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Drug Design, Development and Therapy 2022Pediatric electrolyte supplements injection is mainly used to supplement heat and body fluid, and commonly used in pediatrics. Its compatibility and stability with...
OBJECTIVE
Pediatric electrolyte supplements injection is mainly used to supplement heat and body fluid, and commonly used in pediatrics. Its compatibility and stability with common clinical drugs such as antibiotics was rarely reported to ensure the children's safety and the rational use of drugs. The aim of the present study was to investigate physical and chemical stability of pediatric electrolyte supplements injection mixed with ten commonly used clinical drugs.
METHODS
According to clinical drug concentration, we mix the pediatric electrolyte supplements injection mixed with ten drugs. The compatible solutions were withdrawn at certain time intervals (0, 0.5, 1, 2, 4, 6 hours) after mixing and tested by description, insoluble particles detection, pH determination and high performance liquid chromatography (HPLC) assay of active ingredient as measures of physicochemical compatibility.
RESULTS
No obvious appearance changes were observed when mixing. Furthermore, over the 6 hours post-preparation period the pH values were within the requirements of each drug quality standard and the number of insoluble particles (≥10 and ≥25μm) met requirements of Chinese Pharmacopeia (Edition 2020) except for mezlocillin sodium for injection. The percentages of the initial concentrations maintained at a minimum of 97% in the mixtures within 6 hours.
CONCLUSIONS
Nine commonly used clinical drugs remained stable in the pediatric electrolyte supplements injection for 6 hours at 25°C and avoiding from light. Mezlocillin sodium for injection was not recommended to be combined with electrolyte supplement injection for children because its insoluble particles exceed the standard.
Topics: Child; Chromatography, High Pressure Liquid; Drug Incompatibility; Drug Stability; Electrolytes; Humans; Mezlocillin; Pediatrics
PubMed: 35592087
DOI: 10.2147/DDDT.S363634 -
PloS One 2022Carbapenem-resistant Escherichia coli has emerged as a major public health issue across the world. This study was aimed to determine the virulence content and...
Carbapenem-resistant Escherichia coli has emerged as a major public health issue across the world. This study was aimed to determine the virulence content and phylogenetic groups of carbapenemase-producing E. coli isolates in southwest Iran. One hundred and fifty-two non-duplicate E. coli isolates were collected from various clinical samples. Antibiotic susceptibility and minimum inhibitory concentrations (MIC) were determined according to the Clinical and Laboratory Standards Institute (CLSI) guidelines by Kirby-Bauer disc diffusion and agar dilution methods. Phenotypic screening of carbapenemase enzymes was performed by modified Hodge test (MHT). Detection of carbapenemase genes, phylogenetic groups, and virulence-associated genes were also performed by the PCR assay. The highest and lowest resistance rates were observed against mezlocillin (70.4%) and doripenem (13.1%), respectively. Out of 28 isolates that were resistant to carbapenem antibiotics, 12 (7.9%) strains were phenotypically carbapenemase producers. The blaOXA-48 was the predominant carbapenemase gene, detected in 58.3% of isolates, followed by blaIMP (41.7%) and blaNDM (8.3%). None of the isolates harbored blaVIM and blaKPC genes. Among the twelve carbapenemase-producing strains, urinary isolates were mostly classified into B2 (41.7%) and D (25%) phylogenetic groups, while other clinical isolates belonged to B1 (25%) and A (8.3%) groups. The frequency of virulence-associated genes was also investigated in all isolates and ranged from 6.6% for hly to 75% for fimA. The emergence of carbapenemase-producing strains is a growing concern to public health. Therefore, the proper implementation of monitoring programs is crucial for limiting their dissemination.
Topics: Anti-Bacterial Agents; Bacterial Proteins; Carbapenem-Resistant Enterobacteriaceae; Escherichia coli; Microbial Sensitivity Tests; Phylogeny; Virulence; beta-Lactamases
PubMed: 35536848
DOI: 10.1371/journal.pone.0266787 -
Journal of Pharmaceutical and... Feb 2022To effectively control the polymerized impurities in mezlocillin sodium and sulbenicillin sodium, a HPSEC method with TSK-gel G2000SWxl column and a RP-HPLC method with...
