• 한국임상약학회지
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• 제20권1호
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• pp.50-55
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• 2010

Cefetamet pivoxil is a prodrug of cefetamet possessing a broad spectrum of activity against many aerobic gram-positive and -negative organisms. Although many literatures in abroad had introduced its pharmacokinetics about two decays ago, no data have been revealed in Korean subjects. Therefore, this study was aimed to investigate the pharmacokinetics of cefetamet following a single oral administration of cefetamet pivoxil in Korean healthy volunteers. After an overnight fast, a tablet of cefetamet pivoxil (500 mg) was given to eight volunteers, and blood samples were serially taken up to 12 h. Plasma concentrations of cefetamet were determined by HPLC with UV detection. Cefetamet reached the peak concentration ($2.0{\pm}1.3\;{\mu}g/ml$) at $3.0{\pm}0.8$ h, and mono-exponentially decayed at a half-life of $2.6{\pm}0.9$ h. Three volunteers represented very low systemic exposure compared to the others, which provided very large inter-individual variation in Cmax, and AUC. The present results were discussed and reviewed with the previously published data, and a couple of points are suggested for clinical trials of this drug in Korean subject including bioequivalence study.

• Journal of Pharmaceutical Investigation
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• 제37권6호
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• pp.369-376
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• 2007

Cyclosporine (CsA) and tacrolimus (FK506) have a narrow therapeutic range, and their pharmacokinetic (PK) characteristic varies among individual. They are also substrates for cytochrome P450 (CYP) 3A4, 3A5 genes, and P-glycoprotein, the product of the multidrug resistance 1 (MDR1). The aims were to investigate the relationship between CYP3A and MDR1 genotypes and their PK parameters among healthy subjects. We investigated the genotype for CYP3A and MDR1 gene in human using a polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) method. After oral administration of CsA and FK506 (100 mg and 1 mg, respectively), whole blood samples were taken up to 24 hours. Blood CsA and FK506 concentrations were measured by LC/MS/MS. Each PK parameters were compared using Kruskal-Wallis test according to the CYP3A and MDR1 genotype. We found that the values of AVC for CsA were significantly different among CYP3A5 and MDR1 exon 26 (C3435T) genotypes (P=0.037 and P=0.049). On the other hand, the AUC for FK506 was significantly different only among CYP3A5 genotypes (P=0.013). The results clearly demonstrate the effects of CYP3A5 and MDR1 exon 26 on Cys and FK506 disposition.