Anfossi P, Montesissa C, Pezzi P, Formigoni A
Department of Public Veterinary Health and Animal Pathology, Faculty of Veterinary Medicine, University of Bologna, Ozzano Emilia (BO), Italy.
J Vet Pharmacol Ther. 1996 Aug;19(4):300-4. doi: 10.1111/j.1365-2885.1996.tb00053.x.
The kinetics of free and microgranulated sulfadimidine were compared in milk-fed calves dosed orally (180 mg/kg) in a crossover study. Microgranulation results in delayed absorption of sulfadimidine and poor bioavailability, with the area under the plasma concentration-time curve (AUC(0-infinity)) reduced from 7400 to 3781 micrograms.h/mL, and maximum plasma concentration (Cmax) reduced from 188.1 +/- 39.0 to 84.41 +/- 22.6 micrograms/mL. It is concluded that sulfadimidine microgranulated with long chain fatty acids is not suitable for use in milk-fed calves; the gastrointestinal transit time is too rapid to allow full release of the drug, markedly limiting its bioavailability. In adult animals, or in the young of other animal species in which digesta transit time is slower than in calves, the bioavailability of microgranulated sulfadimidine may be much greater.
在一项交叉研究中,对口服给药(180毫克/千克)的哺乳犊牛体内游离磺胺二甲嘧啶和微颗粒化磺胺二甲嘧啶的动力学进行了比较。微颗粒化导致磺胺二甲嘧啶吸收延迟且生物利用度差,血浆浓度-时间曲线下面积(AUC(0-∞))从7400降至3781微克·小时/毫升,血浆最大浓度(Cmax)从188.1±39.0降至84.41±22.6微克/毫升。得出的结论是,与长链脂肪酸微颗粒化的磺胺二甲嘧啶不适用于哺乳犊牛;胃肠道转运时间过快,无法使药物充分释放,显著限制了其生物利用度。在成年动物或其他动物幼崽中,其食糜转运时间比犊牛慢,微颗粒化磺胺二甲嘧啶的生物利用度可能会高得多。