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优化外用药物输送的共溶剂浓度 III--亲脂性载体对布洛芬渗透的影响。

Optimisation of cosolvent concentration for topical drug delivery III--influence of lipophilic vehicles on ibuprofen permeation.

机构信息

Aesop, Melbourne, Victoria, Australia.

出版信息

Skin Pharmacol Physiol. 2011;24(1):22-6. doi: 10.1159/000315139. Epub 2010 Jul 9.

Abstract

Previously, we have reported the effects of water, ethanol, propylene glycol and various binary and ternary mixtures of these solvents on the permeation of ibuprofen in model membranes and in skin. The present study investigates the influence of lipophilic vehicles on the transport of ibuprofen in silicone membrane and in human skin. The permeation of ibuprofen was measured from mineral oil (MO), Miglyol® 812 (MG) and binary mixtures of MO and MG. The solubility of ibuprofen was 5-fold higher in MG than in MO, however, the permeation of ibuprofen from the pure vehicles and combinations of both was comparable in silicone membrane. Additionally, there were no significant differences in skin permeation for MO and MG vehicles. When the permeation of various hydrophilic and lipophilic vehicles is considered, a trend between flux values for the model membrane and skin is evident (r(2) = 0.71). The findings suggest that silicone membrane may provide information on qualitative trends in skin permeation for vehicles of diverse solubility and partition characteristics.

摘要

此前,我们已经报道了水、乙醇、丙二醇以及这些溶剂的各种二元和三元混合物对布洛芬在模型膜和皮肤中渗透的影响。本研究探讨了亲脂性载体对布洛芬在硅橡胶膜和人体皮肤中传输的影响。从矿物油(MO)、Migllyol® 812(MG)和 MO 与 MG 的二元混合物中测量了布洛芬的渗透。布洛芬在 MG 中的溶解度比在 MO 中高 5 倍,然而,从纯载体和两者的组合中渗透布洛芬在硅橡胶膜中是相当的。此外,MO 和 MG 载体在皮肤渗透方面没有显著差异。当考虑各种亲水性和疏水性载体的渗透时,模型膜和皮肤的通量值之间存在明显的趋势(r(2) = 0.71)。研究结果表明,硅橡胶膜可能为具有不同溶解度和分配特性的载体在皮肤渗透方面提供定性趋势的信息。

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