Design and Evaluation of Ophthalmic Delivery of Bepotastine Besilate From Eye Drop

Abstract

Introduction: The purpose of present study was to design and evaluate bepotastine besilate ophthalmic solution 1.5% to develop a stable formulation using buffering agent, tonicity modifier and preservative. Method: In this study the concentration of preservative and tonicity modifier concentration are adjusted in such a way so that the final formulation will have least concentration of preservative still it will be protected from microorganisms and isotonic so that after instillation when formulation will come in contact with tissues there should not be any swelling, contraction or discomfort. Result: The preservative content was selected in the range of 0.002– 0.012% and tonicity modifier in the range of 0.45–0.9%. Bepotastine besilate ophthalmic solution 1.5% filled in LDPE container having fill volume 5 mL is clear, colourless solution having pH range 6.8–7.0, drop size of 38.6 μl and % water loss after 3 months as 1.9748%. The percent purity of bepotastine besilate and preservative was determined using RP-HPLC method was found to be 100.50 and 51.648% with % RSD as 0.84 and 0.65% respectively. The samples of the formulation also subjected to stability as per ICH guidelines and 6 months data was generated. Draize test protocol was also followed to study invivo eye irritancy of the formulation to produce a safe and effective formulation. Conclusion: Laboratory prepared formulation of bepotastine besilate ophthalmic solution 1.5% has showed good stability at both 25°C and 40°C as the drug and preservative content was within the accepted range. Key words: Bepotastine besilate, Benzalkonium chloride eye drop, Preservative, Ophthalmic preparation, Stability study, Isotonicity.