对乙酰氨基酚HPMC骨架片药物释放影响因素研究

 目的:考察影响对乙酰氨基酚亲水性骨架片体外释药的各种因素。方法:以 羟丙基甲基纤维素(HPMC)为骨架材料，用湿颗粒法将对乙酰氨墓酚制成缓释片考寨HPMC的用量、粘度、粒度、制法、压片压力、片子大小及其它辅料对对乙酰氨基酚HPMC骨架片体外释药的影响。结果:对乙酰氨酚HPMC骨架片的体外释药均符合Higuchi方程。HPMC用量和粒度、制法、片子大小对对乙酰氨基酚的释放速率均有显著性影响。湿法制片的释药比干法压片慢。对乙酰氨基酚的释药速率随HPMC粒度的减小和片子的增大而减慢。HPMC的粒度及不同浓度乙醇作湿润剂对对乙酰氨基酚的释放速率影响不大。对压片压力影响的研究结果表明，对乙酰氨基酚HPMC骨架片的硬度范围不同时，影响有所不同。淀粉，PVP, MCC的加入(每片HPMC含量不变)均减慢对乙酰氨基酚的释放速率，加入量的影响在本实验范围内无显著差异。EC加入量多时(80 mg·片^-1)。对乙酰氨基酚释放速率显著加快。结论:HPMC用量和粘度，制备工艺，片剂大小及其辅料为影响对乙酰氨基酚骨架片释放速率的主要因素。

The factors influencing acetaminophen release from hydroxypropyl methylcellulose matrix tablet

OBJECTIVE: To study the factors influencing acetaminophen release rate from hydroxypropyl methylcellulose (HPMC) hydrophylic matrix tablet. METHODS: The HPMC matrix tablet was compressed by wet method with acetaminophen (ATMP) as a model drug. The effect of the amount, viscosity and particle size of HPMC, preparation method, compressing pressure, tablet size and additives on the drug release from the matrix tablets was observed. RESULTS: In all cases, the plot of drug released against time produced a straight line.The drug release from the tablet made by dry method was faster than wet method. The ATMP release rate was decreased with decreasing the particle size of HPMC and increasing the tablet size. The effect of HPMC viscosity and the alcohol content were not significant.There were different influence in different ranges of tablet hardness. Hydrophilic additives of starch, PVP, MCC could slow the ATMP release but the changes of their amount in this test range insignificantly affected the drug release. The ATMP release rate increased sharply when EC content was 80mg per tablet. CONCLUSION: The amount and particle size of HPMC,preparation method, tablet size as well as the additives are the main factors influencing ATMP release from HPMC extended matrix tablet.