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目的以阿魏酸2,3,5,6-四甲基吡嗪(FATM)的代谢产物TMP为指标,考察TMP在兔体内的药物代谢动力学特性及其组织分布状况,为日后进一步研究开发FATM的临床应用提供理论依据。方法采用兔灌胃口服给药后的血药浓度经时变化研究TMP。用高效液相色谱-紫外检测器进行样本分析。采用房室模型的药动学软件Kinetica计算TMP的药动学参数。结果 TMP在血液中符合一室吸收动力学模型(权重1/C)。TMP的T1/2α和T1/2β均约为0.27 h;Ka为(2.59±0.25)h-1,Tmax为(0.39±0.02)h,Cmax为(1.81±0.14)μg/m L,AUC为(1.91±0.28)μg·m L-1·h。经检测TMP广泛分布与各器官中,且分布较均匀,浓度最高的脏器为肝,浓度为(0.72±0.02)μg·m L-1·h,其他依次为脾,肾,心,脑,在肺部未能检测出TMP。结论实验数据表明,FATM在兔体内可以迅速吸收,并广泛分布于各组织。FATM是一种有应用前景的潜在药物。
OBJECTIVE To investigate the pharmacokinetics and tissue distribution of TMP in rabbits with TMP, a metabolite of 2,3,5,6-tetramethylpyrazine (FATM) in ferulic acid for future research and development The clinical application of FATM provides a theoretical basis. Methods Study on the Changes of Serum Concentration after Oral Administration in Rabbits. Samples were analyzed by high performance liquid chromatography - ultraviolet detector. Pharmacokinetic parameters of TMP were calculated using pharmacokinetic software Kinetica in atrioventricular model. Results TMPs fit the one-compartment kinetics model in the blood (weight 1 / C). TMP was (0.39 ± 0.02) h, Cmax was (1.81 ± 0.14) μg / m L, AUC was ( 1.91 ± 0.28) μg · m L-1 · h. TMP was detected widely distributed in various organs, and the distribution is more uniform, the highest concentration of liver, the concentration of (0.72 ± 0.02) μg · m L-1 · h, followed by the spleen, kidney, heart, brain, TMP was not detected in the lungs. Conclusion The experimental data show that FATM can be rapidly absorbed in rabbits and widely distributed in various tissues. FATM is a potential drug with potential applications.