Triacetin as a transdermal penetration enhancer

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 pKa 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.

Description

[0001] This application is a divisional application of the patent application filed on February 5, 2004, the invention title is "Transdermal Accelerator Triacetin", and the application number of said application is 200410039211.2. technical field [0002] The present invention relates generally to compositions and methods for promoting the release of biologically active substances through biological membranes, including skin and mucous membranes, and more particularly to triacetin-promoted pK a Use of transmembrane or transmucosal release of basic drugs such as oxybutynin of about 8.0 or greater. Background technique [0003] Presently used forms of oral administration of drugs are unsatisfactory for a number of reasons. First, drugs with a short half-life require frequent dosing (2 to 4 times a day), which will lead to poor patient compliance. Second, the drug's short plasma half-life and frequent dosing will create "peaks" and "troughs" in the plasma concentration profile...

AI Technical Summary

Problems solved by technology

[0003] Currently available oral drug delivery methods are unsatisfactory for many reasons

First, drugs with short half-lives require frequent dosing (2 to 4 times daily), which leads to poor patient compliance

Second, the drug's short plasma half-life and frequent dosing will create "peaks" and "troughs" in the plasma concentration profile, which will lead to increased potential for side effects with peak concentrations and loss of therapeutic effect near the end of the dosing interval

Third, the hepatic first-pass metabolism associated with oral administration will result in poor bioavailability of the drug

Increasing the amount of triacetin in the enhancer formulation with a corresponding decrease in the amount of linoleic acid will decrease the amount absorbed and prolong the penetration lag time of the drug oxymorphone, suggesting the importance of triacetin in the enhancer formulation. Relatively low

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