Device for delivery of useful agent

• US 4,014,987 A
• Filed: 06/30/1975
• Issued: 03/29/1977
• Est. Priority Date: 06/04/1974
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Baker, Richard W., Heller, Jorge
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US05/591,443
• Time in Patent Office: 638 Days
• Field of Search: 128/260, 128/130, 424/15, 424/16, 424/19, 424/22, 424/32, 424/33, 424/28, 424/78-81
• US Class Current: 424/432
• 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

A device for the controlled continuous administration of an active agent to an environment of use is disclosed. The device comprises a body of erodible agent release rate controlling material containing an agent dispersed therethrough; the rate controlling material is a hydrophobic poly(carboxylic acid) having one ionizable carboxylic hydrogen for each 8 to 12 carbon atoms, which material erodes at a controlled and continuous rate over a prolonged period of time in response to the environment by a process of carboxylic hydrogen ionization, thereby releasing the dispersed agent at a controlled rate over a prolonged period of time.

Claims

1. A device for the controlled local administration of drug to the vagina comprising a matrix or hollow body made of drug release rate controlling material formed of a hydrophobic poly(acid) represented by the formula:

##STR15## wherein the R'"'"'s are organic radicals independently selected to provide on the average from 8 to 22 total carbon atoms for each carboxylic hydrogen, said body of drug release rate controlling material containing a vaginally acceptable drug dispersed therethrough, the device shaped and adapted for insertion and placement in the vagina, and wherein the release rate controlling material erodes at a controlled rate over a prolonged period of time when the device is in the vagina in response to the environment of the vagina, thereby releasing the dispersed drug to the vagina at a controlled rate over a prolonged period of time.

4. The device for the controlled administration of drug to the vagina according to claim 1 wherein n has a value providing an average molecular weight of from 10,000 to 800,000.

5. The device for the controlled administration of drug to the vagina according to claim 1 wherein the drug is an antifertility progestational steroid.

6. The device for the controlled administration of drug according to claim 1 wherein the device is ring-shaped and adapted for vaginal placement, the poly(acid) is formed of polymerized n-butyl acrylate and acrylic acid, and the drug dispersed therethrough is progesterone.

7. The device for the controlled administration of drug to the vagina according to claim 1 wherein the drug is a member selected from the group consisting of pregn-4-ene-3,20-dione;

19-nor-pregn-4-en-3,20-dione;

17-hydroxy-19-nor-17 α

-pregn-5(10)-3-en-20-yn-3-one;

dl-11β

-ethyl-17 α

-ethynyl-17β

-hydroxypregn-4-en-3-one;

17 α

-ethynyl-17-hyroxy5(10) -estren-3-one;

17 α

-ethynyl-19-norestosterone;

6-chloro-17-hydroxypregn-4,6-diene-3,20-dione;

17β

-hydroxy-6 α

-methyl-17-(1-propynyl) androst-4-en-3-one;

9β

,10α

-pregna-4,6-diene-3,20-dione;

17-hydroxy-17 pregan-4-en-20-yn-3-one;

19-nor-17 α

-pregn-4-en-20-yne-3β

,17-diol;

17-hydroxypregn-4-en-3,20-dione;

17 α

-hydroxy-progesterone and 17-hydroxy-6 α

-methyl-pregn-4-ene-3,10-dione.

8. The device for the controlled administration of drug to the vagina according to claim 1 wherein the drug is an antifertility estrogenic steriod.

9. The device for the controlled administration of drug to the vagina according to claim 1 wherein the drug is a member selected from the group consisting of β

-estradiol;

β

-estradiol 3-benzoate;

17β

-cyclopentane propionate estradiol;

1,3,5(10)-estratriene-3,17β

-diol dipropionate estra-1,3,5(10)-triene-3,17-β

-diol valerate;

estrone;

ethinyl estradiol;

17-ethinyl estradiol-3 methyl ether;

17-ethinyl estradiol-3-cyclopentoether; and

estriol.

2. A vaginal device for the controlled local administration of a drug to a vagina comprising a body having means shaped and adapted for insertion and placement in the vagina, the body having a wall formed of a drug release rate controlling material comprising a hydrophobic poly(carboxylic acid) having from 8 to 22 carbon atoms for each ionizable carboxylic hydrogen, a vaginally acceptable drug dispersed within the material, and wherein the release rate material erodes when the device is placed in the vagina, thereby administering drug at a controlled rate to the vagina over the prolonged period of time.

10. The vaginal device for administering drug to the vagina according to claim 2 wherein the drug is a member selected from the group consisting of penicillin, tetracycline, oxytetracycline, chlorotetracycline and chloramphenicol.

3. A device for the controlled local administration of drug to a vagina comprising a body shaped and adapted for insertion and retention in the vagina, the body having a wall formed of a drug release rate controlling material comprising a terpolymer consisting of at least one α

,β

-unsaturated aliphatic acid in which the alkyl group has 2 to 8 carbon atoms, a vaginally acceptable drug dispersed in the material and wherein the device when placed in the vagina the material erodes at a controlled rate over a prolonged period of time in response to the vaginal environment, thereby dispensing drug to the vagina at a controlled rate over a prolonged period of time.

11. The vaginal device for administering drug to the vagina according to claim 3 wherein the drug is a member selected from the group consisting of prednisolone, cortisone, cortisol and triamcinolone.

12. A method for controlling fertility which comprises placing in the vagina of a mammal a device shaped, sized and adapted for comfortable insertion and placement in the vagina, said device comprising a matrix made of a drug release rate controlling material formed of a hydrophobic poly(carboxylic acid) having the following formula:

##STR16## wherein the R'"'"'s are organic radicals independently selected to provide on the average from 8 to 22 total carbon atoms for each carboxylic hydrogen, said matrix containing a vaginally acceptable drug selected from the group of antifertility progestational and estrogenic steroids dispersed therethrough, and wherein the device when positioned in the vagina releases drug at a controlled rate as the material erodes over a prolonged period of time in response to the environment of the vagina, thereby releasing an effective amount of steroid for controlling fertility in the animal.

13. A method for controlling fertility which comprises placing in the vagina of a mammal a device shaped, sized and adapted for comfortable insertion and placement in the vagina, said device comprising a hollow body formed of a drug release rate controlling material made of a hydrophobic poly(carboxylic acid) having the following formula:

##STR17## wherein the R'"'"'s are organic radicals independently selected to provide on the average from 8 to 22 total carbon atoms for each carboxylic hydrogen, said body containing a vaginally acceptable drug selected from the group of antifertility progestational and estrogenic steroids contained therein, and wherein the device when positioned in the vagina releases drug at a controlled rate as the material erodes over a prolonged period of time in response to the environment of the vagina, thereby releasing an effective amount of steroid for controlling fertility in the animal.