Quantitative analysis of cefixime via complexation with palladium(Ⅱ) in pharmaceutical formulations by spectrophotometry

An optimized and validated spectrophotometric method has been developed for the determination of cefixime in pharmaceutical formulations. The method is based on the complexa- tion reaction between cefixime and palladium ion in the presence of acidic buffer solution （pH 3） in ethanol-distilled water medium at room temperature. The complex absorbed maximally at 352 nm. Beer＇s law is obeyed in the working concentration range of 2.5-35 μg/mL with apparent molar absorptivity of 1.015×104 L/mol cm and Sandell＇s sensitivity of 0.001 μg/cm2/0.001 absorbance unit. The limits of detection and quantitation for the proposed method are 0.175 and 0.583μg/mL, respectively. The effect of common excipients used as additives has been studied in the determination of cefixime. The proposed method has been successfully applied for the determina- tion of cefixime in pharmaceutical formulations. The results obtained by the proposed method were statistically compared with the reference method using t and F values and found no significant difference between the two methods.

Antibacterial activity of eight Iranian plant extracts against methicillin and cefixime restistant Staphylococcous aureus strains

Objective:To assess the antibacterial activity of eight Iranian plant extracts against Staphylococcus aureus(S.aureus) strains which were isolated from infected patients.Methods: The studied strains were isolated from urine,stool,blood and wound of infected patients and identified by biochemical tests.In further,the antibacterial activity of 8 ethanolic local plant extracts including Querqus brantii(Q.brantii),Ziziphus spina-christi(Z.spina-christi),Peganum harmala(P.harmala),Oliveira decumbens(O.decumbens),Galium tricornutum(G.tricornutum), Vitex pseudo negundo(Vi.pseudo negundo),Salvia officinalis(S.officinalis),Vaccaria pyramidata (V.pyramidata) were then evaluated using agar disc diffusion method.Results:A total of 9 isolates were isolated and identified as S.aureus.Antibacterial profile of the strains showed that the strains were resistant to methicillin and cefixime.The highest antibacterial activity against the studied strains were belong to Q.brantii,P.harmala,Z.spina-christi and O.decumbens vent extracts with 11-40 mm,15-28 mm,8-26 mm and 10-20 mm of diameters,respectively. Intermediate antibacterial activity was exhibited by G.tricornutum and Vi.pseudo negundo against some of the studied strains with 7-20 mm and 7-13 mm of diameters,respectively. Noteworthy,out of 9 studied strains;6 and 2 of them were resistant to the G.tricornutum and Vi. pseudo negundo extracts,respectively.The S.officinalis and Va.pyramidata,however,showed no antibacterial activity against the studied strains.Conclusions:The Q.brantii,P.harmala,Z. spina-christi and O.decumbens extracts were shown to possess strong antibacterial activity against methicillin and cefixime resistant S.aureus strains and can be considered as the promising natural antibiotics for treating the studied strains.

ME1207与Cefixime双盲双模拟对照治疗细菌性感染有效性与安全性临床评价

ME1207(Cefditoren pivoxil)是明治制杲株式会社开发的新的三代口服广谱头孢菌素,口服吸收后被酯酶水解成ME1206,对革兰氏阳性、阴性菌均有较强抗菌作用,尤其对金黄色葡萄球菌与葡萄球菌属的抗菌作用超过其他头孢菌素,对β-内酰胺酶稳定,对肠球菌与绿脓杆菌作用较差。本项随机双盲对照试验目的是评价ME1207细菌性感染的有效性与安全性。选用Cefixime(世福素)为对照药,剂量均为200mg,Q12h,疗程7～14天。双盲试验进行呼吸道与泌尿系感染对照试验,开放试验还包括皮肤软组织感染:可评价疗效共122例,包括随机双盲组60例(A药30例,B药32例),开放试验60例:安全性评价为随机双盲组64例(A药30例,B药34例),开放试验61例。揭盲后A药为ME1207:B药为Cefixime。

Interaction of cetyltrimethylammonium bromide with cefixime trihydrate drug at different temperatures and compositions: Effect of different electrolytes

