盐酸左氧氟沙星在大鼠胰腺的药代动力学研究

目的 研究盐酸左氧氟沙星在大鼠胰腺组织的药代动力学.方法 采用微透析技术对大鼠胰腺组织和血液进行同步取样,联合反相高效液相色谱实时检测胰腺组织和血液中盐酸左氧氟沙星的浓度变化,所得药物浓度数据用WinNonlin软件处理.结果 大鼠血液中的游离左氧氟沙星浓度在给药后10 min时最高,为(65.23±12.9)μg/ml,胰腺组织在20 min到达峰浓度(30.56±3.22)μg/ml,然后持续下降;给药后20 min时胰腺组织的药物浓度开始高于血清,并持续至100 min,然后下降,两者浓度始终保持接近.血液、胰腺的药时曲线下面积分别为(2914.38±205.73)min·μg~(-1)·ml~(-1)和(2465.11±258.56)min·μg~(-1)·ml~(-1).结论 微透析采样技术联合反相高效液相色谱检测方法可以准确客观地反映药物在组织和血液中的药代动力学特点,盐酸左氧氟沙星具有较高的胰腺组织药物浓度.

Pharmacokinetics of levofloxacin in rat pancreas

Objective To investigate the pharmaeokinetics of levofloxacin in rat's pancreatic tissue. Methods Pancreatic tissue and blood were sampled in vivo by microdialysis simultaneously. The concentrations of levofloxacin in beth blood and tissues were measured by high performance liquid chromatography. All date were analyzed by WinNonlin software. Results The maximum concentration of free levofloxacin in blood and pancreatic tissue were (65.23 ± 12.9) μg/ml at 10min and (30.56±3.22) μg/ml at 20 min, respectively, then beth continuously decreased. Concentration of free levofloxacin in pancreatic tissue was higher than that in blood from 20min to 100min, then returned to similar level. The area under the concentration curve(AUC)of unbound levofloxacin was(2465.11±258.56)min·μg~(-1)·ml~(-1) in pancreas,and (2914.38±205.73)min·μg~(-1)·ml~(-1) in blood.Conclusions Microdialysis with reversed phase high performance liquid chromatography established in this essay could be used to determine the pharmacokinetics of levofloxacin objectively. High concentration of levofloxacin in pancreatic tissue and blood was observed.