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常用抗生素在动物及人胆汁中的浓度分布和药效学研究 |
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【摘要】 目的 研究常用抗生素在胆汁中的浓度和对致病菌的抗菌活性。方法 分别静脉注射常用6种抗生素后于不同时间收集家兔胆汁标本，采用高效液相色谱法测定各抗生素的浓度，计算出药动学参数；测定胆道手术患者胆汁常用5种抗生素浓度，对临床分离的157株胆道细菌进行抗菌活性分析。结果家兔胆汁平均药峰浓度较高的为：哌拉西林7 950.16 μg/ml，头孢哌酮5 274.52 μg/ml，头孢曲松1 107.01 μg/ml。在患者胆总管和胆囊胆汁中的平均浓度较高的为：头孢哌酮/舒巴坦563.75/14.76和169.90/8.83 μg/ml，哌拉西林/他唑巴坦350.38/16.69和139.81/15.92 μg/ml，头孢曲松249.78和82.06 μg/ml。美罗培南和莫西沙星的体外抗菌活性最强，增加β内酰胺酶抑制剂后的哌拉西林和头孢哌酮复合制剂较单一制剂的抗菌活性显著增强。头孢哌酮/舒巴坦、哌拉西林/他唑巴坦、莫西沙星对胆道致病菌的杀菌指数最大。结论 家兔胆汁中6种测定的抗生素均超过有效杀菌浓度，哌拉西林、头孢哌酮、头孢曲松胆汁药物浓度很高。头孢哌酮/舒巴坦和哌拉西林/他唑巴坦、莫西沙星在人胆汁中杀菌效力最强，可作为肝胆系统感染经验治疗的首选用药。
【关键词】 抗生素； 胆汁； 浓度； 药效学； 高效液相色谱法
Concentration distribution and pharmacodynamics of antibiotics in bile of human and animals LIANG Lijian, ZHENG Jinglei, PENG Baogang, LI Dongming, YIN Xiaoyu, LI Shaoqiang, L Mingde, HUANG Jiefu. Department of Hepatobiliary Surgery, First Affiliated Hospital of Sun YatSen University, Guangzhou 510080, China
【Abstract】 Objective To study the concentrations of general antibiotics in bile of human and rabbit and their antimicrobial activity to the biliary pathogenic bacteria so as to provide guidance for choosing effective antibiotics for hepatobiliary infection. Methods The rabbits were administered intravenously with the equaleffect dose of six antibiotics. Bile (1.5 ml) was collected at different time points after administration for assaying the concentration of antibiotics in the bile by high performance liquid chromatography (HPLC). The bile drug concentrationtime data were processed by software to figure out the pharmacokinetic parameters. For further study, common duct bile and gallbladder bile of patients were collected to measure concentrations of 5 general antibiotics and detect antimicrobial activity of 157 strains of bateria separated for infected bile. The bile antibiotics concentration contrasted to the minimum inhibitory concentration (MIC), and attained the bactericidal index ([1] [2] [3] [4] [5] [6] 下一页
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