左氧氟沙星的体内构型转化与同步一阶导数荧光光谱测定的研究

Transformation of S-(+)-Ofloxacin Enantiomer in Human Body and Determination by Synchronous-derivative Fluorimetry

控制 pH =3 ,用同步一阶导数荧光光谱技术能很好识别和分辨氧氟沙星消旋体的R和S对映体 ,据此建立了两种旋光体同时测定的同步导数荧光光谱法。测定尿样中的对映体含量 ,线性范围为 :0 3 6～ 2 16μg·mL-1(R) ,0 3 6～ 2 89μg·mL-1(S)和 3 16～ 3 1 6μg·mL-1(S) ,检测下限 0 3 6μg·mL-1,回收率 95 %～10 4 % ,相对标准偏差 <6 6%。发现在体内S对映体向R对映体的转化。考察了S对映体的药代动力学行为 ,并测定了转化率。

At pH 3, S, R enantioners of ofloxacin can be well recognized by the synchronous-first derivative fluorimetry. Based on this, a new method for the recognition and determination of enantiomers of ofloxacin, the synchronous-first order dervative fluorimetry has been developed. The linear range is 0.36-2.16 mug.mL(-1)(R), 0.36-2.89 mug-mL(-1) (S), and 3.16-31.6 mug.mL(-1) (S). The detection limit is 0.36 mug.mL(-1), RSD is less than 6.6% and the recovery is within the range of 97%-104%. The transformation of S to R- ( +)-ofloxacin enantiomer in human body is fourded. In 0-3 h after taking ofloxacin tablets by a healthy subject, R-enantiomer can not be detected. At the 6th hour, remarkable amount of R-enantiomer was detected, and then R-/S-enantiomer ratio increased rapidly to 21.3% at the 24th hour for 2.1% at the 6th hour.