Cefatrizine
目录号 : GC25208Cefatrizine, a broad-spectrum, semisynthetic, first-generation cephalosporin with antibacterial activity, binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall.
Cas No.:51627-14-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefatrizine, a broad-spectrum, semisynthetic, first-generation cephalosporin with antibacterial activity, binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall.
[1] Curtis NA, et al. Antimicrob Agents Chemother. 1979 Nov;16(5):533-9.
| Cas No. | 51627-14-6 | SDF | Download SDF |
| 分子式 | C19H28N4O6S2 | 分子量 | 472.58 |
| 溶解度 | DMSO: 95 mg/mL (201.02 mM);Water: 95 mg/mL (201.02 mM);Ethanol: 23 mg/mL (48.67 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 | 2.116 mL | 10.5802 mL | 21.1604 mL |
| 5 mM | 0.4232 mL | 2.116 mL | 4.2321 mL |
| 10 mM | 0.2116 mL | 1.058 mL | 2.116 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。
Cefatrizine activity compared with that of other cephalosporins
Antimicrob Agents Chemother 1979 Feb;15(2):209-12.PMID:426514DOI:10.1128/AAC.15.2.209.
Cefatrizine, a new orally administered cephalosporin, was tested against 400 clinical isolates. Cefatrizine had excellent activity against gram-positive cocci, inhibiting all except enterococci at minimal inhibitory concentrations below 1 mug/ml. Cefatrizine inhibited the majority of Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Salmonella at concentrations below 12.5 mug/ml. Although Cefatrizine was not hydrolyzed by many beta-lactamases, it did not inhibit a number of strains of Enterobacter, Serratia, or indole-positive Proteus. Cefatrizine was more active than cephalothin or cephalexin against E. coli, Klebsiella, Enterobacter, Citrobacter, Salmonella, and Shigella. Its overall activity was less than that of cefoxitin against strains resistant to cephalothin, but its activity against cephalothin-susceptible strains was equivalent to that of cefamandole.
Cefatrizine (SK&F 60771), a new oral cephalosporin: serum levels and urinary recovery in humans after oral or intramuscular administration--comparative study with cephalexin and cefazolin
Antimicrob Agents Chemother 1976 May;9(5):800-3.PMID:949177DOI:10.1128/AAC.9.5.800.
Cefatrizine (SK&F 60771), a new broad-spectrum cephalosporin, was administered in a 0.5-g dose either orally or intramuscularly to volunteers in a crossover study. After oral administration, the average peak serum levels were 5.6 and 22.1 mug/ml for Cefatrizine and cephalexin, respectively. The serum half-life of Cefatrizine appeared to be more extended than that of cephalexin. Urinary recovery of Cefatrizine (35%) was approximately half that of cephalexin (68%) after oral administration. After intramuscular injection of 0.5 g, the average peak serum level of Cefatrizine (12.0 mug/ml) was approximately one-fourth that of cefazolin (44.0 mug/ml). The serum half-life after intramuscular injection was 86 min for Cefatrizine and 118 min for cefazolin. Urinary recovery was 45% of the intramuscularly administered dose, as compared with cefazolin, which was 74%.
Simultaneous determination of Cefatrizine and clavulanic acid in dog plasma by HPLC
J Pharm Biomed Anal 2004 Apr 1;35(1):221-31.PMID:15030898DOI:10.1016/j.jpba.2004.01.010.
A rapid and specific high-performance liquid chromatographic method was developed and validated for the simultaneous determination of Cefatrizine and clavulanic acid in the plasma of beagle dog. The sample pretreatment procedure involved reaction of clavulanic acid with 1,2,4-triazole, which readily produced a derivative with its maximum UV absorption at 314 nm. This derivative was separated in a reverse-phase C-18 column without being interfered by other components present in plasma. Cefatrizine, however, was not derivatized and, therefore determined directly at 269 nm. Sulfanilamide was used as an internal standard. The retention times of sulfanilamide, the derivative, and Cefatrizine were, 3.5, 4.9, and 6.0 min, respectively. The assay showed linearity from 2 to 100 microg/ml for Cefatrizine and from 1 to 50 microg/ml for clavulanic acid. Precision expressed as R.S.D. ranged from 4.2 to 18.2% for Cefatrizine and 5.5 to 15.8% for clavulanic acid. Accuracy ranged from 97.9 to 120% (lower limit of quantitation) for Cefatrizine and from 97.7 to 119.2% for clavulanic acid. Extraction efficiencies for Cefatrizine, clavulanic acid, and internal standard from dog plasma averaged 79.8+/-5.8%, 84.8+/-6.2%, and 89.0+/-3.8%, respectively. This method was employed successfully to follow the time course of the concentration of Cefatrizine and clavulanic acid in beagle dogs following oral administration of Cefatrizine and clavulanic acid.
Pharmacokinetics of oral Cefatrizine in pregnant and non-pregnant women with reference to fetal distribution
Fetal Diagn Ther 2007;22(2):100-6.PMID:17135753DOI:10.1159/000097105.
Objective: To investigate the effect of gestation on the pharmacokinetics of orally administered beta-lactams, choosing Cefatrizine as the model antibiotic. Setting: A tertiary teaching hospital. Design: Prospective study. Methods: In 20 women with affected fetuses, 17 by beta-thalassemia major and 3 with congenital malformations, termination of gestation between 19 and 24 weeks was induced by intra-amniotic administration of prostaglandin F(2)(alpha). Pharmacokinetics of Cefatrizine in maternal and fetal blood were studied after the administration of three 1 g doses of oral Cefatrizine, every 12 h. Twenty female non-pregnant volunteers consisted the control group. Results: Gestation was found to decrease substantially both Cefatrizine oral bioavailability and maximum serum plasma concentration (42.8 and 44.5%, respectively) but increased elimination half-life. This effect can be attributed to a substantial increase of the apparent volume of distribution of Cefatrizine in relation to a moderate increase of clearance that occurs during pregnancy. Fetal serum Cefatrizine levels were lower for the first few hours after administration and then exceeded the corresponding maternal ones. Conclusions: Our results indicate that gestation decreases the oral bioavailability of Cefatrizine. A delay in the maternal drug elimination compared to non-pregnant controls was more pronounced in the fetus.
Cefatrizine: a clinical overview
Drugs Exp Clin Res 1985;11(7):441-5.PMID:3915469doi
Cefatrizine, a new oral cephalosporin, proved effective in the treatment of a wide range of bacterial infections in both adult and paediatric patients. Adverse reactions mild and mainly limited to gastrointestinal disturbances.