Original Article

Pharmacokinetics of leflunomide in Chinese healthy volunteers.

Authors: Jun LI, Hong-Wei YAO, Yong JIN, Yun-Fang ZHANG, Chang-Yu LI, Yuan-Hai LI, Shu-Yun XU

Abstract

AIM: To study the pharmacokinetics of leflunomide in Chinese healthy volunteers.
METHODS: A single (20, 40, and 60 mg) and 30-d -repeated (20 mg/d) oral doses of
leflunomide were performed on 18 (12 males and 6 females) and 6 (4 males and 2
females) Chinese healthy volunteers respectively. A771726, the active metabolite
of leflunomide, in serum was determined by high performance liquid chromatography
(HPLC). Data were analyzed by a 3p97 program on a Legend computer.
RESULTS: Serum concentration curves of A 771726 in single and repeated oral
administration of leflunomide conformed to one compartment model of the first
order absorption. Leflunomide was absorbed rapidly with T1/2,ka of between 1.15 h
and 2.23 h in single oral administration. The major pharmacokinetic parameters of
A771726 in 20, 40, and 60 mg groups were T1/2,ke(h): 211 +/- 18, 170 +/- 24, 252
+/- 26; Tmax(h): 13 +/- 12, 13 +/- 4, 9 +/- 5; Cmax (mg/L): 2.0 +/- 0.5, 5.2 +/-
0.6, 6.7 +/- 1.5; AUC (mg . h . L-1): 647 +/- 137, 1344 +/- 191, 2555 +/- 907,
respectively. In repeated oral administration, steady stat e concentration was
achieved within 30 d. The mean trough concentration was between 32.0 mg/L and
39.7 mg/L. The Cmax, Tmax, AU C0- 24 were (41.5 +/- 2.4) mg/L, (307 +/- 75) h,
and (22099 +/- 1234) mg . h . L-1, respectively.
CONCLUSION: The absorption of leflunomide was rapid, and it s elimination was
slow after oral administration. The pharmacokinetic results showed that it
exhibited first order kinetic characteristics.
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