交替惩罚三线性分解二阶校正荧光分析法快速测定牛奶中洛美沙星含量

笔者利用化学计量学交替惩罚三线性分解二阶校正算法结合荧光分析,在有干扰药物及牛奶中干扰组分共存下,对牛奶中的洛美沙星进行快速分析测定。当三维荧光数据的预估组分数取4时,所得平均回收率达到99.4%±1.3%,预测方差均方根(RMSP)为2.97nmol/L,预测结果良好。实验结果表明,此法可用于干扰组分共存下牛奶中洛美沙星的快速定量测定。     

Corneal critical barrier against the penetration of dexamethasone and lomefloxacin hydrochloride: evaluation by the activation energy for drug partition and diffusion in cornea

The cornea is a solid barrier against drug permeation. We searched the critical barrier of corneal drug permeation using a hydrophobic drug, dexamethasone (DM), and a hydrophilic drug, lomefloxacin hydrochloride (LFLX). The activation energies for permeability of DM and LFLX across the intact cornea were 88.0 and 42.1 kJ/mol, respectively. Their activation energies for permeability across the cornea without epithelium decreased to 33.1 and 16.6 kJ/mol, respectively. The results show that epithelium is the critical barrier on the cornea against the permeation of a hydrophobic drug of DM as well as a hydrophilic drug of LFLX. The activation energy of partition for DM (66.8 kJ/mol) was approximately 3-fold larger than that of diffusion (21.2 kJ/mol). The results indicate that the partition for the hydrophobic drug of DM to the corneal epithelium is the primary barrier. Thermodynamic evaluation of activation energy for the drug permeation parameters is a good approch to investigate the mechanism of drug permeability.     

Preparation of active antibacterial biomaterials based on sparfloxacin,enrofloxacin, and lomefloxacin deposited on polyethylene

Bacterial contamination is one of the biggest drawbacks of implanted biomaterials, which may cause nosocomial infection. Avoiding bacterial adhesion onto the biomaterial surface by preparing active antibacterial biomaterials is an accurate solution. In this study, three of the fluoroquinolones: sparfloxacin, enrofloxacin, and lomefloxacin were selected due to their broad bactericidal effect and immobilized onto low‐density polyethylene surface at two different pH values (pH 3 and pH 6), after tailoring the surface by plasma treatment followed by grafting of polymer brush of N‐allylmethylamine. Surface wettability test and morphological investigations were carried out by water contact angle measurement and scanning electron microscopy analysis, respectively. Chemical characterizations were carried out by Fourier transform infrared spectra and X‐ray photoelectron spectroscopy. Antibacterial activity was checked against Staphylococcus aureus and Escherichia coli strains and results revealed that prepared surfaces were more effective against E. coli than S. aureus especially those prepared at pH 6. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46174.     

基于Mn掺杂ZnS室温磷光量子点检测盐酸洛美沙星方法的研究

利用水相合成法制备了三巯基丙酸包裹的Mn掺杂ZnS量子点(MPA-Mn/ZnSQDs),基于该量子点的室温磷光性质,构建了一种定量检测盐酸洛美沙星(LFLX)的新方法。在最优实验条件下(pH7.4,反应时间10min),LFLX浓度在0.002~1.4μg/mL范围内与MPA-Mn/ZnSQDs的磷光猝灭强度呈良好的线性关系(r=0.993),方法检出限为0.7×10-3μg/mL。该方法相对无共存物质的干扰,并适用于LFLX眼药水及人体尿样中LFLX的快速检测。     

Corneal Critical Barrier against the Penetration of Dexamethasone and Lomefloxacin Hydrochloride: Evaluation by the Activation Energy for Drug Partition and Diffusion in Cornea

