正交设计反向滴加法包合尼群地平及其片剂的制备

发布时间：2018-06-05 07:29

  本文选题：尼群地平 + β-环糊精　； 参考：《中国新药杂志》2015年06期

【摘要】：目的:采用饱和水溶液法制备尼群地平-β-环糊精包合物,并以包合物为原料制成片剂,提高片剂的体外溶出度。方法:以包封率、收率、载药量为指标,采用加权评分法,通过正交设计优选最佳包合工艺。以粉末直接压片法制备尼群地平包合物片剂,测定其在4种不同介质(含0.15%聚山梨酯-80的水溶液、p H1.2盐酸溶液、p H 4.0醋酸盐缓冲液、p H 6.8磷酸盐缓冲液)中的溶出度。结果:采用"反加法",最佳包合工艺为包合温度70℃,尼群地平与β-环糊精摩尔比为1∶2,醇水比为2∶5,包合时间2 h。包合物包封率可达79%,收率为84%,载药量为14%。所制备片剂的体外溶出度显著提高,45 min时溶出度70%。结论:采用最佳包合工艺制备的包合物可显著改善尼群地平的溶出性能,所制备的包合物片剂能达到日本橙皮书的要求。
[Abstract]:Aim: to prepare nitrendipine-尾-cyclodextrin inclusion compound by saturated aqueous solution, and to improve the dissolution rate of the tablet in vitro by using the inclusion compound as raw material. Methods: with the encapsulation efficiency, yield and drug loading as the index, the optimal inclusion process was selected by orthogonal design. Nitrendipine inclusion compound tablets were prepared by direct powder pressing method and their dissolution in four different media (pH1.2 hydrochloric acid solution, pH 4.0 acetate buffer solution, pH 6.8 phosphate buffer solution) was determined. Results: the optimum inclusion temperature was 70 鈩，

本文编号：1981165