Pharmaceutical raw materials Marbofloxacin Powder

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Marbofloxacin Usage and Synthesis.

Marbofloxacin and other veterinary commercial fluoroquinolones have a similar spectrum of antibacterial activity. These drugs have excellent activity against most gram-negative bacilli and cocci, including most species and strains of Pseudomonas aeruginosa, Klebsiella, Escherichia coli, Enterococcus, Campylobacter spp., Shigella, Salmonella, Aeromonas spp., Haemophilus, Aspergillus, Yersinia, and Vibrio spp.

Others generally susceptible include Brucella spp, Chlamydia trachomatis, Staphylococcus (including penicillinase-producing and methicillin-resistant bacteria), Chlamydia, and Mycobacterium. Fluoroquinolones have variable activity against most streptococci and are not usually recommended for the treatment of infections with this genus of bacteria .

These drugs have weak activity against most anaerobes and are not effective in treating anaerobic infections. Drug-resistant strains have emerged as a result of mutations, particularly in Pseudomonas spp, Klebsiella pneumoniae, S. impatiens, and Enterococci, but plasmid-mediated resistance is generally considered to be rare.

Uses and functions of Marbofloxacin.

Fluoroquinolone antimicrobial for the treatment of deep and superficial skin infections and urinary tract infections in dogs, skin and soft tissue infections in cats, and acute upper respiratory tract infections.

It is used for respiratory, digestive, urinary tract and skin infections in cattle, pigs, dogs and cats caused by sensitive bacteria. It is also effective in boils of cow, sheep mastitis and pig mastitis-uteritis-milkless syndrome.

Pharmacological Effect of Marbofloxacin.

Marbofloxacin is a novel fluoroquinolone antimicrobial agent that inhibits bacterial growth by inhibiting the bacterial DNA transcriptase and is antibacterial against Gram-negative and Gram-positive bacteria and mycoplasma. Marbofloxacin can be well absorbed through oral and injectable administration, with low toxicity and side effects.

(1) Pharmacodynamics: wide antibacterial spectrum, strong antibacterial activity. The MIC90 against most Enterobacteriaceae, Pasteurella multocida, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus intermedius were 0.08-0.28, 0.04, 0.94, 0.2, and 0.23 μg/mL, which were comparable to that of enrofloxacin and ciprofloxacin, respectively.

The MIC90 against bovine respiratory pathogens such as Pasteurella multocida, Pasteurella haemolytica, Haemophilus somnolentus and Mycoplasma spp. were 0.02, 0.17, 0.03 and 0.48 μg/mL, respectively.The product was still effective against pathogens resistant to the following drugs, such as erythromycin, lincomycin, chloramphenicol, doxycycline, and sulfonamides.

(2)Pharmacokinetics: rapid and complete absorption after internal administration and injection, low plasma protein binding rate, wide tissue distribution, well distributed in kidney, liver, lung and skin, its concentration in plasma and tissue is higher than the MIC against most pathogenic bacteria.The oral bioavailability of the product is about 80% in pregnant sows and cats, and more than 100% in calves. The product has a large volume of distribution (1.3 L/kg or more), and all tissue concentrations tested were higher than the plasma concentration of the drug, except in the CNS.

It is partially metabolised in the liver to inactive metabolites (N-demethyl MBF and N-oxo MBF). The main route of excretion is renal, with dogs excreting 30-45% of the prototype drug in the urine. The half-life is long, up to 14h and 13h for canine intranasal and subcutaneous injections, and 4.33, 5.26, 5.74 and 10h for calf (intramuscular injection), broiler (intramuscular injection), sow (intranasal injection), and cat (intranasal injection), respectively, resulting in a longer maintenance of the effective blood concentration after administration.

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