伊拉地平缓释胶囊的制备工艺及体外释药研究

目的: 研究伊拉地平缓释胶囊制备工艺,并对其体外释药进行考察. 方法: 采用醇溶上药法(流化床底喷装置)制备伊拉地平微丸,并进行伊拉地平微丸质量评价及粉体学性质研究.用乙基纤维素(EC)和羟丙甲基纤维素(HPMC)为包衣材料,采用流化床进行包衣制备伊拉地平缓释微丸,对缓释微丸体外释放进行评价并考察不同热处理时间以及人工胃液对缓释微丸药物释放的影响,同时对批内和批间释药情况进行比较. 结果: 制备得到的伊拉地平微丸质量良好,不 同热处理时间(1~12 h)对于伊拉地平缓释微丸的释药特性影响不大,在制备过程中可不进行热处理,干燥即可.人工胃液会显著地降低伊拉地平缓释微丸的释药速率,宜将其置于肠溶胶囊中.伊拉地平缓释微丸批间及批内重复性较好,在0.1%十二烷基二甲基氧化胺溶液12 h释放符合零级释药模型动力学过程. 结论: 制备得到的伊拉地平缓释胶囊缓释效果好,达到了释药要求.

Objective: To prepare isradipine sustained-release capsules,and investigate the release profile in vitro. Methods: The pellets containing isradipine were prepared in the fluid-bed by alcohol soluble medicine and then coated with ethylcellulose(EC)and hydroxyl-propyl methyl cellulose(HPMC).The quality and micromeritics of the isradipine pellets were evaluated.The release profile of the isradipine sustained-release pellets and the effects of thermal treatment and artificia1 gastric juice on the release profile were tested and the inter-and intra-batch comparisons of release profile were conducted. Results: The surface of the coated pellets was smooth,glossy and round with good quality.No obvious effect of thermal treatment(1-12 h)on the release profile was observed,indicating that thermal treatment for isradipine sustained-release capsules was not necessary and desiccation was suitable for preparation.The effect of artifica1 gastric juice on the release profile was significant which decreased the release rate,indicating that isradipine sustained-release pellets should be put into enteric capsules.The inter-and intra-batch repeatability was good.The 12 h dissolution profiles of isradipine from the pellets in the 0.1% lauryl dimethy amine oxide solution fit into a zero grade equation. Conclusion: The isradipine sustained-release pellets prepared in this study exhibited ideal sustained-release characteristicsin vitro and the preparation technique was feasible which met the release requirements.

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