Cefuroxime Axetil Research Articles

An outpatient antibacterial stewardship intervention during the journey to JCI accreditation

BackgroundAntibacterial overuse, misuse and resistance have become a major global threat. The Joint Commission International (JCI) accreditation standards include quality improvement and patient safety, which is exemplified by antimicrobial stewardship. There are currently few reports on interventions to improve the quality of outpatient antibacterial prescribing.MethodsA before-after intervention study, aiming at antibacterial use in outpatients, was performed in a university-affiliated hospital with 2.8 million outpatient visits annually during the journey to JCI accreditation (March of 2012 - March of 2013). Comprehensive intervention measures included formulary adjustment, classification management, motivational, information technological, educational and organizational measures. A defined daily dose (DDD) methodology was applied. Pharmacoeconomic data and drug-related problems (DRPs) were statistically compared between the two phases.ResultsThe variety of antibacterials available in outpatient pharmacy decreased from 38 to 16. The proportion of antibacterial prescriptions significantly decreased (12.7% versus 9.9%, P < 0.01). The proportion of prescriptions containing the restricted antibacterials was 30.4% in the second phase, significantly lower than the value of 44.7% in the first phase (P < 0.01). The overall proportion of oral versus all antibacterial prescriptions increased (94.0% to 100%, P < 0.01) when measured as defined daily doses. Statistically significant increases in relative percentage of DDDs of oral antibacterials (i.e., DDDs of individual oral antibacterial divided by the sum of DDDs of all antibacterials) were observed with moxifloxacin, levofloxacin, cefuroxime axetil, ornidazole, clindamycin palmitate, cefaclor, amoxicillin and clarithromycin. Occurrence rate of DRPs decreased from 13.6% to 4.0% (P < 0.01), with a larger decrease seen in surgical clinics (surgical: 19.5% versus 5.6%; internal medicine: 8.4% versus 2.8%, P < 0.01). The total expenditure on antibacterials for outpatients decreased by 34.7% and the intervention program saved about 6 million Chinese Yuan Renminbi (CNY) annually.ConclusionThe one-year intervention program on outpatient antibacterial use during the journey to JCI accreditation reduced the expenditure on antibacterials, improved the appropriateness of antibacterial prescriptions. Quality improvements need integrated multifaceted intervention measures and long-term adherence to the antibiotic stewardship. Approach of i.v. to oral antibacterial switch, classification management, and motivational measures may play the most efficient role in changing antibacterial prescription practices.

The identification, typing, and antimicrobial susceptibility of Pseudomonas aeruginosa isolated from mink with hemorrhagic pneumonia

The biological characteristics and molecular epidemiology of Pseudomonas aeruginosa associated with mink hemorrhagic pneumonia from Shandong province of eastern China were determined in this study. From 2010 to 2011, 30 mink P. aeruginosa isolates were identified from lung, fecal and feed samples of clinical cases and subjected to serotyping, antimicrobial susceptibility testing and pulsed-field gel electrophoresis (PFGE) using SpeI. The P. aeruginosa isolates belonged to four serotypes—21 of type G, four of type I, three of type M, one of type B, and one non-typable strain. The strains were divided into four large groups as determined by PFGE. Isolates from the group 2 were highly homologous and were obtained from the same region as an epidemic. All of the isolates were sensitive to piperacillin, piperacillin/tazobactam, ceftazidime, cefepime, imipenem, amikacin, gentamicin and tobramycin and resistant to ampicillin, cefuroxime and cefuroxime axetil. A high frequency of resistance was found to ampicillin/sulbactam, cefazolin, cefotetan, ceftriaxone, nitrofurantoin, and trimethoprim/sulfamethoxazole (96.7%). Resistance to ticarcillin/clavulanic acid, ciprofloxacin and levofloxacin was less common (13.3%). There was no relationship between antibiotic resistance and serotype distribution of the isolates. The epidemic serotype of P. aeruginosa from the mink hemorrhagic pneumonia in Shandong province was type G, which was a clone of commonly found in this province. These findings reveal the genetic similarities and antimicrobial susceptibility profiles of P. aeruginosa from clinical cases of mink hemorrhagic pneumonia and will facilitate the prevention and control of the disease in Shandong province of China.

