左金胃黏附片的制备与体外释放度研究

Study on Preparation and Release in vitro of Zuojin Gastric-mucoadhesive Tablets

目的：制备左金胃黏附片并评价其体外释药性能。方法：以羟丙基甲基纤维素K15M（HPMC-K15M）、卡波姆934P、HPMC-E50为生物黏附剂和骨架材料,以碱式碳酸镁（发泡材料）、95%乙醇溶液（黏合剂）、微粉硅胶（助流剂、润滑剂）为辅料制备左金胃黏附片。以2、6、10 h黄连总生物碱累积释放度（Q2 h、Q6 h、Q10 h）为指标,采用正交设计试验对HPMC-K15M、卡波姆934P、HPMC-E50、碱式碳酸镁的用量进行优化,并进行验证。考察所制制剂与左金普通片的体外释药特性,并测定其体外黏附力。结果：最优处方为50片用量中含HPMC-K15M 0.7 g、卡波姆934P 0.2 g、HPMC-E50 3.5 g、碱式碳酸镁0.4 g;所制3批样品的Q2 h、Q6 h、Q10 h分别为24.32%、56.10%、77.04%;所制样品1-12 h的体外释药符合Ritger-Peppas方程。左金普通片和左金胃黏附片的Q2 h分别为80.46%、24.04%,Q12 h分别为92.15%、95.83%,胃黏附力分别为24.2、74.0 g/cm^2。结论：成功制得具有缓释作用和黏附性能的左金胃黏附片。

OBJECTIVE：To prepare Zuojin gastric-mucoadhesive tablets and evaluate their drug release properties in vitro.METHODS：Zuojin gastric-mucoadhesive tablets were prepared with hydroxypropyl methyl cellulose K15M（HPMC-K15M）,carbomer 934 P and HPMC-E50 as the bioadhesive and matrix materials,and basic magnesium carbonate（foaming material）,95% alcohol solution（adhesive）and aerosil（glidant and lubricant）as the adjuvants. With the accumulative release of total alkaloids from Coptis chinensis Franch. at 2,6 and 10 h（Q2 h,Q6 hand Q10 h）as the indexes,orthogonal design test was conducted to optimize the amounts of HPMC-K15 M,carbomer 934 P,HPMC-E50 and basic magnesium carbonate,and verification was carried out. Drug release properties in vitro of the preparation and Zuojin conventional tablets were observed and in vitro adhesion thereof determined.RESULTS：The optimal formulation was as follows as that for 50 tablets,HPMC-K15 M of 0.7 g,carbomer 934 P of 0.2 g,HPMC-E50 of 3.5 g and basic magnesium carbonate of 0.4 g. The Q2 h,Q6 hand Q10 hof three batches of prepared samples were24.32%,56.10% and 77.04% respectively. 1-12 h drug release in vitro of prepared samples was in conformity with Ritger-Peppas equation. The Q2 hof Zuojin conventional tablets and Zuojin gastric-mucoadhesive tablets were 80.46% and 24.04%,Q12 hthereof92.15% and 95.83% and gastric adhesion thereof 24.2 and 74.0 g/cm^2,respectively. CONCLUSIONS：Zuojin gastric-mucoadhesive tablets which have sustained-release effect and adhesive property have been prepared successfully.