右美沙芬树脂口服缓释混悬液的制备及其释药特性研究

Preparation of dextromethorphan oral sustained-release suspensions by ion exchange resin and the in-vitro release kinetics

目的:制备右美沙芬树脂口服缓释混悬液,并考察其释药特性。方法:采用离子交换树脂为载体制备含药树脂微粒,用流化床进行包衣,并通过处方优化制备右美沙芬树脂口服缓释混悬液。对含药树脂微粒、含药树脂包衣微粒及含药树脂缓释混悬液进行释药特性研究。结果:含药树脂微粒的释放度随着释放介质离子强度的增加而增大,其释药动力学过程可用Viswanathan方程表征;采用含药树脂包衣微粒制备的右美沙芬树脂口服缓释混悬液的物理稳定性良好,其释药动力学过程符合Higuchi模型。结论:采用离子交换树脂为药物载体,并对该含药树脂微粒进行流化床包衣,可以制备符合Higuchi模型释药的右美沙芬树脂口服缓释混悬液。

Objective：To prepare the dextromethorphan oral sustained-release suspensions and study the in-vitro release kinetics. Methods： The dextromethorphan oral sustained-release suspensions were prepared using ion exchange resin as a carrier, and followed by coating with ethylcellulose using the Wurster fluid bed process. The coated dextromethorphan resinate beads were dispersed in an aqueous suspending vehicle to obtain the dextromethorphan oral sustained-release suspensions. The release kinetics of the dextromethorphan resinate beads, the coated dextromethorphan resinate beads and the oral sustainedrelease suspensions were investigated, respectively. Results：The release rate of the drug from the resinate beads was increased with the rise of ionic strength in media, and the in-vitro release kinetics conformed to Viswanathan equation. The oral sustained-release suspensions containing the coated dextromethorphan resinate beads were physically stable, and the in-vitro release profiles met Higuchi equation. Conclusion：The results indicated that the dextromethorphan sustain-rlelase suspensions made by using ion exchange resin as a carrier and subsequent fluidized bed coating might be achieved, and in-vitro release kinetics could be defined by Higuchi model.