Herein,conductivity measurements have been carried out to explore the interaction between cetyltrimethylammonium bromide(CTAB,a cationic surfactant) and antibiotic drug(cefixime trihydrate(CMT)) in water and also in occurrence of inorganic salts(NaCl,Na2 SO4 and Na3 PO4) over the temperature range of 303.15-323.15 K with an interval of 5 K.In all cases,two critical micelle concentrations(c^*) were achieved for the CMT-surfactant system.Addition of CMT drug to CTAB solution decreases the values of c^* which indicates the interaction between CMT and CTAB.Both values of c^* for CMT-CTAB mixture in the presence of salts are lower in magnitude compared to the aqueous medium which indicates that micellization of the CMT-CTAB mixed system is favorable in salt solution.The values of △Gm^0 were obtained to be negative indicating the spontaneity of the micellization process and the extent of spontaneity further increases by means of rising temperature.The obtained outcomes from the ΔHm^0 and ΔSm^0 values disclose that the interactions between CMT and CTAB are mostly electrostatic along with hydrophobic in nature.The thermodynamic parameters of transfer and enthalpy-entropy compensation phenomenon were also determined and discussed in detail.

Insight into the degradation mechanism of cefixime under crystallization condition

The chemical stability of cefixime was determined by high-performance liquid chromatography （HPLC） under different conditions, including factors such as pH, solvents, initial concentration, temperature and additives. The degradation process follows the first-order kinetics. A pH-rate profile exhibits the U-shape and shows the maximum stability of cefixime at pH = 6. The stability in different pure solvents is ranked as acetone 〉 ethanol 〉 methanol 〉 water, while the degradation rate of cefixime exists a maximum at the ratio of 0.6 in water ＋ methanol mixtures. In addition, the degradation rate increases with the temperature increasing and the activation energy of degradation was found to be 27.078 kJ. mol- 1 in acetone ＋ water mixed solvents. The addition of different additives was proven to either inhibit or accelerate the degradation. The degradation products were analyzed using HPLC, LC-MS and infrared spectroscopy, and the possible degradation pathways in acid as well as alkaline environment were proposed to help us understand the degradation behavior of cefixime.

一种新头孢菌素抗菌素——Cefixime

Cefixime是一种口服的广谱抗菌的头孢菌素。对肠杆菌属、流杆杆菌,酿脓链球菌、肺炎球菌,卡他奈瑟氏双球菌均有效,并耐β-内酰胺酶的水解,对金黄色葡萄球菌作用较弱,对绿脓杆菌无效。抗菌活性:在体外试验采用Cefiximelmg/L或更少剂量便可抑制许多大肠杆菌:肺炎杆菌,克雷白氏菌属,奇异变形杆菌,

Cefixime的体外抗菌活性在MIC与纸片扩散试验间的相关指数

Cefixime是一种可供口服的亚氨甲氧基氨噻唑基头孢菌素,它对人体内的各种草兰氏阳性和阴性菌具有广谱抗菌作用,比其它口服头孢菌素类包括头孢噻肟、头孢克罗、头孢拉定和头孢羟氨苄等的半衰期长(t_(1/2)3h)。

Experimental and Theoretical Investigations on Copper Corrosion Inhibition by Cefixime Drug in 1M HNO₃Solution

Cefixime, a third-generation semi-synthetic cephalosporin antibiotic was used as a copper corrosion inhibitor in 1M HNO3 solution. The study was conducted through the weight loss technique at 298 - 318 K and theoretical studies based on quantum chemistry. The studied drug inhibited the corrosion of copper in 1M HNO3 over the cefixime concentration range (0.02 - 2 mM). The inhibition efficiency increased with an increase in the inhibitor concentration to reach 91.07% at 2 mM, but decreased with an increase in temperature. The thermodynamic functions related to the adsorption of cefixime on the copper surface and that of the metal dissolution were computed and analyzed. The results point out spontaneous adsorption, mainly through a physisorption mechanism following Langmuir adsorption isotherm model and an endothermic dissolution process. Quantum chemical calculations were also performed at B3LYP level with 6-31G (d, p) basis set and lead to molecular descriptors such as EHOMO (energy of the highest occupied molecular orbital), ELUMO (energy of the lowest unoccupied molecular orbital), ΔE (energy gap) and μ (dipole moment). The global reactivity descriptors such as χ (electronegativity), χ (global hardness), S (global softness), and ω (electrophilicity index) were derived using Koopman’s theorem and analyzed. The local reactivity parameters, including Fukui functions and dual descriptors were determined and discussed. Experimental and theoretical results were found to be in good agreement.

