烟酸诺氟沙星和乳酸诺氟沙星在松浦镜鲤体内的药动学比较

Pharmacokinetics of Norfloxacin Nicotinate and Norfloxacin Lactate in Songpu Mirror Carp(Cyprinus carpio specularis)

应用高效液相色谱(HPLC)技术研究以相同浓度(30mg/kg)烟酸诺氟沙星和乳酸诺氟沙星对松浦镜鲤Cyprinus carpio specularis口灌给药后,药物在试验鱼血液、肝胰脏、肾脏中的药动学特征。相同给药剂量下,烟酸诺氟沙星和乳酸诺氟沙星在松浦镜鲤血浆中的血药浓度和时间关系均为一级吸收二室开放模型,吸收半衰期(t_(1/2ka))分别为0.061h、0.043h,消除半衰期(t_(1/2β))分别为29.969h、14.972h,达峰时间(T_(max))分别为0.327h、0.272h,达峰浓度(C_(max))分别为6.247mg/L、13.423mg/L,药时曲线下面积(AUC)分别为53.015mg·h/L、89.907mg·h/L,表观分布容积(V_d)分别为4.347L/kg、2.084L/kg。结果表明:在相同给药剂量下,乳酸诺氟沙星的吸收和消除速率均快于烟酸诺氟沙星,药物种类显著影响药动学特征。

Pharmacokinetics ofnorfloxacin nicotinate and norfloxacin lactate in Songpu mirror carp （Cyprinus carpio speeularis ） was studied in this experiment. The Songpu mirror carp were divided into two groups randomly and orally administed norfloxacin nicotinate and norfloxacin lactate in a single dose of 30 mg/kg, respectively. The blood was collected at 0.25 h, 0.5 h, 0.75 h, 1 h, 1.5 h, 2 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h after administration in the live fish during the whole process. The concentration of norfloxacin nicotinate and norfloxacin lactate was determined by high performance liquid chromatography （HPLC）, and the pharmacokinetics of norfloxacin nicotinate and norftoxacin lactate in plasma of Songpu mirror carp was analysed by DAS3.0. The results showed that after a single oral administration of the same doses respectively, the concentrations versus time of norfloxacin in plasma were all well described by two-department open model with first-order absorption. The absorption half-lives （t1/2ka） were 0.061 h, 0.043 h, respectively; the elimination half-lives （t1/2β） were 29.969 h, 14.972 h, respectively; the peak times （Tmax） were 0.327 h, 0.272 h, respectively; the maximum content （Cmax） were 6.247 mg/L, 13.423 mg/L, respectively; the area under concentration-time curve （A UC） were 53.015 mg h/L, 89.907 mg.h/L, respectively; the apparent volume of distribution （Vd） were 4.347 L/kg, 2.084 L/kg, respectively. The findings indicated that at the same dose, the absorption and elimination rate of norfloxacin lactate was faster than that of norfloxacin incotinate, the pharmacokinetic characteristics being significantly influenced by the drug type.