Oxaprozin連続投与時のPharmacokinetics

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The pharmacokinetics of oxaprozin, an anti-inflammatory agent, were studied in healthy volunteers and dogs. After oral administration of oxaprozin (400 mg) to the volunteers, the maximum serum concentration of 57.0 μg/ml was attained at 5 h and then decreased with a mean half-life of 50.2 h. In the multiple dosing with 400 mg of the drug once a day for 10 d, the serum concentrations reached a plateau within 6 d and the levels were about 80% of those estimated from the single dosing experiments. Total serum clearance (Cl_<tot>/F) where F is the fraction absorbed at steady state was 161 ml/h, which was significantly higher than that (113 ml/h) with the single dosing. Similar tendencies were observed in dogs after the intravenous administrations of oxaprozin (10 mg/kg). On the other hand, the fraction of unbound drug to serum protein was found to be nonlinear to the total drug in clinically relevant concentrations. No significant difference of pharmacokinetic parameters such as area under the concentration versus time curve (AUC_t) or Cl_<tot>/F of unbound drug was observed between single and multiple-doses experiment both in human and dogs. Thus, the clearance of oxaprozin was closely related to the fraction of unbound drug. These results indicate that multiple-doses of oxaprozin resulted in a plateau effect, which was due to the accelerated Cl_<tot> in steady state conditions caused by an increase in the fraction of unbound drug in the serum.
公益社団法人日本薬学会の論文
1987-06-25

Oxaprozin連続投与時のPharmacokinetics

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