复方自乳化半固体珍菊降压胶囊剂的制备及其性质考察

目的制备复方自乳化半固体珍菊降压胶囊剂,以期提高其主要成分(芦丁和氢氯噻嗪)溶出度及生物利用度。方法通过溶解度实验和绘制伪三元相图的方法进行自乳化处方的筛选,以载药量、载油量及粒径等为指标应用单纯形网格法优化处方;采用熔融法制备半固体胶囊并对该半固体胶囊进行稳定性影响因素考察及药物溶出度测定。结果复方自乳化半固体珍菊降压胶囊剂最优处方为泊洛沙姆188-油酸乙酯-聚乙二醇辛基苯基醚-聚乙二醇400(质量比28.6∶8.4∶44.1∶19.1),该制剂中主要成分芦丁和氢氯噻嗪载药量为128.8、57.7 mg.g-1;60℃、光照下含量明显下降;复方自乳化半固体胶囊剂和市售胶囊剂1 h药物溶出度分别为100%、48.1%。结论所制备的复方自乳化半固体胶囊剂具有载药量高、溶出度好的特点。

Self-microemulsifying semi-solid matrix hard capsules to treat hypertension: in vitro study

Objective To develop the formulation of Zhenju Jiangya (traditional Chinese medicines) self-microemulsifying semi-solid matrix hard capsule drug delivery system and evaluate the dissolutions and bioavailabilities of hydrochlorothiazide and rutin. Methods The contents of hydrochlorothiazide and rutin were measured by HPLC. Pseudo-ternary phase diagrams were constructed identifying the efficient self-emulsification region. In vitro dissolution determination was carried out. Results The in vitro dissolution of self-microemulsifying semi-solid matrix hard capsules was about twofold higher than that of commercially available capsules. Conclusions The self-microemulsifying semi-solid matrix hard capsules can be successfully formulated with high drug loading rate and dissolution. It may be a promising alternative for the treatment of hypertension.