邹豪, 马伯良, 郭涛, 蒋雪涛. 盐酸维拉帕米脉冲控释片的研究J. 药学学报, 1999, 34(11): 862-867.
引用本文: 邹豪, 马伯良, 郭涛, 蒋雪涛. 盐酸维拉帕米脉冲控释片的研究J. 药学学报, 1999, 34(11): 862-867.
Zou Hao, Ma Boliang, Guo Tao , Jiang Xuetao, . STUDIES ON PULSED RELEASE TABLET OF VERAPAMIL HYDROCHLORIDEJ. Acta Pharmaceutica Sinica, 1999, 34(11): 862-867.
Citation: Zou Hao, Ma Boliang, Guo Tao , Jiang Xuetao, . STUDIES ON PULSED RELEASE TABLET OF VERAPAMIL HYDROCHLORIDEJ. Acta Pharmaceutica Sinica, 1999, 34(11): 862-867.

盐酸维拉帕米脉冲控释片的研究

STUDIES ON PULSED RELEASE TABLET OF VERAPAMIL HYDROCHLORIDE

  • 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。

     

    Abstract: 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 Cmax , 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.

     

/

返回文章
返回