Oral pharmacokinetics of the acidic drugs, diclofenac and sulfamonomethoxinein male Shiba goats

[摘要] References(28)Cited-By(3)In the present study, weexamined the oral pharmacokinetics of the acidic drugs, diclofenac (DF) andsulfamonomethoxine (SMM), which have different physicochemical properties, in Shiba goats.DF and SMM were intravenously and orally administered to 5 male goats using a crossoverdesign. The Tmax of DF and SMM were reached 1.5 and 5.6 hr after they have beenorally administered, respectively, and this was followed by their slow elimination. Theelimination of both drugs was markedly faster after being intravenously rather than orallyadministered, which indicated flip-flop phenomena after the oral administration. The meanabsorption times (MATs) of DF and SMM were 6 and 15 hr, respectively. This slow absorptionmay have been due to slow gastric emptying in goats. The large difference observed in MATsbetween DF and SMM may have been because DF, which is more lipophilic than SMM, was partlyabsorbed from the forestomach. Therefore, these results suggest that the absorption ofhighly lipophilic drugs from the forestomach may be markedly high in Shiba goats. In caseof drugs whose elimination is quite fast, their efficacies may appear from the early stageafter oral administration even in ruminants, because elimination rate is the determinantfactor of Tmax in flip-flop phenomena. Such drugs may be used orally even inruminants.

[学科分类] 兽医学

[关键词] diclofenac;flip-flop phenomena;goat;oral pharmacokinetic;sulfamonomethoxine