Design and characterization of cefuroxime axetil biphasic floating minitablets

Biphasic floating minitablets of cefuroxime axetil were prepared by melt granulation technique using two different grades of gelucire namely 50/13 and 43/01 to maintain constant plasma drug concentration. Loading dose of cefuroxime axetil was formulated as immediate release (IR) minitablets by using hydrophilic grade of gelucire 50/13. Maintenance dose was formulated as floating sustained release (SR) minitablets by using hydrophobic grade of gelucire 43/01. The prepared IR and SR granules were subjected to micromeritic studies and scanning electron microscopy. Fourier transform infrared spectroscopy (FT-IR) study revealed that drug and selected carriers were compatible. In vitro dissolution study of optimized IR minitablets showed more than 85% of loading dose dissolved within 30 min. Optimized SR minitablets showed zero lag time with floating duration more than 12 h. The drug release from SR minitablets was linear with square root of time with non-Fickian diffusion-controlled release. The optimized batch of minitablets was filled into 0 size hard gelatin capsule. In vitro dissolution study for capsule showed an immediate burst release followed by SR up to 12 h. There is no significant change in dissolution data after storage at 40 °C and 75% RH for three months. Microbiological assay of dissolution samples of optimized minitablets filled in capsules showed proportionate increase in inhibition of growth against Escherichia coli up to 12 h samples. In vivo bioavailability study in albino rabbits showed three times improvement in oral bioavailability.

Oral Adverse Reaction to Cefuroxime Axetil

A 62 year old female patient was referred to the Department of oral medicine due to the severe oral reaction two days after she started to use cefuroxime axetil. Buccal and sublingual mucosa was very inflamed and covered with thick pseudomembranes. Patient was otherwise healthy and did not take any medication. She was advised to stop the suspected drug intake immediately and was given intramuscular methylprednisolone injection (40mg, i.e. 1mg/kg) as well as chlorhexetidine mouthwash with local anaesthetic (Xylocaine) to be used at home three times a day. After seven days the lesions healed completely. Two months after the adverse drug side effect, allergic tests were performed. In vitro tests (indirect degranulation of basophile granulocytes and blast transformation of lymphocytes) as well asepicutaneous test were negative to cefuroxime axetil.

Cefuroxime axetil induced glossitis: a case report

Cefuroxime axetil is a semi synthetic cephalosporin antibiotic, which is prescribed for different types of infections such as lung, ear, throat, urinary tract, and skin. This is the drug of choice in the treatment and prevention of streptococcal infections. In this case, the patient was prescribed cefuroxime axetil, diclofenac, and paracetamol for pharyngitis. The patient developed glossitis 3 hrs after ingestion of above drugs which improved after withdrawing the offending drug. Glossitis is an uncommon, but serious adverse drug effect of cefuroxime axetil. It is important to recognize and manage it to prevent fatality. The case has been reported to the Pharmacovigilance Center Uttar Pradesh Rural Institute of Medical Sciences and Research Saifai, Etawah.

Pharmacokinetic and Bioequivalence Studies of Oral Cefuroxime Axetil 250 mg Tablets in Healthy Human Subjects

The objective of this study was to determine the bioequivalence of two Cefuroxime oral 250 mg tablet formulation. One was the innovators brand (Zinnat®), was taken as reference brand (REF) and the other was a newly developed, optimized and cost effective formulation (TEST). A single dose, open, random sequence, cross over, two treatment study with a one week washout period in between was carried out in 12 healthy male Pakistani young volunteers. Reference and Test tablets were administered to these volunteers with 150 mL of water after an overnight fast. Blood samples were drawn 15 min prior to the administration of dose and at 0.5, 1, 1.5, 2, 3, 4, 5, 6, 7 and 8 hours post dose. The cefuroxime concentrations in the plasma were determined by a modified, simple HPLC method in which the mobile phase was 10 mM solution of ammonium acetate and acetonitrile, pH was adjusted to 5 ± 0.2 with glacial acetic acid. The wavelength of detection was 254 nm having a flow rate of 1ml/min and the retention time of 5.8 min. The method was validated as per the ICH requirements. Both compartmental and non-compartmental methods were used to determine the various PK parameters such as Cmax. Tmax, AUC0-t, AUC0-∞ , AUMC, MRT, t1/2, Kel, Vd and Cl using Kinetica® ver 4.4.1 The bioequivalence between the REF and TEST cefuroxime axetil 250mg formulations was established as the Latin square design of ANOVA does not show any significant difference with a p≥0.05 for period and the 90% confidence interval lies within the acceptable range (80-125%) for the log transformed data of Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, AUMC, MRT, Vd and Cl, showing a comparable plasma profiles generated by both the formulations. It is, thus concluded that both the formulations were bioequivalent.

