Pharmaceutical composition with a synthetic natural progesterone and oestradiol base and its preparation process

• US 6,656,929 B1
• Filed: 03/16/1999
• Issued: 12/02/2003
• Est. Priority Date: 03/09/1998
• Status: Expired due to Term

• Current Assignee: Laboratories Besins Iscovesco
• Original Assignee: Laboratories Besins Iscovesco
• Inventors: Besins, Antoine, Agnus, Benoît
• Primary Examiner(s): Badio, Barbara P.
• Application Number:
  US09/268,353
• Time in Patent Office: 1,722 Days
• Field of Search: 514/170
• US Class Current: 514/170
• 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 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• 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 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

The object of this invention is a pharmaceutical composition with a synthetic natural progesterone and oestradiol base coming in the form of a tablet, characterised by the fact that it has a disintegration time of less than 15 minutes, preferably less than 10 minutes, and more preferably still less than 5 minutes.

Claims

1. A pharmaceutical composition in the form of a tablet comprising synthetic natural progesterone, and oestradiol, said tablet having an excipient content of no more than 20% by weight based on total dry matter weight of the tablet, said tablet having a disintegration time of less than 15 minutes.

2. The pharmaceutical composition according to claim 1, having a disintegration time of less than 10 minutes.

3. The pharmaceutical composition according to claim 2, having a disintegration time of less than 5 minutes.

4. The pharmaceutical composition according to claim 1, wherein the weight ratio between the oestradiol and the synthetic natural progesterone is between 5/100 and 1/100, the ratio being expressed as a function of the total weight of the progesterone in the tablet.

5. The pharmaceutical composition according to claim 1, wherein the tablet has an excipient content of no more than 17%.

6. The pharmaceutical composition according to claim 5, wherein the tablet has an excipient content of no more than 15%.

7. The pharmaceutical composition according to claim 1, having a dissolution profile such that released progesterone content is at least 75% and released oestradiol content is at least 75% in 15 minutes.

8. The pharmaceutical composition according to claim 7, having a dissolution profile such that the released progesterone content is at least 75% and the released oestradiol content is at least 75% in 10 minutes.

9. The pharmaceutical composition according to claim 8, having a dissolution profile such that the released progesterone content is at least 75% and the released oestradiol content is at least 75% in 5 minutes.

10. The pharmaceutical composition according to claim 1, having a hardness between 10 and 80 N.

11. The pharmaceutical composition according to claim 10, having a hardness between 20 and 70 N.

12. The pharmaceutical composition according to claim 11, having a hardness between 30 and 60 N.

13. The pharmaceutical composition according to claim 1, containing diluents, disintegrating agents, lubricants, binding agents and stripping agents.