美沙拉嗪肠溶缓释片的制备与体外释放度考察  

Preparation and in vitro release of Mesalamine Delayed-release Tablets

作　　者：赵世娟 严家瑞 史婷 严真 尹莉芳 ZHAO Shijuan;YAN Jiarui;SHI Ting;YAN Zhen;YIN Lifang(Department of Pharmaceutics,School of Pharmacy,Engineering Research Center for Development and Evaluation of Sustained-Release Intelligent Preparations and Key Functional Excipients of Jiangsu Province,China Pharmaceutical University,Nanjing 210009,China)

机构地区：[1]中国药科大学药学院药剂系,江苏省缓释智能制剂及关键功能性辅料开发与评价工程研究中心,江苏南京210009

出　　处：《药学研究》2021年第7期452-457,共6页Journal of Pharmaceutical Research

基　　金：国家科技重大专项“重大新药创制”项目(No.2017ZX09101001-004)。

摘　　要：目的制备美沙拉嗪肠溶缓释片,考察其体外释放。方法以体外释放相似因子(f_(2))为主要评价指标,通过单因素处方筛选和正交试验设计得到最优处方,重现3批,比较自制美沙拉嗪肠溶缓释片与参比制剂的体外释放行为。结果片芯中羧甲基纤维素钠(CMC 7HXF PH)用量为45 mg,羧甲淀粉钠(CMSNa)用量为35 mg;肠溶包衣层中Eudragit L100和Eudragit S100以2∶3的比例联用,包衣增重为6%。自制肠溶缓释片与参比制剂的相似因子f 2值均大于50。结论自制美沙拉嗪肠溶缓释片与参比制剂体外释放相似,处方工艺稳定可重现,可用于美沙拉嗪肠溶缓释片的制备。Objective To prepare Mesalamine Delayed-release Tablets and investigate the in vitro release behaviors.Methods With the similarity factor(f_(2))in vitro release as the evaluation index,the optimal formulation was determined by single factor experiments and orthogonal experiments.Three batches of mesalamine delayed-release tablets were reproduced and compared with the reference listed drug.Results The amount of sodium carboxymethylcellulose(CMC 7HXF PH)was 45 mg and the amount of sodium starch glycolate(CMSNa)was 35 mg in the tablet core.The ratio of Eudragit L100 to Eudragit S100 was 2∶3 and the coating weight gain was 6%in the enteric coating shell.The f 2 values were all greater than 50.Conclusion The release behaviors of the self-made Mesalamine Delayed-release Tablets and the reference listed drug were similar.The formulation and preparation process were stable and reproducible,which can be applied to prepare Mesalamine Delayed-release Tablets.

关 键 词：美沙拉嗪 缓释片 肠溶包衣 体外释放 

分 类 号：R943[医药卫生—药剂学]