Formulation and evaluation of mucoadhesive sublingual tablet of rosuvastatin calcium

Rosuvastatin calcium is a lipid lowering agent which has been selected as a model drug for investigation, because of its very low bioavailability (20%) due to extensive first pass metabolism. In this work a new attempt was made to enhance the solubility, dissolution rate and oral bioavailability of poorly soluble rosuvastatin calcium by formulating it as direct compression method by using mucoadhesive polymer chitosan and various super disintegrant like sodium starch glycolate and croscarmelose sodium. Solubility of rosuvastatin calcium increased by using complexing agent β-cyclodextrin by kneading method. Mucoadhesive sublingual tablet were evaluated by pre and poss comprssion parameter. Precompression test like bulk density, tap density, angle of repose, cars index and postcompression test include thickness, hardness, friability, weight variation, drug content, disintegration time, wetting time, surface pH, in-vitro drug release and ex-vivo mucoadhesive time. USP II type appraratus is used for measuring mucoadhesion time with fresh got mucus membrane. The order of drug release from the dosage form has been determined. The optimized formulation followed Hixon-Crowel kinetics release. The physiochemical interaction between the drug and polymer were investigated using FTIR and DSC study.Optimized formulation (F4) showed 96.69% in-vitro release within 60 min. The present study concluded that sublingual delivery of mucoadesive rosuvastatin calcium tablets can be a good way to bypass the first pass metabolism and it will render great bio availability.