生物等效性和生物利用度杂志

抽象的

Pharmacokinetic Profile of Nimesulide in Bovine Calves

Lombodar Mahapatra, Gyana R. sahoo, Monoj K. Panda and Subas ch. Parija

The aim of the present study was to investigate pharmacokinetic profile and bioavailability of cyclooxygenase (COX)-2 selective nonsteroidal anti-infalmmatory drug nimesulide in bovine male calves after intravenous (i.v.) and intramuscular (i.m.) administration at a dose of 4.5mg/ kg BW. Blood samples were collected by jugular venipuncture at predetermined times following drug administration. Nimesulide in the plasma was assayed by using a validated HPTLC method. Plasma concentration-time data were subjected to compartmental analysis and pharmacokinetic parameters for nimesulide after i.v. and i.m. administration were calculated according to two and onecompartment open models, respectively. Following i.v. administration, a rapid distribution phase was followed by slower elimination phase. The half-lives during distribution phase (t1/2α) and terminal elimination phase (t1/2β) were 0.15±0.005h and 9.02±0.06h, respectively. The steady-state volume of distribution (vd(ss)), total body clearance (clB) and mean residence time (MRT) of nimesulide were 0.22±0.02L/h/kg, 0.02±0.001 and 11.23±0.04 h, respectively. After i.m administration, maximum plasma concentration (cmax) of nimesulide was 35.84±3.04 μg/ mL attained at 4.0±0.19 h (tmax). Plasma drug levels were not detectable upto 72h. Similarly the t1/2β (20.08±0.79h) MRT (13.76±0.09h) of nimesulide after i.m. administration were significantly longer than the i.v administration. The bioavailability of nimesulide was 89.42% after i.m administration. These pharmacokinetic data suggests that nimesulide given intramuscularly may be useful in the treatment of inflammatory disease conditions in bovines.