Journal of Pharmaceutical Innovation ( IF 2.7 ) Pub Date : 2020-06-02 , DOI: 10.1007/s12247-020-09452-2 Timucin Ugurlu , Ezgi Ilhan
Purpose
A pulsatile drug delivery system containing dexketoprofen trometamol was designed by combining immediate release and colon-targeted mini tablets into a capsule.
Methods
Both immediate release and colon-targeted mini tablets were prepared by wet granulation. Furthermore, colon-targeted mini tablets were coated with Eudragit L 100, Eudragit S 100, Eudragit RS 30D, and ethylcellulose (Surelease®) using Wurster and pan coating methods.
Results
The optimum drug release of the system developed in the study was found to be mini tablets coated with 30% Eudragit S 100 on a 20% Surelease® subcoating for the purpose of colon targeting.
Conclusion
In the finished product, the immediate release part released the drug within the first hour, and less than 5% release was observed from the colon-targeted tablets in a 0.1 N HCl in 2 h. Then, less than 20% release occurred in the colon-targeted tablets up to 6 h in pH 6.8 phosphate buffer solution. The cumulative release rate reached 100% for up to 12 h. To our knowledge, it was the first time dexketoprofen trometamol was designed by combining both immediate release and colon-targeted mini tablets in a one dosage form.
中文翻译:
新型含有右旋酮洛芬的复方药物递送系统的开发和体外评估
目的
通过将速释和靶向结肠的微型片剂组合到胶囊中,设计了一种含有右酮洛芬曲美他莫的搏动药物递送系统。
方法
通过湿法制粒制备速释和靶向结肠的小型片剂。此外,使用Wurster和平底锅包衣方法用Eudragit L 100,Eudragit S 100,Eudragit RS 30D和乙基纤维素(Surelease?)包被靶向结肠的小片剂。
结果
研究中发现,该系统开发的最佳药物释放是为结肠靶向而在20%Surelease®包衣衣上涂有30%Eudragit S 100的迷你片剂。
结论
在最终产品中,速释部分在第一小时内释放了药物,在2小时内在0.1 N HCl中从结肠靶向片剂观察到的释放少于5%。然后,在pH 6.8磷酸盐缓冲溶液中长达6小时的结肠靶向片剂中发生的释放少于20%。长达12小时的累积释放率达到100%。据我们所知,这是首次将速释和结肠靶向小片剂以一种剂型结合使用来设计右旋苯丙胺曲美他莫。