Effects of cefixime on the systemic inflammatory stress response and intestinal mucosal barrier injury in children with infective enteritis

Objective:To investigate the effects of cefixime on the systemic inflammatory stress response and intestinal mucosal barrier injury in children with infective enteritis.Methods:A total of 80 children with infective enteritis who were treated in the hospital between March 2016 and August 2017 were divided into group A (n=40) and group B (n=40) according to the random number table method. Group A received cefaclor anti-infective therapy, group B received cefixime therapy, and both therapies lasted for 1 week. The differences in serum levels of inflammatory mediators, oxidative stress indexes and intestinal mucosal injury markers were compared between the two groups before and after treatment.Results: Before treatment, the differences in serum levels of inflammatory mediators, oxidative stress indexes and intestinal mucosal injury markers were not statistically significant. After 1 week of treatment, serum inflammatory mediators IL-8 and TNF-α levels of group B were lower than those of group A whereas IL-10 level was higher than that of group A;serum oxidative stress indexes ROS and MDA levels were lower than those of group A whereas GSH-Px and CAT levels were higher than those of group A;serum intestinal mucosal injury markers DAO, D-Lactate, FABP and GST levels were lower than those of group A.Conclusion: Cefixime anti-infective therapy can effectively inhibit the inflammatory stress response and reduce the intestinal mucosal barrier injury in children with infective enteritis.

Localized pseudomembranous colitis in the cecum and ascending colon mimicking acute appendicitis

A 61-year-old male was admitted to our hospital due to right lower abdominal pain and watery diarrhea for 3 d.Beginning 3 wk before he arrived in our hospital,he took 3 rd-generation cephalosporin(cefixime) for 2 wk due to chronic left ear otitis media.Colonoscopic examination revealed yellowish patches of ulcerations and swelling covered with thick serosanguineous exudate in the cecum and ascending colon.After 7 d of oral metronidazole treatment,his symptoms completely disappeared.We report a case of localized pseudomembranous colitis in the cecum and ascending colon mimicking acute appendicitis associated with cefixime.

Molecular Characteristics of Cephalosporin-Resistant Neisseria gonorrhoeae Strains in China:A Retrospective Study

Objective:An increasing level of antimicrobial resistance to extended-spectrum cephalosporins has been reported,so we conducted this study to investigate the molecular characteristics of cephalosporin resistant Neisseria gonorrhoeae(NG)strains isolated from China Gonococcal Antimicrobial Resistance Surveillance Programme(China-GRSP).Methods:In total,2,038 NG isolates were collected from the China-GRSP between 2015 and 2016.NG multiantigen sequence typing(NG-MAST),multilocus sequence typing(MLST),and NG sequence typing for antimicrobial resistance(NG-STAR)were used to determine characteristics and resistant determinants of cephalosporin-resistant isolates.The results are described as percentages.Results:Seventy-four(3.6%)cephalosporin-resistant isolates were confirmed.MLST_(ST7363)was the most prevalent MLST among cefixime-resistant(CFX-R)isolates,whereas MLST_(ST7365)(n=8)in was the most prevalent sequence type among ceftriaxone-resistant(CRO-R)isolates.CFX-R strains were mainly associated with penA-X(n=27,44.3%),penA-XIII(n=6,9.8%),penA-XVIII(n=5,8.2%),and CRO-R strains were mainly related to penA-XVIII(n=10,25.6%),penA-43(n=9,23.1%),penA-XIII(n=7,17.9%).Conclusion:The main conclusion of this study is that the predominant cephalosporin-resistant clones in China include locally emerged and imported linages.The CFX-R and CRO-R strains are primarily related to penA mutations,and their predominant genotypes are different.With the increase in international travel,tracking high-risk-resistant clones and identifying outbreaks and their associations with epidemiological characteristics are critical to improve public health.

Investigation of the pharmacokinetics and determination of certain cephalosporins in rabbit plasma by a kinetic spectrophotometric method with the aid of chemometrics

This paper describes a kinetic spectrophotometric method for simultaneous determination of three cephalosporin antibiotics,cephradine,cefaclor and cefixime,with the aid of chemometrics. The method relies on their oxidation with KMnO4 to produce green manganate with different kinetic rates in alkaline medium. The proposed method was successfully applied to a pharmacokinetic study of three cephalosporin antibiotics in rabbit plasma via intravenous injections. The results indicated that the amount of cephradine,cefaclor and cefixime were reduced rapidly in rabbit blood,showing clear dose-dependency and the half-life of cefixime (160 min) was longer than those of cephradine (60 min) and cefaclor (60 min).