摘要
目的制备有机酸诱导型酒石酸美托洛尔延迟缓释片,研究影响药物释放的主要因素。方法采用湿法制粒法制备含药片芯,在片芯中加入有机酸,片芯外依次包裹Opadry?II隔离层和Eudragit RS30D时滞层薄膜衣,通过有机酸与Eudragit RS30D发生离子交换,增大膜的通透性来制备延迟缓释片。考察了有机酸的含量和种类、时滞层包衣增重、释放介质和桨的转速等因素对药物释放的影响,并根据实验结果分析药物释放原理。结果使用不同种类不同含量的有机酸可以得到时滞时间和释药速率不同的延迟缓释制剂,当片芯中酒石酸含量为15%(w/w),时滞层包衣增重为6%(w/w)时,延迟缓释片的时滞时间(释放10%的药物所需时间)约为6 h,而8、12、16 h的释放度分别为20%~35%、50%~70%、≥75%,符合睡前服药、白天缓慢释药,并且覆盖高血压发作的两个高峰期的要求。结论通过改变有机酸的含量、种类和时滞层包衣增重可以得到适合于治疗高血压的延迟释药制剂。
Objective To prepare organic acid-induced type delayed-onset sustained-release metoprolol tartrate tablets and to investigate the main factors affecting the in vitro release. Methods Wet granulation compression method was used to prepare tablet core with different amount of organic acid, then the tablet cores were coated with Opadry?II as the inner coating layer and Eudragit RS30 D as the outer coating layer. Delayed release effect was based on increased membrane permeability by ion exchange between organic acid and Eudragit RS30 D. The factors including organic species, content of tartaric acid, coating levels of Eudragit RS30 D, media and rotation speed, which influence the release behavior, were studied. Explore the mechanism of 'organic acid-induced type drug delivery system' from the analysis of the results. Results Multiple lag time and drug release rates were achieved using different amounts of organic acid and different kinds of organic acids. The results of the in vitro drug release tests suggest that after the lag time(time to release 10% of the drug required) of 6 h, the amounts of drug release was more than 75% within 16 h when the weight gain of time-lag layer was 6%. Conclusion Delayed-release dosage forms that suitable for the treatment of high blood pressure can be obtained by the adjustment of amounts of organic acid, kinds of organic acids and coating levels of time-lag layer.
出处
《中国药剂学杂志（网络版）》
2014年第6期185-192,共8页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
延迟缓释
有机酸诱导
酒石酸美托洛尔
体外释药
pharmaceutics
delayed-onset sustained-release
organic acid-induce
metoprolol tartrate
in vitro drug release
