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This study introduces a novel chemiluminescence (CL) approach utilizing FeS2 nanosheets (NSs) catalyzed luminol–O2 CL reaction for the measurement of three pharmaceuticals, namely venlafaxine hydrochloride (VFX), imipramine hydrochloride (IPM), and cefazolin sodium (CEF). The CL method involved the phenomenon of quenching induced by the pharmaceuticals in the CL reaction. To achieve the most quenching efficacy of the pharmaceuticals in the CL reaction, the concentrations of reactants comprising luminol, NaOH, and FeS2 NSs were optimized accordingly. The calibration curves demonstrated exceptional linearity within the concentration range spanning from 4.00 × 10−7 to 1.00 × 10−3 mol L−1, 1.00 × 10−7 to 1.00 × 10−4 mol L−1, and 4.00 × 10−6 to 2.00 × 10−4 mol L−1 with detection limits (3σ) of 3.54 × 10−7, 1.08 × 10−8, and 2.63 × 10−6 mol L−1 for VFX, IPM, and CEF, respectively. This study synthesized FeS2 NSs using a facile hydrothermal approach, and then the synthesized FeS2 NSs were subjected to a comprehensive characterization using a range of spectroscopic methods. The proposed CL method was effective in measuring the aforementioned pharmaceuticals in pharmaceutical formulations as well as different water samples. The mechanism of the CL system has been elucidated. [ABSTRACT FROM AUTHOR]

In recent years, the total consumption of antibiotics to cure infections has widely increased. Consequently, the concentration of antibiotics in aquatic environments has remarkably heightened. Cefazolin sodium (CFZS) is a first-generation cephalosporin antibiotic with significant bactericidal activities. Immense consumption of CFZS for years along with its persistence in various environments led to its growing deposit in different ecosystems. In this study, the model microalga Chlorella vulgaris was chosen to evaluate the impacts of different concentrations of CFZS on aquatic organisms. Notably, the cell number of the microalgae has declined with the rising concentrations of CFZS. Prepared SEM images and flow cytometry charts confirmed the harmful effects of the antibiotic on the cells of C. vulgaris. Furthermore, CFZS caused an increase in the content of pigments (chlorophyll a, b, carotenoids and anthocyanins), level of non-enzymatic antioxidant compounds (total phenol and flavonoid) and activity of enzymatic antioxidants (CAT, SOD and APX) in C. vulgaris. However, C. vulgaris displayed remarkable potential to remove CFZS from the culture medium. The obtained data may shed light on the establishment of the possible risks of antibiotics to algal populations and also microalgae ability in antibiotics removal. [ABSTRACT FROM AUTHOR]

Purpose: To investigate the comparative effect of two antibacterial treatments in orthopedic surgery. Methods: A total of 96 patients who had undergone orthopedic surgery in Department of Nosocomial Infection Management, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China from January 2021 to December 2022 were retrospectively analyzed and equally divided into two groups based on the postoperative medications administered to prevent infection. The control group was treated with amoxicillin sodium/clavulanate potassium while the study group was treated with cefazolin sodium. The incidence of postoperative infection, pain score, inflammatory factors and quality of life were determined and compared between both groups. Results: The incidence of postoperative infection in the study group was lower than in the control group (p < 0.05). Prior to intervention, the visual analogue scale (VAS) scores of the two groups were similar (p > 0.05), but decreased significantly after intervention (p < 0.05), with the score of the former after intervention lower than that of the latter (p < 0.05). Prior to intervention, the inflammatory factor levels in both groups were identical (p > 0.05); however, the levels fell significantly in both groups after intervention (p < 0.05), but the levels in the study group were lower than in the control group (p < 0.05). The quality of life scores were also higher for both groups after intervention (p < 0.05), but higher for the study group than for the control group (p < 0.05). Conclusion: Cefazolin sodium is more effective than amoxicillin sodium/clavulanate potassium in preventing infection in orthopedic patients after orthopedic surgery. However, there is a need to extend this treatment strategy to other clinical sites in order to validate these findings. [ABSTRACT FROM AUTHOR]

Since bacteria in biofilms are inherently resistant to antibiotics and biofilm‐associated infections pose a serious threat to global public health, new therapeutic agents and schemes are urgently needed to meet clinical requirements. Here two quaternary ammonium‐functionalized biphen[n]arenes (WBPn, n=4, 5) were designed and synthesized with excellent anti‐biofilm potency. Not only could they inhibit the assembly of biofilms, but also eradicate intractable mature biofilms formed by Gram‐positive S. aureus and Gram‐negative E. coli bacterial strains. Moreover, they could strongly complex a conventional antibiotic, cefazolin sodium (CFZ) with complex stability constants of (7.41±0.29)×104 M−1 for CFZ/WBP4 and (4.98±0.49)×103 M−1 for CFZ/WBP5. Combination of CFZ by WBP4 and WBP5 synergistically enhanced biofilm eradication performance in vitro and statistically improved healing efficacy on E. coli‐infected mice models, providing a novel supramolecular strategy for combating biofilm‐associated infections. [ABSTRACT FROM AUTHOR]

