Pharmacokinetic comparison and bioequivalence of two leflunomide formulations in humans: A single dose, randomized, open-label, two-way crossover study

International Journal of Clinical Pharmacology and Therapeutics

Volumn 48, Issue 4, 2010, Pages 291-295

  Park, J Y ^a   Kim, K A ^a   Lee, Y H ^a   Park, S W ^b   Lee, G H ^b   Ryu, J H ^b  

^a Korea University College of Medicine   (South Korea)

^b Hanlim Pharmaceutical Company Ltd   (South Korea)

Author keywords

A77 1726; Bioavailability; Bioequivalence; Leflunomide; Pharmacokinetics

Indexed keywords

AREY; LEFLUNOMIDE; TERIFLUNOMIDE; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG ABSORPTION; DRUG DOSAGE FORM COMPARISON; DRUG FORMULATION; DRUG HALF LIFE; DRUG METABOLISM; HUMAN; HUMAN EXPERIMENT; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; UNSPECIFIED SIDE EFFECT;

EID: 77950962744     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: 10.5414/CPP48291     Document Type: Article

References (14)

1. Chow C, Liu J. Design and Analysis of Bioavailability and Bioequivalence Studies. New York: Marcel Dekker, 1992.
2. Goldenberg MM. Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis. Clin Ther. 1999; 21: 1837-1852.
3. Food and Drug Administration. Guidance for Industry: Bioavailability and Bioequivalence Studies for Orally Administered Drug Products - General Considerations. Center for Drug Evaluation and Research, Food and Drug Administration, 5600 Fishers Lane Rockville, MD 20857. http://www.fda.gov/cder/ guidance/index.htm. Accessed 2 October, 2009.
4. Food and Drug Administration of Korea (KFDA). Korean FDA Guidelines for Bioequivalence Test. Seoul, Korea: KFDA; 1996.
5. Kale VP, Bichile LS. Leflunomide: a novel disease modifying anti-rheumatic drug. J Postgrad Med. 2004; 50: 154-157. (Pubitemid 39069778)
6. Kis E, Nagy T, Jani M, Molnar E, Janossy J, Ujhelly O, Nemet K, Heredi-Szabo K, Krajcsi P. Leflunomide and A771726, its metabolite are high affinity substrates of BCRP- implications for drug resistance. Ann Rheum Dis. 2009; 68: 1201-1207.
7. Li J, Yao HW, Jin Y, Zhang YF, Li CY, Li YH, Xu SY. Pharmacokinetics of leflunomide in Chinese healthy volunteers. Acta Pharmacol Sin. 2002; 23: 551-555. (Pubitemid 34602097)
8. Lucien J, Dias VC, LeGatt DF, Yatscoff RW. Blood distribution and single-dose pharmacokinetics of leflunomide. Ther Drug Monit. 1995; 17: 454-459.
9. Meredith P. Bioequivalence and other unresolved issues in generic drug substitution. Clin Ther. 2003; 25: 2875-2890. (Pubitemid 37510596)
10. Rozman B. Clinical pharmacokinetics of leflunomide. Clin Pharmacokinet. 2002; 41: 421-430.
11. Schuirmann DJ. Acomparison of the two one-sided tests procedure and the power approach for assessing the equivalence of average bioavailability. J Pharmacokinet Biopharm. 1987; 15: 657-680.
12. Sparreboom A, Loos WJ, Burger H, Sissung TM, Verweij J, Figg WD, Nooter K, Gelderblom H. Effect of ABCG2 genotype on the oral bioavailability of topotecan. Cancer Biol Ther. 2005; 4: 650-658. (Pubitemid 41351197)
13. Urquhart BL, Ware JA, Tirona RG, Ho RH, Leake BF, Schwarz UI, Zaher H, Palandra J, Gregor JC, Dresser GK, Kim RB. Breast cancer resistance protein (ABCG2) and drug disposition: intestinal expression, polymorphisms and sulfasalazine as an in vivo probe. Pharmacogenet Genomics. 2008; 18: 439-448. (Pubitemid 351535945)
14. van Roon EN, Yska JP, Raemaekers J, Jansen TL, van Wanrooy M, Brouwers JR. Arapid and simple determination of A771726 in human serum by high-performance liquid chromatography and its application for optimization of leflunomide therapy. J Pharm Biomed Anal. 2004; 36: 17-22. (Pubitemid 39209403)