Simple and Robust Analysis of Cefuroxime in Human Plasma by LC-MS/MS: Application to a Bioequivalence Study.

A simple, robust LC-MS/MS assay for quantifying cefuroxime in human plasma was developed. Cefuroxime and tazobactam, as internal standard (IS), were extracted from human plasma by methanol to precipitate protein. Separation was achieved on a Zorbax SB-Aq (4.6 × 250 mm, 5 μm) column under isocratic conditions. The calibration curve was linear in the concentration range of 0.0525–21.0 μg/mL (r = 0.9998). The accuracy was higher than 90.92%, while the intra- and interday precision were less than 6.26%. The extraction procedure provides recovery ranged from 89.44% to 92.32%, for both analyte and IS. Finally, the method was successfully applied to a bioequivalence study of a single 500 mg dose of cefuroxime axetil in 22 healthy Chinese male subjects under fasting condition. Bioequivalence was determined by calculating 90% Cls for the ratios of C max, AUC0−t, and AUC0−∞ values for the test and reference products, using logarithmic transformed data. The 90% Cls for the ratios of C max (91.4%~104.2%), AUC0−t (97.4%~110.9%), and AUC0−∞ (97.6%~111.1%) values were within the predetermined range. It was concluded that the two formulations (test for capsule, reference for tablet) analyzed were bioequivalent in terms of rate and extent of absorption and the method met the principle of quick and easy clinical analysis.

A Study to Compare the Safety and Efficacy of Levofloxacin Versus Cefuroxime Axetil in Patients with Uncomplicated Lower UTI in a North Indian Medical College and Hospital

(1) Assistant Professor, MBBS, MD, Department of Pharmacology, Gian Sagar Medical College and Hospital, Village Ram Nagar, District Patiala, Punjab, India-140601 (2) Associate Professor, MBBS, MD, Department of Pharmacology, Gian Sagar Medical College and Hospital, Village Ram Nagar, District Patiala, Punjab, India-140601 (3) Professor and Head, MBBS, MD, Department of Pharmacology, Maharishi Markendeshwar Institute of Medical Sciences and Research, Mullana, Ambala, India133207 (4) Professor, MBBS, MD, Department of Medicine, Gian Sagar Medical College and Hospital, Village Ram Nagar, District Patiala, Punjab, India-140601 (5) Professor and Head, MBBS, MD, Department of Microbiology, Adesh institute of Medical Sciences and Research, Bathinda, Punjab, India-151109 (6) Professor & Head, MBBS, DA, MD, Department of Pharmacology, Gian Sagar Medical College and Hospital, Village Ram Nagar, District Patiala, Punjab, India-140601

Development and Validation of UV Spectrophotometric Method for the Determination of Cefuroxime Axetil in Bulk and Pharmaceutical Formulation