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To explore the feasibility of not using antibiotics before and after hemorrhoid surgery is the main objective of the study. A total of 68 patients with hemorrhoids who were admitted to Ningbo Anorectal Hospital from December 2019 to May 2021 were selected, including 36 males and 32 females. They were randomly divided into an experimental group and a control group, 34 patients in each group. The patients in the experimental group were not given antibiotics, while the patients in the control group were given cefazolin sodium 1-2 g and 100 ml of sodium chloride intravenously 30 min before surgery and the same dose of antibiotics was given intravenously after surgery (1 time/12 h), the postoperative administration time is 24 h, not more than 48 h. The intraoperative conditions, postoperative wound infection rate, hospital stay, postoperative recurrence rate and other aspects of the two groups of patients were observed and compared. There was no significant difference in postoperative body temperature, white blood cell count, postoperative wound infection and average hospital stay and recovery time between the two groups. The adverse drug reaction rate in the experimental group was lower than that in the control group. It is safe and feasible not to use antibiotics in the perioperative period of hemorrhoids. [ABSTRACT FROM AUTHOR]

Cephalosporin antibiotics, a group of widely prescribed antibiotics, are frequently detected in wastewater effluent and in the natural aquatic environment. Materials have been sought to effectively degrade the antibiotics. In this study, a novel high-iron clay was prepared with potassium ferrate and montmorillonite via a strong alkaline in situ synthesis method. Degradation of cefazolin sodium (CFZ) by this novel Fe (VI)-clay was investigated. The optimal conditions for the degradation of CFZ were determined using a single factor experiment and response surface optimization method. We found that 89.84% removal efficiency was obtained in 137 min when pH value was 5.16 and Fe (VI)-clay dosage was 0.79 g. The CFZ degradation mechanism was studied by computations on the Frontier Electron Density (FED) in combination with spectroscopic and mass spectroscopic analysis. The spectroscopic characteristics of the products at different stages showed that the oxidation decomposition reaction occurred during the degradation of CFZ by Fe (VI)-clay. Furthermore, FED calculation combined with GC–MS results showed that the degradation pathways of CFZ by the Fe (VI)-clay was mainly the cleavage of β-lactam, thiadiazole, tetrazole, and dihydrothiazine rings. [ABSTRACT FROM AUTHOR]

The aims of studies were to estimate the withdrawal period of antibiotic from milk after the intramammary infusion of cefazolin sodium (CEZ) in cows with difficulties in frequent milk discharge due to disease such as teat injury. The period was compared among cows milked twice a day after 150 or 450 mg of CEZ were administered to all quarters (Study 1, 2) and the cows in which milking of front-right quarter was ceased for five days after administration of these infusions to only that quarter (Study 3). In Studies 1 and 2, the median of 17.66 μg/ml and 83.18 μg/ml of CEZ were detected in the samples of first milking after intramammary administration, respectively; however, there was no residual antibiotic by 72 hr in all cows. In Study 3, the median of 1.96 μg/ml of CEZ was detected in the sample after the resumption of milking at 120 hr, and the residual was eliminated by 174 hr. The withdrawal period may be prolonged by the cessation of milking after administration, and the period is the total time from cessation to 72 hr after the resumption of milking. [ABSTRACT FROM AUTHOR]

Background: Large language models have propelled recent advances in artificial intelligence technology, facilitating the extraction of medical information from unstructured data such as medical records. Although named entity recognition (NER) is used to extract data from physicians' records, it has yet to be widely applied to pharmaceutical care records., Objective: In this study, we aimed to investigate the feasibility of automatic extraction of the information regarding patients' diseases and symptoms from pharmaceutical care records. The verification was performed using Medical Named Entity Recognition-Japanese (MedNER-J), a Japanese disease-extraction system designed for physicians' records., Methods: MedNER-J was applied to subjective, objective, assessment, and plan data from the care records of 49 patients who received cefazolin sodium injection at Keio University Hospital between April 2018 and March 2019. The performance of MedNER-J was evaluated in terms of precision, recall, and F 1 -score., Results: The F 1 -scores of NER for subjective, objective, assessment, and plan data were 0.46, 0.70, 0.76, and 0.35, respectively. In NER and positive-negative classification, the F 1 -scores were 0.28, 0.39, 0.64, and 0.077, respectively. The F 1 -scores of NER for objective (0.70) and assessment data (0.76) were higher than those for subjective and plan data, which supported the superiority of NER performance for objective and assessment data. This might be because objective and assessment data contained many technical terms, similar to the training data for MedNER-J. Meanwhile, the F 1 -score of NER and positive-negative classification was high for assessment data alone (F 1 -score=0.64), which was attributed to the similarity of its description format and contents to those of the training data., Conclusions: MedNER-J successfully read pharmaceutical care records and showed the best performance for assessment data. However, challenges remain in analyzing records other than assessment data. Therefore, it will be necessary to reinforce the training data for subjective data in order to apply the system to pharmaceutical care records., (©Yukiko Ohno, Riri Kato, Haruki Ishikawa, Tomohiro Nishiyama, Minae Isawa, Mayumi Mochizuki, Eiji Aramaki, Tohru Aomori. Originally published in JMIR Formative Research (https://formative.jmir.org), 04.06.2024.)

