目的考察脂肪乳载体对羟基喜树碱胰腺靶向性的影响。方法以大豆磷脂和大豆油为主要辅料,采用两步乳化法制备羟基喜树碱脂肪乳。家兔分别静脉注射单剂量(3.5mg/kg)的羟基喜树碱脂肪乳和羟基喜树碱注射液,内标采用HPLC法测定药物在胰腺组织中的浓度。结果所建立的HPLC法专属性好、灵敏度高;与羟基喜树碱注射液相比,羟基喜树碱脂肪乳显著提高了胰腺中药物的浓度。结论脂肪乳作为载体可以明显提高羟基喜树碱对胰腺的靶向性。

Objective To investigate the effect of lipid emulsion as drug carrier on pancreas targeting capability of hydroxycamptothecin.Methods Hydroxycamptothecin-loaded lipid emulsion was preparedby a two-step emulsifying process with soybean phospholipid and soybean oil as main excipients.Hydroxy-camptothecin-loaded lipid emulsion and hydroxycamtothecin injection were iv administrated tO rabbits at a single dose of 3.5 mg／kg.The hydroxycamptothecin concentration in the pancreas was determined byHPLC with camptothecin as the internal standard.Results The HPLC method for the determination ofhydroxycamptothecin and camptothecin was sensitive and accurate.The hydroxycamptothecin concentra-tion in the pancreas was greatly improved in hydroxycamptothecin-loaded lipid emusion compared with hy-droxycamtothecin injection.Conclusion The pancreatic gland targeting capability is greatly improved,when lipid emulsion is used as drug carrier.