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作 者 ：王莹;祖元刚*;赵修华

期 刊 ：植物研究 2012年 32卷 (3)期 页码：369-372

关键词：羟基喜树碱；纳米颗粒；超声反溶剂法；表征；

Keywords:10-hydroxycamptothecin(HCPT), nanoparticles, anti-solvent ultrasonic method, characterization,

摘 要 ：为提高羟基喜树碱的水溶性及其制剂在体内稳定性，运用超声反溶剂法对羟基喜树碱进行初级颗粒制备。本文根据羟基喜树碱在不同有机溶剂中的溶解度与其在去离子水中的溶解度的不同进行对比，对各项指标进行检测。筛选出制备羟基喜树碱初级颗粒的最佳条件为：HCPT-DMSO浓度为5 mg·mL^-1、H₂O∶DMSO=1∶1、H₂O滴速为4 mL·min^-1，超声时间为10 min。对羟基喜树碱初级纳米颗粒进行检测，SEM扫描结果显示其形貌规则，粒径为746 nm，与羟基喜树碱原粉颗粒相比，粒径明显减小并在其水溶液中分布更为均匀。

Abstract:Hydroxycamptothecin (HCPT) primary particles were prepared using anti-solvent ultrasonic method in order to improve the water-solubility, stability and bioavailability in vivo. Various indexes were tested according to the solubility of HCPT in different organic solvents and water. The optimal preparation conditions were obtained with the HCPT-DMSO concentration of 5 mg·mL^-1, H₂O∶DMSO of 1∶1, titrate speed of 4 mL·min^-1 and the mixing time of 10 min. Various characterizations of the obtained HCPT were carried out. The SEM result demonstrated that the particles were uniform with the mean particle size of 746 nm. The HCPT primary particles have smaller particles size and the higher solubility compared with the raw HCPT.

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