The density (d) and speed of sound (u) for systems containing{cefazolin sodium+ ionic liquid (1-octyl-3-methyl imidazolium bromide, [OMIm] Br) + H2O} and {ceftriaxone sodium+ ionic liquid (1-octyl-3-methyl imidazolium bromide, [OMIm] Br) + H2O}have been measured at T = 298.15 K.The measured data have been applied to calculate,standardpartial molar volume( ),apparent molar isentropic compressibility (Kφ), transfer volume (∆_tr V_φ^0), transfer compressibility (∆_tr K_φ^0)and hydration number (nH), and used to discussvarious solute-solvent interactions. The transfer quantities are positive and increase with molalities of ionic liquid which indicate the dominance of hydrophilic-hydrophilic interactions between the ionic liquid and drugs molecules and dehydration effect of ionic liquid on the solutions.

• A versatile synthetic method for cefazolin anchored citric acid dendrimers is delineated. • The structural elucidation and its purity are analyzed using various spectroscopic, thermal and microscopic techniques. • The drug membrane interactions are enumerated through confocal microscopy, hemolytic and MTT assay studies. • The drug release kinetics and their significance on various pharmacokinetic parameters are elucidated. The potent bacterial infections serve as the primary cause of mortality due to the absence of novel antibacterial therapy. The present investigation synthesized citric acid dendrimers through the divergent method that serves as a suitable platform in fulfilling the prerequisites of drug delivery. The cytotoxicity studies revealed 5.4 ± 0.3% of cell viability at 0.5 μg/ml and 35±0.3% at 300 μg/ml after 36 h. The IC 50 values on Human Alveolar Epithelial (HAE) cells for unmodified dendrimers were 1.36±0.06 mg ml−1while for PEG CZ G5 dendrimers were 35.19±0.15 mg/mlwith 9 ± 0.18% hemolysis. The significant differences were due to the variations in drug content and PEG shield density at the terminal surface. The Reactive Oxygen Species (ROS) uptake and dichlorofluorescein intensity for PEG CZ G2 dendrimers was 24.15 ± 1.24% and 42.3 ± 0.12%whichincreased significantly with the degree of pegylation and revealed 72.5 ± 1.03% and 79.2 ± 0.24%for PEG CZ G5 dendrimers. The increased ROS concentrations altered the mitochondrial functioning and served as a proof for antibacterial effect. Drug release pattern when heuristically fitted into various kinetic models specified zero-order release with non-fickian diffusion. Antibacterial investigations and pharmacokinetic studies revealed that the synthesized generations were quite effective against various bacterial pathogens with optimized concentrations. [ABSTRACT FROM AUTHOR]

This study introduces a novel chemiluminescence (CL) approach utilizing FeS 2 nanosheets (NSs) catalyzed luminol-O 2 CL reaction for the measurement of three pharmaceuticals, namely venlafaxine hydrochloride (VFX), imipramine hydrochloride (IPM), and cefazolin sodium (CEF). The CL method involved the phenomenon of quenching induced by the pharmaceuticals in the CL reaction. To achieve the most quenching efficacy of the pharmaceuticals in the CL reaction, the concentrations of reactants comprising luminol, NaOH, and FeS 2 NSs were optimized accordingly. The calibration curves demonstrated exceptional linearity within the concentration range spanning from 4.00 × 10 -7 to 1.00 × 10 -3  mol L -1 , 1.00 × 10 -7 to 1.00 × 10 -4  mol L -1 , and 4.00 × 10 -6 to 2.00 × 10 -4  mol L -1 with detection limits (3σ) of 3.54 × 10 -7 , 1.08 × 10 -8 , and 2.63 × 10 -6  mol L -1 for VFX, IPM, and CEF, respectively. This study synthesized FeS 2 NSs using a facile hydrothermal approach, and then the synthesized FeS 2 NSs were subjected to a comprehensive characterization using a range of spectroscopic methods. The proposed CL method was effective in measuring the aforementioned pharmaceuticals in pharmaceutical formulations as well as different water samples. The mechanism of the CL system has been elucidated., (© 2024 John Wiley & Sons Ltd.)

Solid-state Nuclear magnetic resonance, thermogravimetric analysis, X-ray diffraction, and Fourier-transform infrared spectroscopy were combined with theoretical calculation to investigate different crystal packings of α-cefazolin sodium obtained from three different vendors and conformational polymorphism was identified to exist in α-cefazolin sodium. Marginal differences observed among cefazolin sodium pentahydrate 1, 2, and 3 were speculated as being caused by the proportion of conformation 2.

Abstract Cefazolin sodium is a broad-spectrum antibiotic used in the treatment of infectious diseases in humans and in the surgical prophylaxis. Thus, since a considerable number of people have access to this drug, it is of great interest of quality control. The aim of this study was development and validation of a green method by Fourier-Transform Infrared (FT-IR) transmission spectrophotometry for the quantification of cefazolin sodium in lyophilized powder. This technique is widely used in the pharmaceutical industry due to its ease of execution, low cost, safety and high precision and accuracy. It has been employed in the quality control routine of numerous pharmaceuticals in order to identify them and quantify their active principles. The proposed method was completely validated according ICH guidelines, showing selectivity, accuracy, precision, robustness and linearity. It was linear over the concentration range of 0.4–1.7 mg with correlation coefficient 0.999, limits of detection and quantification of 0.017 mg and 0.052 mg, respectively, precise, accurate and robust when changes in the time, pressure and mark of potassium bromide were carried out during the preparation of the pellets. The proposed method was successfully applied to the qualitative and quantitative quality control of cefazolin sodium in lyophilized powder. In addition, the method is considered green, clean and sustainable since it uses only a single reagent; it is a fast, low-cost and environmentally friendly method. Graphical Abstract Unlabelled Image Highlights • A sustainable, clean, fast and low cost method was developed for sodium cefazolin. • Infrared method is an eco-friendly alternative to the quality control of the drug. • The method presented linearity, selectivity, accuracy, precision and robustness. • The proposed method contemplates the current needs of green analytical chemistry. [ABSTRACT FROM AUTHOR]

