Oral absorption profiles of sulfonamides in Shiba goats: a comparison among sulfadimidine, sulfadiazine and sulfanilamide

Journal of Veterinary Medical Science

Kazuaki SASAKI²  Yusuke ISHIHARA²  Mohamed ELBADAWY²  Mohamed ABOUBAKR¹  Minoru SHIMODA² 

[1] Pharmacology Department, Faculty of Veterinary Medicine, Benha University, Moshtohor, Toukh, Elqaliobiya, 13736, Egypt;Laboratory of Veterinary Pharmacology, Department of Veterinary Medicine, Tokyo University of Agriculture and Technology, Fuchu, Tokyo 183�?8509, Japan

关键词: goat;    oral pharmacokinetic;    sulfadiazine;    sulfadimidine;    sulfanilamide;    unionization;   

DOI  :  10.1292/jvms.15-0601

学科分类：兽医学

来源: Japanese Society of Veterinary Science

【 摘 要 】

References(15)The oral pharmacokinetics of three sulfonamides, sulfadimidine (pKa 7.5), sulfadiazine (pKa 6.5) and sulfanilamide (pKa 10.5), with different rates of unionization in rumen juice, were compared in Shiba goats to clarify the relationship between drug absorption profiles after their oral administration as well as their degree of unionization in the rumen. Sulfonamides were administered either into the left jugular vein or orally to five male goats at doses of 10 mg/kg body weight, using a crossover design with at least a 3-week washout period. The Tmax of sulfadimidine, sulfadiazine and sulfanilamide reached 2.0 ± 1.2, 6.0 ± 0.0, and 7.8 ± 1.6 hr, respectively, after their oral administration, and this was followed by their slow elimination due to a slow rate of drug absorption from the gastrointestinal tract. The MAT and t1/2ka of sulfadiazine (13.2 ± 2.0 and 10.9 ± 1.08 hr) were significantly longer than those of sulfanilamide (9.09 ± 1.67 and 7.46 ± 1.70 hr) and sulfadimidine (7.52 ± 0.85 and 5.17 ± 0.66 hr). These results suggest that the absorption rates of highly unionized drugs (such as sulfanilamide and sulfadimidine) from the forestomach of goats may be markedly higher than less unionized ones (such as sulfadiazine). The mean oral bioavailability of sulfadiazine was high (83.9 ± 17.0%), whereas those of sulfadimidine and sulfanilamide were low (44.9 ± 16.4% and 49.2 ± 2.11%, respectively).

【 授权许可】

Unknown