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目的研究甲苯磺丁脲人体代谢过程与中国健康志愿者P4502C9基因多态性的关系。方法不同P4502C91/1(n=53)、1/3(n=9)及3/3(n=1)基因型的健康志愿者单次口服甲苯磺丁脲500mg后,用HPLC方法测定血和尿中的甲苯磺丁脲及其代谢产物浓度,研究甲苯磺丁脲的药代过程。结果P4502C91/3与P4502C93/3基因型的受试者与P4502C91/1基因型相比,AUC(0-∞)增加20%和116%,t1/2增加60%和813%,CL0为68%和11%,CLform仅为39%和3%。结论P4502C91/3对甲苯磺丁脲的代谢活性较P4502C91/1显著降低,P4502C93/3代谢活性更低,并呈现基因剂量关系。
Objective To investigate the relationship between tolbutamide in human metabolism and the polymorphism of P4502C9 gene in Chinese healthy volunteers. Methods Healthy volunteers with different P4502C91 / 1 (n = 53), 1/3 (n = 9) and 3/3 (n = 1) genotypes were administered orally with tolbutamide for 500mg, Tolbutamide in urine and its metabolite concentration, the drug process of tolbutamide. RESULTS: Subjects with P4502C91 / 3 and P4502C93 / 3 genotypes showed 20% and 116% increase in AUC (0-∞), 60% and 813% increase in t1 / 2, and 68% CL0 in the P4502C91 / And 11%, CLform only 39% and 3%. Conclusion The metabolic activity of P4502C91 / 3 p-tolbutamide was significantly lower than that of P4502C91 / 1, and P4502C93 / 3 was lower than that of P4502C91 / 3.