盐酸左氧氟沙星在前列腺炎大鼠体内药代动力学探究.docVIP

盐酸左氧氟沙星在前列腺炎大鼠体内药代动力学探究 　 作者：马小林 李英伦 崔恒敏 赵玲 【摘要】 　　目的研究细菌性前列腺炎病理模型下，盐酸左氧氟沙星(Levofloxacin Hydrochloride)在大鼠体内的药代动力学特征。方法36只大鼠造成细菌性前列腺炎病理模型后，单剂量一次灌胃内服盐酸左氧氟沙星［80 mg/(kg·bw)］；采用高效液相色谱法测定血药浓度，血药浓度最低检测限0.001μg/ml，并以DAS 2.0药动学软件对所得数据进行分析。结果药物体内过程符合一级吸收二室模型（权重=1/CC），主要动力学参数及拟合方程如下：T1/2Ka为(45.294±2.07) min,T1/2α为(63.963±15.258)min，T1/2β为(280.535±214.601) min，Tmax为(50±17.321)min，Cmax为(14.905±3.143) mg/L，AUC(0-1440)为(2 561.219±430.592)(mg·min·L-1)，Ka为(0.015±0.001)min-1，MRT（0→1440）为（196.865±50.656）min，拟合方程为：C=66.697·e-0.011t+6.031·e-0.004t-72.728·e-0.015t。结论盐酸左氧氟沙星在细菌性前列腺炎模型大鼠体内吸收迅速，血药浓度较高，分布广泛，消除较为缓慢。 【关键词】 盐酸左氧氟沙星 细菌性前列腺炎 药代动力学 大鼠 高效液相色谱 　　Abstract:ObjectiveTo study the pharmacokinetics of Levofloxacin Hydrochloride in pathological model of rats with bacterial prostatitis. MethodsGive the drug to 36 rats with bacterial prostatitis model at a dosage of 80 mg per kilogram of body weight orally.Plasma Levofloxacin Hydrochloride concentrations were determined by high performance liquid chromatography,with a limit of detection of 0.001μg of Levofloxacin Hydrochloride per milliliter of plasma.Plasma Levofloxacin Hydrochloride pharmacokinetic data were calculated by using DAS2.0 pharmacokinetics software. ResultsThe fate of drug was consistent with finst order absorption and two compartement models (weight=1/CC), major kinetia parameters of pharmacokinetics and equation were as follows: T1/2ka=(45.29±2.07) min, T1/2a=(63.963±15.258) min, T1/2β=(280.535±214.601) min, Tmax=(50±17) min, Cmax=(14.905±3.143) mg/L,AUC(0～1440)=(2561.219±430.592)(mg·min-1·L-1),Ka=(0.015±0.001)(1/min),MRT(0～1440)=(196.865±50.656)min,C=66.697·e-0.011t+6.031·e-0.004t-72.728·e-0.015t.ConclusionLevofloxacin Hydrochloride in pathological model of rats with bacterial prostatits is quickly absorbed with high concentration in plasma, distributed widespread, and eliminated slowly. 　　Key words:Levofloxacin Hydrochloride； Prostatitis； Pharmacokinetics； Rats； HPLC 　　前列腺炎(prostatitis)是男性泌尿系统的常见病与多发病，具有病因病理复杂，症状表现多样化，