酮康唑海藻酸钙凝胶小球的制备工艺研究

目的:考察酮康唑海藻酸钙凝胶小球的制备工艺和最优处方。方法:采用滴制法制备海藻酸钙凝胶小球,以酮康唑的包封率和载药量作为制备工艺优化指标,设计正交试验优选最佳处方;测定最佳处方所制制剂的包封率(EE)和载药量(LD)并与原料药比较体外释放作用。结果:最优处方为海藻酸钠浓度2.0%,海藻酸钠与酮康唑质量比2∶1,氯化钙浓度0.3mol.L-1;EE和LD平均值分别为(90.53±2.32)%、(31.51±2.08)%,与原料药比较缓释性较好。结论:本法工艺简单、可行、稳定,重现性好。

Preparation Technology of Ketoconazole Calcium Alginate Gel Beads

OBJECTIVE:To investigate the preparation technique and optimal formulation of ketoconazole calcium alginate gel beads.METHODS:Ketoconazole calcium alginate gel beads were prepared by droplet method.The orthogonal experiment was carried out with encapsulation efficiency(EE)and drug loading(LD)as indexes to optimize the optimal formulation of the calcium alginate gel beads.The encapsulation efficiency and drug loading amount for the optimized formulation were determined,and the optimized formulation was compared with crude drug in respect of the in vitro drug release behavior.RESULTS:The result showed that the optimal formulation was as follows:2.0% Na-alginate and 0.3mol· L-1 CaCl2 with the ratio of Na-alginate:ketoconazole at 2∶ 1.The average EE and LD were(90.53± 2.32)% and(31.51± 2.08)%,respectively,and the slow-release was better as compared with that of the crude drug.CONCLUSION:The preparation procedure is simple,feasible,stable and reproducible.