氟氧头孢在家兔体内的药代动力学和组织分布研究

Studies on the pharmacokinetics and tissue distribution of flomoxef in rabbits

目的：研究氟氧头孢在家兔体内的药代动力学和组织分布。方法：家兔单剂量静脉推注５０ ｍ ｇ／ｋｇ 氟氧头孢，采用ＨＰＬＣ法测定体液及组织中药物浓度。结果：静脉给药后血浆药－时曲线符合二室开放模型，氟氧头孢体内分布迅速，分布半衰期仅为０．０２３ ｈ，消除半衰期为０．２１３ ｈ， ＡＵＣ为（７９．９４±１３．３１） ｈ·μｇ／ｍ ｌ， 尿液、胆汁、肺、肾脏、卵巢及子宫中药物浓度较高。结论：氟氧头孢是一体内分布广、组织浓度高。

Objective: To study the pharmacokinetics and tissue distribution of flomoxef (Fmox) in rabbits. Methods: Rabbits were given Fmox single intravenous injection 50 mg/kg. The concentrations of Fmox in various body fluids and tissues were determined by HPLC method. Results: The two compartment open pharmacokinetic model was in accordance with plasma concentration time curve following iv 50 mg/kg of Fmox. Fmox was quickly distributed and the half life of distribution ( t 1/2α ) was 0.023 h. The elimination half life( t 1/2β ) was 0.213 h. Aera under the plasma concentration time curve (AUC) was (79.94±13.31)h·μg/ml. The concentrations of Fmox were high in urine, bile, lung, kidney, ovary and uterus. Conclusion: Fmox is a oxacephem antibiotics with wide distribution, high tissue concentrations and short elimination half life.