哌拉西林与氧氟沙星联合抗菌活性的研究(摘要)

目前对于严重的难治性感染性疾病常采用抗菌药物联合治疗。本文根据棋盘法设计,应用微量稀释法研究了酰脲类青霉素哌拉西林(Piperacillin,PIP)与氟喹诺酮类药物氧氟沙星(Ofloxacin,OFLX)的体外联合抗菌活性。

氟嗪酸在健康志愿者和病人体内药代动力学研究

本文以健康志愿者和病人为研究对象,用高效液相色谱法分别测定了在口服单剂量氟嗪酸片(ofloxacin)400mg后,体内血清、尿液中的药物浓度。用中国药理学会编制的药动学计算程序(3p87)处理了20例健康志愿者(老年组10列、成年组10例)和5例病人药动学参数,符合开放式单室模型。其结果如下:主要药动学参数成年组和老年组分别为:t1/2:5.26±.65,5.69±1.07h;Vd:0.77±0.21,1.17±0.55l/kg;AUC;68.

氧氟沙星(泰利必妥)人体药代动力学研究进展

氧氟沙星(ofloxacin,OFL,泰利必妥,Tarivid)为第三代喹诺酮化合物,主要抑制DNA螺旋酶,从而抑制DNA合成,使细菌迅速死亡。它具有广谱、高效抗菌作用,可供口服及注射应用。该药是日本第一制药株式会社于1981年研制成功,1985年在日本和德国上市以来,已在英美等80多个国家临床应用泰利必妥片剂。1987年在我国进行该制剂的临床验证.1988年获得批准在我国应用。

Second and third line treatment options for Helicobacter pylori eradication

Helicobacter pylori is a highly successful bacterium with a high global prevalence and the infection carries significant disease burden. It is also becoming increasingly difficult to eradicate and the main reason for this is growing primary antibiotic resistance rates in a world where antibiotics are frequently prescribed and readily available. Despite knowing much more about the bacterium since its discovery, such as its genomic makeup and pathogenesis, we have seen declining treatment success. Therefore, clinicians today must be prepared to face one, two or even multiple treatment failures, and should be equipped with sufficient knowledge to decide on the appropriate salvage therapy when this happens. This article discusses the factors contributing to treatment failure and reviews the second and thirdline treatment strategies that have been investigated. Established empiric second line treatment options include both bismuth based quadruple therapy and levofloxacin based triple therapy. Antibiotic testing is recommended prior to initiating third line treatment. In the event that antibiotic susceptibility testing is unavailable, third line treatment options include rifabutin, rifaximin and sitafloxacin based therapies.

Development of ELISA and immunochromatographic assay for ofloxacin

Two rapid, sensitive and reliable immunoassay methods, namely competitive indirect enzyme-linked immunosorbent assay (CI-ELISA) and colloidal gold-based immunochromatographic assay (CGIA), were developed to detect ofloxacin (OFL). The linear range of the CI-ELISA was from 0.5 to 128 ng/mL with a limit of detection (LOD) of 0.35 ng/mL. Good recoveries were obtained in analyzing simulated swine urine samples. The CGIA could accurately estimate OFL at concentrations as low as 10 ng/mL in less than 10 min, and test results were read visually without any instrument.

In vitro and in vivo evaluation of gastroretentive floating drug delivery system of ofloxacin

This study aimed to develop hydrophilicmatrix based controlled release gastroretentive drug delivery system of ofloxacin and conducting its in vitro and in vivo evaluations.Effervescent floating gastroretentive drug delivery system of ofloxacin was prepared utilizing Boxe Behnken statistical design with 3 factors,3 levels and 15 experimental trials.Formulation optimization was done by setting targets on selected responses.In vivo studies were carried out for the optimized formulation with 12 healthy human volunteers and obtained pharmacokinetic parameters were compared with themarketed once daily formulation,“Zanocin OD”.Optimized formulation showed satisfactory controlled in vitro drug release for more than 12 h with excellent buoyancy properties(floating lag time<1 min,floating duration>16 h).Optimized and marketed formulations were found to have similar in vitro release profile(f2¼79.22)and also were found to be bioequivalent.Serum ofloxacin concentration was well maintained above its reported minimum inhibitory concentrations for most of the pathogens for sufficiently longer duration.Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product despite their bioequivalence.Bettertherapeutic effect can be expected since ofloxacin exhibits concentration dependent killing.Hence,gastroretention can be a promising approach to enhance bioavailability of ofloxacin with narrow absorption window in upper GIT.

