他克莫司胶囊在4种溶出介质中的体外溶出特性研究

发布时间：2018-10-09 18:20

【摘要】：目的:研究自研他克莫司胶囊在4种溶出介质中的体外溶出特性,并与原研他克莫司胶囊进行比较。方法:采用桨法测定溶出度,转速为50 r/min,介质体积为900 ml。以原研他克莫司胶囊为参比制剂,自研他克莫司胶囊为受试制剂,分别以p H 1.0盐酸溶液、p H 4.5磷酸溶液、p H 6.8磷酸盐缓冲液和水为溶出介质(均含0.005%羟丙基纤维素);以高效液相色谱法测定他克莫司含量,并计算累积溶出度,绘制溶出曲线;采用相似因子(f2)法对2种制剂溶出曲线的相似度进行评价。结果:在4种不同p H的溶出介质中,2种他克莫司胶囊溶出行为相似,90 min时溶出度均达到85%以上,f2均大于50。结论:自研他克莫司胶囊在4种溶出介质中均可以完全释放,与原研胶囊在不同溶出介质中体外溶出行为均相似。
[Abstract]:Aim: to study the in vitro dissolution characteristics of tacrolimus capsules in 4 kinds of dissolution media and compare them with the original tacrolimus capsules. Methods: dissolution was determined by propeller method with a rotational speed of 50 rmin and a volume of 900 ml.. The original tacrolimus capsule was used as the reference preparation, and the tacrolimus capsule was used as the test preparation. Using pH 1.0 hydrochloric acid solution, pH 4.5 phosphoric acid solution, pH 6.8 phosphate buffer solution and water as dissolution medium (both containing 0.005% hydroxypropyl cellulose), the content of tacrolimus was determined by HPLC, the cumulative dissolution was calculated and the dissolution curve was drawn. Similarity factor (f 2) method was used to evaluate the similarity of dissolution curves of two preparations. Results: in 4 different pH dissolution media, the dissolution rates of two kinds of tacrolimus capsules were more than 85% and more than 50% at 90 min. Conclusion: the self-made tacrolimus capsule can be completely released in 4 kinds of dissolution media, which is similar to the dissolution behavior of the original capsule in different dissolution media in vitro.
【作者单位】：华北制药集团新药研究开发有限责任公司/微生物药物国家工程研究中心/河北省工业微生物代谢工程技术研究中心;
【分类号】：R927.2;O657.7

【参考文献】