Pharmacokinetics and Pharmacodynamic evaluation of Nizatidine microspheres on experimental animals

Abstract

Mucoadhesive microspheres overcome the physiological adversities like short gastric residence time promoting the drug bioavailability. In the present investigation Nizatidine loaded Eudragit RS 100 microspheres were prepared by solvent evaporation technique using disparate drug polymer ratios with Eudragit RS 100 polymer and Nizatidine loaded chitosan microspheres were prepared by coacervation phase separation method. The prime objective was to enhance the absorption and bioavailability by prolonging the gastric residence time. Totally six formulations RES1- RES6 Eudragit RS 100 microspheres and six formulations RCP1 – RCP6 Eudragit RS100 microspheres were prepared and evaluated. RES3 and RCP3 showed nearly 90% drug release after 24 h. Hence the Nizatidine loaded Eudragit RS100 microspheres and Chitosan microspheres were further studied for the in vivo study for the suitability of the formulation. The bioavailability of nizatidine after oral ingestion is about 50% and is absorbed via the small intestine and it may be attributed to permeability of the intestine is relatively slow in nature. Hence the current research was to widen the therapeutic efficacy of Nizatidine by formulating microspheres enhance the intestinal permeability as well as bioavailability by performing the anti-ulcer activity.

Keywords: Microspheres, Eudragit RS 100, Chitosan, Bioavailability.