氧氟沙星葡萄糖注射液的抗菌作用

通过对氧氟沙星葡萄糖注射液体内外抗菌作用的研究,认为氧氟沙星葡萄糖注射液是一种抗菌谱广,抗菌活性强的抗菌药,它对革兰氏阳性菌的最小抑菌浓度范围为 0.8～0.3βg/ml,与氧氟沙星原料相比没有降低其药效。氧沙星葡萄糖注射液对革兰氏阳性菌的抗菌作用强于诺氟沙星注射液的4倍左右,对小鼠感染金黄色葡萄球菌(S.aureus)和肺炎杆菌(K.Pncumoniae)强3～6倍。     

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.     

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。     

High-performance liquid chromatographic determination of ciprofloxacin in plasma samples

A new bioanalytical high-performance liquid chromatographic (HPLC) method for the determination of ciprofloxacin with norfloxacin as an internal standard was developed and validated for plasma samples. Norfloxacin is structural homologue of ciprofloxacin and exhibits similar retention properties. The quality of respective peak separation is strongly influenced by amphoteric character of ciprofloxacin and norfloxacin as well. In previously published HPLC methods on conventional C18 reversed-phase [F. Belal, A.A. Al-Majed, A.M. Al-Obaid, Talanta 50 (1999) 765–786; G. Carlucci, J. Chromatogr. A 812 (1998) 343–367], ion pair reagents were added into the mobile phase to suppress peak tailing. In comparison with endcapped and high purity silica reversed-phase sorbent (Purospher RP-18e, Merck), which yielded symmetrical peaks, separation efficiency was further enhanced in our method. Gradient elution mode using acetonitril and phosphate buffer pH 3 on the pentafluorophenylpropyl stationary phase (250–4.6 mm Discovery^® HS F5, 5 μm, Supelco) was carried out. The resolution of 4.1 for ciprofloxacin–norfloxacin peaks was achieved. Sample preparation by SPE C18 (Supelclean) with recovery 72% was performed. Fluorescence detection with λ_excit = 280 nm, λ_emis = 446 nm was used. After the validation, the bioanalytical HPLC method was applied to pharmacokinetic studies.     

二甲酚橙褪色分光光度法测定乳酸诺氟沙星含量

目的二甲酚橙褪色分光光度法测定乳酸诺氟沙星的含量。方法在碱性介质中,乳酸诺氟沙星与二甲酚橙染料反应,形成电荷转移化合物,使二甲酚橙溶液颜色发生明显改变,最大褪色波长在577nm,以此建立了测定乳酸诺氟沙星的褪色分光光度法。结果在pH7.0～12.0的碱性介质条件下,诺氟沙星与二甲酚橙形成2∶1型电荷转移化合物。在最大褪色波长处,乳酸诺氟沙星浓度在6.22×10^-6～9.33×10^-5mol/L范围内褪色程度与乳酸诺氟沙星浓度有良好的线性相关;精密度RSD为3.6%;方法回收率为（92.0±4.6）%。结论二甲酚橙褪色分光光度法操作简便,有较高的灵敏度和良好的选择性。用于乳酸诺氟沙星的含量测定,结果较为满意。     

Synthesis and antibacterial evaluation of novel 8-fluoro Norfloxacin derivatives as potential probes for methicillin and vancomycin-resistant Staphylococcus aureus

A series of novel 8-fluoro Norfloxacin derivatives and the hybrids of its piperazinyl derivatives incorporated with 1,3,5-triazine and pyrimidine were synthesized. All the above compounds were evaluated for their antibacterial activity against Klebsiella pneumoniae, methicillin-resistant Staphylococcus aureus and methicillin & vancomycin-resistant S. aureus. Among all, compounds having Morpholine, N-methyl/phenyl/benzyl/pyrimidinyl piperazines and n-butylamine substitution at C-7 position, have shown increased potency in comparison to norfloxacin and ciprofloxacin.     

龙血竭诺氟沙星治疗褥疮的体会

目的探讨褥疮的治疗护理经验。方法彻底清洗创面后,使用龙血竭诺氟沙星混合粉;每天早晚各换药一次;同时加强患者营养;并实施心理护理。结果全部病例经过龙血竭、诺氟沙星治疗,褥疮创面痊愈。结论及时给予有效的治疗护理,是治疗褥疮的重要保障。     

诺氟沙星与Me-β-CD的包合能力的研究

目的:本文利用紫外可见分光光度法、荧光光谱法、核磁共振法研究了β-CD的衍生物Me-β-CD对诺氟沙星的分子识别作用。对在不同pH溶液中的包合效果进行研究。方法:用紫外、荧光的方法进行包合常数(K)的计算,并进一步用NMR表征了包合物的结构及机制。结果:随着Me-β-CD的浓度增加,包合物的紫外、荧光均增强,而且Me-β-CD易于包合中性型体的诺氟沙星。结论:诺氟沙星与Me-β-CD在溶液中形成了稳定的包合物。     

福氏志贺菌对诺氟沙星耐药性及耐药机制的研究

目的研究福氏志贺菌对诺氟沙星的耐药性及耐药机制。方法收集福氏志贺菌３０株,进行抗菌药物敏感试验,４株耐药菌,１株敏感菌和福氏志贺菌标准菌５１５７３的ｇｙｒＡ基因的Ｎ末端编码区进行ＰＣＲ扩增并克隆和测序。结果福氏志贺菌对诺氟沙星的耐药率高达５３．３％,ｇｙｒＡ基因的序列分析结果揭示存在３个导致氨基酸改变的基因点突变：丝氨酸８３→亮氨酸,天冬氨酸８７→天冬酰氨,天冬氨酸８７→甘氨酸。结论福氏志贺菌对诺氟沙星已有较高的耐药性,ｇｙｒＡ基因点突变与福氏志贺菌对诺氟沙星的耐药性有关。