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奶牛口服磺胺嘧啶和磺胺间甲氧嘧啶的药代动力学。

Oral pharmacokinetics of sulfadiazine and sulfamonomethoxine in female Holstein milking cows.

机构信息

Laboratory of Veterinary Pharmacology, Nippon Veterinary and Life Science University, Tokyo, Japan.

Laboratory of Veterinary Pharmacology, Cooperative Department of Veterinary Medicine, Tokyo University of Agriculture and Technology, Tokyo, Japan.

出版信息

J Vet Med Sci. 2023 Jul 1;85(7):715-720. doi: 10.1292/jvms.23-0110. Epub 2023 May 24.

Abstract

The efficacy of orally administered drugs in cattle is thought to be slow because of the anatomical and physiological features of their forestomach. Thus, parenteral routes are mainly preferred to administer drugs. However, the effect of some drugs with unique physicochemical properties was promptly obtained even after oral administration in clinically ill cattle. Therefore, the present study aimed to investigate pharmacokinetically the usefulness of the oral route in cattle by comparing the oral pharmacokinetic properties of two sulfonamides with different physicochemical properties. Sulfadiazine (SDZ) and sulfamonomethoxine (SMM) were administered by intravenous and oral route to four female Holstein cows with a 4-weeks washout period. Blood samples were collected over time, and SDZ and SMM concentrations in plasma were analyzed by HPLC. Data obtained from the same animal after intravenous and oral administration were simultaneously analyzed with the one compartment model, and kinetic parameters were calculated. The T (mean ± SD) of SMM (2.75 ± 0.96 hr) was significantly achieved earlier than that of SDZ (5.00 ± 1.15 hr). Further, the mean absorption time of SMM (5.24 ± 0.69 hr) was significantly shorter than that of SDZ (5.92 ± 1.11 hr). Also, the half-life of absorption of SMM (3.91 ± 0.51 hr) was significantly shorter than that of SDZ (4.51 ± 0.82 hr). These data suggest that the absorption rates of highly unionized drugs (such as SMM) from the forestomach of cattle may be markedly higher than less unionized ones (such as SDZ).

摘要

由于牛前胃的解剖和生理特征,经口给予的药物在牛体内的疗效被认为较慢。因此,主要通过注射途径给予药物。然而,在临床上患病的牛中,一些具有独特物理化学性质的药物即使经口给予也能迅速获得效果。因此,本研究旨在通过比较两种具有不同物理化学性质的磺胺类药物的口服药代动力学特性,来探讨口服途径在牛体内的应用价值。将磺胺嘧啶(SDZ)和磺胺间甲氧嘧啶(SMM)通过静脉和口服途径给予 4 头荷斯坦奶牛,洗脱期为 4 周。随着时间的推移采集血样,并通过 HPLC 分析血浆中 SDZ 和 SMM 的浓度。使用同一动物静脉和口服给药后获得的数据,用单室模型进行同时分析,并计算动力学参数。SMM(2.75 ± 0.96 小时)的 T(平均值 ± SD)明显早于 SDZ(5.00 ± 1.15 小时)。此外,SMM 的平均吸收时间(5.24 ± 0.69 小时)明显短于 SDZ(5.92 ± 1.11 小时)。同样,SMM 的吸收半衰期(3.91 ± 0.51 小时)明显短于 SDZ(4.51 ± 0.82 小时)。这些数据表明,高度非离子化药物(如 SMM)从前胃中牛的吸收率可能明显高于非离子化程度较低的药物(如 SDZ)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d12/10372257/eb74e32b5567/jvms-85-715-g001.jpg

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