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目的:建立了一种测定小鼠血浆中色胺酮含量的HPLC-UV方法,深入探讨静注色胺酮在小鼠体内的药物动力学过程。方法:采用C18色谱柱(250mm×4.6mm,5μm),甲醇-水(60∶40)作为流动相,检测波长251nm,流速1.0ml/min,室温。采用结构相似的4(3H)-喹唑酮作为内标,研究昆明小鼠被静脉给药后0.167-12.0h期间的浓度-时间(C-t)曲线,计算药物动力学参数。结果:色胺酮质量浓度在0.2-25.0μg/ml范围内线性关系良好,r=0.999 4。LLOQ为0.2μg/ml,LOD为40.0ng/ml。日内日间精密度RSDs均小于2.93%,平均提取回收率大于86.44%。小鼠被静注80 mg/kg色胺酮后,t1/2β为4.00h,V1为3.83L/kg,CL为2.93L/(h·kg),AUC0-12为27.33μg·h/ml,AUC0-∞为28.20μg·h/ml,AUMC0-∞为50.02μg·h2/ml,MRT0-∞为1.83h。结论:本实验建立的HPLC-UV方法操作简单、方便,结果准确、可靠,适用于含色胺酮血浆样品的分析检测与色胺酮的药物动力学研究。色胺酮毒性低、安全性好,在小鼠体内吸收、代谢过程较慢、体内分布广。
OBJECTIVE: To establish a HPLC-UV method for the determination of tryptamine in mouse plasma and to investigate the pharmacokinetics of intravenous injection of trypanamine in mice. Methods: C18 column (250 mm × 4.6 mm, 5 μm) and methanol-water (60:40) were used as the mobile phase. The detection wavelength was 251 nm and the flow rate was 1.0 ml / min at room temperature. The structurally similar 4 (3H) -quinazolone was used as an internal standard to study the concentration-time (C-t) curves of Kunming mice from 0.167-12.0h after intravenous administration, and the pharmacokinetic parameters were calculated. Results: The linearity of the concentration of tryptanthrin in the range of 0.2-25.0 μg / ml was good, r = 0.999 4. LLOQ was 0.2 μg / ml and LOD was 40.0 ng / ml. The intra-day and inter-day precision RSDs were less than 2.93%, the average extraction recovery was more than 86.44%. T1 / 2β was 4.00h, V1 was 3.83L / kg, CL was 2.93L / (h · kg), AUC0-12 was 27.33μg · h / ml after mice were intravenously injected with 80 mg / kg tryptatrone, The AUC0-∞ was 28.20 μg · h / ml, the AUMC0-∞ was 50.02 μg · h2 / ml and the MRT0-∞ was 1.83 h. Conclusion: The HPLC-UV method established in this experiment is simple, convenient, accurate and reliable. It is suitable for the analysis and determination of the pharmacokinetics of tryptatrone in plasma samples. Tryptamycin low toxicity, good safety, absorption in mice, the metabolic process is slow, widely distributed in the body.