环丙沙星对疟原虫子孢子活力的影响

约氏疟原虫子孢子与新型抗生素环丙沙星不同剂量共同孵育３０ｍｉｎ后腹腔接种昆明株小鼠体内．观察环丙沙星对子孢子活力的影响。环丙沙星分为１、２、４、６、μｇ／ｍｌ５种剂量，另外设双抗（青霉素十链霉素）对照组和ＰＢＳ对照组，每组接种５只小鼠，每鼠０．１ｍｌ，内含１０．５×１０４子孢子，３ｄ后尾静脉取血镜检，结果环丙沙星各试验药物组原虫血症出现的平均时间分别为３．８、３．６、３．８、３．８、３．２ｄ，双抗对照组和ＰＢＳ对照组均为３．８ｄ。结果提示环丙沙星剂量达８μｇ／ｍｌ与子孢子孵育３０ｍｉｎ后仍对子孢子活力无影响。     

荧光分光光度法测定盐酸环丙沙星片的含量

采用荧光分光光度法测定盐酸环丙沙星片的含量简便、快速、灵敏度高。线性范围为０．１～０．５μｇ／ｍｌ，平均回收率为１００．０４％，相对标准差为０．６０％。     

环丙沙星短程治疗伤寒20例

本文应用环丙沙星（治疗组）治疗伤寒２０例，开始退热天数１．８±０．７天，热退至正常天数３．５±１．７天。另用诺氟沙星（对照组）治疗伤寒３０例，开始退热天数４．０±１．５天，热退至正常天数７．５±３．０天。结果表明：环丙沙星治疗组总有效率１００％，明显高于诺氟沙星对照组（总有效率８３％，Ｐ＜０．０５）。治疗组中开始退热天数及退至正常天数比对照组均有非常显著差异性（Ｐ＜０．０１），无毒性副作用，未见有复发，值得临床推广。     

乳酸环丙沙星原料药的含量测定方法探讨

目的 :考察乳酸环丙沙星的含量测定方法。方法 :采用紫外分光光度法及双相滴定法测定乳酸环丙沙星原料药的含量。结果 :紫外分光光度法回归方程为 A=0 .0 116 3+0 .12 83C,平均回收率为 (99.7± 0 .4 0 ) % ,双相滴定法测得平均回收率为 (10 0 .4± 0 .11) %。结论 :两种方法结果均较好且无显著区别 ,有利于医院制剂室的检测     

氟喹诺酮类与其它抗菌药物治疗淋病的疗效对比观察

本文对133例单纯性淋病患者用氧氟沙星、环丙沙星、壮观霉素和青霉素G进行疗效对比观察。结果其治愈率分别为100％、100％、96.8％和94.6％,经统计学处理无显著性差异。对所用的四种药物用琼脂双倍稀释法对96株淋球菌进行了体外抗菌活性测定。结果氧氟沙星和环丙沙星耐药率为0,壮观霉素耐药率为6.3％,青霉素耐药率为24.0％,经统计学处理有显著性差异。用Nitrocefin法对96株淋球菌进行了β-内酰胺酶测定,其产青霉素酶淋球菌(PPNG)阳性率为3.1％。     

侧脑室注射环丙沙星对大鼠脑电,脑电功率谱及频率分配的影响

以不同剂量的环丙沙星（３皿ｕｇ·Ｋｇ－１及６００ｕｇｋｇ－１）注入大鼠右侧脑室后，于皮层感觉运动区记录皮层脑电图作脑电功率谱及频率分配分析。注射后两剂量组皮层均先后出现痫样放电（大剂量、小剂量组潜伏期分别为３５．３３±３５．１６和１５３．８８±９４．２１９）脑电功率谱及频率分配分析主要表现为总功率及脑电的快成分（ａ、β和β２）所占百分比增加而功率主峰频段δ波所占百分比减少。提示：环丙沙星对中枢神经系统具有兴奋作用。     

Application of terbium sensitized fluorescence for the determination of fluoroquinolone antibiotics pefloxacin, ciprofloxacin and norfloxacin in serum

