畜牧兽医学报 ›› 2006, Vol. 37 ›› Issue (6): 603-608.doi:

• 基础兽医 • 上一篇    下一篇

氧氟沙星缓释注射液在猪体内的药物动力学研究

呼秀智;肖希龙
  

  1. 1. 中国农业大学动物医学院,北京 100094;2.河北工程大学农学院,邯郸 056021
  • 收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2006-06-25 发布日期:2006-06-25

Studies on Pharmacokinetics of Ofloxacin Sustain-released Injection in Swine

HU Xiu-zhi;XIAO Xi-long   

  1. 1.College of Veterinary Medicine, China Agricultural University, Beijing 100094;2.Agricultural College, Hebei University of Engineering, Handan 056021
  • Received:1900-01-01 Revised:1900-01-01 Online:2006-06-25 Published:2006-06-25

摘要: 研究了氧氟沙星缓释注射液肌注给药后在猪体内的药物动力学特征,给药剂量为10mg/kg,采用反相高效液相色谱荧光检测法(HPLC-FLD)测定血浆中氧氟沙星浓度。采用3p97药物动力学程序软件处理药时数据,得出相关药物动力学参数。静注氧氟沙星注射液在猪体内的药物动力学过程符合无吸收一室开放式模型,肌注氧氟沙星注射液、缓释注射液在猪体内的药物动力学过程均符合一级吸收一室开放式模型。氧氟沙星缓释注射液的吸收半衰期(t1/2ka)为(0.292 0±0.102 4)h, 消除半衰期(t1/2ke)为(6.902 2±0.901 9)h,达峰时间(Tmax)为(1.379 5±0.373 2)h,达峰浓度(Cmax)为(2.148 1±0.296 1)μg/mL,生物利用度为(95.70±12.56)%,在猪体内的持效时间(MIC=0.5 μg/mL)为(15.736 4±1.854 2) h,与氧氟沙星注射液相比,该制剂的吸收半衰期延长,消除半衰期延长,达峰时间延迟,峰浓度降低,生物利用度提高,持效时间延长。

Abstract: The pharmacokinetic properties of ofloxacin (OFL) sustain-released injection in swine were studied by 10 mg/kg dosage administration of OFL. The concentrations of OFL in the plasma were determined by reversed-phase HPLC-FLD. Pharmacokinetic analysis was carried out by using a computer program (3p97, China Pharmacology Association). The OFL concentrations-time data were best described by a one-compartment open model after single intravenous administration of the OFL injection. The OFL concentrations-time data were both described by a one-compartment open model with first order absorption after single intramuscular administration of the OFL sustain-released injection and the OFL injection. The t1/2ka,t1/2ke,Tmax, Cmax and the bioavailability after intramuscular administration of the OFL sustain-released injection were(0.292 0±0.102 4)h, (6.902 2±0.901 9)h, (1.379 5±0.373 2)h,(2.148 1±0.296 1) μg/mL and (95.70±12.56)%,respectively. Moreover, its effective time (MIC=0.5 μg/mL)could be maintained (15.736 4±1.854 2) h. Compared with the OFL injection, t1/2ka and t1/2ke of the OFL sustain-released injection were both extended, and its Tmax was delayed. Its Cmax was reduced, and it had better bioavailability. These experimental results indicated that the OFL sustain-released injection has sustained-released and long-acting properties.