艾拉莫德片在中国健康志愿者体内的药动学

Pharmacokinetics of iguratimod tablets in Chinese healthy volunteers

目的研究健康志愿者单剂量和多剂量口服艾拉莫德后体内的药动学。方法健康志愿者分成2组,分别进行口服艾拉莫德片单剂量(255、0 mg)、多剂量(25 mg)、进食(50 mg)研究。采用HPLC法测定艾拉莫德血药浓度,DAS软件程序进行数据处理。结果255、0 mg单剂量主要药动学参数tmax分别为(4.72±1.49)、(4.58±1.01)h;ρmax分别为(1.08±0.27)(、1.78±0.52)mg.L-1;t12分别为(6.85±2.14)、(7.75±1.32)h;AUC0→t分别为(14.28±3.67)(、23.88±5.21)mg.h.L-1。25 mg多剂量主要药动学参数tmax为(3.82±0.75)h;ρmax为(1.77±0.52)mg.L-1;t12为(10.52±2.54)h;AUC0→t为(26.72±9.29)mg.h.L-1;ρav为(0.76±0.19)mg.L-1,血药浓度波动度DF为(205.64±36.04)%。进食(50 mg)主要药动学参数tmax为(4.33±1.07)h;ρmax为(2.10±0.35)mg.L-1;t12为(6.79±1.34)h;AUC0→t为(24.79±4.44)mg.h.L-1。结论艾拉莫德单剂量组和多剂量组药动学均符合开放型一室模型,连续服用会在人体内蓄积,进食对本药的吸收无影响。

AIM To study the pharmacokinetics of iguratimod tablets in Chinese healthy volunteers. METHODS Twenty-four volunteers were randomly divided into 2 groups： 25 mg group （ single and then multiple dose, po ） and 50 mg group （with and without food, po ）. Iguratimod concentration in plasma was determined by HPLC and pharmacokinetic parameters were calculated by DAS software. RESULTS The main pharmacokinetic parameters were as foUows： tmax of 25 and 50 mg single-dose groups were （4.72 ± 1.49） and （4.58 ± 1.01 ）h, ρmax= were（ 1.08 ± 0.27） and（ 1.78 ± 0.52）mg·L^-1 ; tmax were （6.85 ± 2.14） and （7.75 ± 1.32） h, AUC0→t were （ 14.28 ± 3.67） and （23.88 ± 5.21）mg·h·L^-1, respectively; tmax of 25 mg multiple-dose group was （3.82 ± 0.75） h, ρmax Was （ 1.77 ± 0.52） mg·L^-1, tmax was （ 10.52 ± 2.54） h, AUC0→t was （26.72 ± 9.29） mg·h·L^-1, pay was （0.76 ± 0.19） mg· L^-1 and DF was （205.64 ± 36.04） % ; tmax of 50 mg single dose group after taken food was（4.33 ± 1.07）h, ρmax Was （2.10 ± 0.35） mg· L^-1, tmax was （6.79 ± 1.34） h and AUC0→t was （24.79 ± 4.44） mg·h· L^-1. CONCLUSION The pharmacokinetic parameters of iguratimod tablets are fit for one compartment model when taking single -and multiple-doses by orally in 24 healthy volunteers, It would be accumulated in the body when taking continuously, and the absorption would not be influenced by food.