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目的研究氯沙坦及其代谢产物2-丁基-4-氯-1-[[2’-(1H-四唑-5-基)[1,1‘-联苯基]-4-基]甲基]-lH一咪唑-5-羧酸(E-3174)在中国汉族健康受试者体内的药动学。方法 10名健康受试者,男女各半,口服氯沙坦钾片50 mg,定时采血,用HPLC荧光法测定氯沙坦及其代谢物E-3174血药浓度,DAS2.0软件程序进行数据处理并采用SPSS13.0软件进行统计学分析。结果氯沙坦和E-3174的主要药动学参数如下:ρmax分别为(351±167),(241±60)μg.L-1;tmax分别为(1.35±1.06),(3.60±1.68)h;t1/2分别为(0.82±0.40),(4.66±1.10)h;AUC0-24分别为(498±172),(1 853±194)μg.h.L-1;AUC0-∞分别为(523±184),(1 960±182)μg.h.L-1。结论氯沙坦及其代谢物E-3174的药动学特征和参数在个体间存在较大差异,临床治疗中应实行个体化给药方案。
OBJECTIVE To study the effects of losartan and its metabolites 2-butyl-4-chloro-1 - [[2’- (1H- tetrazolium- 5-yl) [1,1’-biphenyl] Methyl] -lH-imidazole-5-carboxylic acid (E-3174) in Chinese Han healthy subjects. Methods Ten healthy subjects, male and female, were divided into two groups. Oral losartan potassium tablets (50 mg) were given regularly to collect blood. The blood concentration of losartan and its metabolite E-3174 was determined by HPLC fluorescence spectrometry. SPSS13.0 software was used for statistical analysis. Results The main pharmacokinetic parameters of losartan and E-3174 were as follows: ρmax were (351 ± 167) and (241 ± 60) μg.L-1, respectively; tmax was 1.35 ± 1.06 and 3.60 ± 1.68 respectively h and t1 / 2 were (0.82 ± 0.40) and (4.66 ± 1.10) h respectively; AUC0-24 was (498 ± 172) and (1 853 ± 194) μg.hL- ± 184), (1 960 ± 182) μg.hL-1. Conclusion The pharmacokinetic parameters and parameters of losartan and its metabolite E-3174 are quite different among individuals. Individualized dosing regimens should be applied in clinical treatment.