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目的建立口服复方替米沙坦片后替米沙坦血药浓度的液相色谱-质谱(LC-MS/MS)测定法,进行人体药动学研究。方法20名健康受试者随机分成两组,分别口服低剂量(1片)和高剂量(2片)受试制剂复方替米沙坦片,应用LC-MS/MS法测定样品中替米沙坦的血药浓度。结果健康受试者单次口服低剂量复方替米沙坦片后,主要药代动力学参数cmax为(111±75)μg/L,tmax为(1.7±1.1)h,AUC0-t为(1186±877)μg·h·L-1,AUC0-∞为(1268±935)μg·h·L-1,t1/2为(17.6±3.3)h,CLz/F为(52.7±35.7)L/h,Vz/F为(1268±840)L,MRT为(16.8±3.7)h。单次口服高剂量复方替米沙坦片后,主要药代动力学参数cmax为(651±449)μg/L,tmax为(1.3±0.7)h,AUC0-t为(4201±3052)μg·h·L-1,AUC0-∞为(4477±3313)μg·h·L-1,t1/2为(17.7±4.5)h,CLz/F为(41.6±51.9)L/h,Vz/F为(959±1231)L、MRT为(15.0±2.7)h。结论本方法结果准确、灵敏度高,替米沙坦进入人体分布后,其主要药动学参数与文献报道的单方替米沙坦数据一致。
Objective To establish a liquid chromatography-mass spectrometry (LC-MS / MS) method for the determination of telmisartan after oral administration of telmisartan tablets. Methods Twenty healthy volunteers were randomly divided into two groups: oral low dose (1 tablet) and high dose (2 tablet) of test compound telmisartan tablets. LC-MS / MS method was used to determine telmisartan Tan blood concentration. Results After a single oral dose of compound telmisartan tablets in healthy subjects, the main pharmacokinetic parameters cmax were (111 ± 75) μg / L, tmax was (1.7 ± 1.1) h and AUC0-t was (1186 (1268 ± 935) μg · h · L-1, t1 / 2 was (17.6 ± 3.3) h and CLz / F was (52.7 ± 35.7) L / h, Vz / F was (1268 ± 840) L and MRT was (16.8 ± 3.7) h. After a single oral dose of compound telmisartan tablets, the main pharmacokinetic parameters cmax was (651 ± 449) μg / L, tmax was (1.3 ± 0.7) h, AUC0-t was (4201 ± 3052) μg · (44.7 ± 33.13) μg · h · L -1, t1 / 2 was (17.7 ± 4.5) h, CLz / F was (41.6 ± 51.9) L / h and Vz / F (959 ± 1231) L, MRT was (15.0 ± 2.7) h. Conclusion The method is accurate and sensitive. The main pharmacokinetic parameters of telmisartan are consistent with those reported in the literature.