Progestin therapy for maintaining amenorrhea

• US 20010031747A1
• Filed: 04/03/2001
• Published: 10/18/2001
• Est. Priority Date: 10/21/1997
• Status: Active Application

• Current Assignee: Columbia Laboratories (Bermuda) Ltd. (Catalent, Inc.)
• Original Assignee: Columbia Laboratories (Bermuda) Ltd. (Catalent, Inc.)
• Inventors: deZiegler, Dominique, Levine, Howard L., Bologna, William J.
• Application Number:
  US09/825,569
• Publication Number:
  US 20010031747A1
• Time in Patent Office: Days
• US Class Current: 514/171
• 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 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61K 9/7023 Transdermal patches and similar drug-containing composite devices, e.g. cataplasms galenical aspects of iontophoretic devices A61K9/0009; microneedle arrays A61K9/0021; buccal patches A61K9/006
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• 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 5/34 Gestagens

Abstract

The present invention teaches that daily, cyclical vaginal delivery of progestin may be used to provide regular, predictable withdrawal bleeding during hormone replacement therapy. The present invention also teaches that constant administration of progestin in a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer may be used to maintain amenorrhea. Either regimen is accompanied by a significant decrease in adverse side effects.

Claims

1. A method of promoting regular withdrawal bleeding in a woman undergoing cyclical progestin administration comprising cyclical vaginal delivery of progestin via a drug delivery system in an amount sufficient to cause secretory transformation of the endometrium while avoiding significant adverse side effects.

2. The method of

claim 1

wherein the drug delivery system comprises a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer.

3. The method of

claim 2

wherein the polymer is polycarbophil.

4. The method of

claim 3

wherein the progestin is progesterone.

5. The method of

claim 4

wherein the amount of progesterone delivered is about 45 mg to about 90 mg per dose.

6. The method of

claim 4

wherein the drug delivery system additionally comprises at least one adjuvant.

7. The method of either of claims 2 and 5 wherein the drug delivery system is administered daily during a set portion of every calendar month.

8. The method of

claim 3

wherein the woman is also being treated with estrogen.

9. The method of

claim 7

wherein the woman is also being treated with estrogen.

10. A method of maintaining amenorrhea in a woman undergoing constant progestin administration comprising constant vaginal administration of progestin via a drug delivery system in an amount sufficient to cause endometrial atrophy while avoiding significant adverse side effects.

11. The method of

claim 10

wherein the drug delivery system comprises a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer.

12. The method of

claim 11

wherein the polymer is polycarbophil.

13. The method of either of claims 10 and 12 wherein the progestin is progesterone.

14. The method of

claim 10

wherein the progestin is administered about twice per week.

15. The method of

claim 13

wherein the progestin is administered about twice per week.