Cefazolin sodium (CFZ) is a semi-synthetic first-generation cephalosporin used for the treatment of infections caused by Gram‑positive and Gram‑negative microorganisms. Although it is a drug used worldwide, there are only a few green analytical methods described in the literature for its quantification. This work proposes an eco-friendly, low-cost, and rapid analytical method to analyze CFZ in lyophilized powder for injectable solution based on digital images, using thin-layer chromatography (TLC). For the TLC method, the mobile phase was comprised of ethanol and water, and the spots revelation was performed using iodine vapors. The TLC spots were analyzed through digital images, obtained by flatbed scanner, and evaluated using the free software “The Gimp” (GNU Image Manipulation Program), by quantification of pixels in pictures. This method was validated according to the International Conference on Harmonization (ICH) guidelines and presented adequate linearity, accuracy, precision, and robustness. It also showed its selectivity and stability-indicating capability (under acid, alkaline, aqueous, oxidative, and photolytic stress conditions). This is an innovative, easy, and low-cost method that can be used for the analysis of cefazolin sodium in lyophilized powder. Considering that this method does not use toxic organic solvents for the environment and operators, it contributes to the development of green chemistry. [ABSTRACT FROM AUTHOR]

Fundamental and serious efforts have been made over the past years to improve the drug acts, which leads to the discovery of novel drug preparations and delivery systems. The optimal design of such processes requires a molecular-level understanding of the interactions between drug molecules and biomolecules such as proteins. The thermodynamic investigation provides deep insight and knowledge of solute-solvent interactions and selection of appropriate production compounds in pharmaceutical fields. Particularly, the study of drug + biomolecule in aqueous media is the central issue in many types of research. The osmotic coefficient data for aqueous solutions containing the drugs (calcium d -pantothenate (CDP), cefazolin sodium (CFZ.Na), ceftriaxone sodium (CFT.Na)) with simple amino acid, l -alanine, glycine and l -leucine are obtained at 310.15 K using vapor pressure osmometry. Activity coefficients of both components in mixture were estimated using experimental osmotic coefficients. According to the results, the values of osmotic coefficients for the ternary system (drug + water + l -leucine) with a concentration of 0.04 mol∙kg−1 are higher than those values in other systems. The concentration dependence of osmotic coefficients indicates ion-pair formation between the ions of the drugs. Finally, Lin et al. and ECA models were used to correlate the water activity data in the presence of the amino acids obtained for the aqueous solution (drug + water + amino acid). [ABSTRACT FROM AUTHOR]

OBJECTIVE: To compare the efficacy of preoperatively, intraoperatively and postoperatively administration of cefazolin sodium in prevention of wound infection after cesarean section. METHODS: 120 patients undergoing cesarean section admitted into Luoyang Women and Children Medical Care Center in 2017 were retrospectively extracted to he divided into preoperative, intraoperative and postoperative group via different admonistration time, with 40 cases in each. Patients in preoperative group were given the intravenous infusion of cefazolin sodium 0.5 h before surgery; patients in intraoperative group received the intravenous infusion of cefazolin sodium immediately after clamping the umbilical cord during surgery; and patients in postoperative group were treated with the intravenous infusion of cefazolin sodium. The white blood cell count (WBC), recovery time of temperature, complications, postoperative infections, length of stay and hospitalization costs of three groups were observed. RESULTS: There was no significant difference in WBC levels among three groups at 72 h after surgery (P > 0.05). There was no significant difference in the recovery time of temperature between preoperative group and intraoperative group (P > 0.05), but both of which were significantly better than the postoperative group, the difference was statistically significant (P < 0.05). There was no significant difference in the incidence of complications and postoperative infection rate between preoperative group and intraoperative group (P > 0.05), but both of which were significantly lower than the postoperative group, and the difference was statistically significant (P < 0.05). There was no significant difference in length of stay and hospitalization cost between preoperative group and intraoperative group (P > 0.05), but both of which were significantly lower than the postoperative group, and the difference was statistically significant (P < 0.05). CONCLUSIONS: Preoperatively, intraoperatively and postoperatively administration of cefazolin sodium in patients with cesarean section can effectively prevent the wound infection, shorten the length of stay and reduce the hospitalization costs. [ABSTRACT FROM AUTHOR]

