卡托普利/壳聚糖-明胶网络多聚物缓释微球制备工艺的研究

Studies of optimal technology of captopril/chitosan-gelatin net-polymer sustained release microspheres

利用壳聚糖、明胶为载体材料,乳化交联法制备卡托普利/壳聚糖-明胶网络多聚物缓释微球(Cap/CGNPMs), 以部分因子设计试验优化微球的制备处方和工艺.结果表明,壳聚糖分子量(700 000 Da)、药物与载体材料投料比(1∶4)、交联剂组成(甲醛+三聚磷酸钠)、交联度 (1∶0.75)、添加0.75%微晶纤维素为制备Cap/CGNPMs的较理想条件.按较理想处方和工艺制得的Cap/CGNPMs粒径分布范围为220～280 μm,包封率46.23±4.51%,载药量9.95±0.77% , 方法重现性好,体外释药试验证明,Cap/CGNPMs具有良好的缓释延效作用.

The captopril/chitosan-gelatin net polymer microspheres (Cap/CGNPMs) were prepared with chitosan and gelatin by emulsification and cross linked process.Fractional factor design was applied to optimize the formulation and preparation procedure of Cap/CGNPMs. The results indicated that the experimental material ratio (EMR, 1/4),cross linked reagents (CLR, For+TPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres were an optimal condition to prepare Cap/CGNPMs. The size and distribution, embedding ratio and drug loading of Cap/CGNPMs were 220~280 μm, 46.23±4.51% and 9.95±0.77% respectively. The results demonstrated that Cap/CGNPMs had a good characteristic of sustained release of Cap in vitro.