HPLC法测定大鼠血浆中DX-11的质量浓度  

Determination of DX-11 in rat plasma by HPLC

作　　者：刘冬洁[1] 梁宁[1] 王林丽[1] 郑鑫[1] 侯晓虹[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2013年第3期192-196,共5页Journal of Shenyang Pharmaceutical University

基　　金："重大新药创制"创新药物研究开发项目(2009ZX09103-057)

摘　　要：目的建立测定大鼠血浆中DX-11[N(β榄香烯13基)色氨酸]质量浓度的HPLC方法,并应用该法研究DX-11在大鼠体内的药动学。方法色谱柱:Kromasil C18柱(250 mm×4.6 mm,5μm),流动相:甲醇体积分数为0.2%的甲酸水溶液(体积比为75∶25),流速:1.0 mL.min-1,检测波长:220 nm,己烯雌酚作为内标物。结果 DX-11线性:0.2～20.0 mg.L-1,回归方程:Y=1.869×10-1ρ+9.830×10-2(r=0.998 1),定量下限:0.2 mg.L-1,回收率:84.1%～88.9%,日内和日间精密度均不大于10.2%。18只大鼠分别灌胃给予低、中、高3个剂量DX 12后,血浆中DX-11的tmax分别为(1.4±0.2)、(1.8±0.7)、(1.3±0.3)h,ρmax分别为(2.3±0.3)、(3.5±0.6)、(6.4±3.0)mg.L-1,t1/2分别为(1.7±0.7)、(2.3±1.0)、(1.4±0.8)h,AUC(0-∞)分别为(5.4±1.8)、(10.6±1.8)、(21.0±13.1)mg.h.L-1。结论建立并验证的HPLC法适用于DX-11在大鼠体内的药动学研究。Objective To establish a high performance liquid chromatographic method for determining the concentration of DX- 11 . N- （fl-elemene- 13-yl） tryptophan ] in rat plasma. Methods The chromatographic sep- aration was performed on a Kromasil C18 column（250 mm x4.6 mm,5 μm） ,and a mobile phase consisted of methanol - 0. 2 % formic acid （ V： V = 75： 25 ） at a flow rate of 1.0 mL. min - 1. The detection wavelength was set at 220 rim, and the diethylstilbestrol was used as the internal standard. Results A good linearity was obtained from 0. 2 mg- L - 1 to 20.0 mg- L- 1 of DX-11 in rat plasma with a regressive equation of Y = 1. 869 x 10 -lp ＋9. 830 x 10 -2 （ r =0. 998 1 ）. The limit of detection was 0. 2 mg.L-land the recoveries were ranging from 84. 1% to 88.9%. The RSDs of intra- and inter-day were less than 10. 2%. The pharmacoki- netic parameters of DX-11 in rat plasma after i. g. administration of different doses of DX-12 to 18 healthy rats were as follows ： tmax = （1. 4 ±0. 2） ,（1. 8 ±0. 7） ,and（1.3 ±0.3） h,pmax = （2. 3 ±0. 3）, （3.5 ±0. 6）, and（6.4±3.0） mg .L-l, 81/2 = （ 1. 7 ± 0. 7）, （2. 3± 1. 0）, and（ 1.4 ± 0. 8）h, AUC） = （5.4 ±1.8 ）, （ 10. 6±1.8 ）, and （ 21.0 ± 13.1 ） mg. h. L -1, respectively. Conclusions The established method would be applied for the pharmacokinetic study of DX-11 in rat plasma.

关 键 词：高效液相色谱法 DX-11 药动学 

分 类 号：R917[医药卫生—药物分析学]