Claims
- 1. An agent useful for transdermal administration of a pharmacologically active agent, comprising:
- (a) a matrix of a pharmacologically acceptable crosslinked, silicone elastomer, comprising:
- (i) 1-10% by weight of a polydimethylhydrogensiloxane having an average molecular weight of 300-2000;
- (ii) 1-10% by weight of a 2,4,6,8-tetramethyl-2,4,6,8-tetravinylcyclotetrasiloxane; and
- (iii) 10-100 ppm of platinum catalyst in a vinyl group-terminated polydimethylsiloxane having an average molecular weight of 3000-20,000;
- (b) a non-flowable, physiologically acceptable gel microdispersed in said matrix, wherein said gel is based on a combination of a gel-forming thickener, water, and a solvent which is a polyhydric alcohol or a polyvalent ether; and
- (c) an active agent dissolved in the microdispersed gel phase in a concentration of at least 50 wt. % based on the gel phase, wherein said matrix is in the form of a sheet having a thickness of 0.5 to 5 mm.
- 2. An agent of claim 1, wherein the active medicinal agent is a steroid hormone, an ergot compound, a .beta.-receptor blocker, a prostaglandin, a prostacyclin, a cardioactive glycoside, or a pharmacologically active peptide.
- 3. An agent of claim 2, wherein the active medicinal agent is a steroid hormone.
- 4. An agent of claim 3, wherein the agent is an estradiol, norethisterone acetate, levonorgestrel, chlormadinone acetate, cyproterone acetate, desogestrel, gestodene, a testosterone, methandrostenolone or nandrolone.
- 5. An agent of claim 1 wherein said combination upon which the gel is based further comprises water.
- 6. An agent of claim 1, wherein the crosslinked silicone elastomer is an addition-crosslinked silicone RTV elastomer.
- 7. An agent of claim 1, wherein the crosslinked silicone elastomer has a network chain length of 20-500.
- 8. An agent of claim 7, wherein the crosslinked silicone elastomer has a network chain length of 50-250.
- 9. An agent of claim 1 wherein the solvent is ethylene glycol, propylene glycol, glycerol, ethylene gylcol monomethyl ether, ethylene glycol dimethyl ether, dimethylisosorbide, diethylene glycol, a diethylene glycol ether or a polyethylene glycol.
- 10. An agent of claim 1 wherein the thickener is agar-agar, gelatin, gum arabic, a pectin, cellulose, a ether, a polyacrylic compound, a vinyl polymer or a polyether.
- 11. An agent of claim 1 wherein the thickener is a Carbopol or carboxymethylcellulose.
- 12. An agent of claim 1 wherein the content of the gel component containing the active agent is 25-75 wt %.
- 13. An agent of claim 1 wherein the particle size of the gel is 5-500 .mu.m.
- 14. A process for the preparation of an agent useful for transdermal administration of active medicinal agents according to claim 1, comprising suspending the active agent-containing gel in the components required for formation of the crosslinked silicone elastomer, and vulcanizing the thus-obtained suspension.
- 15. In a method of transdermally administering a pharmacologically active compound in an agent suitable for transdermal administration, the improvement wherein the agent is one of claim 1.
- 16. An agent of claim 1, wherein the active medicinal agent exhibits a water solubility of about 5% or lower.
- 17. An agent of claim 2, wherein the gel comprises a gel-forming thickener and an organic solvent having an HLB value from about 2-20.
- 18. An agent of claim 17, wherein the particle size of the gel is 5-500 .mu.m.
- 19. An agent useful for transdermal administration of a pharmacologically active agent, comprising a solid, self-supporting matrix material having dispersed therein a gel with an active agent dissolved therein, wherein:
- said matrix comprises a pharmacologically acceptable, cross-linked, vulcanized silicone elastomer;
- said gel is physiologically acceptable and is microdispersed within said matrix at particle sizes of from 5-500 .mu.m;
- said active agent is present in the gel phase at a concentration of at least 50 wt. % based on the gel phase; and
- said matrix material is in the form of a molded sheet having a thickness of 0.5 to 5 mm.
- 20. An agent of claim 19, wherein the gel is based on a combination of gel-forming thickener, water, and a solvent which is a polyhydric alcohol or a polyvalent ether.
- 21. An agent as in claim 19, which does not contain a backing layer.
- 22. An agent of claim 19, wherein the crosslinked silicone elastomer is prepared from a bicomponent system, comprising 1-10% by weight polydimethylhydrogensiloxane having an average molecular weight of 300-2000, 1-10% by weight of 2,4,6,8-tetramethyl-2,4,6,8-tetravinylchlorotetrasiloxane, and 10-100 ppm of platinum catalyst and vinyl group-terminated polydimethylsiloxane having an average molecular weight of 3000-20,000;
- wherein the thickener is agar, gelatin, gum arabic, a pectin, carboxymethyl-cellulose, a cellulose ether, a polyacrylic compound, a vinyl polymer, or a polyether;
- wherein the solvent is ethylene glycol, propylene glycol, glycerol, ethylene glycol monomethyl ether, ethylene glycol dimethyl ether, dimethyl isosorbide, diethylene glycol, diethylene glycol ethers, or polyethylene glycols; and
- wherein the active agent is estradiol, norethisterone acetate, levonorgestrel, chloromadinone, cyproterone acetate, desogestrel, gestodene, testosterones, methandrostenolone, or nondrolone.
- 23. An agent of claim 19, wherein the silicone elastomer is vulcanized at 40.degree.-100 C.
Priority Claims (1)
Number |
Date |
Country |
Kind |
3333240 |
Sep 1983 |
DEX |
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Parent Case Info
This is a continuation of application Ser. No. 07/363,799, filed June 9, 1989, and now abandoned which is a continuation of application Ser. No. 07/240,666, filed Sept. 6, 1988 (abandoned), which is a continuation of application Ser. No. 07/058,727, filed June 5, 1987 (abandoned), which is a continuation of Ser. No. 06/649,578, filed Sept. 12, 1984 (abandoned).
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
3598123 |
Zaffaroni |
Aug 1971 |
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Continuations (4)
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Number |
Date |
Country |
Parent |
363799 |
Jun 1989 |
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Parent |
240666 |
Sep 1988 |
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Parent |
58727 |
Jun 1987 |
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Parent |
649578 |
Sep 1984 |
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