The cornea is a solid barrier against drug permeation. We searched the critical barrier of corneal drug permeation using a hydrophobic drug, dexamethasone (DM), and a hydrophilic drug, lomefloxacin hydrochloride (LFLX). The activation energies for permeability of DM and LFLX across the intact cornea were 88.0 and 42.1 kJ/mol, respectively. Their activation energies for permeability across the cornea without epithelium decreased to 33.1 and 16.6 kJ/mol, respectively. The results show that epithelium is the critical barrier on the cornea against the permeation of a hydrophobic drug of DM as well as a hydrophilic drug of LFLX. The activation energy of partition for DM (66.8 kJ/mol) was approximately 3-fold larger than that of diffusion (21.2 kJ/mol). The results indicate that the partition for the hydrophobic drug of DM to the corneal epithelium is the primary barrier. Thermodynamic evaluation of activation energy for the drug permeation parameters is a good approch to investigate the mechanism of drug permeability.     

洛美沙星环合物生产工艺改进研究简

洛美沙星环合物是制造盐酸洛美沙星胶囊和盐酸洛美沙星滴眼液等杀菌消炎药的医药中间体.本文是在车间工艺生产基础上,从化学检测着手,运用现代化学实验技术,分析车间工艺生产,找出洛美沙星环合物生产过程中含量不能达到医药生产的优级纯（99％以上）原因,并改进之,指导洛美沙星环合物生产工艺的改进,实现其顺利生产.     

Effect of diclofenac on ocular levels of ciprofloxacin and lomefloxacin in rabbits with endophthalmitis

The purpose of this study was to analyze ciprofloxacin and lomefloxacin penetration into the anterior eye tissues after topical instillation in healthy rabbits and with experimental Staphylococcus aureus endophthalmitis. Additionally, effect of diclofenac sodium eye drops on the distribution of both fluoroquinolones in the inflamed eye tissues was investigated. An intense protocol with frequent antibiotic administration was chosen. Samples from aqueous humor were obtained 2 and 6?h after the start of the treatment. Samples from cornea and iris were obtained at the end of the experiment, after euthanasia of the animals. Drug concentrations were measured by HPLC method. The median levels of ciprofloxacin and lomefloxacin in aqueous humor of healthy animals, 2 and 6?h after drug administration were 6.39–9.65 and 5.30–6.81?µg/ml, respectively. Ciprofloxacin levels were neither changed from the inflammation nor after instillation of diclofenac. In contrary, lomefloxacin concentrations in aqueous humour of inflamed eye were significantly increased 12.15–15.08?µg/ml, especially after diclofenac administration (17.12–27.76?µg/ml). Levels of both fluoroquinolones in cornea (13.08?µg/g for ciprofloxacin and 12.25?µg/g for lomefloxacin) and in iris (0.84?µg/g for ciprofloxacin and 1.34?µg/g for lomefloxacin) were higher than MIC and MBC values against S. aureus ATCC 25923. Although higher lomefloxacin concentrations were observed in the aqueous humor after instillation of diclofenac, the levels of both fluoroquinolones in iris and in cornea were not significantly changed. Topical administration of lomefloxacin and diclofenac in combination improved penetration of the antibacterial agent in the aqueous humor which can be of clinical importance.     

Residues of veterinary antibiotics in manures from feedlot livestock in eight provinces of China

The residue levels of selected fluoroquinolones, sulfonamides and tetracyclines in 143 animal dung samples collected in 2007 from large-scale livestock and poultry feedlots in 8 provinces were determined by using ultrasonic extraction and liquid chromatography. Recoveries from spiked pig dung samples (spike level = 1 mg/kg) ranged from 73.9 to 102.0% for fluoroquinolones, from 81.6 to 92.3% for sulfonamides, and from 57.2 to 72.6% for tetracyclines. Relative standard deviations of the recoveries were less than 10% within the same day. Method quantification limits were measured from 0.031 to 0.150 mg/kg for fluoroquinolones, from 0.023 to 0.082 mg/kg for sulfonamides, and 0.091 to 0.182 mg/kg for tetracyclines in spiked pig manure samples. Analysis of 61 pig, 54 chicken and 28 cow dung samples collected in China revealed that in pig and cow dung, up to 33.98 and 29.59 mg/kg ciprofloxacin, 33.26 and 46.70 mg/kg enrofloxacin, 59.06 and 59.59 mg/kg oxytetracycline, and 21.06 and 27.59 mg/kg chlortetracycline could be detected, respectively. A maximum concentration of 99.43 mg/kg fleroxacin, 225.45 mg/kg norfloxacin, 45.59 mg/kg ciprofloxacin and 1420.76 mg/kg enrofloxacin could be detected in chicken dung. No appreciable sulfonamide antibiotic concentrations (less than 10 mg/kg) were found in any animal dung, and only sulfadimidine was observed, at a maximum concentration of 6.04 mg/kg, in chicken dung. Both enrofloxacin and chlortetracycline were detected with a very high occurrence in three animal manure samples. The residue levels for most antibiotics showed significant statistical differences among the sampling districts and the animal species.     

