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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 HPLC method for the determination of DX-11 [tryptophan 13-yl] tryptophan in rat plasma and to study the pharmacokinetics of DX-11 in rats. Methods The mobile phase was Kromasil C18 column (250 mm × 4.6 mm, 5 μm). The mobile phase consisted of 0.2% methanolic formic acid (volume ratio 75:25), flow rate 1.0 mL.min-1, 220 nm, diethylstilbestrol as internal standard. Results The linearity of DX-11 was 0.2 ~ 20.0 mg.L-1. The regression equation was Y = 1.869 × 10-1ρ + 9.830 × 10-2 (r = 0.998 1). The lower limit of quantitation was 0.2 mg.L-1. : 84.1% ~ 88.9%, intraday and day precision no greater than 10.2%. The tmax of DX-11 in plasma was (1.4 ± 0.2), (1.8 ± 0.7), (1.3 ± 0.3) h, ρmax respectively in 18 rats after intragastric administration of low, medium and high doses of DX 12 Were (2.3 ± 0.3), (3.5 ± 0.6) and (6.4 ± 3.0) mg.L-1, and t1 / 2 were (1.7 ± 0.7), (2.3 ± 1.0) and 0-∞) were (5.4 ± 1.8), (10.6 ± 1.8) and (21.0 ± 13.1) mg.hL-1, respectively. Conclusion The established and validated HPLC method is suitable for the pharmacokinetics of DX-11 in rats.