盐酸丙哌维林缓释胶囊体外释放度及体内外相关性

Dissolution and in vitro-in vivo correlations of propiverine hydrochloride sustained-release capsules

建立了盐酸丙哌维林缓释胶囊体外释放度的HPLC-UV测定方法,色谱柱为Shim-pack VP-ODS C18(150 mm×4.6 mm,5μm),流动相为甲醇-0.05 mol/L磷酸盐缓冲溶液(70∶30),检测波长为230 nm。对影响盐酸丙哌维林缓释胶囊体外释放的各种因素进行了考察,最终确定采用小杯法,以蒸馏水250 mL为溶剂,转速为50 r/min,介质温度为(37±0.5)℃。对体外释放度数据进行多种模型拟合,确定盐酸丙哌维林缓释胶囊体外释放的最佳拟合模型为威布尔模型。采用Loo-Riegelman法计算盐酸丙哌维林缓释胶囊在健康受试者体内的吸收度,与体外释放度进行点对点相关水平分析。结果表明,其体内外相关性良好。

An HPLC-UV method was developed to determine the concentration of propiverine hydrochloride in the dissolution medium.The analyte was chromatographically separated on a Shimadzu Shim-pack VP-ODS C18 column（150 mm×4.6 mm,5 μm） using a mixture of methonal-phosphate buffer（0.05 mol/L）（70 ∶30） as mobile phase.An appropriate method was established for the dissolution testing.The small beaker method of dissolution testing in Chinese Pharmacopoeia was chosen.250 mL distilled water was used as the dissolution medium at 50 r/min and（37±0.5） ℃.Weibull model was selected as the description of propiverine hydrochloride sustained release capsule＇s releasing mechanism.In vitro-in vivo correlation evaluation was studied by Loo-Riegelman method,which proved that in vitro-in vivo correlation was significant.