IP Library Granted Patent US 8,097,604
Granted Patent B2
US 8,097,604 · App. 12/325,529 · Granted Jan 17, 2012

Combination of gestagen and insulin sensitizer for treating PCOS

Assignee: Gruenenthal GmbH
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Quick Facts
Patent No.
US 8,097,604
App. No.
12/325,529
Granted
Jan 17, 2012
Kind
B2
Abstract

The present invention relates to a medicament which contains as the active ingredient combination at least one gestagen with a contraceptive action as the sole hormone component and at least one insulin sensitizer, which medicament is in particular suitable for preventing or treating pathological disorders which are caused by polycystic ovary syndrome (PCOS).

Claims (32)

1. A medicament consisting of an active ingredient combination and one or more conventional auxiliary substances, wherein the active ingredient combination consists of at least one insulin sensitizer and at least one an antiandrogenic gestagen component, wherein the antiandrogenic gestagen component is chlormadinone acetate or selected from the group consisting of:

a) 3α-hydroxy-chlormadinone acetate;

b) 3β-hydroxy-chlormadinone acetate;

c) a mixture of a) and b) in any desired mixing ratio;

d) 3α-hydroxy-17α-acetoxy-5β-pregnan-20-one;

e) 3β-hydroxy-17α-acetoxy-5β-pregnan-20-one;

f) a mixture of d) and e) in any desired mixing ratio;

g) a mixture of a) and/or b) with d) and/or e) in any desired mixing ratio;

h) a mixture of chlormadinone acetate (CMA) with a) and/or b) in a mixing ratio of 10 to 90 wt. % of CMA and 90 to 10 wt. % of a) and/or b), relative to the complete mixture;

i) a mixture of chlormadinone acetate with d) and/or e) in a mixing ratio of 10 to 90 wt. % of chlormadinone acetate and 90 to 10 wt. % of d) and/or e), relative to the complete mixture;

j) a mixture of chlormadinone acetate with c) and f) in a mixing ratio of 10 to 90 wt. % of chlormadinone acetate and 90 to 10 wt. % of c) and f), relative to the complete mixture;

k) a mixture of chlormadinone acetate with g) in a mixing ratio of 10 to 90 wt. % of CMA and 90 to 10 wt. % of g), relative to the complete mixture; and

mixtures thereof, wherein components d), e) or f), listed above, are not used as the sole gestagen or as the gestagen mixture in f), but are instead used only in combination with a further, above-listed gestagen.

2. A medicament according to claim 1 wherein the insulin sensitizer is selected from the group consisting of metformin, the physiologically acceptable salts of metformin and glitazones.

3. A medicament according to claim 2 wherein the insulin sensitizer is selected from the group consisting of roseglitazone, pioglitazone, -metformin hydrochloride and mixtures thereof.

4. A medicament according to claim 1 wherein the medicament is present as a dosage form with a specific number of daily units intended for uninterrupted, deity, oral administration to women.

5. A medicament according to claim 4 , wherein the antiandrogenic gestagen content in each daily unit corresponds to the ovulation inhibition dose of the gestagen.

6. A medicament according to claim 5 , wherein each daily unit consists of the same quantity of the gestagen component.

7. A medicament according to claim 1 wherein each daily unit consists of the same gestagen component.

8. A medicament according to claim 4 wherein a daily unit consists of chlormadinone acetate in a quantity of 1.5 to 10 mg.

9. A medicament according to claim 8 wherein each daily unit of a dosage form consists of chlormadinone acetate in each case uniformly in a quantity of 2, 3, 4, or 5 mg.

10. A medicament according to claim 4 wherein each daily unit consists of the same quantity of the insulin sensitiser component.

11. A medicament according to claim 10 , wherein each daily unit consists of metformin in a quantity of 500 to 2000 mg.

12. A medicament according to claim 4 wherein each daily unit consists of the same insulin sensitiser component.

13. A medicament according to claim 4 wherein the dosage form consists of at least 28 daily units.

14. A medicament according to claim 13 , wherein the maximum number of daily units of a dosage form corresponds to uninterrupted administration for two or more years.

15. A medicament according to claim 13 wherein the maximum number of daily units of a dosage form corresponds to uninterrupted administration for 84 days.

16. A medicament according to claim 5 wherein the antiandrogenic gestagen content in each daily unit is up to 150% above the ovulation inhibition dose of the gestagen component.

17. A medicament according to claim 11 further consists of at least one glitazone in a quantity of 2 to 30 mg.

18. A medicament according to claim 12 wherein the maximum number of daily units of a dosage form corresponds to uninterrupted administration for 1 year.

19. A method for treating pathological disorders caused by polycystic ovary syndrome (PCOS), wherein the disorders are selected from a group consisting of insulin resistance, androgenic disorders, female infertility, oligomenorrhoea, amenorrhoea, hyperandrogenaemia, type II diabetes mellitus (T2DM), cardiovascular diseases, endometrial hyperplasia, mammary carcinoma, ovarian cancer and endometrial carcinoma, comprising the step of administering to a person a pharmaceutical dosage form of the medicament according to claim 1 .

20. A method according to claim 19 wherein the administration of the dosage form results in simultaneous contraception.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2012
From: GRUNENTHAL GMBH
To: RICHTER GEDEON NYRT.
Reel/Frame 028229/0016 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 14, 2009
From: SCHRAMM, GEORG
To: GRUNENTHAL GMBH
Reel/Frame 022104/0697 →
Priority Claims (1)
DE 10 2006 026 026 · Jun 1, 2006 · national
Continuity (2)
Continuation PCTEP2007004700 · May 26, 2007
Related Publication 20090118245A1 · May 7, 2009