兰索拉唑肠溶片体内外相关性研究 - 中国现代应用药学.pdf

兰索拉唑肠溶片体内外相关性研究 王丽瑶1 2 2, 3* 2 2 ，王永禄 ，李学明 ，孙小虎 ，冯沁心 (1.安徽农业大学生命科学学院，合肥 230036 ；2.南京工业大学药学院， 南京 211816 ；3.南京工业大学材料化学工程国家重点实验室，南京 210009) 摘要：目的 考察兰索拉唑肠溶片的体外释放与在beagle 犬体内吸收间的相关性。方法 利用紫外分光光度法测定肠溶 片体外释放度；利用高效液相色谱法测定beagle 犬口服给药后的体内血药浓度；以Wagner-Nelson 法计算其体内吸收分 数，考察体内吸收与体外释放的相关性。结果 兰索拉唑肠溶片的体内吸收分数fa 与体外释放速率ft 的关系为：fa = 0.812 2ft –9.874 6 ，r=0.956 8 。结论 兰索拉唑肠溶片的体外释放与在犬体内吸收相关性良好。 关键词：兰索拉唑肠溶片；释放度；体内外相关性 中图分类号：R943.43 ；R969.1 文献标志码：B 文章编号：1007-7693(2012)03-0239-04 Study on the Correlation between Dissolution in Vitro and Absorption in Vivo of Lansoprazole Enteric-coated Tablets WANG Liyao1 2 2,3* 2 2 , WANG Yonglu , LI Xueming , SUN Xiaohu , FENG Qinxin (1.College of Life Science, Anhui Agricultural University, Hefei 230036, China; 2.College of Pharmacy, Nanjing University of Technology, Nanjing 211816, China; 3.State Key Laboratory of Materials-oriented Chemical Engineering, Nanjing University of Technology, Nanjing 210009, China) ABSTRACT: OBJECTIVE To investigate the dissolution rate in vivo and bioavailability in beagle dogs of lansoprazole enteric-coated tablets, and to evaluate the correlations of the dissolution in vitro and absorption in vivo. METHODS The drug dissolution in vitro was measured by UV spectrophotometer. The plasma concentration in beagle dogs was measured by HPLC. The correlation of dissolution in vitro and bioavailability in vivo was studied by the Wagnner-Nelson method. RESULTS The relationship between the dissolution fraction ft and the absorption fraction fa was fa =0.8122ft –9.874 6, r=0.956 8. CONCLUSION The correlation between dissolution in vitro and absorption in vivo of lansoprazole enteric-coated tablets was good. KEY WORDS: lansoprazole enteric-coated tablet; dissolution; in vivo-i