Analysis of Ornidazole Injection in Clinical Use at Post-marketing Stage by Centralized Hospital Monitoring System

This study aims to analyze the clinical use of ornidazole injection at the post-marketing stage by centralized hospital monitoring system method,and investigate its widespread use in patients,in order to regulate and guide the rational drug use,improve the drug specificity and provide a basis for drug therapy.The study adopts a prospective,multi-center,large sample size,centralized hospital monitoring system.We selected five leading hospitals in Hubei province,and observed the inpatients who received the ornidazole injection from July 1,2015 to October 31,2015.The basic information of patients was recorded,as well as the drug use and adverse events.The statistical analysis was performed based on these data.A total of 4396 individuals were enrolled in this study,most of them were middle-aged female patients and the ornidazole injection was mainly used as prophylactic prior to surgery to prevent the infections,and surgical treatment of anaerobic infections,abdominal infections and pelvic infections.The irrational drug use existed mainly in the prescribing and administration process,including unreasonable dosing frequency,rapid intravenous drip speed and extended duration of drug use.Eleven cases of adverse reactions were collected during the monitoring,incidence rate of adverse reactions was 2.5‰;adverse drug reactions occurred within 30 min.The study results fully reflected the usage of ornidazole injection in the real world.Based on the study,we calculated the adverse reaction incidence of ornidazole and identified the risk factors which may affect the safety of ornidazole injection.Study results strongly recommend that the manufacturers should publish standards for inpatient use and doctors should prescribe with caution accordingly.

Cefoperazone-sulbactam and ornidazole for Gardnerella vaginalis bloodstream infection after cesarean section:A case report

BACKGROUND Gardnerella vaginalis(G.vaginalis)is a facultative anaerobic bacteria known to cause bloodstream infections.However,cases are very rare in clinics.There is very limited clinical experience in the treatment of bloodstream infections caused by G.vaginalis.Therefore,there is an urgent need for effective antibacterial drugs to treat patients with bloodstream infections caused by G.vaginalis.CASE SUMMARY A woman who underwent a cesarean section presented with a sudden onset of high fever 1-d post-surgery.The blood cultures suggested an infection due to G.vaginalis,and treatment with cefoperazone-sulbactam was started.After 5 d of treatment,there was a decrease in the hemogram;however,the temperature and C-reactive protein levels remained high.Based on clinical experience and a review of literature,the treatment was modified to include ornidazole in combination with cefoperazone-sulbactam.Following a week of treatment,the temperature,hemogram and C-reactive protein levels returned to normal,and blood cultures turned negative,suggesting a therapeutic effect of the combination treatment.CONCLUSION This case highlighted the effective use of cefoperazone-sulbactam combined with ornidazole for bloodstream infection caused by G.vaginalis following a cesarean section.

Characterization of ornidazole metabolites in human bile after intraveneous doses by ultraperformance liquid chromatography/quadrupole time-of-flight mass spectrometry

Ultraperformance liquid chromatography/quadrupole time-of-flight mass spectrometry(UPLC/Q-TOF MS)was used to characterize ornidazole metabolites in human bile after intravenous doses.A liquid chromatography tandem mass spectrometry(LC–MS/MS)assay was developed for the determination of the bile level of ornidazole.Bile samples,collected from four patients with T-tube drainage after biliary tract surgery,were prepared by protein precipitation with acetonitrile before analysis.A total of 12 metabolites,including 10 novel metabolites,were detected and characterized.The metabolites of ornidazole in human bile were the products of hydrochloride(HCl)elimination,oxidative dechlorination,hydroxylation,sulfation,diastereoisomeric glucuronation,and substitution of NO_(2) or Cl atom by cysteine or N-acetylcysteine,and oxidative dechlorination followed by further carboxylation.The bile levels of ornidazole at 12 h after multiple intravenous infusions were well above its minimal inhibitory concentration for common strains of anaerobic bacteria.

Synthesis of PAA-g-PNVCL Graft Copolymer and Studies on Its Loading of Ornidazole

A well-defined amphiphilic graft copolymer,consisting of hydrophobic poly(tert-butyl acrylate)(PtBA)backbone and hydrophilic poly(N-vinylcaprolactam)(PNVCL)side chains,was synthesized by successive reversible addition-fragmentation chain transfer(RAFT)polymerization and atom transfer radical polymerization(ATRP).A new acrylate monomer bearing a chlorine-based initiating group,tert-butyl 2-((2-chloropropanoyloxy)methyl)-acrylate,was first RAFT homopolymerized in a controlled way to give a well-defined homopolymer with a narrow molecular weight distribution(M_(w)/M_(n)=1.15).This homopolymer directly initiated ATRP of N-vinylcaprolactam(NVCL)to afford a well-defined PtBA-g-PNVCL graft copolymer(M_(w)/M_(n)=1.22)via the grafting-from strategy without polymeric functionality transformation.PAA-g-PNVCL graft copolymer was prepared by selectively hydrolyzing PtBA-g-PNVCL.Ornidazole(ONZ)-loaded polymeric micelles using PAA-g-PNVCL copolymer as carrier were prepared by physical entrapping.Drug release experiment of the nano-carrier indicated the pH-dependent drug release characteristics.

