Cefquinome sulfate
(Synonyms: 硫酸头孢喹肟) 目录号 : GC60105
A broad-spectrum cephalosporin antibiotic
Cas No.:118443-89-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefquinome is a broad-spectrum cephalosporin antibiotic.1 It is active against clinical isolates of various Gram-positive and Gram-negative bacteria, including Salmonella, E. coli, and methicillin-resistant S. aureus (MRSA; MICs = 0.06-0.5, 0.015-0.5, and 1-16 ?g/ml, respectively). Intramammary administration of cefquinome (75 mg/animal) is curative in a bovine model of E. coli-induced mastitis.2 Formulations containing cefquinome have been used in the treatment of coliform mastitis in veterinary medicine.
1.Chin, N.-X., Gu, J.-W., Fang, W., et al.In vitro activity of cefquinome, a new cephalosporin, compared with other cephalosporin antibioticsDiagn. Microbiol. Infect. Dis.15(4)331-337(1992) 2.Shpigel, N.Y., Levin, D., Winkler, M., et al.Efficacy of cefquinome for treatment of cows with mastitis experimentally induced using Escherichia coliJ. Dairy Sci.80(2)318-323(1996)
| Cas No. | 118443-89-3 | SDF | |
| 别名 | 硫酸头孢喹肟 | ||
| Canonical SMILES | O=C1[C@@H](NC(/C(C2=CSC(N)=N2)=N\OC)=O)[C@@]3([H])SCC(C[N+]4=C5CCCCC5=CC=C4)=C(C(O)=O)N13.O=S([O-])([O-])=O | ||
| 分子式 | C23H26N6O9S3 | 分子量 | 626.67 |
| 溶解度 | DMSO: 125 mg/mL (199.46 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5957 mL | 7.9787 mL | 15.9574 mL |
| 5 mM | 0.3191 mL | 1.5957 mL | 3.1915 mL |
| 10 mM | 0.1596 mL | 0.7979 mL | 1.5957 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Cefquinome sulfate Oily Nanosuspension Designed for Improving its Bioavailability in the Treatment of Veterinary Infections
Int J Nanomedicine 2022 Jun 2;17:2535-2553.PMID:35677677DOI:10.2147/IJN.S348822.
Introduction: Cefquinome sulfate (CS) is the first fourth-generation antibiotic for animals, which has a wide antibacterial spectrum, strong antibacterial activity and low drug resistance. However, it is accompanied by problems of poor therapeutic efficacy. In this context, the use of nanosuspensions have been found to be an attractive strategy. The main objective of this work is to develop a new oily nanosuspension to improve bioavailability and stability of CS formulations. Methods: After screening the formulations, Cefquinome sulfate oily nanosuspension (CS-NSP) was prepared by mortar grinding, using propylene glycol dicaprolate/dicaprate (Labrafac™ PG) as oil medium and caprylocaproyl polyoxyl-8 glycerides (Labrasol®) as stabilizer. The properties of CS-NSP were investigated by testing its physicochemical characteristics, stability, in vitro release, hemolysis, and muscle irritation. The in vivo pharmacokinetics of CS-NSP was studied using rats. Results: Results show that CS-NSP presents suitable stability, physicochemical properties and safety. Moreover, a rapid release and high bioavailability of CS-NSP have also been verified in the study. Pharmacokinetic experiments in vivo showed that the bioavailability of CS-NSP was about 1.6 times that of commercial Cefquinome sulfate injection (CS-INJ, Chuangdao®) (p<0.01). These advantages of CS-NSP were carried out by small particle size and low viscosity, being associated with the use of Labrafac PG and stabilizer Labrasol. Conclusion: The results proved that the new preparation is safe and effective and is expected to become a promising veterinary nanodelivery system.
Comparative pharmacokinetics of intravenous and intramuscular Cefquinome sulfate administration in ducklings and goslings
Am J Vet Res 2020 Nov;81(11):837-877.PMID:33107745DOI:10.2460/ajvr.81.11.873.
Objective: To compare the pharmacokinetics of Cefquinome sulfate in ducklings and goslings after IV or IM administration of a single dose. Animals: 216 healthy Muscovy ducklings (Cairina moschata) and 216 healthy Sichuan white goslings (Anser cygnoides). Procedures: Ducklings and goslings were each randomly assigned to 3 groups (n = 72/group) that received a single dose (2 mg/kg) of injectable Cefquinome sulfate administered IV or IM or of injectable Cefquinome sulfate suspension administered IM. Blood samples were collected at various points after drug administration (n = 6 birds/time point). Plasma cefquinome concentrations were measured by high-performance liquid chromatography with UV detection, and pharmacokinetic parameters were calculated with a 2-compartment model method. Results: After IV injection, mean distribution half-life of cefquinome was longer in goslings (0.446 hours) than in ducklings (0.019 hours), whereas volume of distribution at steady state was greater (0.432 vs 0.042 L/kg) and elimination half-life was slower (1.737 vs 0.972 hours). After IM administration of injectable Cefquinome sulfate, bioavailability of the drug was higher in goslings (113.9%) than in ducklings (67.5%). After IM administration of injectable Cefquinome sulfate suspension, bioavailability was also higher in goslings (123.1%) than in ducklings (96.8%), whereas elimination half-life was slower (6.917 vs 1.895 hours, respectively). Conclusions and clinical relevance: In goslings, IV administration of cefquinome resulted in slower distribution and metabolism of the drug than in ducklings and IM administration resulted in higher bioavailability. The delayed-release effect of the injectable Cefquinome sulfate suspension when administered IM was observed only in goslings.
