续断“发汗”前后两个主要成分在大鼠体内的药代动力学研究

Research on the Pharmacokinetics of Two Main Components in Rats of Dipsaci Radix Before and After Sweating

目的:建立基于高效液相色谱串联质谱法(HPLC-MS)测定大鼠口服“发汗”前后续断中主要成分马钱苷和川续断皂苷Ⅵ的血药浓度测定方法,研究其药代动力学特征。方法:通过给大鼠灌胃服用“发汗”前后续断水煎液,分别于给药前和给药后在指定时间取眼眶窦血。采用HPLC-MS技术测定大鼠血浆中“发汗”前后续断中马钱苷与川续断皂苷Ⅵ的浓度。结果:大鼠口服给药5 min后,血中可以检测到马钱苷与川续断皂苷Ⅵ,“发汗”前续断马钱苷:半衰期为93.79 min,川续断皂苷Ⅵ的半衰期为86.51 min;“发汗”后续断:马钱苷和川续断皂苷Ⅵ的半衰期为69.71 min,85.78 min;“发汗”前续断的马钱苷与川续断皂苷Ⅵ的Cmax和AUC较大,表明“发汗”前续断的马钱苷与川续断皂苷Ⅵ更有利于发挥疗效。结论:该方法适用于“发汗”前后的续断在大鼠体内马钱苷和川续断皂苷Ⅵ血药浓度的测定及药代动力学研究,实验结果表明,未“发汗”续断中的马钱苷与川续断皂苷Ⅵ更有利于发挥疗效。

Objective:A HPLC-MS method was established for the determination of pharmacokinetics of two main components in plasma of rats in crude and sweated Dipsaci Radix,to study the pharmacokinetic characteristics.Methods:The rats were orally administered with water extract of crude and sweated Dipsaci Radix.Orbital sinus blood was taken at the specified time before and after administration.HPLC-MS was used to determine the concentration of loganin and asperosaponinⅥin rat plasma of crude and sweated Dipsaci Radix.Results:Loganin and asperosaponinⅥcould be detected in the blood of rats after oral administration for 5 min.Crude Dipsaci Radix:the half-life t_(1/2)of loganin was 93.79 min,and that of asperosaponinⅥwas 86.51 min.Sweated Dipsaci Radix:loganin t_(1/2)was 69.71 min,asperosaponinⅥt_(1/2)was 85.78 min;the Cmax and AUC of loganin and asperosaponinⅥof crude Dipsaci Radix were larger,indicating that loganin and asperosaponinⅥof crude Dipsaci Radix were more conducive to the efficacy.Conclusion:This method is suitable for the determination of plasma concentration and pharmacokinetic study of loganin and asperosaponinⅥin rats of crude and sweated Dipsaci Radix.The experimental results showed that loganin and asperosaponinⅥin crude Dipsaci Radix are more conducive to the efficacy.