盐酸二甲双胍缓释片的实验研究

目的：研制具双重控释系统的盐酸二甲双胍缓释片,探讨其片芯和包衣的优化处方及释放机制。方法：以氢化蓖麻油作为蜡质控释材料制备片芯,采用丙烯酸树脂作为半渗透性控释包衣材料,制备具双重控释系统的盐酸二甲双胍缓释片。分别以外观、硬度、流动性、可压性及释放度作为考察指标,对片芯和包衣处方进行优化筛选。结果：所制缓释片的体外释放度不受释放介质和转速影响。处方9片芯表面光滑,硬度、流动性和可压性均较好,0．5、1和3小时的释放度分别为40．2％、56．8％和85．7％;处方5包衣可致片剂在5和8小时的释放度分别达50％和80％。本品可稳定释放达12小时,释放行为符合一级速度方程。结论：本品处方工艺可操作性强,释药持续稳定。

An Experimental Study on Sustained-release Tablets of Metformin Hydrochloride

Objective:To research and develop sustained-release tablets of metformin hydrochloride with a "dual controlled release" system and to investigate the optimization of tablet core and coating formulations and their releasing mechanism. Methods:Using hydrogenated castor oil as a controlled release waxy material for the core and Eudragit NE30D as a controlled release material for the semipermeable coating,the target tablets were prepared.Based on the investigation into appearance,hardness,fluidity,tabletability and release rate of the tablets,the core and coating formulations were screened for optimization.Results:In vitro release rate of the tablets was not affected by release medium and revolution.The core prepared with formulation 9 was smooth,with good hardness,fluidity,tabletability and release rate(40.2%,56.8% and 85.7% respectively at 0.5, 1 and 3?h).The tablets coated with formulation 5 showed release rates of 50% and 80% respectively at 5 and 8?h.The target tablets could release steadily for 12?h and their release behavior agreed with first-order equation.Conclusion:The technical process for the target tablets,which showed a steady and sustained release,is easy to operate.