论文部分内容阅读
目的:制备水难溶性药物固体分散体并初步考察其稳定性和片剂处方。方法:选择吲哚美辛为模型药物,采用捏合法制备固体分散体,通过单因素试验考察载体种类、捏合剂和捏合时间对固体分散体体外溶出效果的影响。利用粉末X射线衍射法对固体分散体进行表征,考察固体分散体在40℃,相对湿度(RH)75%条件下放置的稳定性,采用粉末直接压片法对固体分散体进行压片。结果:优选的制备工艺为以泊洛沙姆188为载体,乙醇-水(1∶1)为捏合剂,捏合时间30 min;固体分散体体外溶出效果显著提高,Cmax为原料药的29倍;固体分散体在40℃,RH 75%条件下1个月内稳定;制备的固体分散体片外观光洁美观,各项参数均符合2010年版《中国药典》要求。结论:采用捏合法制备的吲哚美辛固体分散体溶出效果显著提高,稳定性好,易于粉末直接压片。
Objective: To prepare the solid dispersion of poorly water-soluble drug and to investigate its stability and prescription. Methods: Indomethacin was chosen as the model drug, and the solid dispersion was prepared by kneading method. The effect of carrier type, kneading agent and kneading time on the dissolution of solid dispersion in vitro was investigated by single factor test. The solid dispersion was characterized by powder X-ray diffraction. The stability of the solid dispersion was investigated under the conditions of 40 ℃ and relative humidity (RH) of 75%. The solid dispersion was tabletted by powder direct compression method. Results: The optimal preparation process was poloxamer 188 as carrier, ethanol - water (1: 1) as kneading agent and the kneading time as 30 min. The dissolution effect of solid dispersions in vitro was significantly improved, with Cmax of 29 times that of API. The solid dispersion was stable within 1 month at 40 ℃ and RH 75%. The appearance of the prepared solid dispersion tablets was smooth and beautiful, and all the parameters were in line with the requirements of the 2010 edition of “Chinese Pharmacopoeia”. Conclusion: The dissolution of indometacin solid dispersion prepared by kneading method is significantly improved, with good stability and easy powder direct compression.