FORMULATION AND EVALUATION OF GASTRORETENTIVE CEFUROXIME AXETIL FLOATING MICROSPHERES

Laukik S. Chorghe* and Madhuri T. Deshmukh

ABSTRACT

Objective: The objective of this research was to formulate and evaluate Cefuroxime axetil floating microsphere prepared using sodium alginate and carbopol 934. Cefuroxime axetil having extensive hepatic first pass metabolism and low bioavailability problem, determined the need for the development of sustained release formulation. Methods: Cefuroxime axetil floating microspheres were prepared by ionic gelation method Cefuroxime axetil floating microspheres were prepared by ionic gelation method by using carbopol as crosslinking agent. The Cefuroxime axetil floating microsphere was characterized by particle size measurement, process yield, morphology of microsphere, drug entrapment efficiency, differential scanning calorimetry, Fourier transforms infrared (FTIR) study and in-vitro drug release. Results: The Cefuroxime axetil floating microsphere having mean particle size ranged from 493 μm to 660 μm, and the entrapment efficiencies ranged from 94% to 95%. All the cefuroxime axetil microsphere batches showed good in-vitro mucoadhesive property ranging from 74.40% to 97.97. FTIR studies indicated the no drug-polymer interactions in the ideal formulation F2. There were no compatibility issues. and the crystallinity of Cefuroxime was found to be reduced shoeing less intense peak in prepared floating microspheres, which were confirmed by differential scanning calorimeter. Among different formulations, the Cefuroxime microspheres of batch F2 had shown the optimum percent drug entrapment of microspheres. Release pattern of Cefuroxime from F2 microspheres batch followed Higuchi kinetic model. Stability studies were carried out for F2 formulation at 4°C/ambient, 95.611±0.256°% relative humidity revealed that the drug entrapment, floating behavior, and drug release were within permissible limits. Conclusion: The results obtained in this work demonstrate the use of carbopol and sodium alginate polymer for preparation of floating microsphere.

Keywords: Ionic gelation method, Gastroretentive delivery, floating microsphere, Sodium alginate, Carbopol.