A simple, rapid and sensitive spectrofluorimetric method for the determination of fluoroquinolone antibiotics, norfloxacin (NOR), ciprofloxacin (CIP) and pefloxacin (PEF) is described. The method is based on the radiative energy transfer from fluoroquinolones to terbium ions (Tb³⁺) in the presence of tri-n-octylphosphine oxide (TOPO) in weakly acidic (pH 5.5) micellar solution of cetylpyridinium chloride (CPCI). Optimum conditions for the formation of the fluoroquinolone-Tb³⁺-TOPO ternary complexes have been investigated. Under optimized conditions the detection limits are 1.7, 1.2 and 4.4 nM for NOR, CIP and PEF, respectively, while the range of application for all three drugs is 0.05–10 μM. The method has been successfully applied to the determination of NOR, CIP and PEF in serum samples after deproteinization with acetonitrile (serum-acetonitrile; 1:2, v/v). The mean recoveries from serum samples spiked with NOR, CIP and PEF (5.0–50.0 μM) were (90.3 ± 4.9), (105.0 ± 3.6) and (95.3 ± 1.5)%, respectively. Within-run and day-to-day s_r values for 5.0, 25.0 and 50.0 μM of each fluoroquinolone varied from 1.7 to 5.4% and from 3.3 to 12.8%, respectively. The influence of several usually coadministered drugs on the determination of fluoroquinolones in serum has been investigated.     

Decreased ciprofloxacin absorption with concomitant administration of ferrous fumarate

The effect of ferrous fumarate on the relative bioavailability of ciprofloxacin after a single 500 mg oral dose of ciprofloxacin was studied in eight healthy males. Blood samples were collected at regular intervals 0–24 h post-dose. Urine was collected during 24 h to determine the cumulative urine excretion of ciprofloxacin. Ciprofloxacin concentrations in serum and urine were determined by high pressure liquid chromatography. Mean area under the serum concentration—time curve decreased significantly (P<0.001) after ciprofloxacin was taken with 200 mg ferrous fumarate. The relative bioavailability was 30% when ciprofloxacin was given with ferrous fumarate. The maximum blood level decreased from 2.1±0.9 (control) to 0.6±0.2 mg/l (with ferrous fumarate). Further studies are needed to determine if chronic treatment with ferrous fumarate further decreases the relative bioavailability. For the moment administration of ciprofloxacin with ferrous fumarate should therefore be avoided.     

413株细菌对氧氟沙星等3种喹诺酮类药物敏感试验

用氧氟沙星、环丙沙星、诺氟沙星对从我院各种标本分离出的４１３株细菌作敏感试验，试验菌株有金葡球菌、克雷伯氏菌、大肠杆菌、绿脓假单胞菌等常见病原菌。药敏试验结果表明：这３种药物对革兰氏阴性杆菌和部分革兰氏阳性球菌敏感率仍达７０％￣９９％，甚至更高，但比以往文献报道的敏感明显下降。本文提示要合理应用喹诺酮类药物，减少耐药菌株增加。     

Concentrations in plasma, urinary excretion and bactericidal activity of levofloxacin (500 mg) versus ciprofloxacin (500 mg) in healthy volunteers receiving a single oral dose

In a randomised crossover study, 14 volunteers received a single oral dose of 500 mg levofloxacin or 500 mg ciprofloxacin in order to assess plasma concentrations by high-pressure liquid chromatography (up to 24 h), urinary excretion and urinary bactericidal titres (UBTs) at intervals up to 120 h. The median maximum concentration of levofloxacin in plasma was 6.1 mg/L and that of ciprofloxacin was 2.3 mg/L. The median cumulative level of renal excretion of the administered dose of the parent drug was 81.2% for levofloxacin and 36.2% for ciprofloxacin. UBTs were determined for a reference strain and nine clinical uropathogens. The median UBTs of both quinolones measured within the first 12 h were between 0 and 1:≥1024, correlating with the minimum inhibitory concentrations (MICs) of the strains. For Gram-negative strains, the UBTs of both quinolones were comparable despite the lower MICs of ciprofloxacin. During further time courses, however, the UBTs of levofloxacin were significantly higher than those of ciprofloxacin. For Gram-positive strains, for which the MICs of levofloxacin were equal to or lower than those of ciprofloxacin, the UBTs of levofloxacin were already significantly higher from the beginning. It can be concluded that overall the doses of the two tested fluoroquinolones may be considered equivalent with regard to treatment of complicated urinary tract infections, although the recommended dosing is twice daily for ciprofloxacin and once daily for levofloxacin.