Highly sensitive trivalent copper chelate-luminol chemiluminescence system for capillary electrophoresis chiral separation and determination of ofloxacin enantiomers in urine samples

A simple,fast and sensitive capillary electrophoresis（CE） strategy combined with chemiluminescence（CL） detection for analysis of ofloxacin（OF） enantiomers was established in the present work.Sulfonated p-cyclodextrin（β-CD） was used as the chiral additive being added into the running buffer of luminol-diperiodatocuprate（Ⅲ）（K[Cu（HIO6）2],DPC） chemiluminescence system.Under the optimum conditions,the proposed method was successfully applied to separation and analysis of OF enantiomers with the detection limits（S/N=3） of 8.0 nM and 7.0 nM for levofloxacin and dextrofloxacin,respectively.The linear ranges were both 0.010-100 μM.The method was utilized for analyzing OF in urine;the results obtained were satisfactory and recoveries were 89.5-110.8%,which demonstrated the reliability of this method.This approach can also be further extended to analyze different commercial OF medicines.

Synthesis and Characterization of Soy Protein Isolate/MMT Nanocomposite Film for the Control Release of the Drug Ofloxacin

Nanocomposites were prepared by blending soy protein isolate with different percentage of MMT by melt extrusion technique. The nanocomposites were characterized by using, XRD, TEM, SEM and TGA methods. The XRD studies indicated the absence of diffraction peaks for the bio-nanocomposites. From the TEM studies it was ascertained that the degree of exfoliation increased with increase in MMT content. The morphology of the nanocomposites was ascertained from the SEM studies. The degradation pattern of the nano-composites was evaluated from the TG analysis. The drug delivery system of the nanocmposites was investigated by blending the nanocomposites with ofloxacin at different pH media. The various kinetic parameters were evaluated and the mechanism of drug delivery has been postulated based on the kinetic data.

Molecular Characteristics and Drug Susceptibility of Mycobacterium tuberculosis Isolates from Patients Co-infected with Human Immunodeficiency Virus in Beijing,China

70 clinical Mycobacterium tuberculosis strains isolated from AIDS patients in two HIV/AIDS referral hospitals in Beijing were used in this study.M.tuberculosis and non-tuberculosis mycobacterium（NTM）were identified by using multi-locus PCR.M.tuberculosis was genotyped by using 15-locus MIRU-VNTR technique and spoligotyping afterwards.Meanwhile,the drug susceptibilities of the strains to the four first-line anti TB drugs（rifampin,isoniazid,streptomycin, and ethambutol） and the four second-line anti-TB drugs （capreomycin, kanamycin, ofloxacin, and ethionanide） were tested with proportional method. In this study, M. tuberculosis and NTM strains isolated from AIDS patients with TB-like symptoms were identified and genotyping analysis indicated that Beijing genotype was the predominant genotype. In addition, the prevalence of drug-resistant TB, especially the prevalence of XDR-TB, was higher than that in TB patients without HIV infection.

Taste masking of ofloxacin and formation of interpenetrating polymer network beads for sustained release