The present study was undertaken to develop and validate a simple, sensitive, accurate, precise and reproducible UV spectrophotometric method for cefuroxime axetil using methanol as solvent. In this method the simple UV spectrum of cefuroxime axetil in methanol was obtained which exhibits absorption maxima (?max) at 278 nm. The quantitative determination of the drug was carried out at 278 nm and Beer’s law was obeyed in the range of (0.80-3.60) µg/ml. The proposed method was applied to pharmaceutical formulation and percent amount of drug estimated (95.6% and 96%) was found in good agreement with the label claim. The developed method was successfully validated with respect to linearity, specificity, accuracy and precision. The method was shown linear in the mentioned concentrations having line equation y = 0.05x + 0.048 with correlation coefficient of 0.995. The recovery values for cefuroxime axetil ranged from 99.85-100.05. The relative standard deviation of six replicates of assay was less than 2%. The percent relative standard deviations of inter-day precision ranged between 1.45-1.92% and intra-day precision of cefuroxime axetil was 0.96-1.51%. Hence, proposed method was precise, accurate and cost effective. Keywords: UV-Vis spectrophotometer; Method validation; Cefuroxime axetil; Recovery studies. © 2013 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved. doi: http://dx.doi.org/10.3329/jsr.v6i1.14879 J. Sci. Res. 6 (1), 133-141 (2013)

Differentiating amorphous mixtures of cefuroxime axetil and copovidone by X-ray diffraction and differential scanning calorimetry

The amorphous, molecular solid dispersion of cefuroxime axetil and copovidone with the mass ratio 71/29 is compared to its pure components in the amorphous state and to an amorphous mechanical mixture with the same mass ratio. Calorimetric studies demonstrate that all these materials are vitreous. By using X-ray diffraction profiles, a clear difference can be observed between the local order of the solid dispersion and that of the mechanical mixture. More generally, it is shown how the presence or absence of additivity in the diffraction data can be used to distinguish between different amorphous mixtures.

Острый стрептококковый тонзиллит у ребенка. Вопросы, заданные жизнью (ответы науки на вопросы, заданные практикой)

Проблема острого тонзиллита сохраняет свою актуальность в клинической педиатрии. Особую роль при этом играет β-гемолитический стрептококк группы А (Streptococcus pyogenes), обнаруженный у каждого четвертого ребенка с острым бактериальным тонзиллитом. В статье на примере клинического случая описаны характеристика возбудителя, эпидемиология и прогноз заболевания. Авторами рассмотрены современные критерии диагностики и международные подходы к лечению. Обоснована необходимость применения цефуроксима аксетила при эрадикационной терапии Streptococcus pyogenes.

Fosfomycin Trometamol: A Review of Its Use as a Single-Dose Oral Treatment for Patients with Acute Lower Urinary Tract Infections and Pregnant Women with Asymptomatic Bacteriuria

Fosfomycin trometamol (fosfomycin tromethamine) [Monuril(®), Monurol(®), Monural(®)] is approved in numerous countries worldwide, mainly for the treatment of uncomplicated urinary tract infections (UTIs). Fosfomycin has good in vitro activity against common uropathogens, such as Escherichia coli (including extended-spectrum β-lactamase-producing E. coli), Proteus mirabilis, Klebsiella pneumoniae and Staphylococcus saprophyticus, and the susceptibility of uropathogens to fosfomycin has remained relatively stable over time. A single oral dose of fosfomycin trometamol 3g (the approved dosage) achieves high concentrations in urine. Results of recent randomized trials indicate that single-dose fosfomycin trometamol had similar clinical and/or bacteriological efficacy to 3- to 7-day regimens of ciprofloxacin, norfloxacin, cotrimoxazole or nitrofurantoin in women with uncomplicated lower UTIs. In addition, single-dose fosfomycin trometamol had similar bacteriological efficacy to a 5-day course of cefuroxime axetil or a 7-day course of amoxicillin/clavulanic acid in pregnant women with asymptomatic bacteriuria, and similar clinical and/or bacteriological efficacy to a 5-day course of cefuroxime axetil or amoxicillin/clavulanic acid or a 3-day course of ceftibuten in pregnant women with a lower UTI. Single-dose fosfomycin trometamol was generally well tolerated, with gastrointestinal adverse events (e.g. diarrhoea, nausea) reported most commonly. In conclusion, single-dose fosfomycin trometamol is an important option for the first-line empirical treatment of uncomplicated lower UTIs.

