奥美普明对虹鳟（Oncorhynchus mykiss）中磺胺二甲氧嘧啶的生物利用度、分布及药代动力学的影响。

Influence of ormetoprim on the bioavailability, distribution, and pharmacokinetics of sulfadimethoxine in rainbow trout (Oncorhynchus mykiss).

Droy B F, Tate T, Lech J J, Kleinow K M

Department of Veterinary Physiology, Pharmacology and Toxicology, School of Veterinary Medicine, Louisiana State University, Baton Rouge 70803.

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1989;94(1):303-7. doi: 10.1016/0742-8413(89)90183-7.

Abstract

Half lives of distribution and elimination phases of 14C-sulfadimethoxine following i.v. dosing of sulfadimethoxine/ormetoprim (SDM/OMP, 42/8 mg/kg) were 0.4 and 16.1 hr respectively. The apparent volume of distribution was 503.9 ml/kg. 2. In vitro plasma protein binding of 14C-SDM was not altered by increasing concentrations of unlabeled OMP. Similarly, binding of 14C-OMP was not altered by SDM. 3. Peak plasma concentrations of 14C-SDM following oral administration of SDM/OMP were observed at 20 hr with an apparent bioavailability of 38%. 4. Oral dispositional studies revealed the highest concentrations of 14C-SDM in bile, intestine, liver and fat. 5. Parent SDM and N-acetylated SDM were detected in plasma from i.v. and orally dosed animals. 6. The pharmacokinetics and distribution of 14C-SDM were not influenced by OMP co-administration.

摘要

静脉注射磺胺二甲氧嘧啶/奥美普明（SDM/OMP，42/8毫克/千克）后，14C-磺胺二甲氧嘧啶分布相和消除相的半衰期分别为0.4小时和16.1小时。表观分布容积为503.9毫升/千克。2. 未标记的奥美普明浓度增加时，14C-磺胺二甲氧嘧啶的体外血浆蛋白结合率未改变。同样，磺胺二甲氧嘧啶也未改变14C-奥美普明的结合率。3. 口服SDM/OMP后，14C-磺胺二甲氧嘧啶的血浆峰值浓度在20小时出现，表观生物利用度为38%。4. 口服处置研究显示，胆汁、肠道、肝脏和脂肪中14C-磺胺二甲氧嘧啶的浓度最高。5. 在静脉注射和口服给药动物的血浆中检测到母体磺胺二甲氧嘧啶和N-乙酰化磺胺二甲氧嘧啶。6. 奥美普明共同给药不影响14C-磺胺二甲氧嘧啶的药代动力学和分布。