摘要
目的比较左氧氟沙星经灌胃或静注后,在家兔房水和玻璃体中的分布及其药动学过程。方法选取54只家兔,分别灌胃或静注左氧氟沙星24mg/kg,不同时间采集房水和玻璃体,以高效液相色谱法测定其中左氧氟沙星的浓度,3p97软件计算药动学参数。结果静注左氧氟沙星后,房水和玻璃体中的药物浓度明显高于灌胃给药(P<0.05,P<0.01);但给药1h后,玻璃体中的药物浓度与灌胃给药无明显差异(P>0.05)。左氧氟沙星静注给药后在房水和玻璃体中的Cmax和AUC(0→t)明显高于灌胃给药(P<0.05,P<0.01);但灌胃给药后在玻璃体中有更长的消除半衰期(P<0.05),且两种给药途径的达峰时间(tmax)无明显差异(P>0.05)。结论相对于灌胃给药,左氧氟沙星静注给药后在房水和玻璃体中有更高的药物浓度、Cmax和AUC(0→t);但左氧氟沙星经这两种途径给药后,均能迅速到达房水和玻璃体,且维持较长时间的有效抗菌浓度,值得临床联合序贯使用。
Objective To compare the distribution and pharmacokinetics of levofloxacin in aqueous humor and vitreous following intragastric or intravenous administration in rabbits. Methods 54 rabbits were randomized into two groups, intragastric or intravenous groups administered 24 mg/kg levofloxacin, respectively. The aqueous humor and vitreous were sampled at different time point after administration. The concentrations of levofloxacin in aqueous humor and vitreous were detected by HPLC, and the pharmacokinetics parameters were calculated by the 3p97 software program. Results After intravenous administration, the concentrations of levofloxacin in aqueous humor and vitreous were obviously higher than those following intragastric administration（P〈0.05, P〈0.01）, while there was no obvious difference on the concentrations of levofloxacin in vitreous 1 hours after intravenous or intragastric administration（P〉0.05）. The parameters of C andAUC（0→t） in aqueous humor and vitreous after intravenous administration were significantly higher than those after intragastric administration（P 〈 0.05, P 〈 0.01 ）, however, much longer elimination time was achieved in vitreous after intragastric administration （P〈0.05） and there were no obvious difference on the parameter of tmax between these two ways of administration（P〉0.05）. Conclusion Much higher concentration of levofioxacin could be detected, meanwhile much higher Cax and AUC（0→t）could be achieved in aqueous humor and vitreous after intravenous administration compared to intragastric administation, but levofloxacincould be rapidly distributed into both aqueous humor and vitreous and maintained a long period of effective antibiotic concentration after these two ways of administration. These two ways of levofloxacin administration preferred to be used sequentially in clinical practice.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2013年第5期375-380,共6页
Chinese Journal of Antibiotics
关键词
左氧氟沙星
房水
玻璃体
药动学
高效液相色谱
Levofloxacin
Aqueous humor
Vitreous
Pharmacokinetics
High performance liquid chromatography （HPLC）
