依诺沙星对大鼠茶碱药代动力学的影响

Effect of Enoxacin on Pharmacokinetics of Theophylline in Rats

为探讨国产依诺沙星（ Ｅ Ｎ Ｘ）对大鼠血浆茶碱（ Ｔ Ｐ）药动学的影响，给临床合理使用 Ｅ Ｎ Ｘ 提供实验依据。经灌胃给予大鼠单剂量 Ｔ Ｐ２０ｍ ｇ／ｋｇ，同时给予 Ｅ Ｎ Ｘ （３００ｍ ｇ／ｋｇ 及４５０ｍ ｇ／ｋｇ）３次，用 Ｈ Ｐ Ｌ Ｃ法测定给 Ｔ Ｐ后１、２、３、５、７、１２、２４小时的血浆 Ｔ Ｐ浓度。结果显示茶碱以一室药动学模型消除， Ｅ Ｎ Ｘ 使 Ｔ Ｐ浓度明显升高， Ｔ１／２ β延长， Ａ Ｕ Ｃ增大，血浆清除率下降，具有剂量依赖性。由此表明国产 Ｅ Ｎ Ｘ 与 Ｔ Ｐ有明确的相互作用，合用时应予以注意。

In order to obtain an experimental evidence for Enoxacin(ENX) to be correctly used in clinical treatment, we studied the effect of ENX on the pharmacokinetic parameters of theophylline(TP).A single oral dose of TP 20mg/kg was given to rats and ENX(300mg/kg,450mg/kg) was co administered orally three times to those rats. The plasma concentrations of TP were determined by HPLC after TP was administered 1,2,3,5,7,12 and 24 hrs. The results showed that TP was eliminated by one compartment model. TP plasma concentrations and AUC were significantly increased. T 1/2 β of TP was prolonged. The total clearance of TP was decreased when compared with the control. This interaction was dose dependent. It was concluded that the interaction between ENX and TP existed. Concomitant use of ENX with TP should be avoided.