Ceftiofur Free Acid

English name: Ceftiofur Crystalline Free Acid
CAS number: 80370-57-6
Molecular formula: C19H17N5O7S3
Molecular weight: 523.56
Content: calculated as cefotaxime free acid, ≥ 93%
Appearance: White to grayish brown powder
Solubility: Very slightly soluble in acetone, almost insoluble in water or ethanol
Packaging specification: 5kg/aluminum ear
Storage: Light shielded, tightly sealed, cold place

Ceftiofur is a third-generation cephalosporin broad-spectrum antibiotic specially used for animals. It has broad-spectrum antibacterial effect on both gram-positive and gram-negative bacteria, and is mainly used to treat infectious diseases caused by sensitive bacteria in pigs, cattle, horses, dogs and one-day old chickens.
Ceftiofur free acid is the free acid form of cefotaxime, with an effective content of not less than 93%, insoluble in water, with a half-life of about 40 hours, lower blood concentration than cefotaxime sodium, long-lasting sustained-release, and suitable for health care.

Applicable symptoms: Ceftiofur free acid is highly sensitive to bacteria associated with respiratory infections and is mainly used for the treatment and prevention of respiratory diseases (pneumonia, transport fever) caused by sensitive bacteria in large economic animals such as pigs and cows.

Advantages:

(1) Good bactericidal effect: Ceftiofur free acid has a drug concentration 2-4 times higher in infected tissues than in normal tissues, showing a selective concentrated distribution and more effective bactericidal effect.
(2) Special drug for respiratory diseases: Ceftiofur free acid is eliminated very slowly in the lungs, with a duration several times longer than plasma, and highly bound to the lungs. Its apparent distribution volume in the lungs is also much higher than that in plasma. Many respiratory disease pathogens are highly sensitive to Cefotaxime and its metabolite, DFC.
(3) Long lasting efficacy: The metabolite DFC of ceftiofur free acid retains its antibacterial activity and can store bactericidal power in blood or tissues, prolonging the drug's action time and half-life. After a single dose of ceftiofur free acid injection, it can maintain an effective blood concentration for 7 days.
(4) Low drug resistance: With a stable β - lactam ring, Ceftiofur free acid is not easily hydrolyzed or destroyed by drug-resistant bacteria, and is not prone to developing drug resistance and cross resistance.
(5) Good safety: Ceftiofur free acid has low toxicity and no teratogenicity, carcinogenicity, genetic toxicity, or immunotoxicity.

Mechanism of action: The amide group of the β - lactam ring in the chemical structure of ceftiofur free acid is similar to peptidoglycan pentapeptide, which can covalently bind to penicillin binding protein (PBP) to inactivate it, interfere with the synthesis of peptidoglycan, the main component of bacterial cell wall, and irreversibly inhibit the synthesis of bacterial cell wall, causing the bacteria to form filamentous or spherical bodies, and ultimately rupture and die.

Antibacterial spectrum: Actinobacillus pleuropneumoniae, Haemophilus parasuis, Streptococcus suis, Hemolytic Pasteurella, Pasteurella multocida, and Haemophilus influenzae.

Metabolic pathway: Ceftiofur free acid is mainly converted and metabolized through the kidneys. About 2/3 of the injected dose in pigs, cows, and beef cattle is excreted in the urine as DFC conjugates and polar metabolites, and about 1/3 of the dose is excreted in feces.