司帕沙星与洛美沙星的抗生素后效应

对比研究两种新氟喹经物司帕沙星和洛美沙星的抗生素后铲应。方法：应用ＡＶＡＮＴＡＧＥ自动微生物分析仪的光密度法测定抗生素后效应。结论ＳＰＬＣ和ＬＭＬＸ均可产生明显的后效应,提示设计药药方案时均应考虑抗生素后效应的因素。     

甲磺酸帕珠沙星对临床常见致病菌体外抗菌活性及抗生素后效应观察

目的：观察甲磺酸帕珠沙星对临床常见致病菌的体外抗菌作用及对大肠埃希氏菌和肺炎克雷伯氏菌的抗生素后效应（PAE）。方法采用琼脂稀释法测定甲磺酸帕珠沙星对临床常见致病菌的最低抑菌浓度（MIC）;采用稀释法和菌落计数法观察甲磺酸帕珠沙星不同浓度时对大肠埃希氏菌和肺炎克雷伯氏菌的 PAE。结果甲磺酸帕珠沙星对临床常见致病菌存在较强的抗菌活性;药物在浓度为8 MIC、4 MIC、2 MIC 时,对大肠埃希氏菌和肺炎克雷伯氏菌产生明显的 PAE,且随着药物浓度的增大,PAE 值随之增大。结论甲磺酸帕珠沙星对对大肠埃希氏菌和肺炎克雷伯氏菌存在明显的 PAE,且测试菌对甲磺酸帕珠沙星存在浓度依耐性。     

培福沙星抗生素的后效应

目的研究新喹诺酮类药物培福沙星的抗生素后效应(PAE).方法应用AVANTAGE自动微生物分析仪的光密度法测定培福沙星抗生素后效应.结果培氟沙星(PFLX)对金黄色葡萄球菌、表皮葡萄球菌和铜绿假单胞菌均产生明显的PAE,药物随浓度增大而PAE也随之延长,除4×MIC与8 × MIC对金黄色葡萄球菌的PAE结果对比无显著性差异外,其余各药物浓度间对比有显著性差异(p＜0.05),呈浓度依赖性关系.结论PFLX均产生明显的抗生素后效应,呈现明显的剂量依赖性,对于临床合理应用抗生素具有重要实际意义.     

氧氟沙星与哌拉西林单用或联合应用的抗生素后效应

本文应用ＡＶＡＮＴＡＧＥ分析仪的微生物比浊法测定了氧氟沙星（ＯＦＬＸ）与哌拉西林（ＰＩＰＣ）单用或联合应用的抗生素后效应（ＰＡＥ），结果表明ＯＦＬＸ单用时对受试革兰氏阳性球菌和革兰氏阴性杆菌均产生明显的ＰＡＥ；ＰＩＰＣ单用时对革兰氏阳性球菌ＰＡＥ较明显，对革兰氏阴性杆菌ＰＡＥ较小，两药单用时ＰＡＥ值随药物浓度增高而显著增大，而两药联用时，对革兰氏阴性杆菌均呈现协同或相加ＰＡＥ；对革兰氏阳球菌的ＰＡ     

3种氟喹诺酮类药物的体外抗生素后效应研究

目的研究3种氟喹诺酮类药物对铜绿假单胞菌、金黄色葡萄球菌、大肠埃希氏菌的体外抗生素后效应（PAE）,为临床优化氟喹诺酮类药物给药方案提供参考依据。方法采用微量稀释法测定左氧氟沙星（LVFX）、司帕沙星（SPLX）和环丙沙星（CPLX）等3种氟喹诺酮类药物的最低抑菌浓度（MIC）和体外PAE。结果LVFX对铜绿假单胞菌的PAE最长,对金黄色葡萄球菌的PAE最短;SPLX对大肠埃希氏菌的PAE最长,对铜绿假单胞菌的PAE最短;CPLX对大肠埃希氏菌的PAE最长,对金黄色葡萄球菌的PAE最短;三种氟喹诺酮药物对试验菌株均呈现浓度依赖性。结论临床使用氟喹诺酮类药物时应重视其抗生素后效应。     

