非诺贝特体外溶出度考察及其微粉化制剂的研究

目的考察不同厂家非诺贝特固体制剂体外溶出度以及微粉化对非诺贝特溶出度的影响。方法分别以 40 % (φ)乙醇溶液、5 0 % (φ)乙醇溶液、5g/L十二烷基硫酸钠溶液、1 0g/L十二烷基硫酸钠溶液为溶出介质 ,对 4种市售非诺贝特固体制剂的体外溶出度进行考察。采用球磨机制备微粉化非诺贝特 ,对其溶出度进行测定。结果 1 0 g/L十二烷基硫酸钠溶液中微粉化制剂的溶出速率明显快于其余 3种非微粉化制剂 ,初步探讨了非诺贝特固体制剂体外溶出度标准。用相似因子法对自制微粉化胶囊和法国生产的微粉化胶囊的溶出实验数据进行统计分析 ,结果表明两者溶出行为相似 ,相似因子f2 =72 4(5 0≤f2 ≤ 1 0 0 )。结论不同厂家非诺贝特固体制剂的溶出度差异较大 ,微粉化工艺能显著提高非诺贝特的溶出度

Investigation on the drug release of fenofibrate in vitro and the preparation of micronised feonfibrate

Objective To investigate the dissolution of fenofibrate in vitro and study the improvement in the dissolution properties of fenofibrate by micronization.Methods 40%(φ),50%(φ) ethanol solutions and 5 g·L -1, 10 g·L -1 sodium lauryl sulphate(SDS) solutions were selected as media to investigate the dissolution of four preparations of fenofibrate on sale. The micronised preparation was obtained by using a ball mill.The drug release of the micronised preparation was determined by UV.Results The results suggested that the release rate of the micronised preparation was noticeably better than that of non-micronized preparations in 10 g·L -1 SDS. According to the results,the dissolution standard of fenofibrate in vitro was preliminary. The drug release of the micronised preparation was compared with the French micronised product. The drug realease data were also analysed by the statistical method,and the results indicated that the dissolution of the micronised preparation was perfectly similar to that of the French micronised product( f 2=72 4>50).Conclusions The dissolution of four preparations of fenofibrate on sale has remarkable difference and the micronization can enhance the dissolution of fenofibrate.