阿奇霉素泡囊体外释放与体内吸收的相关性

目的 评价阿奇霉素泡囊的体外释放和体内吸收之间的相关性。方法 采用激光粒度仪测定阿奇霉素泡囊的粒径和zeta电位。建立UV法进行体外分析测定其体外释放度，高效液相色谱法进行体内分析测定大鼠口服后的血药浓度，然后分别以Loo-Riegelman法和反卷积分法计算体内吸收分数Fa和输入函数R。结果 阿奇霉素泡囊的粒径为（907.4±0.10）nm，zeta电位为（14.6 ± 0.02）mV。其体内阿奇霉素与内标峰面积之比（A）和阿奇霉素浓度（C）标准曲线回归方程为：A= 19.26C-52.69，r=0.999 0（n=3）；体外482 nm波长处光密度（D）与浓度（C）标准曲线回归方程为：D=0.014 4C-0.070 1，r=0.999 6（n=3），回收率均符合要求。以体外累计释放度Y与Fa和R建立的回归方程分别为：Fa=0.981 8Y + 1.083 1，r=0.956 5、R=0.763 5Y-15.699，r=0.862 7。结论 阿奇霉素泡囊体外释放与体内吸收之间没有相关性。

Correlation of azithromycin niosomes in vitro release with in vivo absorption

Objective To study the correlation of azithromycin niosomes (AN) in vitro release with its in vivo absorption. Methods Laser particle size analyzer was used to measure the particle size and zeta potential of AN. An UV method was established to analyze the in vitro release of AN; HPLC method was used to determine the plasma concentration of azithromycin after a single oral dose of drugs in rats. Then Loo-Riegelman and deconvolution method were used to calculate the absorption fraction (Fa) and input function (R). Results The AN size was (907.4 ± 0.10) nm and its zeta potential was (14.6 ± 0.02) mV. The regression equation of peak area ratio of AN to internal standard (A) and the concentration of azithromycin (C) was: A= 19.26C-52.69, r=0.999 0 (n=3); the in vitro regression equation determined at 482 nm was: D= 0.014 4C-0.070 1, r=0.999 6 (n=3); and the recoveries all met the requirements. If Y was cumulative in vitro release and Fa was the absorption percentage, the regression equation was: Fa=0.981 8Y + 1.083 1, r=0.956 5; if Y was the cumulative in vitro release and R was the input function, the regression equation was: R=0.763 5Y-15.69 9,r=0.862 7. Conclusion There is no correlation between azithromycin in vitro release with its in vivo absorption.