制备环丙沙星的哌嗪化工艺

采用乙氧羰基哌嗪与环丙羧酸缩合的方法，制备了环丙沙星。同时应用正交设计实验，研究了原料配比、温度、时间及溶剂用量对反应收率的影响，在优化条件下收率可达88．0％。     

Mucoadhesive liposomes as ocular delivery system: physical,microbiological, and in vivo assessment

Background: Mucoadhesive drug delivery is a promising strategy to overcome ocular biopharmaceutical constraints. Objective and methods: Ciprofloxacin HCl-loaded reverse phase evaporation liposomes were coated with different concentrations and molecular weights of mucoadhesive biocompatible chitosan polymer to form chitosomes. This colloidal mucoadhesive system was evaluated in vitro and in vivo with respect to deliver the antibiotic to ocular surface. Results and conclusion: The results obtained pointed out that liposome coating process resulted in entrapment efficiency reduction and higher chitosan concentration, and molecular weight showed a more pronounced effect. No morphological differences between coated and uncoated liposomes were observed. Diffusion was the drug release mechanism from chitosomes. Concerning rheological behavior, pseudoplastic flow was characteristic to the prepared chitosomal dispersions. In addition, chitosan coating improved the ocular permeation of ciprofloxacin HCl. Microbiologically; this formulated system enhanced antimicrobial activity of ciprofloxacin HCl against both Gram-positive and Gram-negative bacteria. Moreover, this mucoadhesive system was able to inhibit the growth of Pseudomonas aeruginosa in rabbits' eyes for 24 hours when compared to the marketed preparation. In vivo bacterial conjunctivitis model elucidated that symptoms were controlled by the prolonged release formulation such as that done by the marketed product.     

Synthesis of Vegetable Fat Containing Chitosan Microparticles with Improved Physical and Delivery Properties

The present study describes the encapsulation of vegetable fats (cocoa butter and mango butter) within chitosan microparticles by double emulsion technique to prevent leaching of the internal apolar phase. Leaching studies suggested negligible leaching of the internal phase (～12–14%) when the fats were encapsulated as compared to the control (～40%). Fourier transform infrared spectroscopy and differential scanning calorimeter studies confirmed the successful encapsulation of fats. The release of drug (ciprofloxacin) from the microparticles was diffusion and erosion mediated and were capable to elicit antimicrobial activity against Escherichia coli. The study suggests that the developed microparticles have the potential for controlled delivery of antimicrobials.     

环丙沙星-磷钼多金属氧酸盐的制备及热分解动力学

报道了环丙沙星与十二磷钼酸的多金属氧酸盐化合物,用元素分析、IR、TG-DTA等方法对其进行了表征,结果显示该化合物仍保持Keggin型结构特征。同时,采用TG-DTG技术研究了标题化合物在氮气气氛中的热分解机理及非等温动力学,它的热分解过程经历了3个阶段,其中间体和残余物运用TG-DTG、IR和XRD 技术进行了确证。采用Achar方程、Coats-Redfern方程、Kissinger方程、Flynn-Wall-Ozawa方程和Starink方程对非等温动力学数据进行了分析,得到了第3步热分解反应的机理函数、动力学参数和热分解反应动力学方程,其热分解反应过程受F3（化学反应）机理控制, 表观活化能为351 kJ·mol-1,指前因子为2.57×10 30s-1。     

同时检测恩诺沙星和环丙沙星单克隆抗体的制备

为了产生同时检测恩诺沙星和环丙沙星的抗体,本研究采用戊二醛法制备突出恩诺沙星和环丙沙星共同结构的人工抗原。免疫Balb/c 小鼠的结果显示：使用糖基化载体所制备的免疫抗原,能够大幅提高所产生特异性抗体的滴度。通过细胞融合,筛选出一株对恩诺沙星和环丙沙星IC50 值分别为9.6ng/mL 和10.2ng/mL 的单克隆抗体。     