Preparation of Cefquinome sulfate proliposome and its pharmacokinetics in rabbit
Iran J Pharm Res 2013 Fall;12(4):611-21.PMID:24523741doi
Cefquinome sulfate (CS) is a fourth-generation cephalosporin, which has been developed solely for veterinary use. It shows potent antibacterial activity against a broad spectrum of bacterial species. However, Cefquinome is susceptible to hydrolysis, which limiting its clinical employment efficacies to some extent. So, in this study, to increase Cefquinome sulfate biological half-life, a novel Cefquinome sulfate proliposome was prepared by solid dispersion and effervescent techniques and characterized for morphology, particle size, entrapment efficiency and in vitro release. A Reversed Phase-High Performance Liquid Chromatography (RP-HPLC) method was first chosen and established to determine the drug concentration in plasma after intra muscular (IM) administrating Cefquinome sulfate solution and liposome at a single dosage of 18 mg/kg in rabbit. Then their pharmacokinetics in vivo was compared. Results showed that the received liposome was milky white suspension, spherical or ellipsoidal in shape. The mean particle size was 203±5 nm and the entrapment efficiency was 53.5±0.16%. The cefaquinom sulfate solution and liposome both followed a two compartment model, in vivo. The pharmacokinetic parameters for the solution and liposomal formulations were measured as follows: t1/2 α were (1.214 ± 0.135) h and (1.395 ± 0.113) h, t1/2 β were (8.752 ± 0.846) h and (16.503 ± 1.275) h, AUC(0-24) were (49.582 ± 9.173) (mg·h)/L and (138.727 ± 11.034) (mg·h)/L, CL/F were (0.357 ± 0.015) L/(h·kg) and (0.127 ± 0.012) L/(h·kg), MRT(0-24) were (2.68 ± 0.229) h and (5.945 ± 0.479) h, respectively. It could be clearly seen that t1/2 β of liposome prolonged (p < 0.05), AUC and MRT both increased remarkably (p < 0.01), CL/F decreased. Results indicated that this preparation has more residence time and exhibits some sustained-release tendency.
Cefquinome sulfate behavior after intramammary administration in healthy and infected cows
J Dairy Sci 2011 Jul;94(7):3455-61.PMID:21700031DOI:10.3168/jds.2010-4109.
Maintenance of adequate drug concentration at the site of infection is an important problem in mastitis antibiotic therapy, and the efficacy of intramammary β-lactams can be optimized by maintaining the drug concentration at the site of infection above the minimum inhibitory concentration (MIC) as long as possible. The most important pharmacokinetic and pharmacodynamic parameter for efficacy evaluation is time during which drug concentrations exceed the MIC (t>MIC). In this study, we assessed the pharmacokinetic profile of cefquinome (CFQ) after repeated intramammary administration in healthy cows and cows subclinically infected with Staphylococcus aureus as well as the MIC of Staph. aureus field strains. In addition, the degree of drug passage was investigated from udder to bloodstream by measuring systemic drug absorption in healthy and infected animals. Cefquinome concentrations were quantified by HPLC (UV-visible detection) in milk samples collected from quarters and from blood serum samples. The systemic drug absorption was negligible in healthy and subclinically infected animals (maximum concentration 0.09±0.02 and 0.1±0.01 μg/mL in healthy and subclinically infected animals, respectively). The MIC(90) value for CFQ in Staph. aureus field strains (n=20) was 0.24 μg/mL. The pharmacokinetic and pharmacodynamic evaluation, determined by t>MIC, showed an equal persistence of CFQ in all quarters, indicating an equivalent activity of the drug regardless of the pathological status of the udder. Moreover, with literature data regarding CFQ MIC, the t>MIC has been calculated for other bacterial species.
Preparation of Cefquinome sulfate cationic proliposome and evaluation of its efficacy on Staphylococcus aureus biofilm
Colloids Surf B Biointerfaces 2019 Oct 1;182:110323.PMID:31323449DOI:10.1016/j.colsurfb.2019.06.053.
Staphylococcus aureus (S. aureus) has the propensity to form biofilms, which eventually cause antibiotic resistance and treatment failure. Cefquinome sulfate (CS) is an animal-specific antibacterial agent for S. aureus infection. In this work, CS cationic proliposomes (CSCPs) were prepared by solid-dispersion method combined with effervescent hydration to eradicate bacterial biofilm and improve the antibacterial effect of the drug. CSCPs were readily dispersed in water, thereby forming CS cationic liposomes (CSCLs) as a white, uniform suspension. The CSCLs had an encapsulation efficiency (EE) of 63.21%, a drug loading of 4.04%, an average particle size of 201.5 nm, and a positive zeta-potential of 65.29 mV. In vitro release studies showed that CSCLs had good sustained-release behavior. The CS and CSCL minimal inhibitory concentration (MIC) of S. aureus type culture strain were 1 and 0.48 g/mL, respectively. The eradication effect of CS on bacterial biofilm (BBF) was relatively weak during culture in drug-containing medium for 8 h-24 h. However, the CSCL eradication effect on BBF increased gradually, and the clearance rate of CSCLs on BBF was about twice that of CS. The clearance rate reached 81.30% with 2.5 × MIC in 24 h. All these results indicated that CSCLs can significantly improve the eradication effect of cefquinome on biofilm to inhibit bacterial growth.