AUTHOR=Lei Zhixin , Liu Qianying , Yang Bing , Khaliq Haseeb , Ahmed Saeed , Fan Bowen , Cao Jiyue , He Qigai 

TITLE=Evaluation of Marbofloxacin in Beagle Dogs After Oral Dosing: Preclinical Safety Evaluation and Comparative Pharmacokinetics of Two Different Tablets

JOURNAL=Frontiers in Pharmacology

VOLUME=9

YEAR=2018

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2018.00306

DOI=10.3389/fphar.2018.00306

ISSN=1663-9812

ABSTRACT=<p>The current study evaluates a tested marbofloxacin tablet (MBT) (Petsen), in terms of bioavailability and pharmacokinetics (PK) in a comparison of the commercialized and standard tablet (Marbocyl) in beagle dogs. Four different bacterial species were selected for the determination of the minimal inhibitory concentration (MIC) against marbofloxacin (MBF). Target animal safety studies were conducted with a wide spectrum of dosages of Petsen. Pharmacokinetics and bioavailability of Petsen were observed after the oral administration of a recommended dosage of 2 mg/kg. The MIC<sub>90</sub> of MBF against <italic>Staphylococcus aureus, Escherichia coli, Pasteurella multocida</italic>, and <italic>Streptococcus</italic> were 2.00, 4.00, 0.25, and 0.50 μg/ml, respectively. These results showed that the MBT has an expected antimicrobial activity <italic>in vitro</italic>. The main parameters of <italic>t</italic><sub>1/2β</sub>, Cl<sub>b</sub>, AUC<sub>0−∞</sub>, <italic>C</italic><sub>max</sub>, and <italic>K</italic><sub><italic>e</italic></sub> were 22.14 h, 0.15 L/h, 13.27 μg.h/ml, 0.95 μg/ml, 0.09 h<sup>−1</sup>, and 16.47 h, 0.14 L/h, 14.10 μg.h/ml, 0.97 μg/ml, 0.11 h<sup>−1</sup> after the orally administrated Petsen and Marbocyl, while no biologically significant changes and toxicological significance have been found by their comparison. These findings indicate that the Petsen had a slow elimination, high bioavailability and kinetically similar to the commercialized Marbocyl. Furthermore, no statistically significant differences were distinguished on the continuous gradient dosages of 2, 6, and 10 mg/kg in the term of the clinical presentation. The present study results displayed that the tested MBT (Petsen) was safe, with limited toxicity, which was similar to the commercialized tablet (Marbocyl), could provide an alternative MBT as a veterinary medicine in beagle dogs.</p>