Kang Hyun-Ah, Cho Hea-Young, Lee Yong-Bok
College of Pharmacy and Institute of Bioequivalence and Bridging Study, Chonnam National University, Gwangju 500-757, Korea.
Arch Pharm Res. 2007 Jan;30(1):96-101. doi: 10.1007/BF02977784.
This study evaluated the relationship between the genetic polymorphism in the MDR1 (exon 21) genes and the pharmacokinetics of gabapentin (GBP) in healthy Korean subjects. The healthy Koreans were genotyped with respect to MDR1 (exon 21, 30 subjects) using polymerase chain reaction-based diagnostic testing. The pharmacokinetic profile of GBP was examined. A single oral dose of 300 mg GBP in a capsule was administered to the subjects and the blood samples were taken during a 24 h post-dose interval. The serum GBP concentration was measured using an HPLC-fluorescence detector system. There were no significant (P < 0.05) differences between the genotypes and pharmacokinetic parameters such as AUC(0-1h), AUC(0-1.5h), AUC(0-infinity), Cmax and t1/2. However, there was a trend toward higher values of the absorptive phase characterized by the AUC(0-1h) and AUC(0-1.5h) in 2677T/A subjects. In conclusion, this study suggests that GBP may be a weak substrate for the P-glycoprotein (P-gp) transporter.
本研究评估了健康韩国受试者中多药耐药基因1（MDR1，外显子21）的基因多态性与加巴喷丁（GBP）药代动力学之间的关系。采用基于聚合酶链反应的诊断检测方法，对30名健康韩国人的MDR1（外显子21）进行基因分型。检测了GBP的药代动力学特征。给受试者口服一粒300 mg的GBP胶囊，并在给药后24小时内采集血样。使用高效液相色谱-荧光检测系统测定血清GBP浓度。基因型与药代动力学参数如AUC(0-1h)、AUC(0-1.5h)、AUC(0-∞)、Cmax和t1/2之间无显著差异（P < 0.05）。然而，在2677T/A受试者中，以AUC(0-1h)和AUC(0-1.5h)为特征的吸收相值有升高趋势。总之，本研究表明GBP可能是P-糖蛋白（P-gp）转运体的弱底物。
