Triacetin as a penetration enhancer for transdermal delivery of a basic drug
AssigneeTheratech, Inc.
InventorsDanyi Quan, Ninad A. Deshpanday, Srinivasan Venkateshwaran, Charles D. Ebert
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Abstract
A composition and method for enhancing transdermal penetration of a basic drug are described. The composition comprises a matrix patch comprising an effective amount of a basic drug, preferably having a pK.sub.a of about 8.0 or greater, an effective amount of penetration enhancer consisting essentially of triacetin, and a polymer later preferably comprising a pressure-sensitive adhesive. A preferred basic drug is oxybutynin and acid addition salts thereof. The method for enhancing transdermal penetration comprises applying the matrix patch to a selected area of skin.
Claims22
A method of enhancing the rate of transdermal penetration of a basic drug having a pK.sub.a of about 8.0 or greater comprising applying to a selected application situs a matrix patch comprising
- (a) a biocompatible polymer layer, wherein said biocompatible polymer is an adhesive selected from the group consisting of acrylics, vinyl acetates, natural and synthetic rubbers, ethylenevinylacetate copolymers, polysiloxanes, polyacrylates, polyurethanes, plasticized polyether block amide copolymers, plasticized styrene-rubber block copolymers, and mixtures thereof;
- (b) an effective amount of a percutaneously absorbable basic drug having a pK.sub.a of about 8.0 or greater selected from the group consisting of oxybutynin, scopolamine, fluoxetine, epinephrine, morphine, hydromorphone, atropine, cocaine, buprenorphine, chlorpromazine, imipramine, desipramine, methylphenidate, methamphetamine, lidocaine, procaine, pindol, nadolol, carisoprodol, and acid addition salts thereof;
- and
- (c) an effective amount of a permeation enhancer consisting essentially of triacetin.
A matrix patch for transdermal administration of a basic drug having a pK.sub.a of about 8.0 or greater comprising
- (a) a biocompatible polymer layer, wherein said biocompatible polymer is an adhesive selected from the group consisting of acrylics, vinyl acetates, natural and synthetic rubbers, ethylenevinylacetate copolymers, polysiloxanes, polyacrylates, polyurethanes, plasticized polyether block amide copolymers, plasticized styrene-rubber block copolymers, and mixtures thereof;
- (b) an effective amount of a percutaneously absorbable basic drug having a pK.sub.a of about 8.0 or greater selected from the group consisting of oxybutynin, scopolamine, fluoxetine, epinephrine, morphine, hydromorphone, atropine, cocaine, buprenorphine, chlorpromazine, imipramine, desipramine, methylphenidate, methamphetamine, lidocaine, procaine, pindolol, nadolol, carisoprodol, and acid addition salts thereof;
- and
- (c) an effective amount of a permeation enhancer consisting essentially of triacetin.
Dependencies are inferred from the claim text.