The objective of this study was to carry out taste masking of ofloxacin(Ofl) by ion exchange resins(IERs)followed by sustained release of Ofl by forming interpenetrating polymer network(IPN) beads. Drug-resin complexes(DRCs) with three different ratios of Ofl to IERs(1:1, 1:2, 1:4) were prepared by batch method and investigated for in vivo and in vitro taste masking. DRC of methacrylic acid-divinyl benzene(MD) resin and Ofl prepared at a ratio of 1:4 was used to form IPN beads. IPN beads of MD 1:4 were prepared by following the ionic cross-linking method using sodium carboxymethyl xanthan gum(SCMXG) and SCMXG-sodium carboxymethyl cellulose(SCMXG-SCMC). IPN beads were characterized with FT-IR and further studied on sustained release of Ofl at different pH. In vivo taste masking carried out by human volunteers showed that MD 1:4 significantly reduced the bitterness of Ofl. Characterization studies such as FT-IR, DSC, P-XRD and taste masking showed that complex formation took place between drug and resin. In vitro study at gastric pH showed complete release of drug from MD 1:4 within 30 min whereas IPN beads took 5 h at gastric pH and 10 h at salivary pH for the complete release of drug. As the crosslinking increased the release kinetics changed into non-Fickian diffusion to zero-order release mechanism. MD 1:4 showed better performance for the taste masking of Ofl and IPNs beads prepared from it were found useful for the sustained release of Ofl at both the pH, indicating a versatile drug delivery system.

氧氟沙星与左氧氟沙星治疗急性泌尿系感染的临床疗效与经济学分析

急性泌尿系统感染是临床常见的感染性疾病之一。治疗方案颇多,疗效不一。本研究采用药物经济学方法,对氧氟沙星(ofloxacin)和左氧氟沙星(levo-floxacin)治疗泌尿系感染的方案进行回顾性成本-效果分析,旨在为临床合理、经济用药提供参考。1临床资料1.1病例选择2009年7月～2010年3月来我科就诊的泌尿系统感染者85例(经病史、体征。

Correlations between Gene Resistant Markers and Second-Line Anti-TB Drug Resistance in Pre-XDR and XDR-TB Patients

Background: Extensively drug resistant tuberculosis (XDR-TB) is a serious problem in public health and XDR-TB patients usually develop from multi-drug resistance tuberculosis (MDR-TB) and pre-XDR-TB. The rapid molecular test for drug susceptibility testing (DST) can be used for early detection to prevent XDR-TB. Methods: We examined 34 clinical Mycobacterium tuberculosis (M. tuberculosis) isolates from MDR/XDR-TB patients in the upper north of Thailand that were identified with drug susceptibility profiles by indirect agar proportion method from 2005-2012. Our study investigated the genetic mutations in gyrA for ofloxacin resistance and rrs for kanamycin resistance. The genetic mutations and drug susceptibility test results were analyzed using the exact test. Results: The majority of the ofloxacin resistance was detected in gyrA 21, gyrA 70, gyrA 87, gyrA 102, gyrA 162, and gyrA 187 were at 0%, 12.5%, 37.5%, 0%, 50.0% and 25.0% sensitivity, respectively, and at 96.2, 96.2%, 20.1%, 96.2%, 57.7% and 61.5% specificity, respectively. Kanamycin resistance was found in rrs 512, rrs 241, rrs 223, rrs 414 and rrs 408 at 16.7%, 0%, 0%, 16.7% and 16.7% sensitivity, respectively, and at 96.4%, 92.9%, 82.1%, 82.1% and 71.4% specificity, respectively. This study found no significant correlation between gyrA mutations and ofloxacin resistance and also no correlation between the rrs gene and kanamycin resistance. Conclusion: These primer sequences and PCR products in our study such as gyrA and rrs might be unsuitable to detect ofloxacin and kanamycin resistance in the upper north of Thailand.

复方氟嗪酸滴鼻剂的制备及临床应用

氟嗪酸(ofloxacin)是第三代吡酮酸类抗菌新药,抗菌谱广,抗菌作用强,口服吸收良好,组织分布广泛,体内代谢稳定,自然耐药频率低,毒副反应小,临床上常用于泌尿系、肠道、呼吸道等各种感染。亦用于耳鼻喉科感染。据报道口服给药治疗耳鼻喉科疾病有效率为83.74%。

PVA Nanofibers Containing Ofloxacin-Cyclodextrin Inclusion Complex: Improve Optical Stability of Ofloxacin

