Heat sealable membrane for transdermal drug release

• US 4,951,657 A
• Filed: 04/22/1988
• Issued: 08/28/1990
• Est. Priority Date: 04/22/1988
• Status: Expired due to Term

• Current Assignee: Dow, Inc.
• Original Assignee: Dow, Inc.
• Inventors: Pfister, William R., Lee, Chi-Long, Gornowicz, Gerald A.
• Primary Examiner(s): Pellegrino, Stephen C.
• Assistant Examiner(s): Rose, Sharon
• Application Number:
  US07/184,750
• Time in Patent Office: 858 Days
• Field of Search: 604/304-307, 604/896.1, 128/155, 128/156, 424/443, 424/447-449
• US Class Current: 424/443
• 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: C08G 18/61 Polysiloxanes

Abstract

A transdermal drug delivery system, is provided which includes, in combination, an impermeable backing member, a release rate controlling membrane, and, a reservoir containing a medicinally active ingredient; the improvement in such system is based on the fact that said membrane is heat and pressure sealed to said backing without the use of a separate adhesive and is formed of a substantially linear block copolymer which is a reaction product of an amino functional polydiorganosiloxane which forms soft segments in said reaction product and a diisocyanate which forms "hard" segments, said copolymer having a glass transition temperature between 50° C. and 200° C. said soft segments comprising from 60 to 90 percent by weight, based on the weight of said copolymer.

Claims

1. In a transdermal drug delivery system, comprising in combination:

(a) an impermeable backing member;

(b) a release rate controlling membrane heat and pressure sealed to said backing member without the use of a separate adhesive;

(c) a reservoir positioned between said backing member and said membrane containing a medicinally active ingredient;

(d) means to attach said system to the skin of a patient;

said member comprising a substantially linear block copolymer which is a reaction product of a polydiorganosiloxane oligomer which forms soft segments in a said reaction product and a diisocyanate which forms hard segments, said copolymer having a glass transition temperature between 75°

C. and 200°

C. said soft segments comprising from 60 to 90 percent by weight , based on the weight of said copolymer and said hard segments comprising from about 10 to 40 percent by weight thereof.

2. A device according to claim 1 where said diisocyanate is an aromatic aliphatic or cycloaliphatic diisocyanate.

3. A device according to claim 1 wherein said membrane is in the form of a film having a thickness of from 0.01 to 1 mm.

4. A device according to claim 2 where the organic diisocyanate is p-tolylene diisocyanate, 4,4'"'"'-diphenyl methane diisocyanate, isoporone diisocyante, 4,4'"'"'-dicyclohexylmethanediisocyanate, or isophorone diisocyanate.

5. A device according to claim 1 wherein said soft blocks also contain from 0 to 70 weight per cent of polyalkylene oxide units based on the weight of said copolymer.

6. A device according to claim 1 wherein molecules of a low molecular weight diol are present in said hard blocks.

7. A device according to claim 1 wherein said polydiorganosiloxane is polydimethylsiloxane.

8. A method for forming a transdermal drug delivery device comprising (A) providing an impermeable backing member, (B) positioning a drug containing reservoir over a central portion of said backing member (C) positioning a rate controlling membrane over said reservoir with the periphery thereof extending beyond the perimeter of said reservoir, said periphery overlying said backing without any separate adhesive therebetween, said rate controlling polymeric material being from 0.01 to 1 mm. thick and permeable to said drug, said polymeric material comprising substantially linear block copolymers comprising from 3 to 40 weight percent of hard segments consisting essentially of polyurethane units derived from an organic diisocyanate and an alkylene diol, and from 60 to 97 weight percent of soft segments comprising at least one polydiorganosiloxane unit, said copolymer having a glass transition temperature between 50°

and 200°

C., and (D) sealing the periphery of said membrane to said backing by applying heat and pressure thereto.

9. A method according to claim 8 where said hard segment of the copolymer constitutes from 25 to 35 percent by weight of the copolymer, the organic diisocyanate is an aromatic or cycloaliphatic diisocyanate, the polydiorganosiloxane units contain from 20 to 40 diorganosiloxane repeating units and polyethylene oxide units constitute from 15 to 30 percent by weight of said copolymer, and said layer is in the form of a film having a thickness of from 0.1 to 1 mm.

10. A method according to claim 8 where the organic diisocyanate is p-tolylene diisocyanate, 4,4'"'"'-diphenylmethanediisocyanate or 4,4'"'"'-dicyclohexylmethanediisocyanate, the alkylene diol is 1,4-butanediol, the polydiorganosiloxane units contain from 20 to 40 diorganosiloxane repeating units, and the molar ratio of diisocyanate units to alkylene diol units to the combination of polydiorganosiloxane and polyethylene oxide units is 3:

2;

1, respectively.