己酮可可碱缓释片的制备及体外释放度考察

Studies on the preparation and release characteristics of pentoxifylline sustained-release tablets

目的制备己酮可可碱缓释片并对其体外释放度进行考察。方法以紫外-分光光度法为分析方法,采用相似因子法对己酮可可碱缓释片体外释放行为进行评价,并对优化处方的释药机制进行探讨。结果 KollidonSR用量、黏合剂种类、薄膜衣增加质量和释放介质的pH值对药物释放无明显影响,HPMC规格、用量和转速对药物释放有显著性影响,片剂合格范围内的硬度对药物释放几乎无影响,优化处方的释药过程为药物扩散和骨架溶蚀共同作用。结论单独应用HPMC K4M为骨架材料即可制备具有理想释药行为的己酮可可碱缓释片,其释放度符合《中华人民共和国药典》2010年版标准且与进口己酮可可碱缓释片(瑞潘通)相似。

Objective To prepare the sustained-release tablets of pentoxifylline and investigate the release profile in vitro of the sustained-release tablets. Methods UV-spectrophotometry w as employed as analytical approach. The similarity factor w as used to evaluate release profile of sustained-release tablets in vitro and the release mechanism of optimal prescription w as discussed. Results The quality studies on self-prepared sustained-release tablets show ed that the drug release w as not obviously influenced by the amount of KollidonSR,type of adhesive,coating w eight,and pH value of dissolution solution,but significantly affected by the specification and amount of HPMC and the rotation speed. Hardness of tablets in the qualified range had little effect on drug release. The mechanism of drug release in vitro w as confirmed as the combination result of drug diffusion and matrix erosion. Conclusions Pentoxifylline sustained-release tablets w ith satisfactory release behavior can be prepared by using HPMC K4M alone. The release profile in vitro of the pentoxifylline sustained-release tablets meets the standard of that in the Pharmacopoeia of the People＇s Republic of China and it is similar w ith Pentoxifylline-ratiopharmas400.