诺氟沙星联合加味藿香正气丸治疗急性胃肠炎的108例临床观察

目的探究诺氟沙星联合加味藿香正气丸治疗急性胃肠炎的临床效果,为临床治疗提供理论依据。方法将在2000年3月至2012年8月之间,入院治疗的108位患有急性肠胃炎的患者,随机分为两组（观察组与对照组）。对照组仅使用诺氟沙星治疗,观察组则是诺氟沙星联合加味藿香正气丸治疗。对比观察两组的疗效。结果观察组治疗有效率为为98．1％,对照组为72．2％,观察组患者在腹泻、发热等方面的急性胃肠炎症状明显减少,具有明显的临床疗效优势。结论诺氟沙星联合加味藿香正气丸治疗急性胃肠炎临床疗效良好,可以较好地减少急性胃肠炎的症状,减轻患者痛苦,具有较大临床研究价值。     

诺氟沙星的吸附行为及其测定

诺氟沙星在0.05mol·L^-1NH₄Cl (pH 5.8)溶液中,出现一灵敏的示波极谱还原峰。峰电位为-1.44 V (vs SCE)。峰高与诺氟沙星的浓度在1.0×10^-7～4.0×10^-6mol·L^-1范围内成正比,检出限为5.0×10^-8mol·L^-1,并用于样品的测定。用线性扫描与循环伏安法等手段研究体系的吸附性质。实验表明,该电极过程为具有吸附性的不可逆过程。     

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。     

Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-MG single oral dose in human patients

Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chromatography, and the microbiologically active compounds were quantified by a microbiological assay. Both procedures were correlated (r>0.7); nevertheless, slight differences detected in concentrations depended on the levels of norfloxacin achieved in the biological samples. The serum and tissue concentrations were higher than the concentration of bactericide (4 g·ml^–1), except in one case. The uroepithelium concentration of pefloxacin was proportional to the serum concentration (r=0.79). The urinary concentrations ranged from 1.2 g·ml^–1 to 82.4 g·ml^–1. The mean norfloxacin/pefloxacin ratios were 3% in serum, 8% in uroepithelium, and 44% in urine. The mean uroepithelium/serum concentration ratios were 1 for pefloxacin and 2.3 for norfloxacin. This result shows that, at a time close to that of the maximum concentration, there is good penetration of pefloxacin and norfloxacin into the uroepithelium.     

Studies on Effect of Piperine on Oral Bioavailability of Ampicillin and Norfloxacin

Ampicillin and Norfloxacin are used to treat variety of bacterial infections. These two drugs have low oral bioavailability. Co-administration of Piperine (20mg/kg), an alkaloid from Piper nigrum L. enhanced oral bioavailability of Ampicillin and Norfloxacin in animal model. This is reflected in various pharmacokinetic measurements like Cmax, Tmax, AUC and t½ of the above antibiotics in animal model.     

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。     

诺氟沙星金属盐的合成及体外抑菌实验

目的：合成诺氟沙星金属盐五种化学单体。方法：以诺氟沙星及数种金属盐为原料进行化学合成试验。以固体培养基平板药敏试验方法对诺氟沙星金属盐合成品作体外抑菌试验。并作抑菌活性观察。结果：完成诺氟沙星银、诺氟沙星锌、诺氟沙星铈、诺氟沙星钴、诺氟沙星铋五种金属盐的合成及其初步质量标准制订。结论：初步体外抑菌实验表明。诺氟沙星银、诺氟沙星锌、诺氟沙星铈、诺氟沙星钴、诺氟沙星铋对金葡萄球菌、大肠杆菌、绿脓假单胞菌的抑制作用明显高于磺胺嘧啶银。     

氟哌酸和黄连素对志贺氏菌耐药性质粒消除研究

用氟哌酸和黄连素对２０株携有接合传递耐药性质粒（Ｒ质粒）及１９株携有非接合传递耐药性质粒（ｒ质粒）志贺氏菌进行体外消除研究。结果显示，可被消除的耐药性质粒大多数在２４小时内被消除。氟哌酸对Ｒ质粒及ｒ质粒消除率分别为５％和５２．６％，黄连素对Ｒ质粒及ｒ质粒消除率分别为１０％和５７．９％，两种药物对ｒ质粒消除率明显优于对Ｒ质粒消除率，其原因可能与ｒ质粒分子量小，非传递性及在药物作用下易于丢失有关。氟哌酸和黄连素均为广谱抗菌药物，因此在临床上治疗感染的同时又能消除耐药性质粒，阻止耐性扩散。     

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.