To effectively control the polymerized impurities in mezlocillin sodium and sulbenicillin sodium, a HPSEC method with TSK-gel G2000SWxl column and a RP-HPLC method with C18 analytical column were established to replace the classical gel filtration chromatography with Sephadex G-10 gel as stationary phase. By studying the chromatographic behavior of polymerized impurities in both methods with different chromatographic separation mechanisms, the polymerized impurities in mezlocillin sodium and sulbenicillin sodium were separated and detected effectively. The column switching two-dimension liquid chromatography ion trap/time-of-flight mass spectrometry was applied to characterize the structures of polymerized impurities eluted from the HPSEC method and RP-HPLC method for both drugs. The structures of the polymerized impurities in mezlocillin sodium and sulbenicillin sodium were deduced based on the MS data. The results showed that the polymerized impurities detected by HPSEC method and RP-HPLC method were completely different. Therefore, two methods should be used meanwhile to control the polymerized impurities in mezlocillin sodium and sulbenicillin sodium.
Topics: Chromatography, High Pressure Liquid; Drug Contamination; Mezlocillin; Pharmaceutical Preparations; Sodium; Sulbenicillin; Tandem Mass Spectrometry
PubMed: 35026591
DOI: 10.1016/j.jpba.2022.114584 -
Journal of Chromatographic Science Oct 20223-Chlorocarbonyl-1-methanesulfonyl-2-imidazolidinone (CMI) is a critical intermediate used in the synthesis of mezlocillin drug substance and also a potential genotoxic...
3-Chlorocarbonyl-1-methanesulfonyl-2-imidazolidinone (CMI) is a critical intermediate used in the synthesis of mezlocillin drug substance and also a potential genotoxic impurity with acyl chloride moiety. The content of CMI in mezlocillin should be <0.16 ppm to avoid the carcinogenicity and mutagenicity threats to patients. Therefore, a workable determination of CMI was critically crucial for ensuring the safety of mezlocillin drug products. However, the conventional HPLC method is insufficient for detection limits at ppm or lower levels. Besides, the high activity of acyl chloride also raises a challenge to the direct measurement of CMI. Thus, we explored a simple esterification approach, which converts CMI into methyl 3-(methylonyl)-2-oxoimidazolidine-1-carboxylate completely by optimizing the reaction temperature and time. Furthermore, the selected reaction monitoring model of triple quadrupole mass spectrometer optimized by the Box-Behnken design significantly enhanced the sensitivity of ultra-trace level determination. The limit of detection and limit of quantification of the method were reached 0.014 and 0.02 ppm, respectively, in the following validation study. A sensitive and specific ultra-performance liquid chromatography tandem mass spectrometry method for ultra-trace level determination of acyl chloride potential genotoxic impurity in mezlocillin drug substance has been successfully established in this study, which will provide a practical quality control tool of mezlocillin.
Topics: Chlorides; Chromatography, High Pressure Liquid; Chromatography, Liquid; DNA Damage; Humans; Mezlocillin; Tandem Mass Spectrometry
PubMed: 34718453
DOI: 10.1093/chromsci/bmab119 -
Infection and Drug Resistance 2021We investigated the clonal diversity of carbapenemase-producing isolates from the Shenzhen Children's Hospital, China, and drew conclusions on the clinical and public...
AIM
We investigated the clonal diversity of carbapenemase-producing isolates from the Shenzhen Children's Hospital, China, and drew conclusions on the clinical and public health impact of these isolates as multidrug-resistant.
METHODS
From January 2014 to December 2018, a total number of 36 unique carbapenemase-producing clinical isolates of were collected out of 900 clinical isolates in paediatric patients from the Shenzhen Children's Hospital, China. After carbapenemase production confirmation, antimicrobial susceptibility, resistance determinants and phylogenetic relationship were determined.
