Bramer Tobias, Frenning Göran, Gråsjö Johan, Edsman Katarina, Hansson Per
Department of Pharmacy, Uppsala University, Box 580, SE-751 23, Uppsala, Sweden.
Colloids Surf B Biointerfaces. 2009 Jul 1;71(2):214-25. doi: 10.1016/j.colsurfb.2009.02.008. Epub 2009 Feb 21.
The aim of this study was to apply the regular solution theory of mixed micelles to gain new insights on the drug release mechanism, when using catanionic mixtures as a method of obtaining prolonged release from gels. Synergistic effects were investigated at equilibrium and quantified in terms of regular solution theory interaction parameters. The drug release from catanionic aggregates was studied both in a polymer free environment, using dialysis membranes, and in gels, using a modified USP paddle method. The drug release kinetics was modelled theoretically by combining the regular solution theory with Fick's diffusion laws assuming a contribution to the transport only from monomeric species (stationary aggregates). The theoretical predictions were found to be in reasonably good agreement with experiments. An analysis of the calculated distribution of species between aggregated and monomeric states was shown to provide further insights into the release mechanism.
本研究的目的是应用混合胶束的正规溶液理论,以深入了解药物释放机制,此时使用阴-阳离子混合物作为从凝胶中实现长效释放的一种方法。在平衡状态下研究了协同效应,并根据正规溶液理论相互作用参数进行了量化。使用透析膜在无聚合物环境中以及使用改良的美国药典桨法在凝胶中研究了阴-阳离子聚集体的药物释放。通过将正规溶液理论与菲克扩散定律相结合,假设仅单体物种(固定聚集体)对传输有贡献,从理论上对药物释放动力学进行了建模。结果发现理论预测与实验结果相当吻合。对计算得到的聚集体态和单体态之间物种分布的分析表明,这能进一步深入了解释放机制。