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Pharmacokinetics of Pantoprazole and Pantoprazole Sulfone in Goats After Intravenous Administration: A Preliminary Report
Frontiers in Veterinary Science ( IF 3.2 ) Pub Date : 2021-09-22 , DOI: 10.3389/fvets.2021.744813
Joe S Smith 1, 2 , Jonathan P Mochel 1 , Windy M Soto-Gonzalez 2 , Rebecca R Rahn 2 , Bryanna N Fayne 2 , Olivia G Escher 2 , Anastasia M Geletka 2 , Lainey E Harvill 3 , Joan B Bergman 3 , Sherry Cox 3
Affiliation  

Background: Ruminant species are at risk of developing abomasal ulceration, but there is a lack of pharmacokinetic data for anti-ulcer therapies, such as the proton pump inhibitor pantoprazole, in goats.

Objective: The primary study objective was to estimate the plasma pharmacokinetic parameters for pantoprazole in adult goats after intravenous administration. A secondary objective was to describe the pharmacokinetic parameters for the metabolite, pantoprazole sulfone, in goats.

Methods: Pantoprazole was administered intravenously to six adult goats at a dose of 1 mg/kg. Plasma samples were collected over 36h and analyzed via reverse phase high performance liquid chromatography for determination of pantoprazole and pantoprazole sulfone concentrations. Pharmacokinetic parameters were determined by non-compartmental analysis.

Results: Plasma clearance, elimination half-life, and volume of distribution of pantoprazole were estimated at 0.345 mL/kg/min, 0.7 h, and 0.9 L/kg, respectively following IV administration. The maximum concentration, elimination half-life and area under the curve of pantoprazole sulfone were estimated at 0.1 μg/mL, 0.8 h, and 0.2 hr*μg/mL, respectively. The global extraction ratio was estimated 0.00795 ± 0.00138. All animals had normal physical examinations after conclusion of the study.

Conclusion: The reported plasma clearance for pantoprazole is lower than reported for foals, calves, and alpacas. The elimination half-life appears to be < that reported for foals and calves. Future pharmacodynamic studies are necessary for determination of the efficacy of pantoprazole on acid suppression in goats.



中文翻译:

泮托拉唑和泮托拉唑砜在山羊静脉给药后的药代动力学初步报告

背景: 反刍动物有发生皱胃溃疡的风险,但缺乏抗溃疡疗法(如质子泵抑制剂泮托拉唑)在山羊中的药代动力学数据。

客观的:主要研究目的是评估泮托拉唑在成年山羊静脉内给药后的血浆药代动力学参数。次要目的是描述代谢物泮托拉唑砜在山羊中的药代动力学参数。

方法:泮托拉唑以 1 毫克/公斤的剂量静脉注射给六只成年山羊。在 36 小时内收集血浆样品并通过反相高效液相色谱法进行分析,以确定泮托拉唑和泮托拉唑砜的浓度。通过非房室分析确定药代动力学参数。

结果:静脉给药后泮托拉唑的血浆清除率、消除半衰期和分布容积分别估计为 0.345 mL/kg/min、0.7 h 和 0.9 L/kg。泮托拉唑砜的最大浓度、消除半衰期和曲线下面积分别估计为 0.1 μg/mL、0.8 小时和 0.2 小时* μg/mL。全球提取率估计为 0.00795 ± 0.00138。研究结束后,所有动物的体格检查均正常。

结论:泮托拉唑的报告血浆清除率低于小马驹、小牛和羊驼的报告。消除半衰期似乎小于报告的小马驹和小牛。未来的药效学研究对于确定泮托拉唑对山羊酸抑制的功效是必要的。

更新日期:2021-09-22
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