Cephapirin sodium
(Synonyms: 头孢匹林钠,Cefapirin sodium) 目录号 : GC38188
Cephapirin Sodium (Cefapirin) is the sodium salt form of cephapirin, a semi-synthetic, first-generation cephalosporin antibiotic with bactericidal activity.Cephapirin Sodium is effective against gram-negative and gram-positive organisms.
Cas No.:24356-60-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cephapirin Sodium (Cefapirin) is the sodium salt form of cephapirin, a semi-synthetic, first-generation cephalosporin antibiotic with bactericidal activity.Cephapirin Sodium is effective against gram-negative and gram-positive organisms.
| Cas No. | 24356-60-3 | SDF | |
| 别名 | 头孢匹林钠,Cefapirin sodium | ||
| Canonical SMILES | O=C(C(N12)=C(COC(C)=O)CSC2C(NC(CSC3=CC=NC=C3)=O)C1=O)O[Na] | ||
| 分子式 | C17H16N3NaO6S2 | 分子量 | 445.45 |
| 溶解度 | DMSO : 89mg/mL | 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 | 2.2449 mL | 11.2246 mL | 22.4492 mL |
| 5 mM | 0.449 mL | 2.2449 mL | 4.4898 mL |
| 10 mM | 0.2245 mL | 1.1225 mL | 2.2449 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。
Elimination kinetics of Cephapirin sodium in milk after an 8-day extended therapy program of daily intramammary infusion in healthy lactating Holstein-Friesian cows
J Dairy Sci 2013 Jul;96(7):4455-64.PMID:23684021DOI:10.3168/jds.2012-6487.
The objective of this study was to determine the elimination kinetics of extended therapy with intramammary (IMM) cephapirin in lactating dairy cattle. Eight healthy Holstein-Friesian cows were administered cephapirin (200mg) into all 4 mammary glands every 24 h after milking. Cows were milked 3 times per day and concentrations of cephapirin and desacetyl cephapirin were determined in bucket milk using liquid chromatography-mass spectrometry. Milk concentration-time data after the last of the 8 IMM infusions were fitted using compartment and noncompartmental models. The maximum cephapirin concentration was 128±57 µg/mL (mean ± SD), the elimination rate constant from the central compartment was 0.278±0.046 (h(-1)), clearance was 0.053±0.023 L/h, the half time for elimination was 2.55±0.40 h, and the mean residence time was 2.65±0.79 h. The cephapirin concentration was below the approved tolerance in all cows by 96 h after the last infusion, which is the labeled withholding time for the preparation used. Extended therapy for 8 d provided milk cephapirin concentrations above the minimum inhibitory concentration for common gram-positive mastitis pathogens (0.1 to 1.0 µg/mL) for the duration of therapy and for an additional 16 to 32 h after the end of treatment. Our findings suggest that this IMM Cephapirin sodium formulation, which is labeled for 2 doses 12 h apart, could be administered at a 24-h interval for up to 8 d in cows milked 3 times per day, with no significant effect on residue levels by 96 h after the last treatment. Longer withdrawal times would be prudent for cows with low milk production.
Randomized noninferiority field trial evaluating Cephapirin sodium for treatment of nonsevere clinical mastitis
J Dairy Sci 2018 Aug;101(8):7334-7347.PMID:29778482DOI:10.3168/jds.2017-14002.
The general objective of this study was to evaluate whether Cephapirin sodium is noninferior compared with a positive control broad-spectrum product formulated with a combination of antimicrobials for intramammary treatment of nonsevere clinical mastitis. In addition, we compared the efficacy of treatments on the cure risks of pathogen groups (gram-positive, gram-negative, and cultures with no growth) based on culture results. A total of 346 cows distributed in 31 commercial dairy herds were selected to participate in the study, although only 236 met the criteria for evaluation of microbiological cure. Coagulase-negative staphylococci were the most isolated gram-positive pathogens in pretreatment milk samples, whereas the most common gram-negative bacterium was Escherichia coli. Cows attending the postadmission criteria were treated with 4 intramammary infusions (12 h apart) of one of the following antimicrobials: 300 mg of Cephapirin sodium + 20 mg of prednisolone (CS), or the positive control treatment formulated with a combination of antimicrobials (200 mg of tetracycline + 250 mg of neomycin + 28 mg of bacitracin + 10 mg of prednisolone; TNB). Noninferiority analysis and mixed regression models (overall and considering the pathogen groups) were performed for the following outcomes: bacteriological cure (absence of the causative pathogens in cultures performed in milk samples collected at 14 and 21 ± 3 d after enrollment), pathogen cure (absence of any pathogen on both follow-up samples), clinical cure (absence of clinical sign in the milk and mammary gland at 48 h after the last antimicrobial infusion), extended clinical cure (normal milk and normal gland on the second posttreatment sample collection (d 21), and linear score of somatic cell count cure [linear score of somatic cell count recovery (≤4.0) on d 21 ± 3 after enrollment]. No significant differences were observed between treatments regarding any of the evaluated outcomes in both regression models (overall and considering the pathogen groups). Noninferiority of CS relative to TNB was inconclusive for bacteriological cure (CS = 0.68; TNB = 0.73) and clinical cure (CS = 0.88; TNB = 0.94), as the confidence intervals crossed the pre-stated margin of noninferiority (Δ = -0.15). Cephapirin sodium was noninferior compared with TNB for pathogen cure (CS = 0.36; TNB = 0.35), extended clinical cure (CS = 0.93; TNB = 0.92), and linear score of somatic cell count cure (CS = 0.29; TNB = 0.28). In conclusion, the use of intramammary CS for treatment of nonsevere clinical mastitis has similar efficacy as a treatment regimen with a combination of antimicrobial agents (tetracycline + neomycin + bacitracin), although noninferiority analysis showed inconclusive results for bacteriological and clinical cures.
