Intravaginal rings with insertable drug-containing core

• US 5,972,372 A
• Filed: 05/02/1997
• Issued: 10/26/1999
• Est. Priority Date: 07/31/1996
• Status: Expired due to Term

• Current Assignee: Population Council Inc.
• Original Assignee: Population Council Inc.
• Inventors: Harmon, Troy, Saleh, Saleh Ismail, Bardin, C. Wayne, Nash, Harold A.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): HOWARD, SHARON LEE
• Application Number:
  US08/850,327
• Time in Patent Office: 907 Days
• Field of Search: 424/422, 424/430, 424/432, 206/524.1
• US Class Current: 424/432
• CPC Class Codes: A61F 6/08 Pessaries, i.e. devices worn in the vagina to support the uterus, remedy a malposition or prevent conception , e.g. combined with devices protecting against contagion
• 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

Disclosed is a vaginal ring intended for the release of at least one drug over a prolonged time period. The vaginal ring contains a ring body made of a first polymeric material having at least one hollow internal channel defining an opening to the exterior of the ring body and which channel is adapted to receive a, drug-containing core through the opening, and an intravaginally administerable drug-containing core disposed in the channel. The core is positioned in the vaginal ring body suitably prior to use in order to substantially avoid initial bursts of drug into the tissues of the subject and resultant side effects such as nausea and vomiting. The core contains a pharmaceutically effective amount of at least one intravaginally administerable drug dispersed in a second polymeric material. The first and second polymeric materials may be the same or different. Representative drugs include contraceptive agents and other steroidal substances for use in hormone replacement therapy. Also disclosed are methods for preparing the vaginal rings, kits for assembling the vaginal rings, and methods of using the vaginal rings to achieve intravaginal delivery of drugs to a female.

Claims

1. A vaginal ring, comprising:

a vaginal ring body comprising a first polymeric material having at least one hollow internal channel defining an opening to the exterior of said vaginal ring body and which said hollow internal channel is adapted to receive an intravaginally administerable drug-containing core through said opening;

in combination with a drug-containing core positioned in said hollow internal channel, said drug-containing core containing a pharmaceutically effective amount of at least one intravaginally administerable drug dispersed in a second polymeric material, wherein said first and second polymeric materials may be the same or different;

wherein no portion of said drug-containing core is exposed to said exterior of said vaginal ring body.

2. The vaginal ring of claim 1, wherein said first polymeric material, said second polymeric material, or both said first and second polymeric materials comprise a silicone elastomer.

3. The vaginal ring of claim 1, wherein said first polymeric material, said second polymeric material, or both said first and second polymeric materials comprises a polyurethane.

4. The vaginal ring of claim 1, wherein said drug is a hormonal replacement steroid.

5. The vaginal ring of claim 1, wherein said drug is a contraceptive agent.

6. The vaginal ring of claim 4, wherein said steroid is an estrogenic compound.

7. The vaginal ring of claim 5, wherein said contraceptive agent is a progestational compound.

8. The vaginal ring of claim 1, wherein said core contains a first drug and a second drug.

9. The vaginal ring of claim 8, wherein said first and second drugs are contraceptive agents.

10. The vaginal ring of claim 9, wherein said first contraceptive agent is an estrogenic compound and said second contraceptive is a progestational compound.

11. The vaginal ring of claim 10, wherein said estrogenic compound is ethynylestradiol and said progestational compound is 16-methylene-17α

-acetoxy-19-norpregnene-3, 20-dione).

12. The vaginal ring of claim 10, wherein said estrogenic compound is ethynylestradiol and said progestational compound is norethindrone acetate.

13. The vaginal ring of claim 1, comprising first and second hollow channels and first and second cores positioned in said first and second channels, respectively.

14. The vaginal ring of claim 1, comprising first, second and third hollow channels, and first, second and third cores positioned in said first, second and third channels, respectively.

15. The vaginal ring of claim 1, wherein said pharmaceutically effective amount of said drug is from about 1% to about 65% of the weight of said core.

16. The vaginal ring of claim 1, having an overall diameter of from about 48 mm to about 60 mm.

17. The vaginal ring of claim 1, having a cross-sectional diameter of from about 4 mm to about 10 mm.

18. The vaginal ring of claim 1, wherein said core has a cross-sectional diameter of from about 1.5 mm to about 5 mm.

19. The vaginal ring of claim 1, wherein said core has a length of from about 5 mm to about 40 mm.

20. The vaginal ring of claim 1, wherein said core is positioned in said vaginal ring body such that the cross-sectional diameter of said vaginal ring body exceeds the cross-sectional diameter of said core by an average of about 1 mm in all directions.

21. The vaginal ring of claim 1, wherein said opening of said internal channel is sealed.

22. The vaginal ring of claim 1, further comprising a sealant.

23. The vaginal ring of claim 22, wherein said sealant comprises a silicone medical grade adhesive.

24. The vaginal ring of claim 23, wherein said adhesive comprises a polydimethlysiloxane having methyldiacetoxysilyl end groups.

25. The vaginal ring of claim 1, wherein said vaginal ring body further comprises an intravaginally administerable drug.

26. The vaginal ring of claim 25, wherein said vaginally administerable drug in said vaginal ring body is estradiol.

27. The vaginal ring of claim 25, wherein said vaginally administerable drug in said core is a progestin.

28. The vaginal ring of claim 27, wherein said progestin is 16-methylene-17α

-acetoxy-19-norpregnene-3, 20-dione).

29. A method of preparing the vaginal ring of claim 1 comprising the steps of:

molding said first polymeric material in the form of said vaginal ring body in a single step;

vulcanizing the vaginal ring body; and

inserting said drug-containing core into said hollow internal channel.

30. A method of preparing the vaginal ring of claim 1 comprising the steps of:

molding said first polymeric material in a single step to form said vaginal ring body;

providing said drug-containing core in said hollow internal channel thereby assembling said vaginal ring; and

sealing said channel such that there is no portion of said drug-containing core which is exposed to said exterior of said vaginal ring body.