UVA Radiation Enhances Lomefloxacin-Mediated Cytotoxic,Growth-Inhibitory and Pro-Apoptotic Effect in Human Melanoma Cells through Excessive Reactive Oxygen Species Generation

Melanoma, the most dangerous type of cutaneous neoplasia, contributes to about 75% of all skin cancer-related deaths. Thus, searching for new melanoma treatment options is an important field of study. The current study was designed to assess whether the condition of mild and low-dose UVA radiation augments the lomefloxacin-mediated cytotoxic, growth-inhibitory and pro-apoptotic effect of the drug in melanoma cancer cells through excessive oxidative stress generation. C32 amelanotic and COLO829 melanotic (BRAF-mutant) melanoma cell lines were used as an experimental model system. The combined exposure of cells to both lomefloxacin and UVA irradiation caused higher alterations of redox signalling pathways, as shown by intracellular reactive oxygen species overproduction and endogenous glutathione depletion when compared to non-irradiated but lomefloxacin-treated melanoma cells. The obtained results also showed that lomefloxacin decreased both C32 and COLO829 cells’ viability in a concentration-dependent manner. This effect significantly intensified when melanoma cells were exposed to UVA irradiation and the drug. For melanoma cells exposed to lomefloxacin or lomefloxacin co-treatment with UVA irradiation, the concentrations of the drug that decreased the cells’ viability by 50% (EC₅₀) were found to be 0.97, 0.17, 1.01, 0.18 mM, respectively. Moreover, we found that the redox imbalance, mitochondrial membrane potential breakdown, induction of DNA fragmentation, and changes in the melanoma cells’ cell cycle distribution (including G₂/M, S as well as Sub-G₁-phase blockade) were lomefloxacin in a dose-dependent manner and were significantly augmented by UVA radiation. This is the first experimental work that assesses the impact of excessive reactive oxygen species generation upon UVA radiation exposure on lomefloxacin-mediated cytotoxic, growth-inhibitory and pro-apoptotic effects towards human melanoma cells, indicating the possibility of the usage of this drug in the photochemotherapy of malignant melanoma as an innovative medical treatment option which could improve the effectiveness of therapy. The obtained results also revealed that the redox imbalance intensification mediated by the phototoxic potential of fluoroquinolones may be considered as a more efficient treatment model of malignant melanoma and may constitute the basis for the development of new compounds with a high ability to excessive oxidative stress generation upon UVA radiation in cancer cells.     

在B-R介质中盐酸诺美沙星的光谱性质研究与应用

研究了在不同pH(1.89~11.58)的B ritton-Rob inson(B-R)缓冲溶液中,盐酸诺美沙星的紫外光谱性质,并对其在酸度增大时紫外吸收增强且最大吸收峰产生了红移的机理进行了初步的探讨.提出在最大吸收波长为286 nm,pH 3.78的B-R缓冲溶液中,分光光度法测定盐酸诺美沙星,测得其表观摩尔吸光系数为3.12×104L.mol-1.cm-1,浓度线性范围为1.0~23.0 mg.L-1,检出限为0.59 mg.L-1.该法成功用于药片中盐酸诺美沙星含量的测定,结果满意.方法简便、快速、准确度高.