A simple, sensitive cupric oxide nanoparticles (CuO NPs) enhanced chemiluminescence (CL) method was developed for the measurement of β-lactam antibiotics, including amoxicillin and cefazolin sodium. The method was based on suppression of the CuO NPs-luminol-H2O2 CL reaction by β-lactam antibiotics. Experimental parameters that influenced the inhibitory effect of the antibiotic drugs on the CL system, such as NaOH (mol/L), luminol (µmol/L), H2O2 (mol/L) and CuO NPs (mg/L) concentrations, were optimized. Calibration graphs were linear and had dynamic ranges of 1.0 × 10-6 to 8.0 × 10-6 mol/L and 3.0 × 10-5 to 5.0 × 10-3 mol/L for amoxicillin and cefazolin sodium, respectively, with corresponding detection limits of 7.9 × 10-7 mol/L and 1.8 × 10-5 mol/L. The relative standard deviations of five replicate measurements of 5.0 × 10-6 amoxicillin and 5 × 10-4 cefazolin sodium were 5.43 and 5.01%, respectively. The synthesized CuO NPs were characterized by X-ray diffraction (XRD) and transmission electronmicroscopy (TEM). The developed approach was exploited successfully to measure antibiotics in pharmaceutical preparations. Copyright © 2014 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

OBJECTIVE; To probe into the efficacy of linezolid in treatment of postoperative infection among patients in orthopedics department and its effects on serum inflammatory factors. METHODS; 86 patients with postoperative infection admitted into Zhengzhou Orthopaedics Hospital Affiliated to Henan University from Jim. 2014 to Jun. 2016 were selected and divided into observation group and control group via random number table, with 43 cases in each. The control group was treated with cefazolin sodium, while the observation group was given linezolid. Differences in clinical efficacy, levels of tumor necrosis factor-α (TNF-α), interleukin-6 ( IL-6) , interleukin-8 (IL-8) , incidences of adverse drug reactions between two groups were observed and compared. RESULTS; The total effective rate of observation group (97. 7% , 42/43) was significantly higher than that of the control group (83. 7% , 36/43) , with statistically significantly difference ( P < 0. 05 ) ; after treatment, the TNF-α, JL-6 and IL-8 levels of observation group were significantly lower than those of the control group, with statistically significantly differences (P <0. 05) ; the incidences of adverse drug reactions of observation group and control group were respectively 1 1.6% (5/43) and 14. 0% (6/43) , the difference had no statistical significance (P>0. 05). CONCLUSIONS; The efficacy of linezolid in treatment of postoperative infection among patients in orthopedics department is remarkable, which can significantly improve patients’ clinical symptoms, reduce serum inflammatory factors levels, with low incidence of adverse drug reactions and high safety. [ABSTRACT FROM AUTHOR]

Two unknown impurities were detected in the cefazolin sodium bulk drug substance using gradient reversed-phase high-performance liquid chromate-graphy (HPLC). These impurities were isolated by preparative HPLC and characterized by using spectroscopic techniques like LC-MS, LC-MS/MS, 1D, 2D NMR, and FT-IR. Based on the spectral data, the impurities have been characterized as A/-(2,2-dihydroxyethyl)-2-(1A7-tetrazol-1-yl)acetamide (Impu rity-l) and 2-{carboxy[(1H-tetrazol-1-ylacetyl)amino]methyl}-5-methylidene-5,6-dihydro-2/-/-1,3-thiazine-4-carboxylic acid (Impurity-ll). The structures of these impurities were also established unambiguously by co-injection into HPLC to confirm the retention time. To the best of our knowledge, these two impurities were not reported elsewhere. [ABSTRACT FROM AUTHOR]

ABSTRACT A novel chemiluminescence (CL) method was developed for the determination of cefazolin sodium based on the CL reaction between the [Cu(HIO6)2]5-Cu(III) complex and luminol in alkaline solution. Results showed that CL emission of Cu(III) complex-luminol in alkaline medium was significantly different from that in acidic medium. A possible mechanism of the enhanced effect of cefazolin on CL emission of the [Cu(HIO6)2]5-- luminol system was proposed. The effect of the reaction conditions on CL emissions was examined. Under optimized conditions, a good linear relationship was obtained between CL intensity and concentrations of cefazolin sodium in the range of 2.0 x 10-8 to 2.0 x 10-6 g/mL with a correlation coefficient of R2 = 0.9978. The limit of detection was 4.58 x 10-9 g/mL. The proposed method was applied for the determination of cefazolin sodium in real samples with recoveries of 82.0-109% with an RSD of 0.7-2.1%. The proposed method was successfully used for the determination of cefazolin sodium in injectable powder preparations and human urine with satisfactory results. Copyright © 2012 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Cefazolin sodium can form both α- and β-form crystals. It also can form dehydrated crystalline and amorphous products through different production processes. Because different polymorphic medicines usually have different physical and chemical properties, it is critical to emphasize the crystallization control of polymorphic medicines. Near-infrared (NIR) analysis, which incorporates a combination of NIR spectroscopic techniques and multivariate chemometric methods, is considered a powerful tool for the determination of the crystallinity of polymorphic drugs. The selection of optimal spectral ranges that correlate with the lattice specificity and content specificity is crucial to obtaining a specific NIR model. In the present work, near-infrared (NIR) spectra of cefazolin sodium with different crystal forms created through different processes were studied. The results suggest that wavelengths within the range of 9102.7-8597.5 cm is related to the specificity of the cefazolin sodium crystal lattice and that the range of 6001.6-5496.4 cm is associated with the quantitative content of cefazolin sodium. The two absorptions are caused by the second overtone of the C-H stretching band (3υC-H) and the first overtone of C-H stretching band (2υC-H), respectively. Using these results, we established a suitable method of constructing a universal quantitative model by using mixed samples in different crystal forms as a calibration set, selecting a content-specific range (6001.6-5496.4 cm), and adding lattice-related spectral ranges where appropriate. This may provide a framework for the construction of prediction models for polymorphic medicines. [ABSTRACT FROM AUTHOR]