壳聚糖微球对环丙沙星吸附的研究

采用分光光度法研究了功能高分子壳聚糖及其微球对环丙沙星的吸附及控制释放;考察了吸附时间、初始浓度及pH值对吸附的影响。     

Synthesis and evaluation of ciprofloxacin-loaded carboxymethyl tamarind kernel polysaccharide nanoparticles

Nanotechnology is currently employed as a tool to fight more efficiently against human pathogens. Nanoparticles can be prepared from a variety of materials such as protein, biodegradable polymers and synthetic polymers. Tamarindus indica Linn. or tamarind is one of the most important biodegradable polymer. In the present study, chemically modified polymer of tamarind ‘carboxymethyl tamarind kernel polysaccharide’ (CMTKP) is used for the synthesis of nanoparticulate formulation. Antibacterial activity of CMTKP was analysed which was then enhanced by incorporating a flouroquinolone antibiotic, ciprofloxacin to it. Ciprofloxacin-loaded CMTKP nanoparticles were synthesised via ionotropic gelation technique. Nanosuspension so formed was lyophilised by addition of a cryoprotectant. Nanoparticles obtained were characterised for its particle size, morphology and stability. Interaction studies were confirmed by Fourier transform infrared spectroscopy (FT-IR). Antibacterial activities of ciprofloxacin, CMTKP and ciprofloxacin-loaded CMTKP nanoparticles were tested against two Gram negative and positive bacteria. The antibacterial assay results revealed greatest zone of inhibition by ciprofloxacin-loaded CMTKP nanoparticles in Micrococcus luteus. Toxicity analysis of the prepared formulation was carried out on vero cell lines via resazurin assay which revealed its minimum toxicity.     

Differential patterns of antimicrobial resistance in population subsets of Escherichia coli isolated from waste- and surface waters

The species Escherichia coli comprises different subgroups with distinct phylogeny, physiology and ecology and, thus, presumably, with different roles in antimicrobial resistance dissemination. E. coli strains isolated from raw and treated municipal wastewater and from urban water streams were characterized in terms of phylogenetic groups, antimicrobial resistance patterns and the presence of class 1 and class 2 integrons. Our main objective was to investigate the contribution of the different phylo-groups in antimicrobial resistance dissemination in urban waters. Groups A and B1 were predominant in all types of water, evidencing, respectively, the lowest and the highest resistance prevalence. Municipal wastewater treatment was accompanied by significant increases of ciprofloxacin and streptomycin resistance (p < 0.01). Antimicrobial resistance prevalence differed significantly between the different phylo-groups and within the same group, mainly in group A. Such differences contributed to explain the higher ciprofloxacin and streptomycin resistance rates observed in treated effluent in comparison with the raw wastewater. We conclude that the dynamics of the bacterial populations has a major role on the dissemination of antimicrobial resistance in the environment.     

Dyeing of wool with antibiotics to develop novel infection resistance materials for extracorporeal end use

Two antibiotics, doxycycline (Doxy) and ciprofloxacin (Cipro), were applied under a variety of conditions to wool and to hydrolyzed wool at 40°C. Nylon was used as a synthetic control. Sorption of Doxy was much higher in wool than in nylon, whereas sorption of Cipro was similar in both fibers. FTIR spectroscopy confirmed that a drastic increase in sorption of antibiotics by hydrolyzed wool was attributed to an increase in polar functional groups by peptide scission and in oxidized sulfur groups by cystine oxidation. Both sorption and zone of inhibition (ZOI) values were improved by hydrolysis of wool. Wool hydrolyzed for 20 or 40 min at 40°C and dyed with Doxy at 45°C for 3.5 h maintained around 30 mm of ZOI after 24 h of challenge by a simulated flow of blood. Wool hydrolyzed for 60 min at 40°C and dyed with Cipro at 45°C for 3.5 h also maintained its antibiotic activity for an extended time. For the most part, ZOI values for nylon dyed by both antibiotics were zero within 24 h. This technique produced infection‐resistant biomaterials of potential use in extra‐corporeal biomedical and biological applications. © 2004 Wiley Periodicals, Inc. J Appl Polym Sci 92: 3343–3354, 2004