Abstract

TRANSDERMAL FORMULATION AND EVALUATION OF KETOTIFEN

Sabati A.M.A*, Ahmed Mohamed Othman* and Mohamed Salama

Abstract

Ketotifen is an anti-histaminic drug (H1-antagonist) used as a long term prevention of bronchial asthma and allergic bronchitis .It is available in the market as oral dosage forms (Tablet , Capsule and Syrup), It is a well-known fact that drugs taken orally pass through the G.I.T. where they experience first pass effect in the liver and 50 % of ketotifen is metabolized in the liver.: The purpose of this study was to formulate and evaluate a new transdermal formulations of ketotifen to avoid the first pass effect .The prepared formulations included; Film, Ointment, Cream and emulsion.: The release studies for the above formulations were done by using semi- permeable cellophane membrane and natural rabbit skin (after removing the hair from the abdominal region), by using diffusion cell operating at 37°C ± 0.5 and 50 r.p.m, the receptor media was a phosphate buffer of pH 7 and the amount of drug released was determined spectrophotometrically at λ max 300nm and at specified period of time. The results obtained showed that in case of using the semi- permeable cellophane membrane, the release of ketotifen from the above mentioned bases can be arranged in the following descending order: Film > Emulsion > Ointment (PEG) > Cream. In-vivo studies using rabbit skin as a membrane showed similar results of release of ketotifen from the above mentioned bases to in-vitro studies. This research included the kinetic studies to determine the correlation coefficient (r), the order of the reaction and the half-life for each base. These results suggest the usefulness of Ketotifen to be administered as a transdermal dosage form which is better than other dosage forms.

Keywords: ketotifen, PEG (Polyethylene glycol) , HPMC (Hydroxy propyl methyl cellulose)