MUCOADHESIVE TABLET OF LOSARTAN POTASSIUM FOR UNIDIRECTIONAL BUCCAL DRUG DELIVERY: DEVELOPMENT AND EVALUATION

Objectives : Losartan potassium having oral bioavailability is about 33% due to first pass metabolism. The formulation of Losartan potassium in to bioadhesive tablet will improve bioavailability, to reduce the dosing frequency and to improve the patient compliance. Methods: Tablets prepared by direct compression method. Nine formulations were developed with varying concentrations of polymers like Carbopol 934p, Casein. 32 optimization methods is applied. Tablets were tested for Hardness, Thickness, weight variation, surface pH, drug Content uniformity, swelling index, Mucoadhesive strength, in-vitro drug dissolution study, and Stability study. Results: FTIR and DSC studies show no drug polymers interaction. The most compatible in-vitro drug release profile was achieved with the formulation F9 is 95% after 12 hrs which contains the drug is 25 mg, Carbopol 934p is 60 mg, Casein is 40 mg. The surface pH, Mucoadhesive strength, and swelling index of formulation F9 was found to be 6.7±0.2, 0.1850±0.01N, and 162.83±0.32%, after 8 hrs respectively. The in-vitro release kinetics studies reveal that all formulations show anomalous or non-fickian diffusion. Conclusion: Hence, Carbopol 934p, Casein mucoadhesive polymer in various proportions can be used to prepare mucoadhesive tablet of Losartan potassium having prolong therapeutics effect with enhance patient compliance by avoiding first pass metabolism. Differential Scanning Calorimetry, IR- Infra Red Spectrum, ICH-International Conference on Harmonisation.