Abstract

FORMULATION AND EVALUATION OF ORAL FLOATING IN SITU GEL OF CEFIXIME TRIHYDRATE BY USING ß-CYCLODEXTRIN COMPLEXATION TECHNIQUE FOR SOLUBILITY ENHANCEMENT

Jinal Patel, Panchaxari Dandagi*, Sujay Hulyalkar and Bapu Desai

ABSTRACT

Purpose: Cefixime Trihydrate is third generation cephalosporin antibiotic which is slowly and incompletely absorbed from gastrointestinal tract after oral administration as it is an acidic drug with pH 2.6 & 4.1[pKa(strong acidic) = 3.45, pKa(strong basic) = 2.92] thus to improve gastro retentive time and therapeutic effect with sustained release it is formulated as floating in situ gelling system. Methods: Attempted to enhance the solubility of drug by preparing water soluble complexes of drug by using cyclodextrin inclusion complexation technique. In situ gel formulations were designed using gellan gum and sodium alginate as gelling agent, calcium carbonate as gas generating agent and sodium citrate as complexing agent. Results: All the formulation showed floating within 60 secs and had total floating time of 20h. Formulation F2 considered as ideal because it showed maximum drug release i.e. 89.02% following higuchi‟s diffusion mechanism. Conclusion: The in situ gelling systems formed gel instaneously when comes in contact with SGF and floats for longer duration. Enhanced the gastro retentive time of Cefixime Trihydrate in stomach. The drug content of solution and gel was within acceptable range of 85 to 115% which ensured dose uniformity in the formulation. The drug content was maximum for F2. Drug entrapment efficiency of all the formulations was found to be more than 95% which indicates that there was no significant loss of drug during formulation and Drug released maximum.

Keywords: Cefixime Trihydrate, Entrapment efficiency, Gastrointestinal tract, Gellan gum, Higuchi,s diffusion, In situ gel, Ionic gelation, Sodium alginate.