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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。
Hydroxycamptothecin nanosuspensions (HCPT-Nano) with high supersaturation, high permeability and physical stability were prepared by microprecipitation-high pressure homogenization. Their particle size and distribution, zeta Potential, particle morphology, physical state of existence, storage stability and supersaturated dissolution level were evaluated. The results showed that the particle size of HCPT-Nano was less than 300 nm and distributed evenly. Most of the particles were in the form of rods or lumps. The drug existed in crystalline form and could maintain high supersaturation dissolution level for a long time. Therefore, the addition of cyclosporin (CsA), an inhibitor of P-glycoprotein (P-gp), has provided the possibility of improving the oral bioavailability of HCPT.