盐酸美金刚缓释片的制备及其药物释放影响因素考察  

Preparation of memantine hydrochloride sustained release tablets and influence factors of drug release

作　　者：潘裕生 张金梁 崔梦锁 潘卫三[2] PAN Yu-sheng;ZHANG Jin-liang;CUI Meng-suo;PAN Wei-san(Lepu Pharmaceutical Technology Co.,Ltd,Taizhou Zhejiang 318000;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016)

机构地区：[1]乐普制药科技有限公司,浙江台州318000 [2]沈阳药科大学药学院,沈阳110016

出　　处：《中南药学》2020年第9期1449-1454,共6页Central South Pharmacy

基　　金：释药技术与药代动力学国家重点实验室开放课题(No.2012CB724000)。

摘　　要：目的制备盐酸美金刚骨架缓释片,考察影响药物体外释放行为的因素,并探索片剂在Beagle犬体内的药动学。方法采用单因素实验确定药物释放的影响因素,以自制片与市售片体外释放数据的相似因子作为评价指标,采用正交设计优选出盐酸美金刚缓释片的最佳处方组成。结果HPMC K100M、HPMC E50、PEG 4000用量及包衣增重对药物释放有显著影响,自制盐酸美金刚缓释片剂在12 h内呈现缓慢平稳的释放特征,符合零级释放模型。自制盐酸美金刚缓释片与参比制剂在Beagle犬体内血药浓度-时间曲线相似,相对生物利用度为94.92%,具有生物等效性。结论自制盐酸美金刚缓释片具有稳定的体外释放特征和良好的体内药动学特征。Objective To prepare memantine hydrochloride sustained release tablets and determine the factors affecting the drug release behaviors in vitro,and to explore the pharmacokinetics of the tablets in Beagle dogs.Methods We used single factor experiments to determine the factors that influenced the drug release.The similar factors of in vitro release data of self-made tablets and commercially available tablets were used as evaluation indexes to optimize the formulation of memantine hydrochloride sustained release tablets by orthogonal design.Results The amount of HPMC K100M,HPMC E50,PEG 4000 and the weight gain of the coating had a significant effect on the drug.The self-made sustained release tablets of memantine hydrochloride were released slowly and stably within 12 hours,which was consistent with the zero-order release model.The self-made sustained release preparation of memantine hydrochloride and the reference preparation were bioequivalent with similar blood concentration-time curve in Beagle dogs,and the relative bioavailability was 94.92%.Conclusion The self-made memantine hydrochloride sustained release tablets are stably released in vitro and show good pharmacokinetic characteristics in vivo.

关 键 词：盐酸美金刚 凝胶骨架缓释片 正交设计 体外释放 药动学 

分 类 号：R94[医药卫生—药剂学]