摘要
目的采用Wagner-Nelson法和反卷积分法评价阳离子阿奇霉素微类脂体(azithromycin cationic micron niosomes,ACMNS)的体外释放与体内吸收的相关性。方法采用动态膜透析法研究ACMNS的体外释放行为,高效液相色谱法测定大鼠单剂量灌胃ACMNS和阿奇霉素(AM)后的血药浓度,通过一室模型Wagner-Nelson法和反卷积分法评价ACMNS的体内外相关性。结果以体内吸收百分数Fa和输入函数R分别与体外累积释放率X建立的线性方程分别为:Fa=3.0524X-5.7709,r=0.8976、R=2.3413X-58.687,r=0.5217,r<r_((2,0.05))=0.9500(P<0.05)。结论ACMNS的体外释放与体内吸收之间没有相关性。
AimTo evaluate the correlation between in vitro release and in vivo absorption of azithromycin cationic micron niosomes(ACMNS)by Wagner Nelson method and deconvolution method.MethodsThein vitro release behavior of ACMNS was studied by dynamic membrane dialysis.After a single dose of intragastric administration with ACMNS and AM in rats,the AM concentrations in plasma were determined by high performance liquid chromatography(HPLC).Wagner Nelson and deconvolution method were used to reveal the in vitro/in vivo correlation.ResultsX used as cumulative in vitro release and Fa as the absorption percentage,the regression equation was established:Fa=30524X-57709,r=08976,and X used as cumulative in vitro release and R as input function,the regression equation was established:R=23413X-58687,r=05217.r<r(2,0.05)=09500(P<005).ConclusionThere is no correlation between in vitro release and in vivo absorption of ACMNS.
作者
曾梅
钟萌
冯悦
罗见春
张奇娆
张景勍
ZENG Mei;ZHONG Meng;FENG Yue;LUO Jian chun;ZHANG Qi rao;ZHANG Jing qing(Medicine Engineering Research Center, Chongqing Medical University, Chongqing400016, China;Dept of Pharmacy, Affiliated Hospital of Southwest Medical University, Luzhou Sichuan646099,China;Dept of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, Luzhou Sichuan646099,China)
出处
《中国药理学通报》
CAS
CSCD
北大核心
2017年第12期1713-1717,共5页
Chinese Pharmacological Bulletin
基金
重庆市基础与前沿研究计划重点项目(No cstc2015jcyj BX0027)