Study of the impurity profile and characteristic fragmentation of Δ3 -isomers in Cephapirin sodium using dual liquid chromatography coupled with ion trap/time-of-flight mass spectrometry
Rapid Commun Mass Spectrom 2020 Dec 15;34(23):e8948.PMID:32957160DOI:10.1002/rcm.8948.
Rationale: According to the requirements of the International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH), the structures of impurities in pharmaceutical products present at over 0.1% need to be confirmed. Therefore, the aim of this study is to separate and identify the impurities in Cephapirin sodium drug substances, so as to guide the industry to improve the production process and storage conditions and reduce the amount of impurities in the product. Methods: In the first chromatography dimension, a Boston Green ODS (4.6 mm × 250 mm, 5 μm) column was used, with a mobile phase composed of 0.05 M sodium dihydrogen phosphate aqueous solution and acetonitrile. In the second dimension, the column was a Shimadzu Shim-pack GISS C18 (50 mm × 2.1 mm, 1.9 μm), using 10 mM ammonium formate solution and methanol as the mobile phase. Results: The fragmentation behavior of cephapirin and its impurities and isomers was studied and the structures of impurities were deduced based on the MSn data. For six unknown impurities tentative structures were proposed. The degradation behavior of Cephapirin sodium was also studied. Impurities 1 to 11 were found in commercial Cephapirin sodium samples, indicating that Cephapirin sodium should be stored in closed containers. Conclusions: The contradiction between the non-volatile mobile phase and mass spectrometry was solved by means of multiple heart-cutting approaches and an on-line desalting technique. Twelve impurities and isomers were separated and characterized. These results could be used to improve the methods described in pharmacopoeias for the quality control of Cephapirin sodium.
Effect of milk fraction on concentrations of cephapirin and desacetylcephapirin in bovine milk after intramammary infusion of Cephapirin sodium
J Vet Pharmacol Ther 2009 Aug;32(4):345-52.PMID:19614839DOI:10.1111/j.1365-2885.2008.01048.x.
Clinical mastitis in dairy cows is commonly treated with intramammary (IMM) antimicrobial agents. Pharmacokinetic data are used to design treatment regimens and determine withholding times. In some pharmacokinetic studies, investigators measure antimicrobial concentrations in foremilk, whereas in others, they use bucket milk or do not specify the milk fraction sampled. Our objective was to compare antimicrobial concentrations in foremilk, bucket milk, and strippings after IMM treatment of six healthy Holsteins. One mammary gland/cow was infused with 200 mg of cephapirin (CEPH) after each of the two milkings, using different milking frequencies and treatment intervals in a randomized crossover design. Treated glands were sampled at the first milking following each infusion. Antimicrobial concentrations in milk were measured using HPLC/MS/MS. CEPH concentration was higher in foremilk (geometric mean 44.2 microg/mL) than in bucket milk (15.7 microg/mL) or strippings (18.5 microg/mL), as it was true for desacetylcephapirin (DAC) (59.5, 23.0, and 30.2 microg/mL, respectively). This finding, which was based on milk samples collected at the first milking after IMM infusion, suggests that pharmacokinetic data based on drug concentrations in foremilk may be misleading. Strippings were more representative of bucket milk than foremilk. The relationship between milk fraction and antimicrobial concentration should be investigated for other IMM antimicrobial agents. Meanwhile, it is essential that pharmacokinetic and residue studies report the fraction of milk that was analyzed.
The clinical use of Cephapirin sodium in total hip arthroplasty and measurement of plasma and bone levels
Orthopedics 1980 Feb 1;3(2):131-4.PMID:24822936DOI:10.3928/0147-7447-19800201-07.
Cephapirin sodium, a new parenteral cephalosporin antibiotic recommended for use perioperatively, was administered to 50 consecutive patients undergoing total hip arthroplasty. Blood and bone concentrations extracted simultaneously were measured, and excellent penetration of cephapirin into bone was demonstrated. No infection was observed in any patient after surgery. Few instances of adverse reactions were noted. Although some patients developed phlebitis, no case was severe.