3种氟喹诺酮类药物抗生素后效应的研究

应用AVANTAGF分析仪的光密度法测定了环丙沙星（CPLX）、氧氟沙星（OFLX）和氟罗沙星（FLRX）的抗生素后效应（PAE）．结果表明氟喹诺酮类抗菌药物对革兰氏阳性球菌和革兰氏阴性杆菌均产生明显的PAE．并随抗菌药物浓度的增大、对受试菌的PAE逐渐延长．呈现了明显的浓度依赖性；3种抗菌药物对铜绿假单胞菌的PAE都较长．MIC均较小．显示了良好的杀菌效果：氯罗沙星对除金葡球菌之外的受试菌的PAE均比其它2药较长．PAE的存在提示在临床设计给药方案时．可适当延长给药间期．减少给药次数与剂量．仍能维持抗菌效果。     

磷霉素与环丙沙星联用的体外抗生素后效应研究

对比研究磷霉素单用与联用环丙沙星的抗生素后效应。方法采用微量稀释法测定最低抑菌浓度,微量接菌落计数法测定ＰＡＥ。结果磷霉素对金葡球菌有明显的ＰＡＥ,对大肠埃希菌呈浓依赖性,与环丙沙星合用,浓虎在４ＭＩＣ以上时呈现明显的相加作用。结论两药联用时抗菌作用增强。     

司帕沙星注射液与氧氟沙星注射液随机对照临床试验

目的　评价司帕沙星注射液治疗急性细菌性感染的有效性与安全性。方法　采取随机对照及开放试验 ,以氧氟沙星注射液做对照 ;司帕沙星剂量 2 0 0 mg qd或 q12 h,氧氟沙星剂量 2 0 0 mg q12 h,疗程为 5～14 d。结果　共治疗患者 76例 ,试验组 39例 ,对照组 2 0例 ,开放组 17例。大针剂组 (GI) :试验组、对照组与开放组的有效率分别为 84 .2 1%、85 .0 0 %与 88.89% ;小针剂组 (MI) :各组有效率分别为 85 .0 0 %、85 .0 0 %与10 0 % ,在 GI组中试验组、对照组、开放组的细菌清除率分别为 92 .86 %、87.5 0 %、10 0 % ,在 MI组分别为80 .0 0 %与 87.5 0 %、10 0 % ,试验组与对照组之间的差异无计学意义 (P>0 .0 5 )。试验组的不良反应发生率为15 .0 0 % (GI)、10 .0 0 % (MI) ,对照组为 10 .0 0 % ,无统计学差异 (P>0 .0 0 5 )。开放组的不良反应发生率为0 .0 0 % (GI)与 12 .5 0 % (MI)。结论　司帕沙星注射液抗菌谱广、抗菌活性强 ,为一治疗中、重度急性细菌性感染安全有效的注射用药物。     

抗生素后效应

抗生素后效应是近年来在抗生素化疗领域中受到重视的一种新理论。本文将各种抗生素的抗生素后效应加以综述。     

帕珠沙星与左氧氟沙星治疗尿路感染的疗效比较

目的比较帕珠沙星与左氧氟沙星治疗尿路感染的疗效。方法尿路感染患者60例随机分成帕珠沙星组与左氧氟沙星组各30例,分别给予帕珠沙星300mg,左氧氟沙星200mg,均为静脉滴注,bid,疗程5~14d。结果帕珠沙星组与左氧氟沙星组的有效率分别为96.4%和92.6%,痊愈率分别为85.7%和70.3%,均差异无显著性(P>0.05)。结论帕珠沙星与左氧氟沙星治疗尿路感染的临床疗效相当。     

Crossover assessment of serum bactericidal activity of grepafloxacin, ofloxacin and clarithromycin against respiratory pathogens after oral administration to healthy volunteers

Serum bactericidal activity was studied in a crossover manner in 10 volunteers, after 2-day administration of grepafloxacin 600 mg qd, ofloxacin 400 mg bid and clarithromycin 500 mg bid. Bactericidal activity against clinical isolates of Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis and Klebsiella pneumoniae, was estimated using a standardized microdilution method. Grepafloxacin was highly active against Gram-negative organisms and adequate against pneumococci (mean, 1:13.3). Clarithromycin was very active against both penicillin-susceptible and penicillin-partially-resistant S. pneumoniae (1:102.5) but had poor activity against H. influenzae (1:3.1). Minor adverse effects were commonly associated with grepafloxacin.     

