Pharmacokinetics of baquiloprim and sulphadimidine in pigs after intramuscular administration.
Baquiloprim, a novel 5-substituted 2, 4-diaminopyrimidine, has been developed specifically for veterinary use. It has been formulated as an injectable preparation and combined with sulphadimidine to exploit the synergistic activity of the two antibacterial agents. The formulation was given by deep intramuscular injection to pigs at doses of 10 mg kg-1 and 30 mg kg-1 and the pharmacokinetic properties were investigated. The in vitro activity of the two components was also determined against a range of porcine pathogens. Both components were rapidly absorbed and the maximum concentrations of 0.55 microgram ml-1 baquiloprim and 15.6 micrograms ml-1 sulphadimidine observed after the administration of the lower dose were well in excess of the minimum inhibitory concentration (MIC) values against susceptible pathogens, the highest combined MIC90 being 0.06 microgram ml-1 baquiloprim + 6.25 micrograms ml-1 sulphadimidine. Concentrations above the MIC values of most pathogens were maintained for more than 24 and 48 hours after the administration of the lower and higher doses, respectively. The volumes of distribution of 2.41 litre kg-1 observed after the lower dose and 4.60 litre kg-1 after the higher dose indicated that baquiloprim was well distributed and concentrated in tissues. These findings suggest that the formulation should be effective in the treatment of bacterial infections in pigs.
Pitman-Moore Europe, Harefield, Uxbridge, Middlesex.
A M
AM
Davies
N M
NM
MacKenzie
D000818:Animals; D004305:Dose-Response Relationship, Drug; D005260:Female; D007273:Injections, Intramuscular / Q000662:veterinary; D008297:Male; D011743:Pyrimidines / Q000493:pharmacokinetics*; D013418:Sulfamethazine / Q000493:pharmacokinetics*; D013552:Swine / Q000378:metabolism*; D014018:Tissue Distribution
D011743:Pyrimidines; C072761:baquiloprim; D013418:Sulfamethazine