Comparative pharmacokinetics of ceftaroline in rats, rabbits, and monkeys following a single intravenous or intramuscular injection.
This study assessed the pharmacokinetic profiles for intramuscular and intravenous ceftaroline treatment for rats, rabbits, and monkeys. Ceftaroline, a novel cephalosporin with broad-spectrum activity against Gram-positive and Gram-negative pathogens, demonstrated favorable pharmacokinetic profiles following intramuscular administration in all 3 animal species, comparable to the levels for intravenous dosing. The areas under the plasma concentration-time curve obtained after intramuscular administration were increased in rats and similar in rabbits and monkeys, compared with the levels obtained after intravenous dosing (129%, 7.29%, and 12.7% greater in rats, rabbits, and monkeys, respectively). The data reported here support the development of an intramuscular formulation for ceftaroline.
Ge
Yigong
Y
Cerexa, Inc., Oakland, CA, USA. jge@calixainc.com
Maynard
David
D
Rickert
Douglas E
DE
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002511:Cephalosporins / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D000882:Haplorhini; D007273:Injections, Intramuscular; D007275:Injections, Intravenous; D008297:Male; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D000097583:Ceftaroline
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D000097583:Ceftaroline