氨咖黄敏胶囊中对乙酰氨基酚和咖啡因的人体药动学

Pharmacokinetics of paracetamol and caffeine in paracetamol,caffeine,atificial cow-bezoar and chlorphenamine maleate capsules in healthy volunteers

目的研究氨咖黄敏胶囊中对乙酰氨基酚和咖啡因的人体药动学。方法本试验采用HPLC法测定了18名健康男性受试者口服氨咖黄敏胶囊后不同时刻血浆中对乙酰氨基酚和咖啡因的浓度,用3P97软件拟合房室模型并求出主要药动学参数。结果受试者口服含对乙酰氨基酚750 mg和咖啡因45 mg的氨咖黄敏胶囊制剂后,血浆中对乙酰氨基酚的t_(max)为(1.03±0.76)h,ρ_(max)为(12.00±3.10)mg·L^(-1),t_(1/2)为(4.33±1.18)h,用梯形法计算AUC_(0→t)为(52.51±16.81)mg·h·L^(-1),AUC_(0→∞)为(54.34±17.72)mg·h·L^(-1);血浆中咖啡因的t_(max)为(0.89±0.50)h,ρ_(max)为(1.290±0.379)mg·L^(-1),t_(1/2)为(5.37±2.15)h,用梯形法计算AUC_(0→t)为(7.19±3.03)mg·h·L^(-1),AUC_(0-∞)为(8.26±3.69)mg·h·L^(-1)。结论对乙酰氨基酚在人体内符合二房室模型,咖啡因在人体内符合一房室模型。

AIM To investigate the pharmacokinetics of paracetamol and caffeine in paracetamol, caffeine, afificial cow-bezoar and chlorphenamine maleate capsules. METHODS A sensitive and rapid HPLC method was developed to deten-nine paracetamol and caffeine concentration simultaneously in human plasma. Data of plasma level-time were disposed with 3P97 software. RESULTS The main pharmacokinetic parameters of paracetamol were as follows： t max （ 1.03 ± 0.76）h,ρmax,（12.00 ± 3.10） mg·L^-1, t1/2 （4.33 ± 1.18） h, AUC0→t（52.51 ± 16.81） mg· h·L^-1 , AUC0→∞ （54.34 ± 17.72） mg· h· L^-1, respectively. For caffeine, the main pharmacokinetic parameters were as follows： tmax（0-89 ±0.50） h, ρmax（1.290± 0.379）mg· L^-1, t1/2 （5.37 ± 2.15）h, AUC0→t（7.19 ± 3.03） mg·h·L^-1 , AUC0→∞ （8.26± 3.69） mg· h· L^- 1, respectively. CONCLUSION The plasma concentration-time curves of paracetamol and caffeine appear to fit two and one compartment models, respectively.