琥珀酸去甲文拉法辛缓释微丸的制备及释放特性的研究  

Preparation and release behavior of the Sustained-release desvenlafaxine succinate pellets

作　　者：赵月[1] 邓菲[1] 张博[1] 汪忠军 邓黎[1] 贺英菊[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2017年第3期238-241,共4页West China Journal of Pharmaceutical Sciences

摘　　要：目的采用乙基纤维素水分散体(Surelease~)为包衣材料制备琥珀酸去甲文拉法辛(DVS)缓释微丸,并评价其体外释药性能。方法采用溶液上药法,在蔗糖空白丸芯的基础上旋转锅包衣法上药,通过正交筛选优化上药工艺,再以Surelease~为缓释材料进行包衣,以原研缓释片为参比对微丸的体外释放进行评价,并将释放数据用常用模型拟合,探讨其释放机制。结果所得缓释微丸的载药量和上药率均较高,含量均匀,当聚合物包衣增重32.4%时可达到与原研缓释片一致的释放特性,在pH1.2、pH4.5、水、pH6.8的释放介质中两者的相似因子分别为86.65、69.94、67.47、67.97,体外释放曲线符合一级方程。结论制备的DVS缓释微丸具有较理想的缓释效果。OBJECTIVE To prepare the Sustained -release desvenlafaxine succinate （DVS） pellets coated with the aqueous ethylcellulose dispersion（ Surelease ） and to investigate their drug release behavior. METHODS DVS was loaded onto sugar spheres using hydroalcoholic solution layering techniques. The formulation of drug - layering aquacoating material was optimized by Orthogonal test. DVS - layered pellets were coated by Surelease using coating pan technique. Sustained - release DVS pellets showed a release profile compared to the extended - release commercial product Pristiq tablets. A method for determination of the in vitro release was established and fitted by different curve -fitting equations. RESULTS The sustained -release DVS pellets showed high drug loading capacity, and the content was uniformly. The dissolution profile of the optimal product was similar compared to the commercial product, and the f2 factor in the four dissolution media was 86.65,69.94,67.47,67.97, respectively. First - order equation showed the best correlation with the release profile. CONCLUSION The DVS pellets have sustained -release effect.

关 键 词：琥珀酸去甲文拉法辛 乙基纤维素水分散体 缓释微丸 溶液上药法 锅包衣法 相似因子 释放机制 蔗糖空白丸芯 

分 类 号：R94[医药卫生—药剂学]