Optimization,preparation and in vitro/in vivo evaluation of bupropion hydrochloride/dextromethorphan hydrobromide suspension
Objective To prepare the compound suspension of bupropion hydrochloride(BH)/dextromethorphan hydrobromide(DMH),optimize the formulation and evaluate them in vitro and in vivo.Methods The sedimentation volume ratio,redispersibility and viscosity of suspension system were used as evaluation indexes.The suspending agent,wetting agent and their respective dosages were determined by single factor.The prepared suspension was evaluated in vitro by the content,release,drug leakage and stability tests.In addition,its in vivo pharmacokinetics was also evaluated.Results The optimized formulation was as follows:tragacanth 0.5％,xanthan gum 0.2％,31％high fructose corn syrup HFCS F42,l％Tween 80.The stability test showed that the optimized suspension exhibited good stability(F＞0.9,BH drug content:98％～100％,DMH drug content:96％～98％,all drug release:f2＞50,all drug leakage＜0.3)after the high temperature,strong light and 6 months of acceleration test.The pharmacokinetics of rats after the intragastric administration also showed that the Cmax of BH in the self-made suspension was lower and the tmax was longer than that in the market.The t1/2 and Cmax of DMH were longer and higher,with the bioavailability of 116.53％and 252.25％,respectively.The absorption of BH and DMH in vivo had a simple relative correlation with the release in vitro.Conclusion The BH/DMH compound suspension in this study had good stability and bioequivalence.It was feasible to prepare compound suspension of bupropion and dextromethorphan by ion exchange resin technology.
ion exchange resinbupropion hydrochloridedextromethorphan hydrobromidesuspensionpharmacokineticsbioavailabilityin vitro-in vivo correlation
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