Abstract: Microarc oxidized (MAO) coatings containing Si, Ca and Na elements (SCN) were prepared on titanium. The morphology, phase composition and elemental concentrations of the MAO coating surfaces highly depended on the applied voltages. The MAO coatings containing SCN show an atomic concentration gradient along the coating depth. The chemical states of Ti2+, Ti4+, Ca2+, Si2+ and O2− were observed in all the MAO coatings. The novel cefazolin sodium/chitosan composite films were deposited on the MAO coatings for application in therapy of the inflammation resulting from implanting. The increases of depositing times and cefazolin sodium concentration could increase the accumulative release concentration of cefazolin sodium, and could improve the sustaining-release ability of drug film. Also, the addition of chitosan could improve the sustaining-release ability of drug film, indicated that chitosan is a promising delivery carrier for cefazolin sodium. [Copyright &y& Elsevier]

Abstract: The mechanical and corrosion resistance of hydrophilic sphene/titania composite coatings on titanium formed by a hybid technique of microarc oxidation (MAO) and heat-treatment were investigated. The results indicated that the heat-treatment could improve the hardness, elastic modulus, elastic recovery and corrosion resistance of the MAO coatings, and reinforce the interface bonding between MAO coatings and titanium. A cefazolin sodium/chitosan drug film was prepared on the coating surfaces. The drug load procedures such as the addition of chitosan obviously increased the sustained-release ability of drug films. In addition, the increase of cefazolin sodium concentration could increase the accumulative release concentration of cefazolin sodium. The sustaining-release ability of drug films deposited on the MAO and heat-treated MAO coatings is similar. In the interior of drug film, the physical and chemical bonding reactions such as Coulombic interactions, van der Waals force and H-bonding etc. could be produced, through the chemical group interactions such as –OH and –NH2 groups of chitosan with –Czolin sodium. [ABSTRACT FROM AUTHOR]

Conclusion: Sinusitis is accompanied by deteriorated antioxidant status, which can be alleviated with administration of cefazolin sodium or methylprednisolone. Steroids improve sinusitis when combined with antibiotics. Objective: To evaluate the antioxidant status in response to treatment of maxillary sinusitis with methylprednisolone and cefazolin sodium. Materials and methods: Twenty-eight rabbits were inoculated with Staphylococcus aureus and then treated with saline, methylprednisolone, cefazolin sodium, and methylprednisolone plus cefazolin sodium, twice daily for 7 days. After the animals were sacrificed, mucosa samples were obtained to determine catalase (CAT), superoxide dismutase (SOD), and glutathione reductase (GPx) activities and levels of nitric oxide (NO) and malondialdehyde (MDA). Results: Catalase activity among untreated rabbits and those treated with either methylprednisolone or cefazolin sodium was not different. Activities of SOD and GPx were lower for rabbits treated with cefazolin sodium than for those treated with methylprednisolone and for untreated rabbits (p<0.0001). Rabbits treated with cefazolin sodium had lower NO and MDA levels than those treated with methylprednisolone and untreated rabbits (p<0.0001). Combined administration of cefazolin sodium with methylprednisolone increased CAT, SOD, and GPx activities further and decreased NO and MDA levels further in comparison with their administration alone (p<0.0001). [ABSTRACT FROM AUTHOR]

An online solid phase extraction (SPE) method was developed for the simultaneous screening of cefazolin sodium and cefotaxime sodium in human urine. A short weak anion exchange monolithic column was prepared and used as the selective extraction sorbent. The column exhibited good permeability and biocompatibility. During the online SPE process, most matrices in the urine samples were removed rapidly, while cefazolin sodium and cefotaxime sodium were effectively trapped in this monolithic column. Reversed phase high performance liquid chromatography (HPLC) was performed on a C18 column with ultraviolet detection at 254 nm. The mobile phase consisted of methanol-0.005 mol/L phosphate (21/79, v/v, pH = 5.0) and the flow rate was set to 0.7 mL/min. A good linear relationship was demonstrated at analyte concentrations ranging from 1 to 100 µg/mL. The absolute recovery ranged from 79.4% to 81.5% and the inter- and intra-day relative standard deviations were <5.0%. These results suggest that the online SPE-HPLC method is suitable for the simultaneous monitoring of cefazolin sodium and cefotaxime sodium in human urine samples because it avoids tedious pretreatments and provides a fast, economical, and reproducible method for assaying trace drugs in biological samples. [ABSTRACT FROM AUTHOR]

