中文摘要：

采用微沉淀-高压匀质法制备具有高过饱和溶出水平、高渗透性和物理稳定的口服羟基喜树碱纳米混悬剂（hydroxycamptothecin nanosuspensions,HCPT-Nano）,并对其粒径及分布、zeta电位、粒子形态、物理存在状态、贮存稳定性及过饱和溶出水平等制剂学性质进行了评价。结果表明,HCPT-Nano的粒径小于300 nm且分布均匀,粒子多呈棒状或块状,药物以结晶形式存在,能长期维持较高的过饱和溶出水平。因此,结合P糖蛋白（P-glycoprotein,P-gp）的抑制剂环孢素A（cyclosporin,CsA）的加入,为提高HCPT的口服生物利用度提供了可能性。

英文摘要：

Oral hydroxycamptothecin nanosuspension（HCPT-Nano） with high supersaturated dissolution level,high permeation and well physical stability,was manufactured by microprecipitation-high press homogenization method.Its pharmaceutical properties were investigated,such as size and distribution,zeta potential,particle shape,physical existence condition,supersaturated dissolution level and so on.Particle size was measured by laser diffraction,and the mean diameters before and after lyophilization were 138 ± 11.72 nm and 175 ± 12.74 nm,respectively,for HCPT-Nano.Zeta potentials of HCPT-Nano was over -20 mV.The nanoparticles,being observed by transmission electron microscopy（TEM）,were claviform or column in shape.DSC and X-ray diffraction revealed that HCPT existed in the form of crystal for HCPT-Nano.And HCPT-Nano could maintain higher supersaturated dissolution level for long time.So it supplied the possibility of improving oral bioavailability of HCPT when combining together admoveatur of P-gp inhibitor,CsA.