RESULTS
The isolates showed resistance to ceftazidime, ertapenem, ampicillin, cefazolin, ceftriaxone, cefotetan, ticarcillin, cefaclor, cefpodoxime, azlocillin, cefcapene, mezlocillin and ampicillin-sulbactam. Of the 36 carbapenemase genes coding isolates, was the mostly detected 50% (n=18) followed by and 19% (n=7), 17% (n=6), 8% (n=3) and 5% (n=2), whereas extended-spectrum β-lactamase ( ) was predominantly detected 92% (n=33) followed by 53% (n=19) and 28% (n=10). Pulsed-field gel electrophoresis typing showed eight different patterns, and twenty-five distinct sequences types were observed with ST307 being predominantly identified 11% (n=4), followed by ST2407 8% (n=3). Plasmid replicon typing results indicated that IncFIS, IncHI2, IncFIC and IncFIA plasmids carry and genes.
CONCLUSION
This study reports on the occurrence and spread of carbapenemase and extended-spectrum β-lactamase encoding genes co-existence in sporadic ST307 in paediatric patients from the Shenzhen Children's Hospital, China.
PubMed: 34511949
DOI: 10.2147/IDR.S324018 -
Pakistan Journal of Medical Sciences 2021To investigate the value of dynamic monitoring of serum procalcitonin (PCT) in anti-infective therapy of patients with acute stroke.
OBJECTIVES
To investigate the value of dynamic monitoring of serum procalcitonin (PCT) in anti-infective therapy of patients with acute stroke.
METHODS
This is a case control retrospective study of acute stroke patients conducted from July 2016 to October 2018, in the Department of Neurology, Affiliated Hospital of Hebei University, who who reached within twenty four hours. They, were selected as the study subjects who were divided into infection group and non-infection group according to the inclusion and exclusion criteria. The serum PCT and CRP levels were compared between the two groups at 24 hours, 48 hours and 72 hours. In order to judge the changes of PCT level and the infection of stroke patients, different kinds of antibiotics were used for corresponding treatment. Retrospective analysis of the cases that did not monitor PCT anti infective treatment before July 2016 were compared with the cases that monitored PCT to guide anti infective treatment after July 2016, and compared the efficacy of antibiotics.
RESULTS
The serum PCT level of patients in the infection group was significantly higher than that of patients in the noninfection group (P<0.001). For the patients whose PCT<0.5 ng/ml within 72 hour, anti-infective therapy was not administered. However, for those patients whose PCT<0.5 ng/ml and CRP rose significantly, WBC, body temperature and chest CT were closely monitored. For the patients whose PCT increased slightly (0.5 ng/ml
mezlocillin, were administered. For the patients whose PCT increased moderately (5 ng/ml>PCT>2 ng/ml), mezlocillin/ sulbactam or ceftriaxone/ tazobactam was administered. For patients whose PCT increased significantly (PCT>5 ng/ml), carbapenem antibiotic or a combination of two antibiotics was administered. CONCLUSION
Dynamic detection of serum PCT concentration can make accurate judgment on the severity of bacterial infection in patients with acute stroke and guide the rational application of antibiotics.
PubMed: 34290800
DOI: 10.12669/pjms.37.4.3932 -
BMC Nephrology Nov 2020Glomerular disease patients have a high risk of infection, which contributes to the progression of disease per se and mortality, especially in those with long-term use...
BACKGROUND
Glomerular disease patients have a high risk of infection, which contributes to the progression of disease per se and mortality, especially in those with long-term use of glucocorticoids and (or) immunosuppressive agents. Cases of sporadic nocardiosis have been reported in glomerular disease patients, and this observation was conducted to comprehensively understand the manifestations of and treatments for nocardiosis, which is commonly misdiagnosed as pneumonia or tuberculosis or even as lung cancer or metastatic tumors in glomerular disease patients.
METHODS
We reviewed the demographic characteristics, laboratory abnormalities, radiological features, and treatments of 7 patients with nocardiosis and glomerular disease receiving steroids and immunosuppression therapy at the nephrology department of the Second Xiangya Hospital between 2012 and 2019.
