Pharmacokinetics of a single oral dose of grapiprant in juvenile pigs (Sus scrofa domestica)

IF 1.5 4区 农林科学 Q3 PHARMACOLOGY & PHARMACY
Stephanie Kleine, Chiara E. Hampton, Christopher Smith, Genevieve Bussieres, Pierre-Yves Mulon, Reza Seddighi, Sherry Cox, Joe Smith
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Abstract

Both pet and research pigs can suffer from some degree of pain from surgery, injuries, or osteoarthritis (OA). Despite this, there is a paucity of data on safe and effective analgesia agents in pigs. Grapiprant is an EP4 antagonist that blocks the action of the pro-inflammatory prostanoid, PGE2. It has shown efficacy in attenuating pain associated with ovariohysterectomy and OA in dogs. However, there are no data regarding grapiprant in pigs. Therefore, the pharmacokinetic profile of orally administered grapiprant to juvenile pigs (Sus scrofa domestica) was evaluated in this study. Seven juvenile pigs received 12 mg/kg grapiprant orally. Blood was collected from an indwelling jugular catheter using the push–pull method at set timepoints up to 48 hours. Sample analysis was performed with high-performance liquid chromatography. Mean grapiprant plasma concentration was 164.3 ± 104.7 ng/mL which occurred at 0.8 ± 0.3 h. This study demonstrated that grapiprant concentrations consistent with analgesia in dogs were reached at this dosage in pigs. Further studies are needed to evaluate the efficacy of grapiprant in pigs.

单次口服石墨烯在家猪体内的药代动力学
宠物猪和研究猪都可能因手术、受伤或骨关节炎(OA)而遭受某种程度的疼痛。尽管如此,关于安全有效的猪镇痛药的数据仍然缺乏。Grapiprant是一种EP4拮抗剂,可阻断促炎前列腺素PGE2的作用。它在减轻犬卵巢子宫切除术和OA相关的疼痛方面显示出疗效。然而,没有关于猪体内葡萄柚的数据。因此,本研究评估了口服石墨烯在幼年猪(Sus scrofa domestica)体内的药代动力学特征。7头仔猪口服12 mg/kg石墨烯。在设定的时间点(最长48小时)使用推拉法从留置颈静脉导管中采集血液。采用高效液相色谱法对样品进行分析。石墨烯平均血药浓度为164.3±104.7 ng/mL,出现在0.8±0.3 h。这项研究表明,在猪身上,以这种剂量达到了与狗的镇痛一致的石墨烯浓度。需要进一步的研究来评估石墨烯在猪体内的功效。
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来源期刊
CiteScore
3.10
自引率
15.40%
发文量
69
审稿时长
8-16 weeks
期刊介绍: The Journal of Veterinary Pharmacology and Therapeutics (JVPT) is an international journal devoted to the publication of scientific papers in the basic and clinical aspects of veterinary pharmacology and toxicology, whether the study is in vitro, in vivo, ex vivo or in silico. The Journal is a forum for recent scientific information and developments in the discipline of veterinary pharmacology, including toxicology and therapeutics. Studies that are entirely in vitro will not be considered within the scope of JVPT unless the study has direct relevance to the use of the drug (including toxicants and feed additives) in veterinary species, or that it can be clearly demonstrated that a similar outcome would be expected in vivo. These studies should consider approved or widely used veterinary drugs and/or drugs with broad applicability to veterinary species.
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