四联活菌肠溶胶囊治疗32例慢性腹泻的疗效分析

目的研究探讨四联活菌肠溶胶囊治疗慢性腹泻的临床疗效,并研究其作用机制及原理。方法将近两年来我院接收并诊断为慢性腹泻的60例患者采用完全随机分组法,分为实验组(32例)和对照组(28例),分别给予四联活菌肠溶胶囊和若氟沙星药物进行治疗,观察其疗效与不良反应及并发症,并记录数据。结果治疗2周左右实验组患者的临床总有效率为90.85%,而对照组患者的临床总有效率为71.36%,相比之下四联活菌肠溶胶囊治疗慢性腹泻的临床疗效更加明显。结论四联活菌肠溶胶囊治疗慢性腹泻的临床疗效较好,且无明显不良反应及并发症出现,值得在临床上做进一步探讨研究。     

Norfloxacin-Poly(l-Lysine Citramide Imide) Conjugates and Structure-dependence of the Drug Release

Norfloxacin (Nflx), an antibiotic which is active against some intracellular bacteria, was coupled to a polymeric carrier, namely poly(_l-lysine citramide) via a lysine or an ethylcarbamate spacer to obtain a macromolecular prodrug. The carrier, which derived from the two metabolites citric acid and _l-lysine, is known to be biocompatible and slowly degradable under slight acidic conditions. Conjugates were characterised by UV, ¹H and ¹³C NMR and SEC. The presence of Norfloxacin and the lysine type spacer caused chain aggregation, due to a probable physical cure. The release of Norfloxacin from these prodrugs and from a prodrug where Norfloxacin is bound to the carrier backbone without spacer arm was investigated comparatively in vitro. Conjugation via a carbamate-type linkage appeared as a method to achieve the release of Norfloxacin from a PLCA-type conjugate at neutral.     

一起伤寒爆发流行菌株的药敏试验分析

目的：探讨伤寒菌株耐药谱及当地诊所使用的７个厂家１２个批号治疗用药氟哌酸的疗效。方法应用琼脂扩散法，对５株伤寒杆菌用１２种抗菌素及氟哌酸胶囊自制的纸片进行药敏测定。结果本次流行中分离的菌株具有多重耐药，对氯霉素、羧苄青霉素、氨苄青霉素耐药，对氟哌酸、庆大霉素、丁胺卡拉、头孢三嗪、头孢克罗敏感，在１２个批号的氟哌酸中，有３个批号的氟哌酸与标氟哌酸纸片两者的抑菌环大小有明显差异。结论１９９８年贵州省威     

SCS药物缓释凝胶的制备及其体外释药研究

以壳聚糖硫酸酯作为骨架材料,盐酸诺氟沙星为模型药物。研究壳聚糖硫酸酯凝胶在药物缓释中的应用。探讨盐酸诺氟沙星缓释凝胶的体外释药规律。初步阐明其释药机理。考察支联度、投药量、温度、不同释放介质对释药的影响。结果表明盐酸诺氟沙星缓释凝胶有一定的缓释特性,且具有温度／pH敏感性。     

诺氟沙星胶囊的实时溶出度监测

目的建立诺氟沙星胶囊的实时溶出度的测定方法,以评价药物的质量。方法采用FODT-601型光纤药物溶出度实时测定仪对4个厂家生产的诺氟沙星胶囊的实时溶出过程进行监测。结果选定290 nm为测定波长,诺氟沙星在20～120μg/ml范围内吸收度值与浓度间的线性关系良好。应用本方法监测的不同厂家诺氟沙星溶出度结果与依照《中华人民共和国药典》2010年版（二部）该制剂规定方法监测结果基本一致,但不同生产厂家的溶出曲线存在一定的差异。结论 FODT-601型光纤药物溶出度实时测定仪可反映药物的真实溶出过程,不需取样分析,减少了操作步骤,测定结果准确。     

诺氟沙星滴入兔眼与注入球结膜下其组织分布及药动学比较

用高效液相色谱法对诺氟沙星点眼与球结膜下注射后眼各组织药物浓度进行测定，比较两种给药途径的眼各组织浓度及其药物动力学参数。结果表明，诺氟沙星点眼与球结膜下注射后４ｈ，泪液诺氟沙星浓度分别为２．０８±０．１９与１６．０７±３．１４μｇ／ｍｌ（Ｐ＜０．０１）；角膜分别为０．７１±０．０７与１．６５±０．２４μｇ／ｇ（Ｐ＜０．０１）。泪液ＡＵＣ分别为９８．３３±７．３１与２７９．８２±３１．７ｈ·μｇ／ｍｌ；角膜ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ、Ｔ１／２Ｋｃ分别为１７．４２±１．２１ｈ·μｇ／ｇ、８．９４±０．８μｇ／ｇ、０．５７±０．０６ｈ、０．９１７±０．１６ｈ与２０．０１±１．０１ｈ·μｇ／ｇ、１０．０５±０．０７μｇ／ｇ、０．４５±０．０５ｈ、１．１５±０．２０ｈ；房水ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ分别为１．１３±０．２１ｈ·μｇ／ｍｌ、０．３９±０．０５μｇ／ｍｌ、０．６２±０．０９ｈ与１．７９±０．０７ｈ·μｇ／ｍｌ、１．００±０．１５μｇ／ｍｌ、０．４７±０．１０ｈ。诺氟沙星点眼与球结膜下注射两种给药途径的上述药动学参数有明显差异（Ｐ＜０．０５或０．０１）。     

