单剂量加替沙星口服在Beagle犬体内药代动力学研究

Pharmacokinetics of a Single Dose of Oral Gatifloxacin in Beagle Dogs

目的探讨加替沙星口服后在Beagle犬体内药代动力学。方法将18只Beagle犬分为3组,分别灌服34,17,8.5mg/kg加替沙星,于给药后0.5,1,2,4,6,8,12,24,36,48,60h取血,以高效液相色谱法测定血药浓度,用3P97程序分析。结果高、中、低剂量组动物吸收相半衰期(t1/2ka)分别为(0.82±0.96),(0.78±0.77),(1.33±0.43)h,消除相半衰期(t1/2ke)分别为(7.33±1.79),(6.32±3.28),(5.34±2.60)h,达峰时间(tmax)分别为(6.32±2.32),(3.95±2.18),(5.77±1.62)h,峰浓度(Cmax)分别为(6.31±2.66),(2.67±0.64),(0.64±0.30)mg/mL。药时曲线下面积(AUC0→60)分别为(110.86±43.76),(41.93±5.58),(8.58±2.70)μg·h/mL。结论加替沙星口服易吸收,血药浓度高,代谢慢,临床使用方便。

Objective To study the pharmacokinetics of a single dose of oral gatifloxacin capsules in Beagle dogs. Methods 18 Beagle dogs were divided into 34,17,8.5 mg/kg groups,single dose of 34,17,8.5 mg/kg of gatifloxacin was administrated. The blood samples were taken at 0. 5,1,2,4, 6,8,12,24,36,48,60 h after oral administration. The concentration of gatifloxacin in serum was determined by a HPLC method,pharmacokinetic parameters were calculated with pharmacokinetic program （3P97）. Results The concentration- time curves of gati- floxacin fitted to one - compartment model, t1/2ke was （0.82 ± 0. 96）, （0. 78 ± 0. 77）, （1.33 ± 0. 43）h respectively, t1/2ke was （7.33 ± 1.79）, （6. 32 ± 3.28）, （5.34 ± 2.60） h respectively, tmax was （6.32 ± 2.32）, （3.95 ± 2.18）, （5.77 ± 1.62） h respectively, Cmax was （6.31 ± 2.66）, （2.67 ± 0. 64）, （0.64±0.30） mg/mL respectively, AUC0→60 was （110.86 ± 43.76）, （41.93 ± 5.58）, （8.58 ± 2. 70） μg· h/mL respectively. Conclusion The gatifloxacin was absorbed rapidly, and high in plasma, and metabolized slowly. The convenience is oral administration gatifloxacin in clinical practice.