Postantibiotic effects and postantibiotic sub-MIC effects of erythromycin, roxithromycin, tilmicosin, and tylosin on Pasteurella multocida

When intermittent dosing is used during treatment, the concentrations of antibiotics fluctuate and subinhibitory concentrations may occur between doses. Postantibiotic effects (PAEs) and postantibiotic subinhibitory effects (PA SMEs) on bacteria may provide additional, valuable information for the rational use of a drug in clinical practice. In this study tilmicosin was the most active antibiotic tested against P. multocida type D with MICs ranging from 4–16 mg/l. Roxithromycin and tilmicosin induced a statistically significantly longer PAE than did tylosin against P. multocida types A and D (P<0.05). The duration of PAEs and PA SMEs were proportional to the concentrations of drugs used for exposure. The PA SMEs were substantially longer than PAEs on P. multocida. Tilmicosin had a longer PA SME compared with erythromycin, roxithromycin and tylosin for P. multocida. The computerized incubator used in the present study provided an efficient and convenient determination of PAE and PA SME, allowing frequent measurements of the bacterial growth.     

Postantibiotic effects and postantibiotic sub-MIC effects of erythromycin, roxithromycin, tilmicosin, and tylosin on Pasteurella multocida

When intermittent dosing is used during treatment, the concentrations of antibiotics fluctuate and subinhibitory concentrations may occur between doses. Postantibiotic effects (PAEs) and postantibiotic subinhibitory effects (PA SMEs) on bacteria may provide additional, valuable information for the rational use of a drug in clinical practice. In this study tilmicosin was the most active antibiotic tested against P. multocida type D with MICs ranging from 4–16 mg/l. Roxithromycin and tilmicosin induced a statistically significantly longer PAE than did tylosin against P. multocida types A and D (P<0.05). The duration of PAEs and PA SMEs were proportional to the concentrations of drugs used for exposure. The PA SMEs were substantially longer than PAEs on P. multocida. Tilmicosin had a longer PA SME compared with erythromycin, roxithromycin and tylosin for P. multocida. The computerized incubator used in the present study provided an efficient and convenient determination of PAE and PA SME, allowing frequent measurements of the bacterial growth.     

异质性耐万古霉素溶血葡萄球菌的抗生素后效应研究

目的检测万古霉素对异质性耐万古霉素溶血葡萄球菌（heterogeneous-vancomycin-resistant Staphylococcus haemolyticus,h-VRSH）的抗生素后效应（postantibiotic effect，PAE），探讨h-VRSH的存在对万古霉素体外杀菌活性的影响。方法采用微量稀释法检测金葡菌标准菌株ATCC29213和h-VRSH（原代培养）的最低抑菌浓度（MIC），以菌落平板计数法检测最低杀菌浓度（MBC）和PAE；分析万古霉素对h-VRSH耐药性产生的影响，以及这种耐药性的稳定性。结果金葡菌ATCC29213的MIC和MBC分别为1和16μg／ml，h-VRSH（原代）的MIC和MBC分别为2和64μg／ml；两者PAE分别为0．9和2．4h。结论与敏感菌株不同，h-VRSH的PAE明显延长；原代培养MIC为2μg／ml的h-VRSH其MBC可达到64μg／ml，高于万古霉素有效血药浓度峰值（20～40μg／m1）。提示单独使用万古霉素已经不能完全清除h-VRSH，葡萄球菌对万古霉素的异质性耐药不容忽视。     

舒巴克坦对头孢哌酮体外抗生素后效应的影响

目的 考察合用β-内酰胺酶抑制剂舒巴克坦（ＳＢＴ）前后头孢哌酮（ＣＰＺ）对４种致病菌抗生素后效应（ＰＡＥ）的变化。方法 采用特异性β-内酰胺酶鉴定试剂Ｎｉｔｒｏｃｅｆｉｎ挑选大肠埃希氏杆菌、金黄色葡萄球菌、变形杆菌和绿脓假单胞菌的产酶菌株，用比浊法测定受试菌株在不同ＣＰＺ浓度时的ＰＡＥ值。结果 合用ＳＢＴ后，ＣＰＺ对产酶菌株的ＰＡＥ均有不同程度的延长，低浓度时（１／２，１倍ＭＩＣ）ＰＡＥ增加更明显（Ｐ＜０．０５）。结论 合并ＣＰＺ和ＳＢＴ的给药方案对治疗产β-内酰胺酶菌株引起的感染有利，尤其在体内药物浓度较低时，合并用药可以更长时间地抑制细菌生长。     

