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在绵羊微骨折关节缺损模型中,经Vetdrop®经皮治疗后卡洛芬浓度测量的初步研究。

Preliminary study on carprofen concentration measurements after transcutaneous treatment with Vetdrop® in a microfracture joint defect model in sheep.

作者信息

Sidler Michèle, Fouché Nathalie, Meth Ingmar, von Hahn Friedrich, von Rechenberg Brigitte, Kronen Peter W

机构信息

Musculoskeletal Research Unit (MSRU), Equine Hospital, Vetsuisse Faculty, University of Zurich, Zurich, Switzerland.

Veterinary Anaesthesia Services International, Winterthur, Switzerland.

出版信息

BMC Vet Res. 2014 Dec 9;10:268. doi: 10.1186/s12917-014-0268-6.

DOI:10.1186/s12917-014-0268-6
PMID:25488522
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4263071/
Abstract

BACKGROUND

The present preliminary study describes concentration time courses of the NSAID carprofen in the plasma and synovial fluid in a microfrature sheep model after transcutaneous treatments with a novel application device (Vetdrop®). To treat circumscribed inflammatory processes a transcutaneous application device could potentially be beneficial. After transcutaneous application normally lower systemic concentrations are measured which may reduce the incidence of side effects, whereas efficacy is still maintained. In this study carprofen was used based on its capacity to provide analgesia after orthopaedic procedures in sheep and it is considered that it may have a positive influence on the healing of cartilage in low concentrations.

RESULTS

In all transcutaneously treated animals, carprofen plasma concentrations exceeded those of synovial fluid, although plasma levels remained significantly reduced (300-fold) as compared to carprofen administered intravenously. Furthermore, in contrast to the intravenously treated animals, a modest accumulation of carprofen in plasma and synovial fluid was observed in the transcutaneously treated animals over the 6-week treatment period.

CONCLUSIONS

The transcutaneously administered carprofen using the Vetdrop® device penetrated the skin and both, plasma- and synovial concentrations could be measured repeatedly over time. This novel device may be considered a valuable transcutaneous drug delivery system.

摘要

背景

本初步研究描述了在绵羊微骨折模型中,使用新型给药装置(Vetdrop®)经皮给药后,非甾体抗炎药卡洛芬在血浆和滑液中的浓度-时间过程。对于治疗局限性炎症过程,经皮给药装置可能具有潜在益处。经皮给药后,通常测得的全身浓度较低,这可能会降低副作用的发生率,同时仍能维持疗效。在本研究中,使用卡洛芬是基于其在绵羊骨科手术后提供镇痛的能力,并且认为其在低浓度下可能对软骨愈合有积极影响。

结果

在所有经皮治疗的动物中,卡洛芬的血浆浓度超过滑液浓度,尽管与静脉注射卡洛芬相比,血浆水平仍显著降低(300倍)。此外,与静脉治疗的动物相比,在6周的治疗期内,经皮治疗的动物血浆和滑液中观察到卡洛芬有适度的蓄积。

结论

使用Vetdrop®装置经皮给药的卡洛芬穿透了皮肤,并且随着时间的推移可以反复测量血浆和滑液浓度。这种新型装置可被视为一种有价值的经皮给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a76/4263071/899e38335642/12917_2014_268_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a76/4263071/06c70234eff9/12917_2014_268_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a76/4263071/724871fd3989/12917_2014_268_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a76/4263071/899e38335642/12917_2014_268_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a76/4263071/06c70234eff9/12917_2014_268_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a76/4263071/724871fd3989/12917_2014_268_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a76/4263071/899e38335642/12917_2014_268_Fig3_HTML.jpg

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