Vaginal drug dispensing device

• US 4,016,251 A
• Filed: 05/30/1975
• Issued: 04/05/1977
• Est. Priority Date: 08/17/1972
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Hussain, Anwar, Higuchi, Takeru
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US05/582,131
• Time in Patent Office: 676 Days
• Field of Search: 128/260, 128/130, 424/15, 424/16, 424/19, 424/22, 424/28, 424/31-33, 424/78
• US Class Current: 424/432
• CPC Class Codes: A61F 6/14 intra-uterine type
• CPC Class Codes: A61F 6/142 Wirelike structures, e.g. loops, rings, spirals
• CPC Class Codes: A61F 9/0017 implantable in, or in contact with, the eye, e.g. ocular inserts
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• 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: A61K 9/0039 Devices retained in the uterus for a prolonged period, e.g. intrauterine devices for contraception
• CPC Class Codes: A61K 9/7084 Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
• 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

Drug-delivery device for releasing a drug at a continuous and controlled rate for a prolonged period of time is comprised of a shaped body of polymeric material containing a pharmaceutically acceptable drug and permeable to passage of the drug by diffusion. The polymeric material is an ethylene-vinyl acetate copolymer having a vinyl acetate content of about 4 to 80% by weight and a melt index of about 0.1 to 1000 grams per 10 minutes.

Claims

1. A vaginal insert comprising a reservoir for containing a drug, a drug in the reservoir, a polymeric barrier through which the drug passes by diffusion as it is released from the reservoir, the improvement wherein said barrier is an ethylene-vinyl acetate copolymer having a vinyl acetate content of 4 to 80% by weight and a melt index of about 0.1 to 1000 grams per ten minutes.

2. A vaginal dispensing device shaped and size adapted for insertion and placement in the vagina and formed of a non-toxic, flexible, polymeric release rate controlling material containing a vaginal acceptable drug capable of diffusing through the material at a controlled and continuous rate over a prolonged period of time, the improvement wherein said polymeric material is comprised of an ethylene-vinyl acetate copolymer having a vinyl acetate content of 4 to 80% by weight and a melt index of about 0.1 to 1000 grams per ten minutes.

3. A vaginal dispensing device according to claim 2 wherein the ethylene-vinyl acetate copolymer has a vinyl acetate content of 4 to 50%, a frequency of acetoxy groups on the polyethylene backbone of 1/150 to 1/8 and a density of 0.920 to 0.980.

4. A vaginal dispensing device according to claim 2 wherein the drug is an anti-infective drug.

5. A vaginal dispensing device according to claim 2 wherein the device is ring-shaped with drug housed therein.

6. A vaginal dispensing device according to claim 2 wherein the drug is a member selected from the group consisting of progestational and estrogenic steroids.

7. A vaginal dispensing device according to claim 6 wherein the device contains from 250 nanograms to 5 grams of the drug.

8. A vaginal dispensing device comprising a polymeric membrane surrounding a reservoir containing a drug and formed of a drug release rate controlling material, the improvement wherein the material is comprised of a biologically compatible ethylene-vinyl acetate copolymer having a vinyl acetate content of about 4 to 80% and a melt index of 0.1 to 1000 grams per ten minutes, and wherein said drug is dispensed from the device at a controlled and continuous rate over a prolonged period of time by passing through the copolymer.

9. A vaginal dispensing device according to claim 8 wherein the device is a container and said drug is contained in the interior thereof.

10. A vaginal dispensing device according to claim 8 wherein the reservoir is comprised of a solid matrix with drug therein.

11. A vaginal dispensing device according to claim 8 wherein the copolymer has a vinyl acetate content of 4 to 50%, a frequency of acetoxy groups on the polyethylene backbone of 1/150 to 1/8 and a density of 0.920 to 0.980.

12. A vaginal dispensing device according to claim 8 wherein the drug is a member selected from the group consisting of progestational, estrogenic and anti-infective drugs.

13. A vaginal dispensing device according to claim 12 wherein the device contains from 250 nanograms to 5 grams of the drug.

14. A vaginal dispensing device according to claim 12 wherein the progestational drug is progesterone.

15. A vaginal dispensing device according to claim 12 wherein the progestational drug is a member selected from the group consisting of 19-nor-progesterone, norethinione, medroxyprogesterone, norethynodrel and 17α

-hydroxy-progesterone.

16. A vaginal dispensing device according to claim 12 wherein the anti-infective drug is a member selected from the group consisting of penicillin, tetracycline, chloramphenicol, sulfacetamide, sulfamethazine, sulfadiazine, sulfamerazine, sulfamethizole and sulfisoxazole.

17. A vaginal dispensing device according to claim 8 wherein the drug is a member selected from the group of anti-inflammatories consisting of hydrocortisone, cortisone, dexamethasone, fluocinolone, triamincolone, medrysone, and prednisolone.

18. A vaginal dispensing device according to claim 12 wherein the estrogenic drug is a member selected from the group consisting of estrone, 17β

-estradiol and ethinyl estradiol.

19. A vaginal dispensing device according to claim 8 wherein the reservoir is comprised of a liquid matrix with drug therein.

20. A vaginal dispensing device according to claim 8 wherein the device is ring-shaped with drug housed in the reservoir thereof.

21. A method for controlling fertility which method is comprised of placing in the vagina of a warm blooded animal a vaginal dispensing device shaped and size adapted for insertion and comfortable placement in the vagina and formed of a non-toxic, flexible, polymeric release rate controlling material containing a dosage unit amount of a vaginally acceptable antifertility steroid selected from the group consisting of progestational and estrogenic steroids capable of diffusing through the material at a controlled and continuous rate of a prolonged period of time, the improvement wherein said polymeric material is comprised of an ethylene-vinyl acetate copolymer having a vinyl acetate content of 4 to 80% by weight and a melt index of 0.1 to 1000 grams per ten minutes and permeable to the steroid with the steroid dissolving in an passing through the ethylene-vinyl acetate copolymer in a fertility controlling effective amount for controlling fertility in the animal.

22. A method for controlling fertility which method is comprised of placing in the vagina of a warm blooded animal a vaginal dispensing device shaped and size adapted for insertion and comfortable placement in the vagina and formed of a polymeric membrane surrounding a reservoir containing a dosage unit amount of a vaginally acceptable antifertility steroid selected from the group consisting of progestational and estrogenic steroids capable of diffusing through the material in a controlled rate and continuously over a prolonged period of time, the improvement wherein the material is comprised of a vaginal compatible ethylene-vinyl acetate copolymer having a vinyl acetate content of about 4 to 80% and a melt index of 0.1 to 1000 grams per ten minutes and to the steroid with the steroid dissolving in and passing through the ethylene-vinyl acetate copolymer in a fertility controlling effective amount for controlling fertility in the animal.