桂利嗪胃内滞留漂浮型缓释片的制备

Preparation of cinnarizine floating sustained-release tablets

目的:制备桂利嗪胃内滞留漂浮型缓释片,对影响药物释放的处方因素和工艺因素进行考察。方法:首先以微晶纤维素和枸橼酸为载体制备桂利嗪固体分散体,然后以羟丙甲基纤维素(Hydroxypropyl Methyl Cellulose,HPMC)、聚乙二醇6000(Polyethylene Glycol-6000,PEG6000)、十八醇为骨架材料,用单因素方法考察HPMC种类、用量、制片压力、片径等因素对释药速率的影响,然后通过正交设计确定最优处方,制备桂利嗪胃内滞留漂浮型缓释片。结果:成功制备了桂利嗪胃内滞留漂浮型缓释片;选用改良溶解法制备桂利嗪固体分散体,处方为桂利嗪、枸橼酸、微晶纤维素的质量比为1:1:3;选用HPMCK4M为桂利嗪胃内滞留型缓释片的骨架材料;确定了HPMC,PEG6000,十八醇的用量和粘合剂的浓度;确定了制片的压力和片径。结论:HPMC种类、用量,PEG6000和十八醇的用量对释药速率有显著影响;其他工艺因素对片剂的释放影响较小。

Objective：To prepare and characterize the cinnarizine floating sustained-release tablets.Methods：Solid dispersions were prepared with microcrystalline cellulose and citric acid as the carrier.The impact of the types of HPMC,dosage,and the film pressure,film track and other factors on drug release rate was measured using single-factor approach,and then the optimal prescription was obtained with the orthogonal design.Results：The floating sustained-release cinnarizine tablets were obtained successfully.The preparing method of solid dispersion improved cinnarizine dissolved preparation.The optimized prescription consisted of cinnarizine,citrate,microcrystalline cellulose mass with the ratio of 1：1：3.HPMC K4M was selected as the skeleton material.The concentrations of HPMC,PEG 6000,octadecanol and adhesive,the pressure and tablet diameter were measured.Conclusion：HPMC type,dosage,PEG 6000 and octadecanol usage have a more significant impact on the rate of drug release than other factors.