Naora K, Katagiri Y, Ichikawa N, Hayashibara M, Iwamoto K
Department of Pharmacy, Shimane Medical University Hospital, Izumo, Japan.
J Pharmacobiodyn. 1990 Feb;13(2):90-6. doi: 10.1248/bpb1978.13.90.
In order to clarify the possibility of pharmacokinetic interaction between quinolone and fenbufen, the plasma concentration-time profiles and serum protein binding of enoxacin, fenbufen and its active metabolite, felbinac, were investigated in rats. The rats were administered an intravenous dose of enoxacin (5 mg/kg) and fenbufen (10 mg/kg) alone or concomitantly. Coadministration with fenbufen tended to prolong the plasma elimination half-life of enoxacin by about 20%, whereas it showed no effect on the area under plasma concentration-time curve, total body clearance or distribution volume of enoxacin. The extent of enoxacin binding to rat serum tended to be slightly reduced by fenbufen in vivo and in vitro. Plasma concentration-time curves, pharmacokinetic parameters and serum protein binding of fenbufen and felbinac were not affected at all by the coadministration with enoxacin. These aspects suggest that there may be only a minor possibility of the pharmacokinetic interaction between enoxacin and fenbufen.
为了阐明喹诺酮类药物与芬布芬之间药代动力学相互作用的可能性，研究了依诺沙星、芬布芬及其活性代谢产物非诺洛芬在大鼠体内的血药浓度-时间曲线和血清蛋白结合情况。大鼠分别单独或同时静脉注射依诺沙星（5mg/kg）和芬布芬（10mg/kg）。与芬布芬合用时，依诺沙星的血浆消除半衰期有延长约20%的趋势，而对依诺沙星的血药浓度-时间曲线下面积、总体清除率或分布容积无影响。在体内和体外，芬布芬均使依诺沙星与大鼠血清的结合程度略有降低。依诺沙星与芬布芬合用时，芬布芬和非诺洛芬的血药浓度-时间曲线、药代动力学参数及血清蛋白结合均未受到任何影响。这些结果表明，依诺沙星与芬布芬之间药代动力学相互作用的可能性可能较小。
