反相高效液相色谱法检测小鼠血浆中FG020326方法的建立  

A method for determining the concentration of FG020326 in mice plasma by RP-HPLC

作　　者：戴春岭[1] 李苏[1] 梁永钜[1] 廖海[1] 邓文静[1] 闫琳[1] 符立梧[1] 

机构地区：[1]华南肿瘤学国家重点实验室

出　　处：《中国药理学通报》2007年第1期131-134,共4页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助课题(No30371659)

摘　　要：目的建立测定多药耐药（multidrug resistance，MDR）逆转剂FG020326在KM小鼠血浆中血药浓度的方法。方法将KM小鼠（20．0～25．1）g随机分组，每组6只，♀♂各半，尾静脉注射，给药量为30mg·kg^-1，分时取血、处理。采用反相色谱柱，应用外标法测定FG020326在KM小鼠血浆中的血药浓度。结果在所建立的方法学下，FG020326的保留时间为7．9min；标准曲线为·↑Y=0．0144X-0．0285（r=0．9998），在162．5～41600μg·L^-1血浆浓度范围内呈良好的线性关系，最低检测浓度40μg·L^-1（S／N=3）；在650、2600、20800μg·L^-1低、中、高3个浓度下的绝对回收率为68．66％～84．63％，相对回收率为92．58％～110．88％；日内及日间RSD均小于3．2％（n=5）。在室温及冷冻-解冻试验中，FG020326具有良好的稳定性，RSD分别小于1．3％和6．0％。尾静脉单次给药后，FG020326在体内过程符合二室模型，T1/2α为0．088h，T1/2β为5．33h，AUC0-∝。为14183h·μg·L^-1，Vd为0．37L。结论该方法快速、准确、简便，能够满足FG020326药代动力学研究要求。Aim To establish a method to determine the concentration of FG020326 in the plasma of KM mice by reverse phase high-performance liquid chromatography. Methods KM mice were used throughout the experiment and their body weights ranged from 20. 0 to 25. 1 g. All of them were distributed randomly to different test groups which each had 6 mice. FG020326 was administered at a dose of 30 mg · kg^-1 via tail vein. The external standard method was used for the quantitation of FG020326. Results Under the condition of HPLC, the retention time of FG020326 was 7. 9 min. The standard curve was ·↑Y = 0. 0144X - 0. 0285 （ r = 0. 9998 ） with a validated quantitation range of 162.5～4 1600μg · L^-1, and the lowest concentration of detection in mice plasma was 40μg · L^-1（ S/N = 3 ）. At the concentration of 650,2 600,20 800 μg · L^-1, absolute recovery rates were ranged from 68.66% to 84. 63% and relative recovery rates were ranged from 92.58% to 110. 88%. The RSD of the precision within-day and between-day were less than 3.2%. At ambient temperature and four freeze-thaw cycles, FG020326 was stable and the RSD was less than 1.3% and 6.0%, respectively. The concentration-time curve of FG020326 was well fitted to a two-compartment model. T1/2α and T1/2β were 0. 088 h and 5.33 h, respectively. AUC0→∞ was 14 183 h·μg·L^-1 and Vd was 0. 37 L. Conclusion The assay method is shown to be sensitive, suitable and accurate for determination of FG020326 in mice plasma.

关 键 词：FG020326 药代动力学 反相高效液相色谱 多药耐药 

分 类 号：R-332[医药卫生] R446.1