PREPARATION AND CHARACTERIZATION OF AMORPHOUS CEFUROXIME AXETIL

In the present study, amorphous form of cefuroxime axetil was prepared and characterized by various methods. The result showed that the amorphous form of cefuroxime axetil with hydrophilic carriers was successfully obtained by freeze drying. The amorphous form showed a substantially higher dissolution rate and saturation solubility than cefuroxime axetil and physical mixture. The molecular behaviour of the drug in all samples were characterized by X-ray powder diffraction, Fourier transformed infrared spectroscopy, scanning electron microscopy and differential scanning calorimetry. The dissolution and saturation solubility studies of the samples were performed. The X-ray powder diffraction, Fourier transformed infrared spectroscopy and differential scanning calorimetry provided useful information to support the amorphousness of the samples.

Development and evaluation of taste-masked dry suspension of cefuroxime axetil for enhancement of oral bioavailability

Cefuroxime axetil (CA) is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally. This work was to mask the bitter taste of CA and enhance its oral bioavailability. Dry suspensions were prepared by means of wet granulation method and solid dispersion method. Binders, suspending agents and other compositions involved in the formulation were optimized. The differential scanning calorimetry (DSC) analysis indicated that CA was amorphous in the solid dispersion with stearic acid as the carrier, which contributed to an improvement of the dissolution rate. Taste evaluation was performed by three volunteers and taste masking was successfully achieved by the methods mentioned above. A pH 7.0 phosphate buffer was adopted to study the in vitro dissolution performance of the three formulations, i.e., two self-made dry suspensions and the commercial one. With a better release characteristic and a satisfying taste masking ability, the solid dispersion suspension was selected as the optimal formulation for the further pharmacokinetic study in beagle dogs. The values of Cmax and AUC0–12 for the solid dispersion suspension were about 1.78-fold and 2.17-fold higher than these of reference suspension, respectively. The obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability.

Acute Bacterial Sinusitis in Children

On the basis of strong research evidence, the pathogenesis of sinusitis involves 3 key factors: sinusostia obstruction, ciliary dysfunction, and thickening of sinus secretions. On the basis of studies of the microbiology of otitis media, H influenzae is playing an increasingly important role in the etiology of sinusitis, exceeding that of S pneumoniae in some areas, and b-lactamase production by H influenzae is increasing in respiratory isolates in the United States. On the basis of some research evidence and consensus,the presentation of acute bacterial sinusitis conforms to 1 of 3 predicable patterns; persistent, severe, and worsening symptoms. On the basis of some research evidence and consensus,the diagnosis of sinusitis should be made by applying strict clinical criteria. This approach will select children with upper respiratory infection symptoms who are most likely to benefit from an antibiotic. On the basis of some research evidence and consensus,imaging is not indicated routinely in the diagnosis of sinusitis. Computed tomography or magnetic resonance imaging provides useful information when complications of sinusitis are suspected. On the basis of some research evidence and consensus,amoxicillin-clavulanate should be considered asa first-line agent for the treatment of sinusitis.

In vitro/in vivo comparison of cefuroxime release from poly(ε‐caprolactone)–calcium sulfate implants for osteomyelitis treatment

This study aimed to investigate the release of cefuroxime axetil (CF) and calcium from poly(ε-caprolactone) (PCL)-calcium sulfate (CaS) implants (PCL:CaS 2:1-10% CF; PCL:CaS 2:1-20% CF; PCL:CaS 1:1-10% CF) for treating infectious bone diseases. Bioactivity, crystallinity and strength, and release profiles under standard and pressurized release conditions were studied. PCL:CaS 2:1-20% CF had slower release than 10% loading. These groups had no significant change in CF and Ca release in response to pressure. The PCL:CaS 1:1 group had the slowest release despite having higher CaS, probably due to more compaction of discs. In contrast, pressure caused significant differentiation of CF and Ca(2+) release. The presence of CaS enhanced mechanical properties and bioactivity of discs. SEM and XPS results showed calcium-phosphate containing accumulations on surfaces upon SBF incubation. CF-loaded implants were applied in a rabbit osteomyelitis model. In vivo CF release was enhanced with increased CaS proportions, suggesting that in vivo release conditions are closer to pressurized in vitro conditions. In the control group, there was still some inflammation in the bone and no complete coverage with bone was achieved in the defect site. Discs provided a suitable surface for regeneration of bone. However, bone formation in the PCL:CaS 1:1 disc implanted group was more complete and regular than in the 2:1 group.

