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In vivo pharmacokinetic evaluation of carprofen delivery from intra-articular nanoparticles in rabbits: A population modelling approach
Research in Veterinary Science ( IF 2.2 ) Pub Date : 2021-05-21 , DOI: 10.1016/j.rvsc.2021.05.012
A Parra-Coca 1 , A Boix-Montañés 2 , A C Calpena-Campmany 2 , H Colom 2
Affiliation  

Osteoarthritis is treated with COX or fosfolipase A2 inhibitors such as carprofen, a propionic acid NSAID. The enhancement of its action over the articular cartilage is mandatory to facilitate its therapeutic application. Drug uptake into the cartilage requires high synovial fluid concentrations, anticipating its rapid distribution towards bloodstream. Thus, intraarticular administration improves local targeting of the drug, lining with the site of action.

A pharmacokinetic study in rabbits has been performed to evaluate carprofen nanoparticles after intraarticular administration. Pharmacokinetic analysis of plasma profiles through a modelling approach, has demonstrated the rapid distribution of drug outside of synovial chamber but mainly remaining in plasma. The data modelling has demonstrated the existence of two release-absorption processes when the nanoparticles are administered in the synovial space. Additionally, results are predictive of the PK profile of some other species such as cat, dogs or humans.



中文翻译:

兔关节内纳米颗粒对卡洛芬释放的体内药代动力学评估:一种种群建模方法

骨关节炎用COX或磷磷脂酶A2抑制剂(例如卡洛芬,丙酸NSAID)治疗。为了促进其治疗应用,必须增强其对关节软骨的作用。软骨中的药物吸收需要高的滑液浓度,并预期其会迅速向血液中分配。因此,关节内给药改善了药物的局部靶向,与作用部位相吻合。

关节内给药后,已在兔体内进行了药代动力学研究,以评估卡洛芬纳米颗粒。通过建模方法对血浆分布进行药代动力学分析,结果表明滑膜腔外药物迅速分布,但主要保留在血浆中。数据模型已经证明,当在滑膜空间中施用纳米颗粒时,存在两种释放-吸收过程。此外,结果可预测某些其他物种(如猫,狗或人)的PK分布。

更新日期:2021-05-25
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