奥沙西罗亲水凝胶骨架片制备及体外释药特性研究

目的制备奥沙西罗亲水凝胶骨架缓释片,考察处方、工艺以及释放条件对体外释药行为的影响,解析其机理。方法以羟丙甲纤维素(HPMC)为骨架材料,乙基纤维素(EC)为阻滞剂,采用湿颗粒压片法制备奥沙西罗亲水凝胶骨架片,考察HPMC用量、HPMC黏度、EC用量、制备方法、压片压力、释放介质及转速对奥沙西罗骨架片体外释药的影响。结果奥沙西罗骨架片体外释药符合Higuchi方程,药物释放机制是骨架溶蚀和药物扩散的综合效应;HPMC用量与黏度、阻滞剂用量、制备方法、压片压力对释放速率均有显著性影响;释放介质的pH值及转速对释放速率无显著性影响。结论调整处方HPMC用量可制得12 h给药1次的骨架缓释片。

Preparation of Oxaceprol matrix tablet and study of factors influencing its releasing behavior

Purpose To prepare Oxaceprol delayed release matrix tablets,and to evaluate the effect of formula composition,preparation method and release conditions on the drug release behavior.Elucidating the mechanism of drug releasing.Methods Hydroxypropyl methylcellulose(HPMC) as matrix material,preparation by wet method compression.Investigating the pharmaceutical properties by dissolution test.Evaluating the amount and viscosity of HPMC,varieties and amount of blocking agents,the pH of dissolution medium and the speed of basket rotation effect on the drug release behavior.Optimizing the formula.Results The release behavior of Oxaceprol matrix tablets is following Higuchi equation,and is mainly affected by amount of HPMC.The releasing mechanism was in line with synthetical effect of dissolution and corrosion.Conclusion Amount of HPMC is the mainly influencing factor of Oxaceprol matrix tablet releasing.We could get a 12 h-lag tablet,in a certain formula composition.