液固压缩技术速释茯苓皮总三萜片中松苓新酸和去氢依布里酸的机制探索

Investigation of Immediate-release Mechanism of Dehydrotrametenolic Acid and Dehydroeburicoic Acid in Poriae Cutis Total Triterpenoids Tablets Based on Liquid-solid Compacts Technique

目的:探讨液固压缩技术速释茯苓皮总三萜片中松苓新酸和去氢依布里酸的机制。方法:以松苓新酸和去氢依布里酸为指标成分,比较茯苓皮总三萜液固压缩片与原料药体外溶出度的差异,采用差示扫描量热法(DSC)对茯苓皮总三萜原料药、液固压缩片粉末和液固压缩片辅料混合粉末进行物相表征。结果:液固压缩技术可显著提高松苓新酸和去氢依布里酸的溶出速率。茯苓皮总三萜液固压缩片中松苓新酸和去氢依布里酸在120 min时的总溶出度92%,t50(溶出总浓度50%所需时间)和tD(溶出总浓度63.2%所需时间)分别为11.18,22.71 min;总三萜原料中松苓新酸和去氢依布里酸的总溶出度29%,t50和tD分别为231.06,359.23 min。DSC分析显示辅料对茯苓皮总三萜不存在相互作用,液固压缩片粉末的DSC曲线上,主药吸收峰完全消失,说明药物在液固粉末中是以非晶型形式存在。结论:液固压缩技术可改善茯苓皮总三萜的溶出度,使难溶性药物快速释药。

Objective： To investigate the mechanism of improving dissolution of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets by liquid-solid compacts technique. Method： Taking dissolution of dehydrotrametenolic acid and dehydroeburicoic acid as indexes, difference of dissolution between liquid-solid compressed tablets and crude drug of total triterpenoids in Poriae Cutis was compared, crude drug, liquid-solid compacts tablets powder and excipients were characterized by differential scanning calorimetry （DSC）. Result： Liquid-solid compacts technique could significantly improve dissolution of dehydrotrametenolic acid and dehydroeburicoic acid. Total dissolution of these two ingredients in liquid-solid compressed tablets was 92% at 120 min, total dissolution of them in crude drug was 29% at 120 min. DSC showed that characteristic peaks of drug in liquid-solid tablets had vanished, and suggested that drugs may be present in liquid-solid compressed tablets as amorphous substance. Conclusion： Liquid-solid compacts technique can increase dissolution of total triterpenoids in Poriae Cutis and allow rapid release of poorly soluble drugs.