Cefazolin sodium is a first-generation cephalosporin antibiotic and has been used worldwide since the early 1970s. It is used for the treatment of bacterial infections in various organs, such as the respiratory tract, skin and skin structure, genital tract, urinary tract, biliary tract, and bone and joint infections. It has also been used for septicemia due to susceptible gram-positive cocci (except Enterococcus), some gram-negative bacilli including E. coli, Proteus, and Klebsiella may be susceptible, and for perioperative prophylaxis. After the introduction of penicillins and other cephalosporins, occasional outbreaks of methicillin-resistant Staphylococcus aureus were noted. As a result, vancomycin use was increased; however, very recently and most alarmingly, vancomycin-resistant strains have been described. In this setting, to avoid the risk of the development of vancomycin-resistant strains further, vancomycin use should be curtailed. In consideration of this historical background, the appropriate use of antibiotics, such as dosage, dosage intervals, and the duration of administration is required not only for the protection of patients' health but also for the prevention of the development of drug resistance. Cefazolin has been used in clinical practice for about 40 years, and a large body of evidence has been accumulated, and its efficacy and safety are well established compared with other antibiotics. Therefore, cefazolin has been chosen as a first-line anti-microbial for prophylaxis after various surgical procedures, including cardiovascular surgery, hysterectomy, arthroplasty and so on. Based on these facts, especially for the prophylaxis of surgical site infections, the first-generation cephalosporin, cefazolin, is now being "re-visited". [ABSTRACT FROM AUTHOR]

Microcalorimetry was applied to study the effect of cephalosporins (cefazolin sodium and cefonicid sodium) on the E. coli growth. The microbial activity was recorded as power-time curves through an ampoule method with a TAM Air Isothermal Microcalorimeter at 37°C. The parameters such as the growth rate constant ( k), inhibitory ratio ( I), the maximum power output ( P m) and the time corresponding to the maximum power output ( t m) were calculated. The change tendencies of k, with the increasing of concentration ( C) of the two cephalosporins, are similar which show that cefazolin sodium and cefonicid sodium have the same inhibitory mechanism. The experimental results reveal that cefonicid sodium has a stronger antibacterial activity towards E. coli than that of cefazolin sodium and this was coincide with the clinical manifestations. [ABSTRACT FROM AUTHOR]

Purpose. A case of cefazolin-induced hypoprothrombinemia in a patient with renal failure is reported. Summary. A 50-year-old African-American woman was transferred from the orthopedics service to the internal medicine service for management of acute renal failure. Before her transfer, she had spinal surgery and subsequently developed a wound infection complicated by Escherichia coli bacteremia. After trials of multiple antibiotics, she developed acute interstitial nephritis and renal failure. On the day of her transfer to the internal medicine service, i.v. cefazolin sodium 1 g was administered every 24 hours to eradicate the E. coli detected in blood cultures. Her baseline International Normalized Ratio (INR) was 1.3. On day 7 of cefazolin therapy, her INR increased to 4.0. Because of her recent history of bleeding and hypotension, vitamin K 10 mg i.v. was administered, followed by 5 mg orally for the next two days. Her INR decreased and normalized at 1.1. The patient had no changes to other drug therapies and had no medical conditions known to independently affect prothrombin time during this episode. The score on the Naranjo et al. adverse-event probability scale revealed a probable relationship between cefazolin and hypoprothrombinemia in this patient. Conclusion. A patient with a postsurgery wound infection and acute renal failure developed hypoprothrombinemia after receiving cefazolin for seven days. [ABSTRACT FROM AUTHOR]

Abstract: Human serum paraoxonase (PON1, EC 3.1.8.1.) is a high-density lipid (HDL)-associated, calcium-dependent enzyme; its physiological substrates are not known. In this study, a new purification strategy for human PON1 enzyme was developed using two-step procedures, namely ammonium sulfate precipitation and sepharose-4B-l-tyrosine-1-napthylamine hydrophobic interaction chromatography. SDS-polyacrylamide gel electrophoresis of the enzyme indicates a single band with an apparent MW of 43 kDa. Overall purification rate of our method was found 227-fold. The V max and K m of the purified enzyme were determined 227.27 EU and 4.16 mM, respectively. The in vitro effects of commonly used antibiotics, namely gentamycin sulfate and cefazolin sodium was also investigated on the purified human serum PON1 enzyme and human liver PON1 enzyme from human hepatoma cell (HepG2). Gentamycin sulfate and cefazolin sodium caused a dose- and time-dependent decrease on PON1 activity in HepG2 cells. Moreover, gentamycin sulfate and cefazolin sodium were effective inhibitors on purified human serum PON1 activity with IC50 of 0.887 and 0.0084 values, respectively. The kinetics of interaction of gentamycin sulfate and cefazolin sodium with the purified human serum PON1 indicated a different inhibition pattern. Cefazolin sodium showed a competitive inhibition with K i of 0.012±0.00065 mM. However, Gentamycin sulfate was inhibited in non-competitive manner with K i of 0.026±0.015. In order to determine the inhibition statue of these drugs on a living system, the effects of same antibiotics on PON1 enzyme activity of mouse serum PON1 and liver PON1 were investigated in vivo. Gentamycin sulfate (3.2 mg/kg) and cefazolin sodium (106.25 mg/kg) leads to the significant decrease in mouse serum PON1 after 2, 4, 6 h and 2, 4 h drug administration, respectively. Cefazolin sodium did not exhibit any inhibition effect for the liver PON1, in vivo. [Copyright &y& Elsevier]

