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目的在消化性溃疡病人中观察兰索拉唑的药代动力学的变化,进一步了解该药的代谢规律。方法选取经胃镜检查确诊为消化性溃疡的患者为试验组(G组,n=6)及健康志愿者为对照组(C组,n=6),口服兰索拉唑胶囊30mg,定时取血通过高压液相方法测定血药浓度。利用3P87药代动力学程序模拟药时曲线,计算药代动力学参数。结果兰索拉唑符合一房室模型。试验组中,5位患者的吸收速率常数Kα较对照组的Kα明显增加,吸收半衰期T12α及达峰时间Tmax明显减少。血药浓度高峰Cmax有明显提高。而清除速率常数Kβ、清除半衰期T12β也有较明显的差别,其表观分布容积V/F、清除率CL/F及血药浓度曲线下面积AUC差别均不显著。1位幽门不全梗阻患者的药代动力学曲线表明吸收明显延迟。结论兰索拉唑口服后,分布广泛,代谢迅速。消化性溃疡患者应用时,其吸收速率和其排泄明显加快。血药浓度高峰明显增加,对于治疗该病可能具有重要的意义。
Objective To observe the changes of the pharmacokinetics of lansoprazole in patients with peptic ulcer to further understand the metabolism of the drug. Methods The patients diagnosed as peptic ulcer by gastroscopy were selected as experimental group (G group, n = 6) and healthy volunteers as control group (C group, n = 6). Lansoprazole capsules Blood pressure was measured by HPLC method. The 3P87 pharmacokinetics program was used to simulate drug-drug curves and calculate pharmacokinetic parameters. Results Lansoprazole conformed to a one-compartment model. In the experimental group, Kα in 5 patients was significantly increased compared with Kα in control group, T12α in absorption half-life and Tmax in peak time were significantly decreased. Blood concentration peak Cmax significantly increased. Clear clearance rate constant Kβ, clearance half-life T12β also have obvious difference, the apparent volume of distribution V / F, clearance rate CL / F and plasma concentration curve under the area AUC difference was not significant. The pharmacokinetic profile of one patient with pyloric obstruction showed a significant delay in absorption. Conclusion After oral administration of lansoprazole, widely distributed, rapid metabolism. Peptic ulcer patients in the application, the absorption rate and its excretion was significantly accelerated. Significantly increased peak plasma concentration, for the treatment of the disease may have important significance.