Vaginal ring

• US 4,822,616 A
• Filed: 02/13/1987
• Issued: 04/18/1989
• Est. Priority Date: 10/28/1980
• Status: Expired due to Fees

• Current Assignee: Schering Ag (Merck & Co., Inc.)
• Original Assignee: Schering Ag (Merck & Co., Inc.)
• Inventors: Reck, Hans-Jurgen, Windt, Fred, Zimmermann, Ingfried
• Primary Examiner(s): Swisher, Nancy A. B.
• Application Number:
  US07/014,316
• Time in Patent Office: 795 Days
• Field of Search: 424/430-433, 424/422, 424/424, 604/890, 604/891
• 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
• CPC Class Codes: A61M 31/002 Devices for releasing a drug at a continuous and controlled rate for a prolonged period of time artificial gland structures or devices A61F2/022; intra-uterine contraceptive devices A61F6/14; tampons for introducing into the vagina A61F13/20, A61L15/00; suppositories or bougies for intra-vaginal or intra-uterine application A61K9/02; physical forms of medicinal preparations for sustained or differential drug release A61K9/20, A61K9/50

Abstract

A vaginal ring comprises a supporting ring 1 free of active agent. A layer 2, which contains an active agent such as a steroid, is applied on its outer rim, optionally in a continuous groove provided in the supporting ring. This layer, in turn, is coated with a layer 3 devoid of active ingredient. All components preferably comprise an LTV silicone elastomer. The ratio of the thickness of the layer 2, containing an active agent, to the layer 3, free of active agent, is about 5-50:1. As a result, a long-term and uniform release rate is achieved for the active agent.

Claims

1. A vaginal ring spaced from an axis of revolution, the ring having an inside diameter and an outside diameter, a radial thickness with respect to the axis and an axial thickness in the direction of the axis, the ring having first and second exposed radial surfaces and the ring further comprising:

a supporting ring made of a pharmacologically acceptable material and being essentially free of medicament;

the supporting ring having a first annular surface between inner and outer circumferential peripheries extending in a radial direction and generally facing in a first axial direction, the supporting ring having a second annular surface extending in a radial direction with respect to the axis and facing in an axial direction opposite that of the first annular surface, the second annular surface being completely exposed;

a first annular layer made of a pharmacologically acceptable material and containing a pharmacologically active agent, the first annular layer extending in the axial direction and overlying radially the first annular surface of the supporting ring between the inner and outer circumferential peripheries thereof; and

a second pharmacologically acceptable layer overlying the first annular layer in the axial direction;

said second layer being essentially medicament free and being permeable to the active agent in the first layer;

said second layer being thinner than the first layer in a ratio of 5-50;

1, and also being in contact with the supporting layer at the inner and outer circumferential peripheries of the supporting layer, the second pharmacologically acceptable layer controlling the rate of migration of the activation from the first layer into the vagina.

2. The vaginal ring of claim 1, wherein the first surface of the supporting includes a groove therein inboard of the inner and outer circumferential peripheries in which the first layer containing the pharmacologically active ingredient is inserted.

3. A vagainal ring of claim 1, wherein the thickness of the second layer is 10-1000 μ

m.

4. A vaginal ring of claim 1, wherein the thickness of the second layer is 100-500 μ

m.

5. A vaginal ring of claim 3, wherein each of said two layers comprises an LTV silicone elastomer.

6. A vaginal ring of claim 5, wherein the second layer consists essentially of an LTV silicone elastomer of the following composition:

75-98% by weight of polydimethylvinylsiloxane

1-10% by weight of tetramethyltetravinylcyclotetrasiloxane

2-20% by weight of polydimethyl hydrogen siloxane, and

10-100 ppm of platihum catalyst.

7. A vaginal ring of claim 6, wherein the supporting ring consists essentially of an LTV silicone elastromer of the following composition:

80-98% by weight of polydimethylvinylsiloxane

1-10% by weight of tetramethyltetravinylcyclotetrasiloxane

2-20% by weight of polydimethyl hydrogen siloxane

0.5-10% by weight of highly disperse silicic acid, and

10-100 ppm of a platinum catalyst

and the first layer consists essentially of an active agent and an LTV silicone elastomer and has the following composition;

75-98% by weight of polydimethylvinylsiloxane

1-10% by weight of tetramethyltetravinylcyclotetrasiloxane

1-10% by weight of polydimethyl hydrogen siloxane

10-100 ppm of a platinum catalyst, and

1-10% by weight of active agent.

8. A vaginal ring of claim 1, wherein the active agent in the first layer is a steroidal progestogen, a steroidal estrogen or a combination thereof.

9. A vaginal ring of claim 8, wherein the active agent is ethynylestradiol, ethisterone, norethisterone acetate, norethynodrel, levonorgestrel, or gestoden or a mixture thereof.

10. A method of vaginally administering a pharmacologically active agent to a host in need of such administration which comprises inserting a vaginal ring of claim 1, into the vagina of the host.

11. A method of claim 10, for inhibiting ovulation in a host wherein the active agent in the vaginal ring is effective to inhibit ovulation.

13. A vaginal ring of claim 1, wherein each of said two layers comprises an LTV silicone elastomer.

12. A vaginal ring of claim, wherein the ratio of the thickness of the first layer to that of the second layer is about 20-40:

1.