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目的研究复方缬沙坦分散片在健康人体的相对生物利用度并评价其生物等效性。方法用双周期自身随机交叉试验设计。20名健康受试者分别口服受试制剂(复方缬沙坦分散片)或参比制剂(缬沙坦氢氯噻嗪片)1片,采用LC-MS/MS测定血浆中缬沙坦、氢氯噻嗪浓度,以DAS2.0软件计算主要药动学参数,并对2种制剂进行生物等效性评价。结果单次口服受试制剂和参比制剂后的主要药动学参数:缬沙坦的t1/2分别为(4.6±s1.2)和(4.8±1.2)h、ρmax分别为(1504±733)和(1309±631)μg·L-1、tmax分别为(2.1±0.4)和(2.3±0.8)h、AUC0～36分别为(7039±3256)和(6522±3515)μg·h·L-1;氢氯噻嗪的t1/2分别为(5.1±2.6)和(5.2±2.2)h、ρmax分别为(67±17)和(69±22)μg·L-1、tmax分别为(1.8±0.5)和(2.0±0.6)h、AUC0～36分别为(311±73)和(319±97)μg·h·L-1。受试制剂中缬沙坦、氢氯噻嗪的相对生物利用度分别为(112±27)%、(100±21)%。结论2种制剂具有生物等效性。
Objective To study the relative bioavailability of compound valsartan dispersible tablets in healthy volunteers and to evaluate its bioequivalence. Methods Two-cycle random crossover design. Twenty healthy subjects were treated with valsartan and hydrochlorothiazide respectively by oral administration of 1 tablet of valsartan and valsartan hydrochlorothiazide tablets. The concentrations of valsartan and hydrochlorothiazide in plasma were determined by LC-MS / MS. The DAS 2.0 software calculates the main pharmacokinetic parameters and evaluates the bioequivalence of the two formulations. Results The main pharmacokinetic parameters of single oral test formulation and reference formulation were as follows: t1 / 2 of valsartan were (4.6 ± s1.2) and (4.8 ± 1.2) h respectively, and ρmax were (1504 ± 733 ) And (1309 ± 631) μg · L-1, tmax were (2.1 ± 0.4) and (2.3 ± 0.8) h respectively, and AUC0 ~ 36 were 7039 ± 3256 and 6522 ± 3515 μg · h · L -1 and t1max of hydrochlorothiazide were (5.1 ± 2.6) and (5.2 ± 2.2) h, respectively. The values of ρmax were (67 ± 17) and (69 ± 22) μg · L-1, ) And (2.0 ± 0.6) h, AUC0 ~ 36 were (311 ± 73) and (319 ± 97) μg · h · L-1, respectively. The relative bioavailability of valsartan and hydrochlorothiazide were (112 ± 27)% and (100 ± 21)%, respectively. Conclusion The two preparations have bioequivalence.