title: Effect of CYP2C9*3 mutant variants on meloxicam pharmacokinetics in a healthy Chinese population.
abstract: The aim of this study was to investigate the effect of the CYP2C9*3 (CYP2C9 1075 A>C) polymorphism on meloxicam pharmacokinetics in a Chinese population. Twenty-four healthy volunteers were enrolled in this study. The pyrosequencing technique was used to identify polymorphisms of CYP2C9. The concentration of meloxicam in plasma was determined by a high-performance liquid chromatography assay with mass spectrographic analysis. The Drug and Statistics Software (DAS, version 2.0) was used for curve fitting and calculations of pharmacokinetic parameters. The effects of CYP2C9*3 variant genotypes on meloxicam pharmacokinetics were compared with those of the wild type genotype. Among the 24 volunteers, two AC heterozygotes were observed in the multi-dose group. CYP2C9*3 was found to play an important role in the metabolism of meloxicam by reducing its enzymatic activity. Therefore, results of this study provide helpful information regarding inter-individual pharmacokinetic variability in the Chinese population.
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China may1008_zhang@yeah.net.
authors.forename: M
authors.initials: M
authors.lastname: Zhang
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China.
authors.forename: Y
authors.initials: Y
authors.lastname: Yang
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China.
authors.forename: G
authors.initials: G
authors.lastname: Zhao
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China.
authors.forename: X
authors.initials: X
authors.lastname: Di
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China.
authors.forename: L
authors.initials: L
authors.lastname: Xu
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China.
authors.forename: N
authors.initials: N
authors.lastname: Jiang
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China.
authors.forename: J
authors.initials: J
authors.lastname: Xu
authors.affiliation: Department of Pharmacology, the Military General Hospital of Beijing PLA, Beijing, China.
authors.forename: X
authors.initials: X
authors.lastname: Xu
mesh_terms: D000328:Adult; D001189:Aryl Hydrocarbon Hydroxylases / Q000097:blood / Q000235:genetics*; D002681:China; D065729:Cytochrome P-450 CYP2C9; D005260:Female; D005838:Genotype; D064368:Healthy Volunteers; D059014:High-Throughput Nucleotide Sequencing; D006801:Humans; D008297:Male; D000077239:Meloxicam; D009154:Mutation; D013843:Thiazines / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics*; D013844:Thiazoles / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics*
chemical_list: D013843:Thiazines; D013844:Thiazoles; C450260:CYP2C9 protein, human; D065729:Cytochrome P-450 CYP2C9; D001189:Aryl Hydrocarbon Hydroxylases; D000077239:Meloxicam