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US5723145A Expired / Lapsed US ⏱️ 0.0 years remaining

Transdermal absorption preparation

Assignee: Ono Pharmaceutical Co Ltd
•
Filing: 1997-07-22
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Granted: 1998-03-03
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Expires: 2017-07-22
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Abstract

Abstract The present invention provides a transdermal absorption preparation whereby a drug, which takes effect with a small amount, and is liable to be decomposed, solid at ordinary temperatures, water-soluble and less absorbable into the skin, can be stored stably for a long period of time and, can be transdermally administered at a high releasing ratio and yet releasing slowly, when applied to the skin. The constitution of the present invention is as follows: a transdermal absorption preparation which comprises a drug-storing layer containing a drug and having a drug-releasing face coated with a drug-releasing controlling membrane, wherein said drug-storing layer comprises as a base a heat-sensitive segmented polyurethane represented by the general formula: R--A--(U)--F--(U)--B--R' wherein A and B each represents a polymer of ethylene oxide, propylene oxide, tetramethylene oxide or 1,2-butylene oxide, or a random or block copolymer thereof, R and R' each represents a terminal H, CH 3 , C 2 H 5 , C 3 H 7 or C 4 H 9 , A=B or A≠B, R=R' or R≠R', F represents a constituting structure which is a moiety of a diisocyanate compound excluding two isocyanate groups, and (U) represents a urethane bond, and at least one of A and B is hydrophilic and at the same time at least one of A and B has a characteristic that it melts near the temperature of human skin, and wherein said drug-releasing controlling membrane is a phase-separated membrane comprising a mixture of a crosslinked gelatin phase and the uncrosslinked segmented polyurethane phase.

Inventors

  • 👤 Yasuo Shikinami
  • 👤 Kunihiro Hata
  • 👤 Seiei Sasatani
  • 👤 Masao Sudoh

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 04:51
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 214 words
A transdermal absorption preparation which comprises a drug-storing layer containing a drug and having a drug-releasing face coated with a drug-releasing controlling membrane, wherein said drug-storing layer comprises as a base a heat-sensitive segmented polyurethane represented by the general formula: R--A--(U)--F--(U)--B--R' wherein A represents a polymer of ethylene oxide, propylene oxide, tetramethylene oxide or 1,2-butylene oxide, or a random or block copolymer thereof, B represents a random or block copolymer of ethylene oxide, propylene oxide, tetramethylene oxide and/or 1,2-butylene oxide, R and R', which may be the same or different, each represents a terminal H, CH 3 , C 2 H 5 , C 3 H 7 or C 4 H 9 , F represents a constituting structure which is a residual moiety of a diisocyanate compound excluding two isocyanate groups, and (U) represents a urethane bond, and at least one of A and B is hydrophilic and at the same time at least one of A and B has a characteristic that it melts near the temperature of human skin (30° to 40° C.); wherein the viscosity of the seqmented polyurethane after melting is about 2,000 centipoise or less; and wherein said drug-releasing controlling membrane is a phase-separated membrane comprising a mixture of a crosslinked gelatin phase and an uncrosslinked segmented polyurethane phase.
Claim 2
Dependent Claim 214 words
A transdermal absorption preparation which comprises a drug-storing layer containing a drug and having a drug-releasing face coated with a drug-releasing controlling membrane, wherein said drug-storing layer comprises as a base a heat-sensitive segmented polyurethane represented by the general formula: R--A--(U)--F--(U)--B--R' wherein A represents a polymer of ethylene oxide, propylene oxide, tetramethylene oxide or 1,2-butylene oxide, or a random or block copolymer thereof, B represents a random or block copolymer of ethylene oxide, propylene oxide, tetramethylene oxide and/or 1,2-butylene oxide, R and R', which may be the same or different, each represents a terminal H, CH 3 , C 2 H 5 , C 3 H 7 or C 4 H 9 , F represents a constituting structure which is a residual moiety of a diisocyanate compound excluding two isocyanate groups, and (U) represents a urethane bond, and at least one of A and B is hydrophilic and at the same time at least one of A and B has a characteristic that it melts near the temperature of human skin (30° to 40° C.); wherein the viscosity of the seqmented polyurethane after melting is about 2,000 centipoise or less; and wherein said drug-releasing controlling membrane is a phase-separated membrane comprising a mixture of a crosslinked gelatin phase and an uncrosslinked segmented polyurethane phase.
Claim 3
Dependent Claim 20 words
A transdermal absorption preparation as claimed in claim 1, wherein A in the general formula is an ethylene oxide polymer.
Claim 4
Dependent Claim 27 words
A transdermal absorption preparation as claimed in claim 1, wherein B in the general formula is a random or block copolymer of ethylene oxide and propylene oxide.
Claim 5
Dependent Claim 30 words
A transdermal absorption preparation as claimed in claim 1, wherein A is an ethylene oxide polymer and B is a random or block copolymer of ethylene oxide and propylene oxide.
Claim 6
Dependent Claim 30 words
A transdermal absorption preparation as claimed in any of claims 1, 2, or 4, wherein a number average molecular weight of said ethylene oxide polymer is from 800 to 1,200.
Claim 7
Dependent Claim 37 words
A transdermal absorption preparation as claimed in claim 1, wherein a total molecular weight of said segmented polyurethane serving as a base of a drug-storing layer is a number average molecular weight of from 1,000 to 6,000.
Claim 8
Dependent Claim 20 words
A transdermal absorption preparation as claimed in claim 1, wherein glycerin and/or polyglycerin is contained in the drug-releasing controlling membrane.
Claim 9
Dependent Claim 49 words
A transdermal absorption preparation as claimed in claim 1, wherein said diisocyanate is a diisocyanate selected from the group consisting of p-phenylene diisocyanate, 2,4-toluylene diisocyanate, 4,4-diphenylmethane diisocyanate, naphthalene 1,5-diisocyanate, hexamethylene diisocyanate, tetramethylene diisocyanate, lysine diisocyanate, xylylene diisocyanate and hydrogenated 2,4-toluylene diisocyanate, hydrogenated 4,4-diphenylmethane diisocyanate, dicyclohexyldimethylmethane p,p'-diisocyanate, and isophorone diisocyanate.

References Cited (Backward Citations)

JPS63108019A Cited
JPS63146812A Cited
US4997656A Cited
EP0299758A2 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 2001-03-02 2001-09-01 2002-03-03 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2005-03-02 2005-09-01 2006-03-03 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2009-03-02 2009-09-01 2010-03-03 $7700.00 Window Closed / Lapsed

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