Ceftiofur sodium (sodium ceftiofur)
(Synonyms: 头孢噻呋钠; sodium ceftiofur) 目录号 : GC32159
Ceftiofur sodium is a semisynthetic, beta-lactamase-stable, broad-spectrum cephalosporin with antibacterial activity.
Cas No.:104010-37-9
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
Ceftiofur sodium is a semisynthetic, beta-lactamase-stable, broad-spectrum cephalosporin with antibacterial activity.
[1] R J Yancey Jr, et al. Am J Vet Res. 1987 Jul;48(7):1050-3.
| Cas No. | 104010-37-9 | SDF | |
| 别名 | 头孢噻呋钠; sodium ceftiofur | ||
| Canonical SMILES | [O-]C(C(N12)=C(CSC(C3=CC=CO3)=O)CS[C@]2([H])[C@H](NC(/C(C4=CSC(N)=N4)=N\OC)=O)C1=O)=O.[Na+] | ||
| 分子式 | C19H16N5NaO7S3 | 分子量 | 545.54 |
| 溶解度 | DMSO : ≥ 40 mg/mL (73.32 mM) | 储存条件 | Store at -20°C |
| 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 | 1.833 mL | 9.1652 mL | 18.3305 mL |
| 5 mM | 0.3666 mL | 1.833 mL | 3.6661 mL |
| 10 mM | 0.1833 mL | 0.9165 mL | 1.833 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。
A comprehensive review of Ceftiofur sodium and hydrochloride formulations for treatment of acute bovine foot rot
Vet Ther 2003 Spring;4(1):83-93.PMID:12756639doi
Seven well-controlled studies conducted under multiple management conditions demonstrated that ceftiofur, a late-generation veterinary parenteral cephalosporin, is effective for the treatment of bovine foot rot in beef and dairy cattle. Two preliminary dosage titration studies using a challenge model compared the efficacy of ceftiofur (1.1 mg or 2.2 mg ceftiofur equivalents [CE]/kg administered once daily for 3 days) with placebo. One preliminary clinical study evaluated the efficacy of Ceftiofur sodium (1.0 mg CE/kg once daily for 3 days) in lactating dairy cows. Two clinical trials evaluated the efficacy of Ceftiofur sodium versus placebo for naturally occurring foot rot, and two trials compared the efficacy of Ceftiofur sodium or hydrochloride (1.0 mg CE/kg) with oxytetracycline (6.6 or 10 mg/kg), each administered once daily for 3 days, for treatment of acute foot rot in beef cattle. All trials demonstrated the efficacy of ceftiofur for treatment of acute bovine foot rot. Ceftiofur and oxytetracycline were comparable in efficacy, with ceftiofur having excellent injection-site tolerance and short or no milk discard or preslaughter withdrawal.
PK/PD modeling of Ceftiofur sodium against Haemophilus parasuis infection in pigs
BMC Vet Res 2019 Aug 1;15(1):272.PMID:31370843DOI:10.1186/s12917-019-2008-4.
Background: Ceftiofur sodium is widely used in China. Our aim was to determine Ceftiofur sodium activity and optimize dosing regimens against the pathogen Haemophilus parasuis using an in vitro and ex vivo pharmacokinetics/pharmacodynamics modeling approach. By adopting these strategies, we wanted to extend the effective life of Ceftiofur sodium in reduce drug-resistance in pigs. Results: We established an H. parasuis infection model in pigs, and assessed the pharmacokinetics of Ceftiofur sodium in both healthy and infected animals. After Ceftiofur sodium (10 mg/kg, i.m.) administration to healthy and H. parasuis-infected pigs, plasma based desfuroylceftiofur (a metabolite of Ceftiofur sodium) was measured by High Performance Liquid Chromatography. The pharmacokinetics of Ceftiofur sodium (desfuroylceftiofur) was consistent with a two-compartment open model, with first-order absorption. We observed no significant differences (P > 0.05) in pharmacokinetic parameters between healthy and infected pigs. Pharmacodynamics data showed that Ceftiofur sodium was highly inhibitory against H. parasuis, with MIC, MBC, and MPC values of 0.003125, 0.0125 and 0.032 μg/mL, respectively. Desfuroylceftiofur in plasma also had strong bactericidal activity. Almost all H. parasuis cultured in plasma medium of Ceftiofur Sodium-inoculated healthy pigs, at each time point, were killed within 24 h. A weaker antibacterial activity was measured in infected-pig plasma medium at 18, 24, 36, and 48 h, after Ceftiofur sodium inoculation. Pharmacokinetic parameters were combined with ex vivo pharmacodynamic parameters, and the bacteriostatic effect (36.006 h), bactericidal effect (71.637 h) and clearance (90.619 h) within 24 h, were determined using the Hill equation. Dose-calculation equations revealed the optimal dose of Ceftiofur sodium to be 0.599-1.507 mg/kg. Conclusions: There were no significant differences in Ceftiofur sodium pharmacokinetic parameters between healthy and infected pigs, although pharmacokinetics/pharmacodynamics fitting curves showed obviously differences. The optimal dose of Ceftiofur sodium was lower than recommended (3 mg/kg), which may provide improved treatments for Glässers disease, with lower drug-resistance possibility.
Pharmacokinetics of Ceftiofur sodium in equine pregnancy
J Vet Pharmacol Ther 2017 Dec;40(6):656-662.PMID:28317126DOI:10.1111/jvp.12399.