Ofloxacin is an antibiotic with a wide range of activity against bacterial infections, but due to the high potential for toxicity when exposed to light, resolving this problem and further stabilizing the drug are among the posed challenges. Inclusion complex formation between α-cyclodextrin (α-CD), ofloxacin (OFL) and polyethylene glycol (PEG) was prepared via two methods to produce nanocontainers with desirable stability. The effect of PEG as compatible solubilizing agent and mixing condition (in ultrasonic bath) were investigated in formation of an inclusion complex between α-CD/OFL. Obtained complexes were examined by FTIR, H-NMR, SEM, EDX and UV which indicated the formation of an inclusion complex between α-CD/OFL, in turn, is a mixture of the cage and channel structures. Differences between 1H-NMR, FTIR and XRD spectra of OFL, CDs and inclusion complex indicated the formation of α-CD/OFL and supramolecular containers in solid phase. These inclusion complexes loaded in PVA-based nanofibers for smart nanofibers with controlled release manner and higher stability of OFL. Obtained nanofiber showed that nanofibers containing CDs/OFL under sonic energy containing higher degree of OFL.

5.3.Bacterial disease

920038 Clinical effect and laboratoryobservation of ofloxacin in the treatment oftyphoid fever,bacillary dysentery and gonor-rhea.ZOU Qiyuan (邹启园),et al.Dept InfectDis,1st Affil Hosp,Chongqing Med Univ,630042.Chin J Intern Med 1991;30 (9)

Degradation of ofloxacin using peroxymonosulfate activated by nitrogen-rich graphitized carbon microspheres:Structure and performance controllable study

Nitrogen-rich graphitized carbon microspheres(NGCs)with hierarchically porous were constructed by self-assembly.Under different heat treatment conditions,the structure,morphology and properties of NGCs were studied by using multiple characterization techniques.The results showed that the chemical microenvironments(e.g.surface chemistry,degree of graphitization and defective,etc.)and microstructures properties(e.g.morphology,specific surface area,particle size,etc.)could be delicately controlled via thermal carbonization processes.The degradation of ofloxacin(OFLX)by NGCs activated peroxymonosulfate(PMS)was studied systematically.It was found that the synergistic coupling effect between optimum N or O bonding species configuration ratio(graphitic N and C=O)and special microstructure was the main reason for the enhanced catalytic activity of NGC-800(calcination temperature at 800°C).Electron paramagnetic resonance(EPR)experiments and radical quenching experiments indicated that the hydroxyl(·OH),sulfate(SO4^·-)and singlet oxygen(^1O_(2))were contributors in the NGC-800/PMS systems.Further investigation of the durability of chemical structures and surface active sites revealed that undergo N bonding species configuration reconstruction and cannibalistic oxidation during PMS activation reaction.The used NGC-800 physicochemical properties could be recovered by heat treatment to achieve the ideal catalytic performance.The findings proposed a valuable insight for catalytic performance and controllable design of construction.

Cuprous Oxide/Nitrogen-doped Graphene Nanocomposites as Electrochemical Sensors for Ofloxacin Determination

Cu2O/nitrogen-doped grapheme（NG） nanocomposite material was prepared via a facile one step chemical reduction and characterized by means of X-ray diffraction（XRD） and scanning electron microscopy（SEM）. A new electrochemical sensor was then fabricated by coating Cu2O/nitrogen-doped graphene nanocomposite with Nation on glassy carbon electrode（Cu2O/NG/Nation/GCE）. The electrochemical response of this modified electrode toward of- loxacin was examined by cyclic voltammetry. The results indicate that Cu2O/NG/Nafion composite-modified elec- trode exhibits higher catalytic activity in the electrochemical oxidation of ofloxacin compared with glassy carbon electrode（GCE）, Cu2O/Nafion modified electrode（Cu2O/Nafion/GCE）, and N-doped graphene/Nation modified electrode（NG/Nafion/GCE）. Under optimal conditions, the peak current was found to be linearly proportional to the concentration of ofloxacin in the 0.5-27.5 μmol/L and 27.5-280 μmol/L ranges with a lower detection limit of 0.34 μmol/L, higher sensitivity of 39.32 μA-L-mmoV1 and a shorter reaction time of less than 2 s. In addition, Nation can enhance the stability of the modified electrode and prevent some negative species. Thus the modified electrode exhibits good selectivity and a long working life. The Cu2O/NG/Nafion composite modified electrode shows promising application in electrochemical sensors, biosensors, and other related fields because of its excellent properties.