6种骨架材料对维拉帕米的缓释效果研究

目的:为维拉帕米选择不同的骨架材料制备缓释片提供参考。方法:分别以羟丙基甲基纤维素K100M、海藻酸钠420、乙基纤维素M70、复配辅料聚醋酸乙烯酯/聚乙烯吡咯烷酮混合物、硬脂酸、氢化蓖麻油为骨架材料,按《中国药典》盐酸维拉帕米缓释片项下对累积释放度的相应要求确定上述6种缓释骨架材料对应的载药量,制备盐酸维拉帕米缓释片;以蒸馏水为介质,桨法释放,紫外分光光度法在229 nm波长处测定6种缓释片12 h内的累积释放度。结果:6种缓释片的载药量分别为50%、50%、25%、50%、18%、37.5%,12 h的累积释放度分别为81.3%、89.3%、82.7%、88.1%、92.8%、83.5%。结论:6种骨架材料均有缓释作用,综合载药量和累积释放度考虑,海藻酸钠420作为维拉帕米的缓释骨架材料效果更为理想。

Study on 6 Kinds of Framework Materials on Sustained-release Effects of Verapamil

OBJECTIVE： To provide reference for the selection of different framework materials in the preparation of verapamil sustained-released tablet. METHODS： HPMC K100M, sodium alginate 420, ethyl cellulose M70, compound excipients polyvinyl acetate/polrvidone mixture, stearic acid and hydrogenated castor oil as framework material, the drug-loading amount of above 6 kinds of sustained-release framework material were determined according to the requirements of accumulative release of Verapamil hydrochloride sustained-release tablet stated in Chinese Pharmacopeia. The verapamil was released by paddle method using distilled water as medium. Accumulative release rate of 6 kinds of sustained-release tablets were determined by UV spectrophotometry in 229 nm within 12 h. RESULTS： The drug-loading amount of 6 kinds of sustained-release tablets were 50%, 50%, 25%, 50%, 18% and 37.5%, respectively; accumulative release rate at 12 h of them were 81.3%, 89.3%, 82.7%, 88.1%, 92.8% and 83.5%, respectively. CONCLUSIONS： 6 kinds of framework material all show the property of sustained-release effects. Sodium alginate 420 is the best for verapamil as framework material according to drug-loading amount and accumulative release rate.