目的 考察β-環(huán)糊精-聚乙二醇-7-乙基-10-羥基喜樹堿(β-CD-PEG-SN38)膠束在大鼠體內(nèi)的藥動(dòng)學(xué)。方法 采用HPLC-MS/MS法測(cè)定血漿中SN38的質(zhì)量濃度,利用三隔室模型進(jìn)行β-CD-PEG-SN38藥動(dòng)學(xué)數(shù)據(jù)擬合。結(jié)果 大鼠ivβ-CD-PEG-SN38膠束溶液后,游離型SN38和鍵合型SN38的AUC分別是1 490.7、5 060.3 ng/(mL∙h),在大鼠血漿中占主導(dǎo)的是鍵合型的SN38。結(jié)論 方法操作簡(jiǎn)單、實(shí)用,可為SN38的靶向給藥研究提供參考。

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

國(guó)家自然科學(xué)基金資助項(xiàng)目（82360705）；江西省雙千計(jì)劃（jxSq2023201078）；江西省教育廳科研課題（GJJ2200911）；南昌市重大科技攻關(guān)項(xiàng)目（2020-201-15）