阿奇霉素缓释干混悬剂释放度测定及Beagle犬体内外相关性评价

Release of azithromycin extended release for oral suspension and evaluation of in vitro-in vivo correlation in beagle dogs

目的进行阿奇霉素缓释干混悬剂体外释放度的测定及比格犬体内外相关性评价。方法按2010版中国药典释放度测定法测定阿奇霉素缓释干混悬剂体外释放度,用液相色谱-串联质谱(LC/MS/MS)法测定阿奇霉素在比格犬体内的血药浓度,并用WinNonlin Professional v5.2进行数据处理。结果以体内吸收分数(fa)对体外累积释放度(F)进行线性回归,得方程fa=1.1553F-52.931(r=0.9475)。结论体内吸收分数与体外累积释放度具有良好的相关性,阿奇霉素缓释干混悬剂所采用的释放度测定方法合理,可以较好反映体内吸收情况。

Objective To study the release of azithromycin extended release for oral suspension and to evaluate the correlation between in vitro and in vivo in Beagle dogs.Methods Release test method in azithromycin extended release for oral suspension adopted by ChP was used for determination of release in vitro.The concentrations of azithromycin in Beagle plasma were determined by LC/MS/MS.Results The linear equation based on the accumulation（F） and absorption percentage（fa）was fa=1.1553F-52.931 and the correlation coefficient was 0.9475.Conclusion To a certain extent,the vitro release test in ChP could reflect the vivo absorption.