依托泊苷明胶微球的制备

Preparation of etoposide-loaded gelatin microsphere

目的制备难溶性药物依托泊苷(VP16)明胶微球,并对其形态学性质和载药特性进行研究。方法以PVP为分散介质,采用加液研磨法制得难溶性药物依托泊苷固体分散体,通过正交试验设计,筛选乳化缩聚法制备肺靶向依托泊苷明胶微球的最佳制备工艺。结果微球平均粒径为17.21μm,其中10～30μm的占89.58%,载药量为(20.94±0.13)%,药物包封率为(86.27±0.65)%。结论以PVP为载体将药物制成固体分散体后再用乳化缩聚法制得的依托泊苷明胶微球外观均匀圆整,分散性良好,粒径分布符合肺靶向要求,载药量较高。

OBJECTIVE To select an efficient procedure to prepare the etoposide-loaded gelatin microsphere (VP-GMS) and to study the properties of its morphology and drug loading.METHODS Use PVP as dispersion base milled with liquid to make the unsoluable etoposide microcrystalline.Carry out experiments following orthogonal design,use all balanced datas of the distribution of the diameter,drug loading and the degree of nonadhension to find the optimum procedure of emulsion polycondensation techniques.RESULTS The VP-GMS produced by the selected procedure had a mean diameter of 17.21μm,including 89.58% of them ranging from 10μm to 30μm.The drug loading was about 20.94% and the embedding ratio was 86.27%.CONCLUSION The VP-GMS prepared by emulsion polycondensation techniques is regular in its morphology with a high drug loading.The diameter distribution conforms to the requires.