CAJ | 학술논문

为考察托氟沙星纳米乳的体外抑菌活性及体内药效作用，用CLSI推荐的微量肉汤稀释法测定托氟沙星纳米乳的最低抑菌浓度（MIC）和最低杀菌浓度（MBC），并与盐酸左氧氟沙星进行比较；以鼠伤寒沙门菌人工感染的雏鸡为研究对象，测定不同浓度托氟沙星纳米乳的体内药效作用。体外抑菌试验表明，托氟沙星纳米乳对无乳链球菌、金黄色葡萄球菌、多杀巴氏杆菌、大肠埃希菌、痢疾志贺菌、鼠伤寒沙门菌、甲型副伤寒沙门菌的 MIC 为0．25μg／mL～2．00μg／mL，其抑菌活性是托氟沙星原药的2倍～4倍，盐酸左氧氟沙星的2倍～8倍；MBC 为0．25μg／mL～4．00μg／mL，其抗菌活性是托氟沙星原药的2倍～8倍，盐酸左氧氟沙星的2倍～8倍。体内药效试验结果表明，低剂量（40 mg／L）和中剂量（60 mg／L）的托氟沙星纳米乳可显著降低鼠伤寒沙门菌感染雏鸡的死亡率和体重损失。托氟沙星纳米乳以纳米乳作为药物载体，增强了托氟沙星对临床常见细菌的体内外抵抗作用，提高了托氟沙星的临床应用价值。
위고찰탁불사성납미유적체외억균활성급체내약효작용，용CLSI추천적미량육탕희석법측정탁불사성납미유적최저억균농도（MIC）화최저살균농도（MBC），병여염산좌양불사성진행비교；이서상한사문균인공감염적추계위연구대상，측정불동농도탁불사성납미유적체내약효작용。체외억균시험표명，탁불사성납미유대무유련구균、금황색포도구균、다살파씨간균、대장애희균、이질지하균、서상한사문균、갑형부상한사문균적 MIC 위0．25μg／mL～2．00μg／mL，기억균활성시탁불사성원약적2배～4배，염산좌양불사성적2배～8배；MBC 위0．25μg／mL～4．00μg／mL，기항균활성시탁불사성원약적2배～8배，염산좌양불사성적2배～8배。체내약효시험결과표명，저제량（40 mg／L）화중제량（60 mg／L）적탁불사성납미유가현저강저서상한사문균감염추계적사망솔화체중손실。탁불사성납미유이납미유작위약물재체，증강료탁불사성대림상상견세균적체내외저항작용，제고료탁불사성적림상응용개치。
The aim of this study was to investigate the antibacterial activity in vitro and pharmaceutical effect in vi-vo of tosufloxacin nanoemulsion.Microtiter broth dilution method recommended by Clinical and Laboratory Stand-ards Institute (CLSI)was adopted to determine the MIC and MBC of tosufloxacin nanoemulsion and compared with that of levofloxacin hydrochloride;the pharmaceutical effect was evaluated by oral administration to the model chicks successfully infected with Salmonella typhimurium containing different concentrations of tosufloxacin nano-emulsion.The results showed the MICs of tosufloxacin nanoemulsion against Streptococcus agalactiae ,Staphylo-coccus aureus ,Pasteurella multocida,Escherichia coli,Shigella dysenteriae ,Salmonella typhimurium,Salmonella paratyphi-A were 0.25 μg/mL-2.00 μg/mL.Their MICs were about 2-4 and 2-8 fold stronger than that of its o-riginal form and levofloxacin hydrochloride respectively;the MBCs were 0.25 μg/mL-4.00 μg/mL and about 2-8 fold stronger than that of its original form and levofloxacin hydrochloride.Invivo ,the tosufloxacin nanoemulsion in low(40 mg/L)and middle doses(60 mg/L)significantly reduced the mortality and weight loss of the model chicks caused by Salmonella typhimurium,obviously ameliorated the symptoms.It can be concluded that tosufloxacin nanoemulsion as a novel type of drug can enhance the efficacy of tosufloxacin on common bactrerials and expand the clinical application value.