LOW-DOSED SOLID ORAL DOSAGE FORMS FOR HRT

• US 20130140210A1
• Filed: 04/12/2011
• Published: 06/06/2013
• Est. Priority Date: 04/15/2010
• Status: Abandoned Application

• Current Assignee: Bayer Intellectual Property GmbH (Bayer AG)
• Original Assignee: Bayer Intellectual Property GmbH (Bayer AG)
• Inventors: Mletzko, Stephan, Schrmann, Rolf, Gude, Kerstin
• Application Number:
  US13/641,431
• Publication Number:
  US 20130140210A1
• Time in Patent Office: Days
• US Class Current: 206/461
• 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 31/566 having an oxo group in position 17, e.g. estrone
• CPC Class Codes: A61K 31/585 containing lactone rings, e.g. oxandrolone, bufalin
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system

Abstract

The present invention relates to a low-dosed dosage form for hormone replacement therapy (HRT). More particularly, the present invention concerns a solid oral dosage form comprising about 0.5 mg estradiol and about 0.5 mg drospirenone, and at least one pharmaceutically acceptable excipient. Despite the low E2 and DRSP doses it has surprisingly been found that a very high proportion of the women suffering from moderate to severe hot flushes actually respond to this treatment. Accordingly, the dosage form of the invention may be used as maintenance HRT or may be used already when HRT is initiated.

Claims

1. A solid oral dosage form comprising about 0.5 mg estradiol and about 0.5 mg drospirenone, and at least one pharmaceutically acceptable excipient.

2. The dosage form according to claim 1, wherein said dosage form is a tablet.

3. The dosage form according to claim 1 or 2, wherein said estradiol is in the form of estradiol hemihydrate.

4. The dosage form according to claim 1, wherein said estradiol is in the form of a pharmaceutically acceptable ester of estradiol.

5. A packaging unit consisting of a number of separately packaged and individually removable solid oral dosage forms as defined in claim 1, and intended for oral administration for a period of at least 21 days.

6. The packaging unit according to claim 5, wherein said oral administration is for a period of 28 days.

7. The packaging unit according to claim 5, wherein the number of dosage forms is 28 or a multiple of 28.

8. The packaging unit according to claim 7, wherein the number of dosage forms is a 2 to 12 multiple of 28.

9. The packaging unit according to claim 4, wherein said packaging unit is a blister pack.

16. A method for preventing, treating or alleviating vasomotor symptoms in a woman, said method comprising administering a dosage form as defined in claim 1 to a woman in need thereof.

17. A method for lowering the frequency of breakthrough bleedings, or increasing the incidence rate of amenorrhea, in a woman, said method comprising administering a dosage form as defined in claim 1 to a woman in need thereof.

18. The method of claim 16, wherein said vasomotor symptoms are moderate to severe vasomotor symptoms.

19. The method of claim 16, wherein said vasomotor symptoms are hot flushes.

20. The method of claim 16, wherein said woman is a postmenopausal woman.

21. The method of claim 17, wherein said woman is a postmenopausal woman.

10-15. -15. (canceled)