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1 490.7、5 060.3 ng/(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 of β-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 with β-CD-PEG-SN38 micelle, AUC of free type and bonded type SN38 was 1 490.7、5 060.3 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.

R969.1

国家自然科学基金资助项目（82360705）；江西省双千计划（jxSq2023201078）；江西省教育厅科研课题（GJJ2200911）；南昌市重大科技攻关项目（2020-201-15）