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夫西地酸乳膏和倍他米松二丙酸酯乳膏在复合临时制剂中的稀释对制剂性能的影响。

The effect of dilution of fusidic acid cream and betamethasone dipropionate cream in complex extemporaneous mixes on formulation performance.

机构信息

Centre for Research in Topical Drug Delivery and Toxicology, University of Hertfordshire, College Lane, Hatfield AL10 9AB, UK.

MedPharm Ltd, Unit 3 Chancellor Court, 50 Occam Road, Surrey Research Park, Guildford GU2 7AB, UK.

出版信息

Int J Pharm. 2022 Aug 25;624:121988. doi: 10.1016/j.ijpharm.2022.121988. Epub 2022 Jul 6.

Abstract

The Aron regimen is an unconventional therapy which entails frequent applications of an extemporaneously prepared three component system (a topical antibiotic, a corticosteroid and an emollient), with the intention of decolonising the skin of S. aureus whilst treating atopic dermatitis. The impact of heavily diluting these topical medicinal products, to differing extents, on formulation performance is not well understood thus was investigated in this study. Following a single application of a range of compounded Aron mixes (fusidic acid and betamethasone dipropionate diluted to varying extents in an emollient base), significant reductions in the expected drug flux across silicone membrane, ex vivo percutaneous absorption and skin retention of both drugs relative to the marketed products were observed. This was attributed to a number of complex formulation effects making such changes difficult to predict in a clinical setting. Further investigations are required to evaluate the impact of frequent applications of the Aron mix to widespread areas on clinical efficacy, antimicrobial resistance and long term side effects.

摘要

Aron 疗法是一种非传统的治疗方法,它需要频繁应用一种临时制备的三组分系统(局部抗生素、皮质类固醇和保湿剂),旨在使金黄色葡萄球菌的皮肤去殖民化,同时治疗特应性皮炎。然而,人们对这些局部药物产品进行不同程度的大量稀释对配方性能的影响了解甚少,因此本研究对此进行了调查。在单次应用一系列混合的 Aron 制剂(将夫西地酸和倍他米松二丙酸酯以不同程度稀释于保湿剂基质中)后,与市售产品相比,硅橡胶膜中药物通量、体外经皮吸收和两种药物在皮肤中的滞留均显著降低。这归因于一些复杂的配方效应,使得在临床环境中难以预测这些变化。需要进一步研究来评估频繁应用 Aron 混合物到广泛区域对临床疗效、抗菌耐药性和长期副作用的影响。

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