帕利哌酮缓释片的制备及其体外释放度评价  

Preparation and in vitro Release of Paliperidone Sustained-release Tablets

作　　者：曹悦[1,2] 马莉 张庭 崔京浩[1] 曹青日[1] 

机构地区：[1]苏州大学药学院,江苏苏州215123 [2]北京卫生职业学院,北京100053 [3]万特制药(海南)有限公司,海南海口570314

出　　处：《中国医药工业杂志》2016年第11期1418-1422,共5页Chinese Journal of Pharmaceuticals

摘　　要：采用湿法制粒制备片芯，再包缓释衣层得到帕利哌酮缓释包衣片。以pH1．0盐酸中自制缓释片与原研制剂（Invega ）释放曲线的相似度为指标，优化了片芯的骨架材料和pH调节剂种类、缓释包衣层组分和包衣增重。结果确定的优化处方为：片芯中羟丙甲纤维素E6与K100的比例为2：1、加入磷酸二氢钠为pH调节剂，缓释衣层中缓释材料Kollicoat SR 30D与致孔剂Kollicoat IR比为85：15（固体物料质量比）、包衣增重为6％。在pH1．0盐酸、pH4．0乙酸盐缓冲液、pH6．8磷酸盐缓冲液和水中，优化的自制缓释片与原研制剂（Invega ）释放曲线相似因子分别为60、59、61和67。可见，二者的体外释放行为基本相似。The tablet cores loaded with paliperidone were prepared with wet granulation, then coated with a sustained-release layer to obtain the title tablets. The matrix materials and pH modifiers of the tablet cores, formulation composition and weight gain of sustained-release coating layer were optimized with the release similarity between the self-made tablets and the reference listed drug （RLD） product （Invega ） as the index. The results showed that the optimal formulation was as follows： the matrix materials of the cores were hypromellose （HPMC） E6 and K100 in a weight ratio of 2 ： 1, sodium dihydrogen phosphate was added into the cores as the pH modifier, the prepared tablet cores were coated with Kollicoat SR 30D sustained-release layer with Kollicoat IR as a pore-forming agent in a weight ratio of 85 ： 15 and weight gain of 6%. In pH 1.0 hydrochloric acid solution, pH 4.0 acetate buffer, pH 6.8 phosphate buffer and water, the calculated similarity factor ） values were 60, 59, 61 and 67, which indicated that the release profiles between the optimal self-made tablets and RLD product were similar.

关 键 词：帕利哌酮 缓释片 释放度 相似因子 相似度评价 

分 类 号：R944.4[医药卫生—药剂学]