Orbifloxacin is a fluoroquinolone drug used widely in companion animal medicine. At twice the MIC, the PAEs (post-antibiotic effects) of orbifloxacin ranged from -0.28-0.93 h (mean, 0.29 h) for E. coli and -0.18-1.18 h (mean, 0.37 h) for P. aeruginosa[2]. Orbifloxacin could have success against susceptible mastitis pathogens in goats[3]. Oral ORB (Orbifloxacin, 2.5 mg/kg and 5 mg/kg) may alter the total counts and composition of fecal coliform, but is unlikely to yield highly fluoroquinolone-resistant mutants of E. coli and C. freundii in cats, possibly because of the high drug concentration in feces[4]. In addition, orbifloxacin was an effective, safe, and convenient antibiotic for the treatment of superficial and deep staphylococcal pyoderma in dogs[5]. Orbifloxacin and the peptide AK15 possess significant bactericidal activity against Mycobacterium tuberculosis (Mtb) in vitro. Orbifloxacin also showed an effective ability on the clearance of intracellular Mtb and protect mice from a strong inflammatory response but not AK15[6].
Orbifloxacin/奥比沙星 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Staphylococcus aureus ATCC 25923
16.0, 32.0, 64.0 µg/mL
18 hours
To evaluate the antimicrobial activity of Orbifloxacin against Staphylococcus aureus ATCC 25923. The results showed good linearity (r = 0.9992), precision (RSD = 2.88%), and accuracy (100.31%).
Pharmaceutics. 2011 Aug 29;3(3):572-81
Escherichia coli KVCC 1400306
2 μg/ml (MIC)
18-20 hours
To evaluate the antibacterial activity of Orbifloxacin against the sensitive E. coli KVCC 1400306, showing MIC of 2 μg/ml and MBC of 4 μg/ml.
Front Pharmacol. 2022 Sep 15;13:989395
Escherichia coli KVCC 543
0.5 μg/ml (MIC)
18-20 hours
To evaluate the antibacterial activity of Orbifloxacin against the sensitive E. coli KVCC 543, showing MIC of 0.5 μg/ml and MBC of 1 μg/ml.
Front Pharmacol. 2022 Sep 15;13:989395
Escherichia coli KVCC 1423
128 μg/ml (MIC)
18-20 hours
To evaluate the antibacterial activity of Orbifloxacin against the resistant E. coli KVCC 1423, showing MIC of 128 μg/ml and MBC of 256 μg/ml.
Front Pharmacol. 2022 Sep 15;13:989395
THP-1 cells
0 to 64 μg/ml
48 hours
Evaluate the cytotoxicity of Orbifloxacin on THP-1 cells, results showed that Orbifloxacin exhibited distinct cytotoxicity toward THP-1 cells even at low concentrations
Front Microbiol. 2021 Jun 30;12:658637
RAW264.7 cells
0 to 64 μg/ml
48 hours
Evaluate the cytotoxicity of Orbifloxacin on RAW264.7 cells, results showed that Orbifloxacin was not cytotoxic at a concentration of 8 μg/ml
Front Microbiol. 2021 Jun 30;12:658637
Orbifloxacin/奥比沙星 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Beagle dogs
Healthy Beagle dogs
Intravenous and intramuscular injection
2.5 mg/kg
Single dose
Study the pharmacokinetics (PK) and pharmacodynamics (PD) of Orbifloxacin in Beagle dogs. Results showed rapid, concentration-dependent killing against the clinical isolates, but the recommended dose is unlikely to be clinically effective against some strains like S. intermedius.
Evaluate the in vivo anti-tuberculosis activity of Orbifloxacin in a mouse model, results showed that Orbifloxacin significantly reduced bacterial burden in the lungs and alleviated inflammatory responses
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