Preparation and bioavailability of bupropion hydrochloride sustained-release pellets

Aim:To prepare bupropion hydrochloride(BH)24-hour sustained-release pellets and to determine its oral bioavailability in rats.Methods:BH 24-hour sustained-release pellets were prepared through the method of extrusion-spheronization and then were coated by ethyl cellulose-based aqueous disperse system using Mini-Glatt.And BH plasma concentrations in rats receiving administration of BH pellets or commercially available BH tablets were determined by HPLC.The pharmacokinetic parameters were estimated by Kinetica software.Results:The cumulative release percents of BH sustained-release pellets in 2,12 and 24 h were 10%,80% and 95%,respectively.The plasma concentration-time curves of BH sustained-release pellets and BH tablets in rats after oral administration were fitted to two-and one-compartment models,respectively.AUCs of BH sustained-release pellets and BH tablets were found to be(1 523.79±323.30)ng ·h/mL and(1 379.67±253.61)ng ·h/mL,respectively;cmaxs were(163.80±32.93)ng/mL and(451.91±144.54)ng/mL,respectively;and tmaxs were(4.67±0.52)h and(0.5±0)h respectively.The relative bioavailability of BH sustained-release pellets to commercial BH tablets was(110.46±17.07)%.Conclusion:The prepared BH 24-hour sustained-release pellets are bioequivalent to the commercial BH tablets.