Abstract
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. The present investigation is aimed at design and evaluate bi-layered buccal-adhesive tablet of rosuvastatin calcium by direct compression method using bio-adhesive polymers in combination of Carbopol and sodium carboxy methyl cellulose (CMC), Carbopol and sodium alginate. All the formulation were subjected to quality control(QC) test and evaluation test like thickness, weight variation, hardness, drug content, swelling index, surface pH, ex-vivo Mucoadhesive strength, in-vitro drug release and ex-vivo permeation studies. The modified in- vitro assembly was used to measure and compare the bio-adhesive strength of tablet with fresh porcine buccal mucosa as a model tissue. The tablets were evaluated for in vivo release in pH6.6 citrate buffer for 6hr in standard dissolution apparatus. The order of drug release from the dosage form has been determined. The optimized formula followed non-fickian release mechanism with zero order kinetics. The physiochemical interaction between the drug and polymer were investigated using FTIR. The results of post compressional characteristic were found to be within the pharmacopoeial limits. Optimized formulation containing Carbopol, sodium alginate showed good bio-adhesion strength and 96.0% of in-vitro release of drug in 6hrs, and 86.11% permeation of drug through porcine buccal mucosa. The excipients used in study did not alter physic-chemical properties of the drug, FTIR is confirmed. The present study concludes that buccal delivery of rosuvastatin calcium tablets can be a good way to bypass the first pass metabolism and it will render great bio availability.