Pharmaceutical composition based on estrogen and progesterone

• US 6,165,491 A
• Filed: 08/03/1998
• Issued: 12/26/2000
• Est. Priority Date: 04/27/1998
• Status: Expired due to Fees

• Current Assignee: Effik Sca Bat
• Original Assignee: Effik Sca Bat
• Inventors: Terracol, Didier, Grasset, Etienne, Galdona, Javier Gil
• Primary Examiner(s): Azpuru, Carlos A.
• Application Number:
  US09/128,324
• Time in Patent Office: 876 Days
• Field of Search: 424/430, 424/451, 424/434
• US Class Current: 424/430
• 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 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• 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 9/4858 Organic compounds

Abstract

A pharmaceutical composition, intended for menopausal replacement therapy, comprising a suspension of progesterone in a lipophilic medium solution of a 17-estradiol salt in the lipophilic medium, the weight ratio of progesterone to the base 17-estradiol being 25 to 600.

Claims

1. A pharmaceutical composition comprising a suspension of progesterone in a lipophilic medium containing 17-estradiol valerate dissolved in said lipophilic medium, the weight ratio of progesterone to the corresponding base of 17-estradiol base is 25 to 600.

2. A composition of claim 1 wherein the progesterone is in the form of micronized particles having a particle size of 1 to 100 microns.

3. A composition of claim 1 wherein the lipophilic medium is a plant oil.

4. A composition of claim 1 wherein the lipophilic medium also contains a surfactant.

5. A composition of claim 4, wherein the surfactant is an amphoteric surfactant.

6. A composition of claim 5, wherein the surfactant is a soybean lecithin.

7. A composition of claim 5 wherein the surfactant is present in proportions of 0.5 to 5% by weight relative to the weight of oil.

8. A composition of claim 1 containing from 50 to 300 mg of progesterone in particulate form and 0.5 to 2 mg, expressed as base 17-estradiol, in the form of 17-estradiol valerate.

9. A process for preparing a composition of claim 1 wherein in a first stage, the 17-estradiol valerate is dissolved in a lipophilic medium and the progesterone then is added in particulate form and is mixed with the lipophilic estrogen solution.

10. The process of claim 9 wherein the mixture of estradiol valerate and of lipophilic medium is heated to a temperature to bring about complete dissolution of the estradiol valerate.

11. A menopausal hormone replacement composition formulated for oral or vaginal administration and containing an effective amount of a composition of claim 1.

12. A medicinal product of claim 11 in the form of a soft capsule intended for oral or vaginal administration.

13. A method of treating a female human for menopausal hormone deficiency comprising administering to a female human in need thereof an amount of a composition of claim 1 sufficient to relieve said deficiency.