RESULTS
It was found that all 7 patients had been receiving methylprednisolone for renal disease at a median dose of 20 mg per day and a median duration of 4 months before developing nocardiosis. There were 4 males and 3 females, and the median age was 52.14 years. All 7 patients had hypoalbuminemia at the time of admission. In addition, various cystic abscesses in the subcutaneous tissue, with or without lung and brain involvement, were observed in these patients. Encouragingly, body temperatures returned to normal, and subcutaneous abscesses diminished or disappeared with compound sulfamethoxazole treatment alone or in combination with linezolid, imipenem and mezlocillin/sulbactam.
CONCLUSIONS
It was shown that multisite abscesses, including subcutaneous, pulmonary and cerebral abscesses, were the common manifestations of nocardiosis in glomerular disease patients. Sulfonamide was the first-line antibiotic therapy for nocardiosis, and combinations of other antibiotics were also needed in some serious cases.
Topics: Abscess; Aged; Anti-Bacterial Agents; Brain; Brain Abscess; Female; Glomerulonephritis; Glucocorticoids; Humans; Immunocompromised Host; Immunosuppressive Agents; Lung; Lung Abscess; Magnetic Resonance Imaging; Male; Middle Aged; Nocardia Infections; Sulfonamides; Tomography, X-Ray Computed
PubMed: 33243202
DOI: 10.1186/s12882-020-02179-9 -
Molecules (Basel, Switzerland) Aug 2020The SARS-CoV-2 outbreak caused an unprecedented global public health threat, having a high transmission rate with currently no drugs or vaccines approved. An alternative...
The SARS-CoV-2 outbreak caused an unprecedented global public health threat, having a high transmission rate with currently no drugs or vaccines approved. An alternative powerful additional approach to counteract COVID-19 is drug repurposing. The SARS-CoV-2 main protease is essential for viral replication and an attractive drug target. In this study, we used the virtual screening protocol with both long-range and short-range interactions to select candidate SARS-CoV-2 main protease inhibitors. First, the Informational spectrum method applied for small molecules was used for searching the Drugbank database and further followed by molecular docking. After screening of drug space, we identified 57 drugs as potential SARS-CoV-2 main protease inhibitors that we propose for further experimental testing.
Topics: Allosteric Site; Antiviral Agents; Betacoronavirus; COVID-19; Catalytic Domain; Coronavirus 3C Proteases; Coronavirus Infections; Cysteine Endopeptidases; Drug Repositioning; Gene Expression; High-Throughput Screening Assays; Humans; Mezlocillin; Molecular Docking Simulation; Pandemics; Pneumonia, Viral; Protease Inhibitors; Protein Binding; Protein Conformation, alpha-Helical; Protein Conformation, beta-Strand; Protein Interaction Domains and Motifs; Raltegravir Potassium; SARS-CoV-2; Thermodynamics; Viral Nonstructural Proteins; Virus Replication
PubMed: 32842509
DOI: 10.3390/molecules25173830 -
Analytical Methods : Advancing Methods... Jul 2020For the multiple and rapid detection of β-lactams, the broadly specific penicillin-binding protein (PBP) that recognizes the β-lactam structure was prepared. A...
For the multiple and rapid detection of β-lactams, the broadly specific penicillin-binding protein (PBP) that recognizes the β-lactam structure was prepared. A chromatographic strip based on europium chelate-loaded fluorescent microspheres was assembled with a goat anti-mouse antibody (C line) and penicillin coating (T line). The penicillin coating competes with free β-lactam antibiotics to bind PBP-labeled fluorescent microspheres. The strip can theoretically detect all kinds of β-lactams, including amoxicillin, ampicillin, oxacillin, ceftazidime, lenampicillin, cefoperazone, sultamicillin, cefotaxime, ceftriaxone, sulbenicillin, piperacillin, cephalothin, flucloxacillin, and mezlocillin, in samples within 10 min. The europium chelate-labeled lateral flow assay does not cross-react with other antibiotics, including chloramphenicol, tetracycline, sulfamethazine, enrofloxacin, gentamicin or lincomycin. In short, we developed a very useful method for preliminary screening of β-lactams.
Topics: Anti-Bacterial Agents; Chemistry Techniques, Analytical; Europium; Penicillin-Binding Proteins; beta-Lactams
PubMed: 32701084
DOI: 10.1039/d0ay01140a