高效液相色谱法测定人血浆和脑脊液中左氟沙星浓度及药代动力学研究  

DETERMINATION OF LEVOFLOXACIN IN PLASMA AND CEREBROSPINAL FLUID WITH HPLC AND ITS PHARMACOKINETICS IN PATIENTS UNDERGOING NEUROSURGICAL OPERATIONS

作　　者：罗顺德[1] 雷嘉川[1] 张如鸿[1] 蔡鸿生 李荣凌[1] 

机构地区：[1]湖北医科大学附一医院临床药理研究室

出　　处：《药学学报》1998年第12期937-940,共4页Acta Pharmaceutica Sinica

摘　　要：目的旨在测定左氟沙星药代动力学。用ＲＰＨＰＬＣ法，以环丙沙星为内标，反相Ｃ１８为分析柱，１０ｍｍｏｌ·Ｌ－１磷酸二氢钾—１０ｍｍｏｌ·Ｌ－１溴化四丁铵—乙腈（４５∶４５∶１０）为流动相，磷酸调至ｐＨ３０，检测波长２９５ｎｍ，测定血浆和脑脊液中左氟沙星浓度，平均回收率分别为７４７６％和８２４３％，日内日间误差小于５％，最低检测浓度血浆１０μｇ·Ｌ－１，脑脊液６μｇ·Ｌ－１。１０名开颅手术病人单次口服左氟沙星片３００ｍｇ的血液和脑脊液药代动力学特征均符合开放性一室模型。A RP HPLC method was developed to determine the concentrations of levofloxacin in plasma and cerebrospinal fluid and its pharmacokinetics were studied in patients undergoing neurosurgical operations. C 18 H 37 column was eluted with the mobile phase consisting of 10 mmol·L -1 KH 2PO 4-10 mmol·L -1 (C 4H 9) 4Br-CH 3CN(45∶45∶10, pH 3 0) and the utraviolet absorbance was monitored at 295 nm. Ciprofloxacin was used as internal standard. The mean recoveries were 74 76% in plasma and 82 43% in cerebrospinal fluid, with the lowest detectable limits of 10 μg·L -1 and 6 μg·L -1 , respectively. The RSD for the intra day and inter day were all less than 5%. A single oral administration of 300 mg levofloxacin tablet was given to 10 patients undergoing neurosurgical operations. The pharmacokinetic parameters in blood and in cerebrospinal fluid could be described by one compartment open model. The pharmacokinetic parameters were: blood K e 0 12±0 04 h -1 , T 1/2 6 05±1 68 h, T max 1 05±0 29 h, C max 3 67±0 42 mg·L -1 , AUC 33 43±7 32 mg·h·L -1 , CL s 9 46±2 53 L·h -1 , V d 77 49±7 39 L; cerebrospinal fluid K e 0 11±0 04 h -1 , T 1/2 6 95±1 88 h, T max 3 56±1 24 h, C max 1 68±0 25 mg·L -1 , AUC 23 70±5 62 mg·h·L -1 , CL s 13 70±5 11 L·h -1 , V d 126 61±13 20 L.

关 键 词：高效液相色谱法 左氟沙星 药代动力学 

分 类 号：R978.19[医药卫生—药品] R927.2[医药卫生—药学]