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磺胺二甲嘧啶在绵羊血浆和腮腺唾液中的比较药代动力学

Comparative pharmacokinetics of sulfamethazine in plasma and parotid saliva of sheep.

作者信息

Pulido E, Meot F, Sumano H, Boivin R

机构信息

Departement de Physiologie, Ecole Nationale Vétérinaire de Lyon, France.

出版信息

J Vet Pharmacol Ther. 1998 Apr;21(2):138-43. doi: 10.1046/j.1365-2885.1998.00120.x.

DOI:10.1046/j.1365-2885.1998.00120.x
PMID:9597652
Abstract

Salivary output in sheep is large enough to be considered a physiologic body fluid compartment. The hypothesis for this work was that pharmacokinetics of sulfamethazine in saliva was similar to that in plasma. A reliable technique was developed to measure parotid salivary output. Mean output of saliva was 3.18 +/- 1.04 L from a single parotid gland per day with a mean flow of 2.21 +/- 0.43 mL/min. Using concentrations of sulfamethazine in parotid saliva made it possible to calculate the total passage of sulfamethazine to parotid saliva, which was calculated to be 3.5% of the total dose. Pharmacokinetic variables obtained for sulfamethazine in plasma and in saliva were closely related (AUC 1408 micrograms.h/mL and AUC 1484 micrograms.h/mL; Vdarea 0.434 L/kg and Vdarea 0.374 L/kg; t 1/2 beta 4.30 h and 3.46 h, respectively) and no substantial differences were observed. The convenience of using salivary concentrations of sulfamethazine for drug monitoring is discussed.

摘要

绵羊的唾液分泌量足够大,可被视为一个生理体液腔室。这项研究的假设是,磺胺二甲嘧啶在唾液中的药代动力学与在血浆中的相似。开发了一种可靠的技术来测量腮腺唾液分泌量。单个腮腺每天的唾液平均分泌量为3.18±1.04升,平均流速为2.21±0.43毫升/分钟。利用腮腺唾液中磺胺二甲嘧啶的浓度,可以计算出磺胺二甲嘧啶进入腮腺唾液的总量,经计算占总剂量的3.5%。在血浆和唾液中获得的磺胺二甲嘧啶的药代动力学变量密切相关(曲线下面积分别为1408微克·小时/毫升和1484微克·小时/毫升;表观分布容积分别为0.434升/千克和0.374升/千克;消除半衰期分别为4.30小时和3.46小时),未观察到实质性差异。讨论了利用磺胺二甲嘧啶唾液浓度进行药物监测的便利性。

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