Gastroretentive hydrodynamically balanced systems of ofloxacin: In vitro evaluation

Hydrodynamically balanced systems (HBSs) of ofloxacin were prepared using lactose, HPMC K4M, PVP K 30, and liquid paraffin, which may increase the mean residence time in the gastrointestinal tract, and may be able to provide maximum drug at the site of absorption to improve oral bioavailability. All these formulated HBS capsules were floated well over 6 h with no floating lag time. They also showed sustained drug release over 6 h. Time for 50% release of ofloxacin was within the range, 2.47 ± 0.02 to 3.07 ± 0.08 h. The in vitro drug release from these HBS capsules was dependent on HPMC K4M, PVP K 30, and liquid paraffin content. The drug release pattern of these HBS capsules containing ofloxacin followed the Higuchi model with the anomalous transport mechanism.     

用流式细胞仪分析抗生素后效应中细菌的生物学特征

目的　了解亚胺培南、环丙沙星、庆大霉素、头孢他啶四种抗生素对大肠埃希氏菌、铜绿假单胞菌抗生素后效应 (PAE)中细菌的大小及核酸含量的改变。方法　将处于亚胺培南、环丙沙星、庆大霉素、头孢他啶后效应中的大肠埃希氏菌、铜绿假单胞菌 ,用碘化丙啶 (PI)染色 ,流式细胞仪检测。结果　亚胺培南、环丙沙星PAE中 ,两种菌体积与核酸含量均增大 ;庆大霉素PAE中 ,两种菌体积与核酸含量不变 ;头孢他啶作用后的大肠埃希氏菌体积、核酸含量增大 ,铜绿假单胞菌没有变化。结论　这些变化与抗生素作用机制有关。用流式细胞仪能快速、直观分析细菌的生物学特征。     

加替沙星和环丙沙星体外抗生素后效应期间大肠埃希氏菌菌体大小及DNA含量变化研究

目的　研究加替沙星和环丙沙星体外抗生素后效应期间大肠埃希氏菌 ATCC2 5 92 2菌体大小及 DNA含量变化 ,为探讨 PAE形成机理提供实验依据。方法　于加替沙星 (1、2、4 MIC)及环丙沙星 (1、2、4 MIC)体外 PAE期间不同时间点吸取培养物 ,以荧光探针碘化丙啶进行染色 ,经流式细胞仪分析大肠埃希氏菌 ATCC2 5 92 2菌体大小及 DNA含量变化。结果　加替沙星 (1、2、4 MIC)和环丙沙星 (1、2、4 MIC) PAE期间大肠埃希氏菌 ATCC2 5 92 2菌体显著增大 ,胞内 DNA含量明显增加 ,且呈剂量依赖性 ,当加替沙星 4 MIC与蛋白合成抑制剂氯霉素及 RNA合成抑制剂利福平联用时 (终浓度分别为 0 .0 2和 0 .16 mg/ L) ,这一变化被抑制。结论　应用流式细胞仪辅以荧光探针碘化丙啶可检测加替沙星及环丙沙星 PAE期间细菌菌体大小和DNA含量变化 ,该方法快捷、简便、直观。     

HPLC测定氧氟沙星胶囊中氧氟沙星的含量

目的建立高效液相色谱法测定氧氟沙星胶囊中氧氟沙星的含量。方法用D ikm a-C18色谱柱,以0.05 mol/L枸橼酸-乙腈(79∶21)用三乙胺调节pH值至4.0为流动相,检测波长293 nm。结果线性范围:20~40μg/m l;r=0.9993。加样回收率为99.8%,RSD=0.65%。结论本法测定氧氟沙星胶囊的含量,方法专属性强,简便,可靠,测定结果准确。