Pharmacokinetics of Lopinavir after Administration of Kaletra in Healthy Japanese Volunteers(Biopharmacy)

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The pharmacokinetic parameters of lopinavir (LPV) were examined by administering Kaletra (LPV+ ritonavir) to 8 healthy Japanese volunteers both in the fasting and postprandial conditions. LPV showed a biphasic decline, which was slower in the initial phase and became more rapid in the later phase. The behavior of LPV in the initial phase could be modeled using a one-compartment model with first-order absorption. In the fasting study, calculations based on the pharmacokinetic model revealed that the time to reach the maximum concentration (T_<max>), maximum concentration (C_<max>), half-life (T_<1/2>), lag time, apparent volume of distribution (Vd/F) and oral clearance (Cl/F) were 3.2±1.0h, 6.9±1.9μg/ml, 10.0±3.7h, 0.71±0.32 h, 51.0±12.41 and 4.2±2.6l/h, respectively. On the other hand, in the postprandial study, the calculated T_<max>, C_<max>, T_<1/2>, lag time, Vd/F and Cl/F were 5.6±2.0h, 7.6±1.8μg/ml, 16.7±7.0 h, 2.35±0.78h, 48.0±15.91 and 2.1±0.61/h, respectively. The values for the area under the curve for data collected over a 24-h period (AUC_<24h>) in the fasting and postprandial studies were 86.0±27.7 and 102.1±31.0 μg・h/ml, respectively. The T_<1/2> had a tendency to be prolonged after food intake, but there were 2 cases with shortened T_<1/2>. Food intake prolonged the lag time 3-fold and as a result, the post prandial T_<max> was 2 times longer.
公益社団法人日本薬学会の論文
2004-02-01