Abstract��
OBJECTIVE To study the pharmacokinetics of leflunomide in Chinese healthy volunteers. METHOD S A single oral doses of leflunomide(20,40,60 mg) were performed in 18 (12 males and 6 females) Chinese healthy volunteers respectively in a randomized crossover way.The concentrations of A771726,leflunomide's active metabolite,in serum were determined by HPLC.Data were analyzed by using a 3P97 program on a Legend computer. RESULTS The serum concentration��time curves of A����771726�� following single oral administration of leflunomide conformed to one compartment model of the first order absorption.Leflunomide was absorbed rapidly with t1/2KaKa of between 0.048 and 0.093 day.The major pharmacokinetic parameters of A771726in 20,40,60 mg groups were t1/2Ka��(0.09��0.12)��(0.1��0.3)and(0.05��0.03)d��t1/2Ke:(8.8��0.8)��(7.1��1.0) and (10.5��1.1) d; tmax:(0.6��0.5)��(0.55��0.16) and (0.38��0.29) d;cmax(2.0��0.5)��(5.20��0.17) and (6.7��1.5) mg��L-1;AUC0��28d:(27��6)��(56��8) and (106��30) mg��d��L-1,respectively. CONCLUSION The absorption of leflunomide was rapid,and its elimination was slow after oral administration.The pharmacokinetic results showed that it exhibited first order kinetic characteristics.
.Pharmacokinetics of leflunomide in Chinese healthy volunteers following single oral administration[J] Chinese Pharmaceutical Journal, 2003,V38(01): 45-47
2003, Vol. 38 
