盐酸维拉帕米脉冲控释片的研究  

STUDIES ON PULSED RELEASE TABLET OF VERAPAMIL HYDROCHLORIDE

作　　者：邹豪[1] 马伯良[2] 郭涛[3] 蒋雪涛[1] 

机构地区：[1]第二军医大学药学院,上海200433 [2]吉林空军医院,吉林132011 [3]沈阳军区总医院,沈阳110015

出　　处：《药学学报》1999年第11期862-867,共6页Acta Pharmaceutica Sinica

摘　　要：目的：制备适于临睡前服用、间隔４ ｈ 后于次日凌晨释放出治疗药物的脉冲控释片。方法：以均匀设计优化盐酸维拉帕米压制包衣片的处方组成，体外溶出度测定、体内γ闪烁扫描示踪考察药物释放滞后时间（ Ｔｌａｇ） ，在家犬、人体内的药代动力学研究，考察脉冲控释片在体内控时效果。结果：均匀设计得出的多元线性回归方程优化筛选了控时３，４ ，５ ｈ 的脉冲片处方，体外脉冲控时４ ｈ 的ＩＶ 型脉冲片，在家犬体内和体外控时３ ｈ 的ＩＩＩ型脉冲片在受试者体内均实现给药后４ ｈ 脉冲释放。结论：脉冲控释片仅改变了制剂的释药开始时间，而对药物的峰浓度、生物利用度等无影响，实现设计中的脉冲释放，为防治高血压的凌晨发作提供了良好的剂型选择。AIM: To prepare an orally applicable pulsed release tablet, (PRT), which allows for rapid drug release after a predetermined lag time of 4 h. METHODS: Uniformed design was used to optimize the composition of the outer shell of dry coated tablet. γ Scintigraphic evaluation and pharmacokinetic studies in dogs and humans were used to establish methodology capable of showing the subsequent in vivo performance of the pulsed release tablet. RESULTS: Multiple regression results can be used to design various pulsed release tablets with lag times of 3, 4 and 5 h. The result of the in vivo study suggested that formulation III in humans and formulation IV in dogs could be released after a lag time of 4 h. CONCLUSION: Pulsed release tablet prepared in the experiment only changed the time of pulsed release while C max , AUC etc were not different from those of core tablet. The new system was useful to reduce the early morning symptoms of ischemic heart disease.

关 键 词：盐酸维拉帕米 脉冲控释片 定时给药系统 

分 类 号：R972[医药卫生—药品]