• YAKHAK HOEJI
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• v.36 no.3
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• pp.259-268
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• 1992

A procedure for the determination of KR-30075 and its metabolites in plasma and urine by high performance liquid chromatography is described. For the study of pharmacokinetic properties of KR-30075, a new PDE III inhibitor, the plasma concentration and urinary excretion after an oral administration of KR-30075 (4 mg/kg) in the male rat (Sprague Dawley) were determined by high performance liquid chromatography. The best extraction efficiency of KR-30075 and KR-30072 is obtained with ethyl ether adjusted to pH 4.0. Retention times of both KR-30072 and KR-30075 were within 5 min and resolution was complete at the flow rate of 1.0 ml/min. The sensitivity and specificity of this HPLC assay appears to be satisfactory for the pharmacokinetic study of KR-30075 and its metabolites. One-compartment open model with first-order absorption was applied to evaluate the pharmacokinetic parameters of KR-30075 according to Minimum AIC Estimation. $T_{max}$ was 1 hr, $C_{max}$ was $0.789{\pm}0.31\;{\mu}g/ml$ and elimination half $T_{1/2}$ was 6.31 min after oral administration of 4 mg/kg KR-30075 to male rats.

• YAKHAK HOEJI
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• v.46 no.1
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• pp.63-68
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• 2002

The purpose of this study was to estimate the population pharmacokinetics of clarithromycin in healthy adult Korean and to investigate the factors influencing the pharmacokinetics of clarithromycin. The population pharmacokinetic parameters of clarithromycin were calculated with the data from healthy adult Koreans. A total of 798 plasma concentrations obtained from 78 subjects after administration of a single oral dose of 250 mg or 500 mg were used for the modeling. The concentration-time data were fitted to a one-compartment open model assuming a first-order absorption and elimination with no lag time. The correlations between various factors [such as sex, age, height, weight, sect creatinine (Scr) and dose and pharmacokinetic parameters were estimated with stepwise linear recession analyses. The selected covariates were incorporated in the population model of NONMEM, and the importance of each covariate was investigated by means of backwards elimination. The apparent clearance (CL/F) was significantly correlated to Scr and sex, and the apparent volume of distribution (Vd/F) was significantly correlated to Scr and height in a nonlinear relationship. The population values of Ka was 1.8 h $r_{-1}$, CL/F was 37.71 L/hr, Vd/F was 200 L and t/ sub 1/2 / was 3.68 hrs for a male Korean with 170 m height and 1.0 mg/dL Scr.