β-环糊精-聚乙二醇-7-乙基-10-羟基喜树碱胶束在大鼠体内的药动学研究

Pharmacokinetics ofβ-cyclodextrin-polyethyleneglycol-SN38 micelle in rat

目的考察β-环糊精-聚乙二醇-7-乙基-10-羟基喜树碱(β-CD-PEG-SN38)胶束在大鼠体内的药动学。方法采用HPLC-MS/MS法测定血浆中SN38的质量浓度,利用三隔室模型进行β-CD-PEG-SN38药动学数据拟合。结果大鼠ivβ-CD-PEG-SN38胶束溶液后,游离型SN38和键合型SN38的AUC分别是1490.7、5060.3ng/(mL·h),在大鼠血浆中占主导的是键合型的SN38。结论方法操作简单、实用,可为SN38的靶向给药研究提供参考。

Objective To study pharmacokinetics ofβ-cyclodextrin-polyethyleneglycol-SN38(β-CD-PEG-SN38)micelle in rat.Methods Contents of SN38 were determined by HPLC-MS/MS method,and a three-compartment model were used to estimate the pharmacokinetics parameters.Results After iv administered withβ-CD-PEG-SN38 micelle,AUC of free type and bonded type SN38 was 1490.7、5060.3 ng/(mL∙h),and the dominant SN38 in rat plasma was the bonded type.Conclusion This method is simple and practical to operate,and can provide reference for targeted drug delivery research of SN38.