Pharmaceutical composition based on micronized progesterone, preparation method and uses thereof

• US 7,431,941 B2
• Filed: 11/13/2002
• Issued: 10/07/2008
• Est. Priority Date: 11/13/2001
• Status: Expired due to Term

• Current Assignee: Besins Healthcare Luxemborg SARL (Besins Healthcare, Inc.)
• Original Assignee: Besins International Belgique
• Inventors: Besins, Antoine, Besse, Jéröme
• Primary Examiner(s): Woodward; M P
• Assistant Examiner(s): Barham; Bethany
• Application Number:
  US10/495,242
• Publication Number:
  US 20050004076A1
• Time in Patent Office: 2,155 Days
• Field of Search: 424/489
• US Class Current: 424/456
• 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 seed 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. A pharmaceutical composition comprising micronized progesterone, soy bean lecithin, and sunflower oil, wherein at least 80% of the particles of said micronized progesterone is characterized by a particle size of between 1 and 15 μ

m, as measured in the composition.

2. The pharmaceutical composition according to claim 1, in which the progesterone/sunflower oil ratio is between 0.15/1 and 3/1.

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

4. The pharmaceutical composition according to claim 1, comprising an oestrogen, or an ester-type derivative thereof.

5. The pharmaceutical composition according to claim 1, wherein at least the progesterone is in suspension in the sunflower oil.

6. The pharmaceutical composition according to claim 1, in the form of a soft capsule.

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

12. The pharmaceutical composition according to claim 1, in which the progesterone/sunflower oil ratio is between 0.40/1 and 1/1.

13. The pharmaceutical composition according to claim 1, in which the progesterone/sunflower oil ratio is 0.67/1.

14. The pharmaceutical composition according to claim 1, wherein the soy bean lecithin/sunflower oil ratio is between 0.0 1/1 and 0.2/1.

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

16. The pharmaceutical composition according to claim 1, wherein the soy bean lecithin/sunflower oil ratio is 0.067/1.

17. The pharmaceutical composition according to claim 4, wherein the oestrogen, or the ester-type derivative thereof, is selected from the group consisting of 17-beta-oestradiol, oestrone, 17-alpha-ethinyl oestradiol and oestradiol valerianate, or phyto-oestrogens.

18. The pharmaceutical composition according to claim 4, wherein the oestrogen, or the ester-type derivative thereof, is 17-beta-oestradiol.

7. A pharmaceutical product comprising a dosage unit of a pharmaceutical composition comprising micronized progesterone, soy bean lecithin, and sunflower oil, wherein at least 80% of the particles of said micronized progesterone is characterized by a particle size of between 1 and 15 μ

m, as measured in the composition. wherein the dosage unit comprises between 2 mg and 600 mg of micronized progesterone.

19. The pharmaceutical product according to claim 7, wherein the dosage unit comprises between 30 mg and 300 mg of micronized progesterone.

20. The pharmaceutical product according to claim 7, wherein the dosage unit comprises between 100 mg and 200 mg of micronized progesterone.

8. A method for preparing a pharmaceutical composition comprising micronized progesterone, soy bean lecithin, and sunflower oil, wherein at least 80% of the particles of said micronized progesterone is characterized by a particle size of between 1 and 15 μ

m, as measured in the composition, comprising the following successive steps;

mixing (A) sunflower oil with (B) soy bean lecithin with stirring, in order to obtain a mixture; and

adding the micronized progesterone, with stirring, to said mixture to obtain a homogeneous suspension.

9. 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 comprising micronized progesterone, soy bean lecithin, and sunflower oil, wherein at least 80% of the particles of said micronized progesterone is characterized by a particle size of between 1 and 15 μ

m, as measured in the composition.

10. The method according to claim 9, in which the pharmaceutical composition further contains an oestrogen, or an ester-type derivative thereof.

21. The method according to claim 10, wherein the oestrogen, or the ester-type derivative thereof, is selected from the group consisting of 17-beta-oestradiol, oestrone, 17-alpha-ethinyl oestradiol and oestradiol valerianate, or phyto-oestrogens.

22. The method according to claim 10, wherein the oestrogen, or the ester-type derivative thereof, is 17-beta-oestradiol.