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Swine as the Animal Model for Testing New Formulations of Anti-Inflammatory Drugs: Carprofen Pharmacokinetics and Bioavailability of the Intramuscular Route
Pharmaceutics ( IF 5.4 ) Pub Date : 2022-05-12 , DOI: 10.3390/pharmaceutics14051045
Lidia Gómez-Segura 1 , Antoni Boix-Montañes 2, 3 , Mireia Mallandrich 2, 3 , Alexander Parra-Coca 4 , José L Soriano-Ruiz 5 , Ana Cristina Calpena 2, 3 , Álvaro Gimeno 6 , David Bellido 7 , Helena Colom 2, 3
Affiliation  

Carprofen (CP) is a non-steroidal anti-inflammatory drug (NSAID) frequently used to treat respiratory diseases in numerous small animals, but also in large species. CP is a formidable candidate for further therapeutic research of human inflammatory diseases using the pig as an animal model. However, CP administration in swine is very uncommon and respective pharmacokinetics/bioavailability studies are scarce. A simultaneous population pharmacokinetic analysis after CP intravenous and intramuscular administrations in pigs has shown high extent and rate of absorption and a similar distribution profile with respect to man and other mammals. However, clearance and half-life values found in swine suggest a slower elimination process than that observed in man and some other animal species. Although not reported in other species, liver and kidney concentrations achieved at 48 h post-intramuscular administration in pigs were ten times lower than those found in plasma. Simulations pointed to 4 mg/kg every 24 h as the best dosage regimen to achieve similar therapeutic levels to those observed in other animal species. All these findings support the use of pig as an animal model to study the anti-inflammatory effects of CP in humans.

中文翻译:

以猪作为测试抗炎药物新配方的动物模型:卡洛芬的药代动力学和肌内途径的生物利用度

卡洛芬 (CP) 是一种非甾体类抗炎药 (NSAID),常用于治疗许多小动物和大型物种的呼吸道疾病。CP 是使用猪作为动物模型对人类炎症性疾病进行进一步治疗研究的强大候选者。然而,猪中的CP给药非常罕见,并且相应的药代动力学/生物利用度研究也很少。猪静脉注射和肌肉注射 CP 后同时进行的群体药代动力学分析表明,猪的吸收程度和吸收率较高,并且与人和其他哺乳动物的分布情况相似。然而,在猪中发现的清除率和半衰期值表明,消除过程比在人类和其他一些动物物种中观察到的要慢。尽管在其他物种中没有报道,但肌肉注射后 48 小时猪的肝脏和肾脏浓度比血浆中的浓度低十倍。模拟表明,每 24 小时 4 毫克/公斤是达到与其他动物物种中观察到的相似治疗水平的最佳剂量方案。所有这些发现都支持使用猪作为动物模型来研究 CP 对人类的抗炎作用。
更新日期:2022-05-12
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