Intravaginal drug delivery device

• US 5,788,980 A
• Filed: 10/24/1996
• Issued: 08/04/1998
• Est. Priority Date: 11/01/1995
• Status: Expired due to Term

• Current Assignee: Aventis Pharma SA (Sanofi )
• Original Assignee: Roussel Uclaf
• Inventors: Nabahi, Shohre
• Primary Examiner(s): BROUILLETTE, D GABRIELLE
• Application Number:
  US08/740,095
• Time in Patent Office: 649 Days
• Field of Search: 424/430, 424/432, 424/433, 424/486
• US Class Current: 424/430
• CPC Class Codes: A61K 9/0036 Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms

Abstract

An intravaginal drug delivery device for prolonged release of an active ingredient comprising a biocompatible polymer matrix containing an active ingredient to be released and an effective amount of at least one fatty acid ester and a method of inducing contraception in female warm-blooded animals, including humans.

Claims

1. An intravaginal drug delivery device for prolonged release of an active ingredient consisting essentially of at least one polyorganosiloxane ring matrix containing an active ingredient to be released, and an amount of 1 to 50% by weight of at least one fatty acid ester.

2. A device of claim 1 wherein said fatty acid ester is present in an amount of from 5 to 20% by weight.

3. A device of claim 1 wherein said fatty acid ester is formed from a fatty acid comprising from 2 to 20 carbon atoms.

4. The device of claim 3 wherein said fatty acid is selected from the group consisting of caproic acid, lauric acid, myristic acid, oleic acid, linoleic acid, adipic acid and lanolic acid.

5. A device of claim 1 wherein said fatty acid ester is formed from an alcohol of 2 to 20 carbon atoms.

6. A device of claim 5 wherein said alcohol is an alkanol of 2 to 4 carbon atoms.

7. A device of claim 1 wherein said fatty acid ester is isopropyl myristate.

11. A device of claim 1 wherein said active ingredient is selected from the group consisting of progesterone, medroxy-progesterone, norethisterone, trimegestone and norethisterone acetate.

12. A device of claim 1 wherein the active ingredient is a mixture of trimegestone and 17β

-estradiol.

13. A device of claim 1 wherein the active ingredient is selected from the group consisting of an antidepressant/anxiolitic, an Anxiolitic, a Vitamin B6, a Vitamin D, a Vitamin E, an antifungal, an opoid analgesic, a non-opoid analgesic and an antiviral or a compound for its use in the treatment of endometriosis.

14. A device of claim 1 wherein the active ingredient is selected from the group consisting of Fluphenazine, Flupenthixol, Haloperidol, Buspirone, Alprazolam, Trifluoperzine, Piridoxine, Pridoxal, Pyridoxamine, Cholecalciferol, Dihydrotachysterol, Ergocalciferol, Alfacalcidol, d-Alpha-Tocopherol, Clotrimazole, Enconazole, Iltraconazole, Buprenorphine, Levorphanol, Phenoperidine, Fentanyl, Methadone, Mefenamic acid, Acylclovir, Vidarabine, Arildone, Idoxuridine, Gestrinone and Mifepristone.

15. A device of claim 14 wherein the active agent is Mifepristone.

17. A method of inducing contraception in a female warm-blooded animal comprising injecting into the animal'"'"'s vagina a device of claim 1 wherein the active ingredient is a contraceptive compound.

8. An intravaginal drug delivery device for prolonged release of estrogen and/or progestogen in an amount of 1 to 50% by weight consisting essentially of at least one polyorganosiloxane ring matrix containing an active ingredient to be released, and an amount of 1 to 50% by weight of at least one fatty acid ester.

9. A device of claim 8 wherein the estrogen and/or progestogen is present in an amount of up to 15% by weight.

10. A device of claim 9 wherein said estrogen is 17β

-estradiol.

16. A method of treatment of a female warm-blooded animal to combat condition resulting from oestrogen defficiency comprising intravaginally administering into the animal'"'"'s vagina a device of claim 8.

18. An intravaginal drug delivery device for prolonged release of an active ingredient consisting essentially of at least one polyorganosiloxane ring matrix containing an active ingredient to be released, and an amount of 1 to 50% by weight of at least one fatty acid ester, wherein the polyorganosiloxane matrix is a central polymer matrix core surrounded by a rate controlling membrane comprising the same polymer as the polymer matrix.

19. An intravaginal drug delivery device for prolonged release of an active ingredient consisting essentially of at least one polyorganosiloxane ring matrix containing an active ingredient to be released daily of up to 500 μ

g per day sustained up to 12 months in a zero order pattern, and an amount of 1 to 50% by weight of at least one fatty acid ester.