Non-bioequivalence of various trademarks of enrofloxacin and Baytril in cows.
Including Baytril, in various parts of the world many commercial preparations of enrofloxacin for parenteral administration are being employed for the treatment of bacterial diseases in cows. To optimize clinical responses and to minimize development of bacterial resistance to this agent, the copied pharmaceutical preparations must comply with some key pharmacokinetic features when bioequivalence studies are performed. To assess whether or not there was bioequivalence among nine commercial preparations of enrofloxacin and the original one, a controlled pharmacokinetic study was carried out. These was done utilizing the microbiological agar-diffusion test as quantitative/qualitative analytical method. A non-compartmental model defined kinetic variables. Results for Baytril revealed that maximal serum concentration (Csmax) was only matched by one preparation while area under the curve (AUC) of the serum concentration/activity of enrofloxacin and metabolites in time was not matched by any preparation. Time to Csmax (Tmax), elimination half-life, and shape of the time-serum concentrations of enrofloxacin profiles obtained for the nine generic preparations differ significantly somehow from the corresponding data obtained for the reference enrofloxacin. The need for studies to demonstrate bioequivalence becomes mandatory if similar preparations of enrofloxacin become commercially available. Enrofloxacin should be used selectively and cautiously to limit development of bacterial resistance. Non-bioequivalence of relevant pharmacokinetic values, such as Csmax and bioavailability (AUC) would facilitate development of bacterial resistance and limit the useful life span of this antibacterial agent.
Sumano
L H
LH
Departament of Physiology and Pharmacology, School of Veterinary Medicine, National Autonomous University of Mexico, Mexico City, Mexico. sumano@servidor.unam.mx
Ocampo
C L
CL
Gutiérrez
O L
OL
D000818:Animals; D000890:Anti-Infective Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D019540:Area Under Curve; D001419:Bacteria / Q000187:drug effects; D002417:Cattle / Q000097:blood / Q000378:metabolism*; D002418:Cattle Diseases / Q000188:drug therapy*; D004352:Drug Resistance, Microbial; D000077422:Enrofloxacin; D024841:Fluoroquinolones; D007408:Intestinal Absorption; D015363:Quinolones / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D011897:Random Allocation; D013810:Therapeutic Equivalency
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; D000077422:Enrofloxacin