Eleven pregnant pony mares (D270-326) were administered Ceftiofur sodium intramuscularly at 2.2 mg/kg (n = 6) or 4.4 mg/kg (n = 5), once daily. Plasma was obtained prior to ceftiofur administration and at 0.5, 1, 2, 4, 8, 12, and 24 hr after administration. Eight pony mares were re-enrolled in the study at least 3 days from expected foaling to ensure steady-state concentrations of drug at the time of foaling. Mares were administered Ceftiofur sodium (4.4 mg/kg, IM) daily until foaling. Parturition was induced using oxytocin 1 hr after Ceftiofur sodium administration. Allantoic and amniotic fluid, plasma, and colostrum samples were collected at time of foaling. Serial foal plasma samples were obtained. Placental tissues were collected. Desfuroylceftiofur acetamide (DCA) concentrations were measured in samples by high-performance liquid chromatography (HPLC). Mean (±SD) peak serum concentrations of DCA were 3.97 ± 0.50 μg/ml (low dose) and 7.45 ± 1.05 μg/ml (high dose). Terminal half-life was significantly (p = .014) shorter after administration of the low dose (2.91 ± 0.59 hr) than after administration of the high dose (4.10 ± 0.72 hr). The mean serum concentration of DCA from mares at time of foaling was 7.96 ± 1.39 μg/ml. The mean DCA concentration in colostrum was 1.39 ± 0.70 μg/ml. DCA concentrations in allantoic fluid, amniotic fluid, placental tissues, and foal plasma were below the limit of quantification (<0.1 μg/ml) and below the minimum inhibitory concentration of ceftiofur against relevant pathogens. These results infer incomplete passage of DCA across fetal membranes after administration of Ceftiofur sodium to normal pony mares.
Pharmacokinetics of Ceftiofur sodium in cats following a single intravenous and subcutaneous injection
J Vet Pharmacol Ther 2019 Nov;42(6):602-608.PMID:31529627DOI:10.1111/jvp.12814.
Ceftiofur, a third-generation cephalosporin antibiotic, is being extensively used by pet doctors in China. In the current study, the detection method was developed for ceftiofur and its metabolites, desfuroylceftiofur (DCE) and desfuroylceftiofur conjugates (DCEC), in feline plasma. Then, the pharmacokinetics studies were performed following one single intravenous and subcutaneous injection of Ceftiofur sodium in cats both at 5 mg/kg body weight (BW) (calculated as pure ceftiofur). Ceftiofur, DCE, and DCEC were extracted from plasma samples, then derivatized and further quantified by high-performance liquid chromatography. The concentrations versus time data were subjected to noncompartmental analysis to obtain the pharmacokinetics parameters. The terminal half-life (t1/2λz ) was calculated as 11.29 ± 1.09 and 10.69 ± 1.31 hr following intravenous and subcutaneous injections, respectively. After intravenous treatment, the total body clearance (Cl) and volume of distribution at steady-state (VSS ) were determined as 14.14 ± 1.09 ml hr-1 kg-1 and 241.71 ± 22.40 ml/kg, respectively. After subcutaneous injection, the peak concentration (Cmax ; 14.99 ± 2.29 μg/ml) was observed at 4.17 ± 0.41 hr, and the absorption half-life (t1/2ka ) and absolute bioavailability (F) were calculated as 2.83 ± 0.46 hr and 82.95%±9.59%, respectively. The pharmacokinetic profiles of Ceftiofur sodium and its related metabolites demonstrated their relatively slow, however, good absorption after subcutaneous administration, poor distribution, and slow elimination in cats. Based on the time of drug concentration above the minimum inhibitory concentration (MIC) (T>MIC) calculated in the current study, an intravenous or subcutaneous dose at 5 mg/kg BW of Ceftiofur sodium once daily is predicted to be effective for treating feline bacteria with a MIC value of ≿.0 μg/ml.
Comparative plasma pharmacokinetics of Ceftiofur sodium and ceftiofur crystalline-free acid in neonatal calves
J Vet Pharmacol Ther 2016 Jun;39(3):271-6.PMID:26542633DOI:10.1111/jvp.12275.
The objective of this study was to compare the plasma pharmacokinetic profile of ceftiofur crystalline-free acid (CCFA) and Ceftiofur sodium in neonatal calves between 4 and 6 days of age. In one group (n = 7), a single dose of CCFA was administered subcutaneously (SQ) at the base of the ear at a dose of 6.6 mg/kg of body weight. In a second group (n = 7), a single dose of Ceftiofur sodium was administered SQ in the neck at a dose of 2.2 mg/kg of body weight. Concentrations of desfuroylceftiofur acetamide (DCA) in plasma were determined by HPLC. Median time to maximum DCA concentration was 12 h (range 12-48 h) for CCFA and 1 h (range 1-2 h) for Ceftiofur sodium. Median maximum plasma DCA concentration was significantly higher for calves given Ceftiofur sodium (5.62 μg/mL; range 4.10-6.91 μg/mL) than for calves given CCFA (3.23 μg/mL; range 2.15-4.13 μg/mL). AUC0-∿and Vd/F were significantly greater for calves given CCFA than for calves given Ceftiofur sodium. The median terminal half-life of DCA in plasma was significantly longer for calves given CCFA (60.6 h; range 43.5-83.4 h) than for calves given Ceftiofur sodium (18.1 h; range 16.7-39.7 h). Cl/F was not significantly different between groups. The duration of time median plasma DCA concentrations remained above 2.0 μg/mL was significantly longer in calves that received CCFA (84.6 h; range 48-103 h) as compared to calves that received Ceftiofur sodium (21.7 h; range 12.6-33.6 h). Based on the results of this study, CCFA administered SQ at a dose of 6.6 mg/kg in neonatal calves provided plasma concentrations above the therapeutic target of 2 μg/mL for at least 3 days following a single dose. It is important to note that the use of ceftiofur-containing products is restricted by the FDA and the use of CCFA in veal calves is strictly prohibited.