Effect of Sodium Taurocholate on Omeprazole Buccal Adhesive Tablet: Physicochemical Characterization and Pharmacokinetics in Hamster

Abstract

To formulate an omeprazole buccal adhesive tablet with improved bioavailability using sodium taurocholate, omeprazole buccal adhesive tablets were prepared with sodium alginate, HPMC, magnesium oxide and different quantities of sodium taurocholate. Their physicochemical properties, such as the mucoadhesive force, stability in human saliva and release, were examined. Moreover, the absolute bioavailability was assessed by comparing the buccal administration to an omeprazole solution given intravenously to hamsters. Sodium taurocholate barely influenced the mucoadhesive force of the tablets; however, it affected the drug stability in human saliva. It positively influenced the fast drug release, but did not affect the release mechanism. In particular, omeprazole buccal adhesive tablets [omeprazole/sodium alginate/HPMC/magnesium oxide/sodium taurocholate (20/24/6/50/10 mg/tab)] showed an absolute bioavailability of about 30% in hamsters. They remained attached to the cheeks without disintegration. Moreover, they were stable in human saliva for at least 4 h. Thus, it was concluded that this omeprazole buccal adhesive tablet could be a useful possible commercial pharmaceutical product.