拉莫三嗪缓释片的制备及体外释放行为考察  

Preparation of Lamotrigine Sustained-release Tablets and Study on the in vitro Release Behavior

作　　者：朱宣羽 张燕 丁子莹 操锋 

机构地区：[1]中国药科大学药学院药剂系,南京211198 [2]国家食品药品监督管理总局药品评审中心,北京100089

出　　处：《中国药房》2017年第34期4872-4875,共4页China Pharmacy

摘　　要：目的:改进原研制备工艺,仿制拉莫三嗪缓释片,并考察其体外释放行为。方法:采用羟丙基甲基纤维素(HPMC)E4M CR和HPMC K100LV CR制备缓释骨架片芯,以尤特奇~?L30D-55为肠溶材料包衣,制备拉莫三嗪缓释片。以与原研制剂体外释放度的相似因子f_2为指标,采用单因素法筛选处方中乳糖用量、HPMC E4M CR和HPMC K100LV CR质量比、HPMC用量及包衣增质量。结果:片芯处方为拉莫三嗪50 mg、HPMC K100LV CR 40 mg、HPMC E4M CR 61.4 mg、乳糖128 mg,最佳包衣增质量为3%。自制制剂和原研制剂在含0.5%十二烷基硫酸钠的pH 6.8磷酸盐缓冲液、pH 4.5乙酸-乙酸钠缓冲液和水中的体外释放行为均相似。结论:成功仿制了拉莫三嗪缓释片,且工艺比原研制剂更加简单、易行。OBJECTIVE：To improve the original preparation technology,imitate Lamotrigine sustained-release tablets,and study its in vitro release behavior. METHODS：Hydroxypropylmethylcellulose（HPMC） E4M CR and HPMC K100 LV CR were used to prepare the sustained-release matrix core. Using Eudragit~？ L30 D-55 as enteric coating material,Lamotrigine sustained-release tablets were prepared. Using the similar factor f_2 of in vitro release rate of original preparation as index,single factor was used to screen the amount of lactose,mass ratio of HPMC E4M CR and HPMC K100 LV CR,amount of HPMC and weight of coating layer in the formulation. RESULTS：The formulation of matrix core was as follow as lamotrigine 50 mg,HPMC K100 LV CR 40 mg,HPMC E4M CR 61.4 mg,lactose 128 mg,and the optimal weight of coating layer of 3%. The in vitro release of self-made and original preparations were similar in pH 6.8 phosphate buffer containing 0.5% sodium dodecyl sulfate,pH 4.5 acetic acid sodium acetate buffer and water. CONCLUSIONS：Lamotrigine sustained-release tablets are successfully imitated,and the technology is more simple and feasible than original preparation.

关 键 词：拉莫三嗪 缓释片 肠溶包衣 体外释放 

分 类 号：R943[医药卫生—药剂学]