Abstract

PREPARATION AND EVALUATION OF DOMPERIDONE TRANSDERMAL PATCHES

Maha M. Ali and Nawal A. Rajab*

Abstract

Background:Domperidone is a dopamine antagonist with antiemetic properties having a plasma half-life 7-9 hr. with 13-17% oral bioavailability. Objective: The aim of the present study is to prepare a domperidone transdermal adhesive matrix patch to improve its therapeutic efficacy, patient compliance and to reduce the frequency of dosing and side effects, as well as to avoid its extensive first pass metabolism. And then evaluate the physicochemical and mechanical properties as well as in vitro release and rat skin permeation of domperidone. Methods: Different formulas of the patches were prepared by solvent/evaporation casting technique using Chitosan, Eudragit E100, Eudragit RS 100 and Eudragit L100 as polymers with many suitable plasticizer. The physicochemical parameters like drug content, thickness, and weight variation, mechanical parameters like elongation%, elastic modulus and strain as well as drug release and permeation study were evaluated for the prepared patches.FTIR, DSC, SEM, and X-ray diffraction analysis were done to estimate any physicochemical between domperidone and other components of the prepared transdermal patch. In addition to that, skin adhesion, sensitivity test and stability study were done for the optimized transdermal patch.Results: The prepared patches containing Eudragit L100 as polymer and propylene glycol as plasticizer with concentration of 10, 20 and 30% w/w for FL7, FL8 and FL9 respectively showed the best physicochemical and mechanical properties. FL7 transdermal patch with a minimal concentration of propylene glycol 10% gave the uniform dissolution profile of 93.37% domperidone released within 24 hours. The using of dimethyl formamide ( 5% DMF) as a permeation enhancer significantly improved (p

Keywords: Domperidone, transdermal delivery system, matrix type patches, in vitro release and permeation study.