Intravaginal drug delivery device

• US 6,039,968 A
• Filed: 06/22/1998
• Issued: 03/21/2000
• Est. Priority Date: 06/24/1997
• Status: Expired due to Term

• Current Assignee: Aventis Pharma SA (Sanofi )
• Original Assignee: Hoechst Marion Roussel (Sanofi )
• Inventors: Nabahi, Shohre
• Primary Examiner(s): Azpuru, Carlos A.
• Application Number:
  US09/102,302
• Time in Patent Office: 638 Days
• Field of Search: 424/433
• US Class Current: 424/433
• 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

The invention provides an intravaginal drug delivery system having a first intravaginal part comprising at least one active agent in a polymer matrix, said first part being provided in association with a second part comprising a removable polymer membrane arranged to absorb excess active agent. Use of a polymer membrane in this way serves to substantially reduce the initial high burst of active from the intravaginal part following administration. It also reduces the levels of release of active during the first few weeks of use. Also provided is an intravaginal drug delivery device comprising at least one active agent dispersed in a polymer matrix, wherein the concentration of active agent at the outer surface of the device at the time of use is not substantially higher than the concentration of the active agent in the remainder of the device.

Claims

1. An intravaginal drug delivery system having a first intravaginal part comprising at least one active agent in a polymer matrix, said first part being provided in association with a second part comprising a polymer membrane to be removed before use which absorbs active agent.

2. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer membrane wholly surrounds the intravaginal part.

3. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer membrane substantially corresponds to the shape of the intravaginal part.

4. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer membrane lies in contact with the outer surface of the intravaginal part.

5. An intravaginal drug delivery system as claimed in claim 1 wherein said intravaginal part is provided with a coating comprising an inert lubricant.

6. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer membrane comprises a polymer material having a water vapour transmission (measured at a temperature of 20°

C., a relative humidity of 85% and a film thickness of 50 μ

m) of from 1 to 10,000 g/m².d (wherein d=24 hours).

7. An intravaginal drug delivery system as claimed in claim 6 wherein said polymer material has a water vapour transmission of from 1 to 300 g/m².d.

8. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer membrane comprises a polymer material selected from the group consisting of polyolefins, polyvinylchloride, polyurethanes, polyamides, silicone elastomers and mixtures thereof.

9. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer membrane comprises at least one organopolysiloxane, optionally together with one or more fatty acid esters.

10. An intravaginal drug delivery system as claimed in claim 9 wherein said organopolysiloxane is a polydimethylsiloxane or a polyvinylmethylsiloxane.

11. An intravaginal drug delivery system as claimed in claim 1 wherein the thickness of the polymer membrane is in the range of from 10 to 3,000 μ

m.

12. An intravaginal drug delivery system as claimed in claim 1 wherein the thickness of the polymer membrane is in the range of from 10 to 2,000 μ

m.

13. An intravaginal drug delivery system as claimed in claim 1 wherein said intravaginal part comprises a core of inert elastomer surrounded by an active agent-containing polymer matrix.

14. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer matrix is surrounded by a rate-controlling sheath.

15. An intravaginal drug delivery system as claimed in claim 14 wherein said rate-controlling sheath comprises at least one organopolysiloxane, optionally together with one or more fatty acid esters.

16. An intravaginal drug delivery system as claimed in claim 1 wherein said polymer matrix comprises at least one organopolysiloxane, optionally together with one or more fatty acid esters.

17. An intravaginal drug delivery system as claimed in claim 1 wherein said active agent is selected from the group consisting of antibiotics, antiviral and antifungal agents, analgesics, antidepressants, hormones and vitamins.

18. An intravaginal drug delivery system as claimed in claim 17 wherein said active agent comprises an oestrogen and/or a progestogen.

19. An intravaginal drug delivery system as claimed in claim 18 wherein said oestrogen is 17 β

-oestradiol or ethinyl estradiol.

20. An intravaginal drug delivery system as claimed in claim 18 wherein said progestogen is progesterone, medroxyprogesterone, norethisterone, norethisterone acetate, trimegestone or norethindrone acetate.

21. A method for the manufacture of an intravaginal drug delivery system as claimed in claim 1, said method comprising coating a polymer matrix containing at least one active agent with a polymer membrane to be removed before use which absorbs active agent.

22. A method for the manufacture of an intravaginal drug delivery system as claimed in claim 1, said method comprising the following steps:

(a) dispersing at least one active agent in a polymer matrix whereby to form a core;

(b) optionally surrounding said core with a rate-controlling sheath; and

(c) providing the resulting device with a removable polymer membrane capable of absorbing active agent.