小檗碱及8-羟基二氢小檗碱溶出性能比较

Comparative Study on the Dissolution Character between Berberine and 8-hydroxy Dihydroberberine

目的比较小檗碱(Ber)及8-羟基二氢小檗碱(Hdber)的溶出性能。方法采用高效液相色谱法测定含量,色谱柱为C18柱,流动相为水-乙腈-磷酸二氢钾-十二烷基硫酸钠(500 mL∶500 mL∶3.4 g∶1.7 g)(三乙胺或磷酸调节pH至5.4),检测波长356 nm;采用桨法考察体外溶出情况。结果 37℃,Ber在水中达溶解平衡时间约30 min,Hdber为90 min;达溶解平衡时,Ber浓度约45μmol·L-1,Hdber为0.35μmol·L-1。结论该方法简便、稳定、可靠,Hdber在水溶液中的溶解速率及溶出度远小于Ber。

Objective To compare the dissolution character of berberine（Ber） and 8-hydroxy dihydroberberine（Hdber）.Methods An high performance liquid chromatography（HPLC） method was established for determination of Ber and Hdber with C18 column.The mobile phase was cyanides-water-lauryl sodium sulfate-KH2PO4（500 mL-500 mL-3.4 g-1.7 g）,adjusted to pH 5.4 with phosphoric acid or triethylamine,and the detection wave length was set at 365 nm.A paddle method was used to investigate their dissolution character.Results The dissolution equilibrium time of Ber was 30 min at 37 ℃,while Hdber needed 90 min.When reached the dissolved equilibrium,the concentrations of Ber and Hdber were 45 μmol·L^-1 and 0.35 μmol·L-1,respectively.Conclusion The method is convenient,stable and reliable,and the dissolution rate of Hdber is significantly lower than that of Ber.