim 11, wherein the progesterone/oil ratio is 0.67/1.

23. The pharmaceutical composition according to claim 11, wherein the soy bean lecithin/oil ratio is between 0.01/1 and 0.2/1.

24. The pharmaceutical composition according to claim 11, wherein the soy bean lecithin/oil ratio is between 0.040/1 and 0.1/1.

25. The pharmaceutical composition according to claim 11, wherein the soy bean lecithin/oil ratio is 0.0067/1.

26. The pharmaceutical composition according to claim 11, further comprising an estrogen or an ester-type derivative thereof.

27. The pharmaceutical composition according to claim 26, wherein the estrogen, or the ester-type derivative thereof is selected from the group consisting of 17-beta-estradiol, estrone, 17-alpha-ethinyl estradiol and estradiol valerianate, or phyto-estrogens.

28. The pharmaceutical composition according to claim 26, wherein the estrogen, or the ester-type derivative thereof is 17-beta-estradiol.

29. The pharmaceutical composition according to claim 11, wherein at least the progesterone is in suspension in the oil.

30. The pharmaceutical composition according to claim 11, in the form of a soft capsule.

31. The pharmaceutical composition according to claim 11, in unit dosage form comprising between 2 mg and 600 mg of micronized progesterone.

32. The pharmaceutical composition according to claim 31, comprising between 30 mg and 300 mg of micronized progesterone.

33. The pharmaceutical composition according to claim 31, comprising between 100 mg and 200 mg of micronized progesterone.

34. A method for preparing a pharmaceutical composition according to claim 11, comprising:

mixing at least one oil selected from the group consisting of sesame oil, colza oil, and almond oil with soy bean lecithin in order to obtain a mixture; and

adding micronized progesterone to said mixture to obtain a homogeneous suspension.

35. A method for the treatment of a physiological condition linked to insufficiency of progesterone secretion comprising the step of administering to the patient a pharmaceutical composition according to claim 11.