复方低分子肝素口服结肠靶向给药胶囊的研制

目的:研制用于溃疡性结肠炎治疗的复方低分子肝素口服结肠靶向给药胶囊。方法:通过考察颗粒的流动性、吸湿性,筛选复方制剂的最佳处方。从外观性状、装量差异、含量测定、体外溶出试验4个方面对制得胶囊进行质量检查。结果:筛选出最佳处方为可溶性淀粉:糊精:低聚木糖质量比为2∶3∶3;建立了天青A法测定低分子肝素含量,并进行了方法学考察;所制得的胶囊在人工胃液及在pH 6.8的人工肠液中不崩解,在pH 7.8的人工肠液中快速崩解释放。结论:所研制的复方低分子肝素口服结肠靶向胶囊符合规定。

Preparation and quality control of oral colon-targeting capsules of low molecular weight heparin

Objective: To prepare oral colon-targeting capsules of low molecular weight heparin and investigate its quality standards.Methods: The formula of oral colon-targeting capsules of low molecular weight heparin was optimized by evaluating the liquidity and hygroscopicity of particles.The quality control of the capsules was studied,including appearance,content,content uniformity and dissolution experiment in vitro.Results: The optimized formula consisted of sugar,dextrin and xylo-oligosaccharides in a ratio of 2∶3∶3.Azure A method was established for determination of low molecular weight heparin.The capsule was disintegrated and released rapidly in the artificial intestinal juice at pH 7.8,but not in the artificial gastric juice and intestinal juice at pH 6.8.The capsule was consistent with the quality standards.Conclusions: The capsule prepared meets the requirements of oral colon-targeting preparation.