Room and high temperature kinetic and spectroscopic features of the radical species produced in gamma irradiated cefazolin sodium (here after CS) were investigated in detail using electron spin resonance (ESR) spectroscopy to determine the feasibility of its sterilization by radiation and to explore the dosimetric properties of this semi-synthetic representative of cephalosporins. Irradiated CS exhibits an unresolved ESR doublet as other cephalosporins reported up to date. Signal intensity data derived from microwave saturation, dose–response, decays at room and at high temperature studies were analysed assuming a model of two radical species giving rise to doublet and singlet ESR signals. Spectroscopic parameters of these species were determined through spectrum simulation calculations. Decay parameters calculated from annealing studies at seven different temperatures were used to calculate the activation energies of the contributing species. Radiosensitivity of CS to gamma rays was found to be relatively low in the dose range of 0–25?kGy. This conclusion was considered as an indication of the feasibility of radiosterilization of CS by gamma radiation. Five different functions were tried to explore dose–response data of CS in the dose range of 0–25?kGy and it was concluded that a function comprising a linear and a quadratic terms of applied dose describes best experimental results. [ABSTRACT FROM AUTHOR]

HP (2–20) is a peptide derived from the N-terminus of Helicobacter pylori ribosomal protein L1 that has been shown to have antimicrobial activity against various species of bacteria. When we tested the effects of HP (2–20), we found that this peptide displayed strong activity against pathogens from a patient with gallstones, but it did not have hemolytic activity against human erythrocytes. We also found that HP (2–20) had potent activity against cefazolin sodium-resistant bacterial cell lines, and that HP (2–20) and cefazolin sodium had synergistic effects against cell lines resistant to the latter. To investigate the mechanism of action of HP (2–20), we performed fluorescence activated flow cytometry using pathogens from the patient with gallstones. As determined by propidium iodide (PI) staining, pathogenic bacteria treated with HP (2–20) showed higher fluorescence intensity than untreated cells, similar to melittin-treated cells, and that HP (2–20) acted in an energy- and salt-dependent manner. Scanning electron microscopy showed that HP (2–20) caused significant morphological alterations in the cell surface of pathogens from the patient with gallstones. By determining their 16S rDNA sequences, we found that both the pathogens from the patient with gallstones and the cefazolin sodium-resistant cell lines showed 100% homology with sequences from Pseudomonas aeruginosa. Taken together, these results suggest that HP (2–20) has antibiotic activity and that it may be used as a lead drug for the treatment of acquired pathogens from patients with gallstones and antibiotic-resistant cell lines. [Copyright &y& Elsevier]

Two simple, accurate, sensitive and selective procedures for the determination of eight cephalosporins are described. These procedures are based on the formation of ion-pair complexes between the drugs and ammonium reineckate, the formed precipitates are quantitatively determined either colourimetrically or by atomic absorption spectrometrically. The methods consist of reacting drugs with Reinecke''s salt in an acidic medium at 25±2°. The first colourimetric procedure (procedure I) is based on dissolving the formed precipitate with acetone, the volume was completed quantitatively and the absorbance of the solution was measured at 525 nm against pure solvent blank. Also, the formed precipitates on the atomic absorption spectrometric procedure (procedure II) are quantitatively determined directly or indirectly through the chromium precipitate formed or the residual unreacted chromium in the filtrate at 358.6 nm. The optimum conditions for precipitation have been carefully studied. Beer''s law is obeyed for the studied drugs in the range 5–35 μg ml−1 with correlation coefficients ≮0.9989. Both procedures I and II hold well accuracy and precision when applied to the analysis of the cited cephalosporins in different dosage forms with good recovery percent ranged from 98.7±0.90 to 100.1±0.74 without interference from additives. [Copyright &y& Elsevier]

The hygroscopicity behavior of the pentahydrate, monohydrate, amorphous, and dehydrated forms of solid cefazolin sodium (CEZ) was studied under different relative humidity (RH) conditions. Between 42 and 86% RH, the pentahydrate (α form), the monohydrate, and their dehydrated forms absorbed atmospheric moisture equivalent to their hydrate numbers. The pentahydrate demonstrated a hysteresis effect at 15 and 31% RH. On the other hand, the water content of the amorphous form increased linearly with increases in RH. The noncrystalline state was maintained below 56% RH. For the dehydrated α form there was a distinct birefringence when viewed under polarizing light, the X-ray diffraction pattern was weak and diffuse, and the infrared (IR) spectra were discernibly different from that of the amorphous form. The freeze-dried CEZ showed hygroscopic behavior almost similar to that of the dehydrated α form. Two-component mixtures of various CEZ forms showed a linear relationship between the water content and the mixing ratio when stored at 31, 42, and 56% RH. From the hygroscopicity data, the crystallinity of freeze-dried CEZ could be estimated as the percentage of the dehydrated α form. [ABSTRACT FROM AUTHOR]

The stability of pharmacy-compounded cefazolin sodium eye drops was studied experimentally using three series of model solutions that were divided into two groups depending on the storage conditions at (5 ± 3)°C and (25 ± 2)°C in the dark. The influence of stress factors such as lighting and temperature (40 ± 2)°C on the model solutions was studied. The cefazolin sodium content during the stability study was determined by HPLC. The organoleptic characteristics (color, aroma, transparency) were also evaluated. The test results established that pharmacy-compounded cefazolin sodium eye drops were stable for 14 d when stored in a refrigerator (5 ± 3)°C. [ABSTRACT FROM AUTHOR]