Suppr超能文献

雄性柴山羊中酸性药物双氯芬酸和磺胺间甲氧嘧啶的口服药代动力学

Oral pharmacokinetics of the acidic drugs, diclofenac and sulfamonomethoxine in male Shiba goats.

作者信息

Elbadawy Mohamed, Sakiyama Takara, Abohatab Rania, Sasaki Kazuaki, Shimoda Minoru

机构信息

Laboratory of Veterinary Pharmacology, Department of Veterinary Medicine, Tokyo University of Agriculture and Technology, Fuchu, Tokyo 183-8509, Japan.

出版信息

J Vet Med Sci. 2015 Jan;77(1):21-6. doi: 10.1292/jvms.14-0261. Epub 2014 Oct 10.

Abstract

In the present study, we examined the oral pharmacokinetics of the acidic drugs, diclofenac (DF) and sulfamonomethoxine (SMM), which have different physicochemical properties, in Shiba goats. DF and SMM were intravenously and orally administered to 5 male goats using a crossover design. The T(max) of DF and SMM were reached 1.5 and 5.6 hr after they have been orally administered, respectively, and this was followed by their slow elimination. The elimination of both drugs was markedly faster after being intravenously rather than orally administered, which indicated flip-flop phenomena after the oral administration. The mean absorption times (MATs) of DF and SMM were 6 and 15 hr, respectively. This slow absorption may have been due to slow gastric emptying in goats. The large difference observed in MATs between DF and SMM may have been because DF, which is more lipophilic than SMM, was partly absorbed from the forestomach. Therefore, these results suggest that the absorption of highly lipophilic drugs from the forestomach may be markedly high in Shiba goats. In case of drugs whose elimination is quite fast, their efficacies may appear from the early stage after oral administration even in ruminants, because elimination rate is the determinant factor of T(max) in flip-flop phenomena. Such drugs may be used orally even in ruminants.

摘要

在本研究中,我们检测了具有不同理化性质的酸性药物双氯芬酸(DF)和磺胺间甲氧嘧啶(SMM)在柴山羊体内的口服药代动力学。采用交叉设计对5只雄性山羊分别静脉注射和口服DF与SMM。口服DF和SMM后,分别在1.5小时和5.6小时达到T(max),随后是缓慢消除阶段。静脉注射后两种药物的消除明显快于口服给药,这表明口服给药后出现了翻转现象。DF和SMM的平均吸收时间(MAT)分别为6小时和15小时。这种缓慢吸收可能是由于山羊胃排空缓慢所致。DF和SMM的MAT存在较大差异,可能是因为比SMM亲脂性更强的DF部分从前胃吸收。因此,这些结果表明,柴山羊从前胃吸收高亲脂性药物的能力可能明显较高。对于消除相当快的药物,即使在反刍动物中,其疗效也可能在口服给药后的早期阶段显现出来,因为在翻转现象中消除速率是T(max)的决定因素。这类药物甚至在反刍动物中也可口服使用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/afe1/4349534/bab0c0730440/jvms-77-021-g001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验