单硝酸异山梨酯缓释片分割后的体内外评价  

In vivo and in vitro evaluation of isosorbate mononitrate sustained release tablets after segmentation

作　　者：寻明金 郭辉 冯中 能婷 李文芳 张贵民 XUN Ming-jin;GUO Hui;FENG Zhong;NENG Ting;LI Wen-fang;ZHANG Gui-min(International Pharmaceutical Engineering Lab in Shandong,Shandong New Times Pharmaceutical Co.,Ltd.,Linyi Shandong 273400;National Engineering and Technology Research Center of Chirality Pharmaceutical,Lunan Pharmaceutics Group Co.,Ltd.,Linyi Shandong 276000)

机构地区：[1]山东新时代药业有限公司,山东省药物国际化工程实验室,山东临沂273400 [2]鲁南制药集团股份有限公司,国家手性制药工程技术研究中心,山东临沂276000

出　　处：《中南药学》2022年第11期2501-2505,共5页Central South Pharmacy

基　　金：“重大新药创制”科技重大专项(No.2018ZX09303-012)。

摘　　要：目的观察单硝酸异山梨酯缓释片整片和半片在体外溶出和体内药动学的情况。方法采用f_(2)相似因子法比较原研制剂及自制单硝酸异山梨酯缓释片整片和半片在4种溶出介质中溶出曲线的相似性。同时比较两者在比格犬体内的药动学特征。结果单硝酸异山梨酯缓释片整片和半片在体外的溶出行为相似,f_(2)均大于50%,且整片和半片在长期和加速条件下质量符合要求。单硝酸异山梨酯缓释片整片和半片在比格犬体内的药代动力学参数t_(max)和t_(1/2)差异无统计学意义,AUC半片大约是整片的一半。结论单硝酸异山梨酯缓释片整片和半片在体外溶出和体内的药代动力学情况相似且质量稳定。Objective To determine the in vitro dissolution and in vivo pharmacokinetics of the whole and half isosorbide mononitrate sustained release tablets.Methods f_(2) similarity factor method was used to compare the dissolution curves of the original preparation and isosorbide mononitrate sustained release tablets in 4 dissolution media.The pharmacokinetic characteristics in Beagles were compared.Results The in vitro dissolution behavior of the whole and half isosorbide mononitrate sustained release tablets was similar,and f_(2) was more than 50%.The quality of both whole and half tablets met the requirements under long term and accelerated conditions.There was no significant difference in the pharmacokinetic parameters t_(max) and t_(1/2) of the whole and half tablets in Beagles.The AUC of the half tablets was about half of that of the whole tablets.Conclusion The pharmacokinetics of whole and half isosorbide mononitrate sustained release tablets in vitro and in vivo are similar and the quality is stable.

关 键 词：单硝酸异山梨酯缓释片 整片 半片 体外溶出 药动学 

分 类 号：R96[医药卫生—药理学] R927.1[医药卫生—药学]