The plasma and tissue kinetics of sulfadiazine and its metabolite in Ictalurus punctatus after oral gavage at two temperatures

Abstract

AbstractA plasma and tissue kinetic study of sulfadiazine (SDZ) and its metabolite, N4‐acetyl sulfadiazine (ACT‐SDZ), was characterized in channel catfish (Ictalurus punctatus) following a single oral dose of 50 mg/kg at 18 and 24°C. Samples were collected at predetermined time points and determined by ultra‐performance liquid chromatography. The classical one‐compartmental method was used to estimate the pharmacokinetic parameters. Results showed that the changing of temperature was markedly influential on the kinetics of SDZ and ACT‐SDZ in plasma and tissues. When the temperature was increased from 18 to 24°C, the elimination half‐life (K10_HF) of SDZ was decreased in gill, kidney, and muscle + skin, but increased in liver and plasma. The K10_HF of ACT‐SDZ also had a decreased trend in gill, liver, and plasma but had comparable values in kidney and muscle + skin. The absorption half‐life (K01_HF), time to peak concentration (Tmax), and area under concentration–time curve (AUC0‐∞) of SDZ and ACT‐SDZ all exhibited declined tendencies in plasma and tissues. The apparent volume of distribution (V_F) of SDZ in plasma was increased from 0.53 to 1.48 L/kg, and the apparent systemic total body clearance (Cl_F) was increased from 0.028 to 0.060 L/h/kg. In a word, K01_HF, Tmax, and AUC0‐∞ of SDZ and ACT‐SDZ were decreased in plasma and tissues with the increase of temperature, whereas the V_F and Cl_F of SDZ were increased. Meanwhile, we calculated the percentage of time profile of SDZ concentration more than minimum inhibitory concentration to total time (%T > MIC) to guide clinical usage of SDZ. When the dosage interval was 24 h, the values of %T > MIC were all >90% in plasma and most tissues. Therefore, we recommend an oral dose of SDZ at 50 mg/kg once per 24 h at 18–24°C against the fish pathogens with an MIC value of ≤6.4 μg/mL.