Pharmacokinetics of sarafloxacin in pigs and broilers following intravenous, intramuscular, and oral single‐dose applications

Abstract

Pharmacokinetics of sarafloxacin, a fluoroquinolone antibiotic, was determined in pigs and broilers after intravenous (i.v.), intramuscular (i.m.), or oral (p.o.) administration at a single dose of 5 (pigs) or 10 mg/kg (broilers). Plasma concentration profiles were analysed by a noncompartmental pharmacokinetic method. Following i.v., i.m. and p.o. doses, the elimination half-lives (t1/2beta) were 3.37 +/- 0.46, 4.66 +/- 1.34, 7.20 +/- 1.92 (pigs) and 2.53 +/- 0.82, 6.81 +/- 2.04, 3.89 +/- 1.19 h (broilers), respectively. After i.m. and p.o. doses, bioavailabilities (F) were 81.8 +/- 9.8 and 42.6 +/- 8.2% (pigs) and 72.1 +/- 8.1 and 59.6 +/- 13.8% (broilers), respectively. Steady-state distribution volumes (Vd(ss)) of 1.92 +/- 0.27 and 3.40 +/- 1.26 L/kg and total body clearances (ClB) of 0.51 +/- 0.03 and 1.20 +/- 0.20 L/kg/h were determined in pigs and broilers, respectively. Areas under the curve (AUC), mean residence times (MRT), and mean absorption times (MAT) were also determined. Sarafloxacin was demonstrated to be more rapidly absorbed, more extensively distributed, and more quickly eliminated in broilers than in pigs. Based on the single-dose pharmacokinetic parameters determined, multiple dosage regimens were recommended as: a dosage of 10 mg/kg given intramuscularly every 12 h in pigs, or administered orally every 8 h in broilers, can maintain effective plasma concentrations with bacteria infections, in which MIC90 are <0.25 microg/mL.

Distribution of enrofloxacin in intestinal tissue and contents of healthy pigs after oral and intramuscular administrations

“…administration was superior to p.o. administration of sarafloxacin in pigs (Ding et al ., 2001), danofloxacin in cattle and swine (Mann & Frame, 1992) and for enrofloxacin in broiler chickens (Bugyei et al ., 1999), calves and piglets (Scheer, 1988), homing‐pigeons (Dorrenstein & Verburg, 1988), chickens (Abd‐El‐Aziz et al ., 1997) and ducks (Intorre et al ., 1997). Only one study described faster absorption and higher C max after p.o.…”

Determination of the presence and pharmacokinetic profile of ciprofloxacin by TLC and HPLC method respectively in broiler chicken after single oral administration

“…17,19 This small volume of distribution indicates that ciprofloxacin was not well distributed into tissue after po administration in broiler. Maximum concentration, 0.26 ± 0.03 mg l À1 , after po administration of ciprofloxacin in this study was observed at 4.40±0.1 h. which is much higher than sarafloxacin, enrofloxacin, danofloxacin 13,17,19 and ciprofloxacin. 8,20 This higher value indicates that ciprofloxacin reached slowly to its peak concentration than sarafloxacin, enrofloxaci, danofloxacin and ofloxacin after po administration in broiler.…”

“…14 The plasma half-life, t ½ , after oral administration in broiler was estimated to be 5.25 ± 0.02 h, much higher than i.v. administration of ciprofloxacin and enrofloxacin 15,16 and oral administration of sarafloxacin, 13 but apparently shorter than oral administration of danofloxacin and enrofloxacin. 17,18 This value is almost same to po administration of ofloxacin in broiler.…”

“…This low bioavailability may be due to the result of feeding state. Area under the plasma concentration versus time curve (AUC) was estimated to be 13.397±0.13 mg ml À1 h À1 , was higher than sarafloxacin, 13 danofloxacin, enrofloxacin 18 and ciprofloxacin. 20…”

“…There are many papers published on the pharmacokinetics of these antibacterial agents in various animal species. 13 Although the pharmacokinetics of ciprofloxacin after oral administration in broiler has been described in some literature, [7][8][9] there is no previous literature on the TLC analysis of plasma sample containing ciprofloxacin after oral administration in broiler chickens; besides, there is no previous study to determine the concentration of ciprofloxacin for per hour interval. From Table 1, we see that the average retention factor of each plasma sample and standard ciprofloxacin is almost same (0.54).…”