Lipase-Catalyzed Resolutions of both Enantiomers of Ornidazole and Secnidazole

The resolutions of both enantiomers of the ornidazole and sec-nidazole were achieved with high enantiomeric excesses (ee > 99%) by acylation of the corresponding racemates with vinylac-etate in the presence of lipase Amano AK (from Pseudomonas sp.). The assignments of the absolute configurations of ( + ) or ( - )-ornidazole and secnidazole are described.

注射用氨曲南与奥硝唑氯化钠注射液的配伍稳定性考察

目的:研究氨曲南与奥硝唑氯化钠注射液配伍的稳定性。方法:采用RP-HPLC测定氨曲南和奥硝唑的含量,同时观察配伍液外观变化及监测pH值变化。结果:氨曲南与奥硝唑氯化钠注射液配伍后,氨曲南色谱峰出现肩峰,配伍液1小时即呈现颜色变化。结论:氨曲南与奥硝唑氯化钠注射液不宜配伍使用。

注射用氨曲南与奥硝唑葡萄糖注射液的配伍稳定性考察

目的:研究氨曲南与奥硝唑葡萄糖注射液配伍的稳定性。方法:采用RP-HPLC测定氨曲南和奥硝唑的含量,同时观察配伍液外观变化及监测PH值变化。结果:氨曲南与奥硝唑葡萄糖注射液配伍后4h呈现颜色变化。奥硝唑色谱峰5h时出现肩峰。结论:氨曲南与奥硝唑葡萄糖注射液可以配伍使用,但宜在4h内滴注完毕。

Boosted sustained-release with iron-based MOF-derived mesoporouscarbon-spheres as a nitroimidazole drugs carrier

Metal-organic framework(MoF)with a buildable internal structure has aroused great interest focus as self-sacrificing precursors of porous carbon(PC).However,as a drug carrier,the MOF-derived PC developed thus far are generally composed of irregular powder shape due to their crystalline nature,which consequently causing the cerebral infarction,cerebral thrombosis,and other blood diseases.In this article,we propose a novel approach to constructing amorphous carbon microspheres(AcMs)by dis-torting the topological network through hydrothermal treatment precursors of MIL-101(Fe).Then,a distinctive MIL-101(Fe)-derived spherical porous carbons(MSPC)is achieved through high temperature calcination toward ACMs.Effects of the glucose initial concentration and hydrothermal treatment time on the sphericity of the as-prepared mesoporous MsPC were investigated in depth.And the loading capacities and sustained-release performances of nitroimidazole drugs over MsPC through simulation internal environment of human body at different pH values was systematically evaluated.The nitro-imidazole drugs loading rate and release time of MsPC are 10% and 17 h under preferred process.Furthermore,the MSPC exhibited very low toxicity on Hela cells and 293T cells at the concentrations tested(10-800μg mL^(-1)).This study,therefore,supports the potential of the mesoporous carbon spheres as a carrierfor nitroimidazole drug delivery.

Simultaneous determination of three 5-nitroimidazoles in foodstuffs by differential pulse voltammetry and chemometrics

The voltammetric behaviour of three 5-nitroimidazoles,metronidazole,tinidazole and ornidazole,was investigated,and a method was developed for the simultaneous determination of these compounds,based on their reduction at a hanging mercury drop electrode（HMDE） in pH 8.95 buffer with differential pulse voltammetric（DPV） approach.Well defined voltammetric waves with peak potentials of -692,-640 and -652 mV were observed for these compounds,respectively.It is difficult to determine them individually from their mixtures without preseparation,for their voltammetric peaks overlapped seriously,so the chemometrics were used to resolve the overlapped voltammogram and quantify the mixtures.The proposed method was successfully applied to the determination of three 5-nitroimidazoles in milk and honey samples.

Construction of piezoelectric BaTiO_(3)/MoS_(2) heterojunction for boosting piezo-activation of peroxymonosulfate

The rapid recombination of charge carriers in piezoelectric materials has always been the problem that limits their piezoelectric performance for removal of organic pollutants in water.Herein,we construct a piezoelectric Ba TiO_(3)/MoS_(2)(BTO/MS)that follows a type II heterojunction charge transfer system to inhibit the recombination of electron-hole(e^(-)-h^(+))pairs,which is beneficial to the activation of peroxymonosulfate(PMS)for the removal of antibiotic ornidazole(ORZ)pollutants.The optimal ratio of BTO/MS for ORZ degradation under the piezo/PMS process is 13.9,3.6,62.1 and 2.0 times higher than that of the BTO/piezo,MS/piezo,(BTO/MS)/PMS and(BTO/MS)/piezo processes,respectively.The high efficiency charge separation in the piezoelectric heterojunction of BTO/MS promotes the activation of PMS,resulting in the synergy of pizeocatalysis and PMS oxidation during the process of ORZ degradation.This study provides an idea for enhancing piezo-activation of PMS by constructing heterojunctions in piezoelectric materials.