Extraction and Mechanism Investigation of Trace Cefuroxime Axetil Using Ionic Liquid-Salt Aqueous Two-phase System

Extraction and Mechanism Investigation of Trace Cefuroxime Axetil Using Ionic Liquid-Salt Aqueous Two-phase System

SCF Preparation of Drug Particle Using Size Adjustable Nozzle

The preliminary study of the three-channel size adjustable coaxial nozzle which was used in supercritical fluid particles preparation technology was given in this paper, what's more, we considered the influence of some experimental conditions on the preparation product, such as pressure, nozzle size. According to the problem of reunion of cefuroxime axetil particles appeared in the preparation process, this paper elaborates the mechanism of reunion, and adopted the method of adding surfactants to solve the reunion problems effectively.

English

The aim of the present investigation was to increase the gastric residence time of cefuroxime axetil by preparing gastro retentive mucoadhesive tablet, thereby improving bioavailability of cefuroxime axetil. Tablets were prepared using different mucoadhesive polymers such as hydroxypropylmethyl cellulose K4M, carbopol 974P, sodium alginate, and chitosan in combination ratios by wet granulation method. All the batches were subjected to various evaluation parameters such as physicochemical properties, swelling index,&nbsp;in vitro&nbsp;residence time, and&nbsp;in vitro&nbsp;drug release. Optimized formulation containing carbopol 974P and chitosan in combination (F6) exhibited maximum&nbsp;in vitro&nbsp;residence time of 10.05 h and&nbsp;in vitro&nbsp;release up to 45.89% in 10 h. The F6 formulation was further subjected to&nbsp;in vitro&nbsp;permeation, scanning electron microscope (SEM), stability studies and&nbsp;in vivo&nbsp;residence time. SEM revealed smooth surface characteristics with increasing pore diameter, indicating the diffusion mechanism of release. Stability was conducted as per International Conference on Harmonisation (ICH) guidelines at 40 &plusmn; 20&deg;C/75 &plusmn; 5% relative humidity (RH) and the values were within permissible limits.&nbsp;In vivo&nbsp;X-ray photographs taken during the experiment showed mucoadhesion to the gastric mucosa up to 10 h. &nbsp; Key words:&nbsp;Cefuroxime axetil, gastro retentive, mucoadhesive polymers, X-ray study.

Nervous System Lyme Disease: Diagnosis and Treatment

The tick-borne spirochete responsible for Lyme disease is highly antibiotic-sensitive. Treatment related misconceptions can be attributed to confusion in three principal realms: (1) the appropriate approach to diagnosis (who should be treated); (2) necessary and appropriate treatment; and (3) what actually constitutes nervous system infection and to what extent this mandates different treatment. Contrary to often-repeated assertions, laboratory-based diagnosis-in the appropriate setting-is as valid as it is in most other serologically diagnosed infections. Treatment is highly effective in the vast majority of patients, including those with nervous system disease. Nervous system infection, most typically meningitis, cranial neuritis, radiculoneuritis, and other forms of mononeuropathy multiplex, is highly antibiotic responsive. The encephalopathy that can be seen in some patients with active infection represents the same phenomenon that occurs in patients with many other inflammatory disorders, is not evidence of central nervous system (CNS) infection, and does not require any different, more prolonged, or more intensive treatment. In patients with infection not involving the CNS, oral treatment with amoxicillin, cefuroxime axetil, or doxycycline for 2-4weeks is almost always curative. Despite historic preferences for parenteral treatment with ceftriaxone, cefotaxime, or meningeal dose penicillin, patients with the forms of nervous system involvement listed above are highly responsive to oral doxycycline. Parenteral regimens can be reserved for those very rare patients with parenchymal CNS involvement, other severe forms of infection, or the approximately 5% of patients who fail to respond to oral regimens.