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目的:研究沙丁胺醇气雾剂在健康受试者的药物动力学和生物利用度.方法:十名健康男性志愿者单剂量吸入1.2 mg沙丁胺醇气雾剂或口服沙丁胺醇水溶液.用HPLC法测定人血浆中沙丁胺醇浓度.以非房室模型计算药物动力学参数,计算气雾剂相对水溶液的生物利用度.结果:气雾剂和口服溶液的药物动力学参数如下:T_(max)(0.22±0.07)和(1.8±0.6)h,C_(max)(3.4±1.1)和(3.9±1.4)μg·L~(-1),T_(1/2)(4.5±1.5)和(4.6±1.1)h,AUC_(0-20min)(0.9±0.3)和(0.16±0.10)μg·h·L~(-1).两种给药途径的T_(max)和AUC_(0-20 min)之间差异显著(P<0.01).AUC_(0-20min)(nihal)为 AUC_(0-20 min)(po)的 8倍.沙丁胺醇气雾剂相对口服溶液的生物利用度为 57％±24％.结论:沙丁胺醇气雾剂在人体的吸收过程与口服溶液差异有显著性.
AIM: To study the pharmacokinetics and bioavailability of albuterol aerosol in healthy volunteers.Methods: Ten healthy male volunteers were given a single inhalation of 1.2 mg salbutamol aerosol or oral salbutamol.HPLC was used to determine the plasma levels of Salbutamol concentration.Pharmacokinetic parameters were calculated by non-compartmental model to calculate the bioavailability of aerosol relative to aqueous solution.Results: The pharmacokinetic parameters of aerosol and oral solution were as follows: T max (0.22 ± 0.07) and (1.8 ± 0.6) h, C max (3.4 ± 1.1) and (3.9 ± 1.4) μg · L -1, T 1/2 (4.5 ± 1.5) and (4.6 ± 1.1) h, AUC_ (0-20min) (0.9 ± 0.3) and (0.16 ± 0.10) μg · h · L -1 .The difference between T max and AUC 0-20 min of the two routes of administration was significant (P0.01) .AUC_ (0-20min) (nihal) was 8 times of AUC_ (0-20 min) (po) .The bioavailability of salbutamol aerosol relative to oral solution was 57% ± 24% .Conclusion: Salbutamol aerosol in the human body during the absorption process and oral solution differences were significant.