骨水泥链珠中莫西沙星体外洗提动力学研究

In vitro Elution Kinetics Study of Moxifloxacin in Bone Cement Beads

目的建立测定不同时间盐酸莫西沙星骨水泥链珠体外洗提液中莫西沙星含量的方法,研究其体外洗提动力学特征。方法采用高效液相色谱法,色谱柱为Inertsil ODS-3柱(4.6×150mm,5μm),流动相为1%三乙胺溶液(磷酸调节pH 3.8)-乙腈(83∶17),流速为1.0mL·min^-1,检测波长为296nm,柱温为40℃,进样量为10μL。结果盐酸莫西沙星在1~80μg·mL^-1范围内线性关系很好(r=1);精密度RSD<2.0%;加样回收率为98.75%~100.84%(RSD=1.21%,n=9)。盐酸莫西沙星骨水泥链珠中莫西沙星在336h内的释放总量为48mg,释放率26.7%,释放过程中T 1/2为118h,T max为24h,C max为32.92μg·mL^-1,AUC 0-t为3576μg/(mL·h),AUC 0-∞为4378μg/(mL·h),莫西沙星的体外洗提符合二室模型特征。结论该方法操作简便,重复性好,灵敏度高,可用于莫西沙星的体外测定。本研究可为盐酸莫西沙星骨水泥链珠的临床使用时长、用量及制备莫西沙星骨水泥链珠缓释制剂提供参考。

OBJECTIVE A method for determining the content of moxifloxacin in the eluate of moxifloxacin hydrochloride cement beads at different times was established.The in vitro elution kinetics was also studied.METHODS Using high performance liquid chromatography,the column was Inertsil ODS-3(4.6×150nm,5μm),and the mobile phase was 1%triethylamine solution(phosphoric acid adjusted pH 3.8)-acetonitrile(83∶17)at a flow rate of 1.0mL·min^-1,detection wavelength was 296nm,column temperature was 40℃,and injection volume was 10μL.RESULTS Moxifloxacin hydrochloride had a good linear relationship in the range of 1-80μg·mL^-1(r=1);precision RSD<2.0%;spiked recovery was 98.75%-100.84%(RSD=1.721%,n=9).The total release of moxifloxacin in the bone chain of moxifloxacin hydrochloride was 48mg in 336h,the release rate was 26.7%,T 1/2 was 118h during release,T max was 24h and C max was 32.92μg·mL^-1.AUC 0-t was 3576μg/(mL·h),AUC 0-∞was 4378μg/(mL·h),and the in vitro elution of moxifloxacin was consistentwith the characteristics of the two-compartment model.CONCLUSION The method is simple,reproducible and sensitive,and can be used for in vitro determination of moxifloxacin.This study can provide reference for the clinical use length and amount of moxifloxacin bone cement chain beads and the preparation of moxifloxacin sustained-release bone cement chain beads preparation.