脂质饮食对诺氟沙星在Beagle犬体内药动学的影响

目的:研究脂质饮食对诺氟沙星在Beagle犬体内药动学的影响。方法:取6只Beagle犬均分为两组,分别在空腹或进食脂质状态下灌服诺氟沙星胶囊40 mg/kg,2周后两组犬交叉实验;采用高效液相色谱法测定给药前与给药后0.5、1、2、3、4、6、8、10、12、24 h的血药浓度,用3p97软件计算诺氟沙星的药动学参数。结果:诺氟沙星在Beagle犬空腹和进食脂质状态下的药-时曲线均符合一室模型;空腹和进食脂质状态下诺氟沙星的主要药动学参数分别为t1/2(3.82±1.10)、(4.30±1.78)h,tmax(0.72±0.37)、(2.94±1.12)h,cmax(0.93±0.18)、(0.92±0.43)μg/ml,AUC0-24 h(6.26±0.98)、(8.45±1.78)μg·h/ml;两种状态间比较,除tmax差异有统计学意义(P<0.01)外,其余参数差异无统计学意义(P>0.05)。结论:脂质饮食可明显延迟诺氟沙星的达峰时间。     

Effects of norfloxacin and butylated hydroxyanisole on the freshwater microalga Scenedesmus obliquus

The toxic effects of norfloxacin (NOR) and butylated hydroxyanisole (BHA) on the microalga Scenedesmus obliquus were assessed in terms of growth rate, concentration of chlorophyll a, activities of 7-ethoxyresorufin-o-dealkylases (EROD), glutathione s-transferase (GST), catalase (CAT) and total malondialdehyde content (MDA). The 96 h EC₅₀ was 38.49 and 11.12 mg/l for NOR and BHA, respectively. Growth of S. obliquus was affected slightly under low concentrations of BHA (<4 mg/l) and NOR (<15 mg/l) over the 96 h exposure period. With the increasing concentrations of these two compounds, growth of S. oblique decreased significantly. Growth inhibition was 82.4% at 60.0 mg/l for NOR and 60.6% at 16.0 mg/l for BHA after 96 h. A similar trend was also observed for chlorophyll a. NOR and BHA affected Phase I and Phase II enzyme activities differently. Upon exposure to NOR, EROD was induced at concentration <15.0 mg/l and depressed at concentrations >30 mg/l significantly. CAT and GST exhibited similar trends during the exposure period. Compared to controls, MDA content only showed high induction at high concentrations of NOR (>30 mg/l). However, EROD activity did not display any change compared to control responses during BHA exposure, whereas GST showed significant induction for all concentrations over the exposure period. CAT activity showed induction at low concentration and depression at high concentration. MDA content increased with the rise of BHA during the exposure period. These types of assays, revealing toxic effects of NOR and BHA to phototrophs, could be employed to assess the potential risks of these xenobiotics to aquatic ecological systems.     

Spectrophotometric determination of some fluoroquinolone antibacterials by binary complex formation with xanthene dyes

Two simple, rapid and sensitive spectrophotometric methods for the determination of levofloxacin, norfloxacin and ciprofloxacin have been performed in pure form, pharmaceutical tablets and spiked human urine. Both methods are based on the formation of a binary complex between the drugs and one of the two xanthene dyes, eosin Y or merbromin in aqueous buffered medium. Under the optimum conditions, the binary complexes showed absorption maxima at 547 nm for eosin Y and 545 nm for merbromin. Using eosin Y, the calibration graph was linear over the range 2-8 microg ml(-1) for the three drugs with mean percentage recoveries 99.935 +/- 0.648, 99.973 +/- 0.678 and 100.011 +/- 0.606 for levofloxacin, norfloxacin and ciprofloxacin, respectively. While in case of merbromin, the concentration range was 2-15 microg ml(-1) with mean percentage recoveries 99.960 +/- 0.491, 100.017 +/- 0.510 and 99.980 +/- 0.506 for the three drugs, respectively. The proposed methods were successfully applied to determine these drugs in their tablet formulations and spiked human urine and the results compared favorably to that of reference methods. The suggested methods have the advantage of being applicable for the determination of the three drugs without prior extraction. They are recommended for quality control and routine analysis where time, cost effectiveness and high specificity of analytical techniques are of great importance.     

口服氢氧化铝对静注诺氟沙星体内药动学的影响

利用紫外分光光度法测定家兔血中的诺氟沙星浓度,对静注诺氟沙星在口服铝盐前后的体内药动力学的情况进行了研究。结果显示单独静注诺氟沙星与同时口服铝盐两种方案给药的药动学参数无显著性差异。本实验为临床合理用药提供了参考资料。