盐酸雷诺嗪缓释片的处方设计及体外释放

The formulation design and in vitro release of ranolazine hydrochloride sustained-release tablets

目的:制备盐酸雷诺嗪缓释片并对释药因素进行考察。方法:采用HPMC、EC和Eudragit RL100组成的混合型骨架材料制备了盐酸雷诺嗪缓释片,对影响释药的因素,如HPMC的黏度、制粒用乙醇的体积分数、片形、片重、压片压力、包衣、释放介质、转速等进行了考察,并在此基础上通过正交设计试验优选最佳处方和工艺。结果:盐酸雷诺嗪缓释片的体外释药行为符合Higuchi方程;制粒用乙醇的体积分数、片形、片重、压片压力、测定转速对RH缓释片的释放速率有明显影响;而HPMC的黏度、释放介质的pH值和包衣对药物的释放速率没有明显影响。结论:采用HPMC、EC和Eudragit RL100组成的混合型骨架材料,制备了日服2次的盐酸雷诺嗪缓释片。

ORJECTIVE To prepare the ranolazine hydrochloride sustained-release （RHSR） tablets and inspect the influencing factors of release. METHODS The RHSR tablets were prepared by using HPMC, EC and Eudragit as the mix matrix material. The the viscosity of HPMC; the alcohol content in adhesives; different tablet shape, weight and hardness; tablet coating; different dissolution medium and stirring rate were evaluated, respectively. Based on the studies of single factor experimentations, optimal formulation and technics were selected by orthogonal design test. RESULTS The release behavior of the RHSR tablets followed the Higuchi equation. The alcohol content in adhesives, tablet shape, weight and hardness, stirring rate had marked influence on the release rate of RHSR tablets markedly, while the viscosity of HPMC, the pH of dissolution medium and tablet coating had unconspicuous intluence on the release rate of RHSR tablets. CONCLUSION RHSR tablets of twice daily administration were developed by using HPMC, EC and Eudragit as the mix matrix material.