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法罗培南、比阿培南的体外抗结核活性研究

Research on Activities of in vitro Anti-Tuberculosis of Faropenem and Biapenem
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摘要 目的:优化法罗培南(FP)、比阿培南(BP)联合β-内酰胺酶抑制剂的种类与配比,筛选出具有最强抗结核活性的组方。方法:采用微孔板阿尔玛蓝染色法(microplate alamar blue assay,MABA),通过测定结核分枝杆菌标准株H37Rv的最低抑菌浓度(MIC)确定FP、BP联合β-内酰胺酶抑制剂的种类与配比,以临床分离株验证药物组合的抗结核活性;采用MABA法测定药物组合与6种二线抗结核药两两联合应用的MIC,计算分级抑菌浓度(FIC)以评价药物的体外相互作用。结果:FP、BP与克拉维酸钾(CLV)以CLV固定质量浓度2.5μg/ml组合对H37Rv的MIC分别为2、1μg/ml;FP/CLV对88%的临床分离株的MIC比FP的MIC低2~4倍,BP/CLV对92%的临床分离株的MIC比BP的MIC低4~8倍;FP/CLV与对氨基水杨酸钠、丙硫异烟胺,BP/CLV与卷曲霉素、氨基水杨酸钠和丙硫异烟胺为协同作用,BP/CLV与利奈唑胺、左氧氟沙星为部分协同作用,BP/CLV与氯苯酚嗪为相加作用,其他联合为无关作用。结论:FP/CLV、BP/CLV两种组合有良好的抗结核活性,BP/CLV活性更强,且与常用的二线抗结核药有良好的联合作用。 OBJECTIVE:To optimize the type and matching of faropenem(FP)and biexpenem(BP)combined with lactamase inhibitors,so as to screen out the composition with the strongest anti-tuberculous activity.METHODS:The microplate alamar blue assay(MABA)was adopted to determine the type and matching of FP and BP combined with lactamase inhibitors by measuring the minimum inhibitory concentration(MIC)of mycobacterium tuberculosis standard strain H37Rv,and the anti-tuberculosis activity of the drug combinations was verified by clinical isolated strains;the MIC of drug combination in two-drug combinations with six anti-tuberculous drugs were determined by MABA method,and the in vitro drug interactions was evaluated by calculating the fractionated inhibition concentration(FIC).RESULTS:The MIC of FP and BP combined with potassium clavulanate(CLV)in fixed CLV concentration of 2.5μg/ml against H37Rv were respectively 2μg/ml and 1μg/ml;for the MIC of clinical isolated strains,the FP/CLV were 2-4 times lower than FP in 88%of strains,and the BP/CLV were 4-8 times lower than BP in 92%of strains;FP/CLV was synergistic with sodium aminosalicylate and protionamide,BP/CLV was synergistic with capromycin,sodium aminosalicylate and protionamide,BP/CLV was partially synergistic with linezolid and levofloxacin,BP/CLV and clofazimine had additive effect,and other combinations were unrelated.CONCLUSIONS:FP/CLV and BP/CLV have good anti-tuberculous activity,BP/CLV is more active and has a good combination with commonly used second-line anti-tuberculous drugs.
作者 赵伟杰 刘婧 李芃 郭振勇 ZHAO Weijie;LIU Jing;LI Peng;GUO Zhenyong(Office of Drug Clinical Trial Institutions,Beijing Chest Hospital Affiliated to Capital Medical University,Beijing 101149,China;Dept.of Pharmacy,Beijing Chest Hospital Affiliated to Capital Medical University,Beijing 101149,China)
出处 《中国医院用药评价与分析》 2021年第5期513-516,521,共5页 Evaluation and Analysis of Drug-use in Hospitals of China
基金 十三五“重大新药创制”(No.2017ZX09304009)。
关键词 法罗培南 比阿培南 抗结核活性 相互作用 Faropenem Biapenem Activity of anti-tuberculosis Interaction
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