Release characteristics of anionic drug compounds from liquid crystalline gels. Part II. The effects of ion pairing and buffering on the passive delivery of anionic drugs across non-rate-limiting membranes.
Release characteristics of anionic drug compounds from liquid crystalline gels. Part II. The effects of ion pairing and buffering on the passive delivery of anionic drugs across non-rate-limiting membranes.
复制标题
阴离子药物化合物从液晶凝胶中的释放特性。
DOI：
10.1016/j.ijpharm.2005.12.020
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发表时间：
2006
影响因子：
5.8
通讯作者：
J. Corish
中科院分区：
文献类型：
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作者：
D. Fitzpatrick;J. Corish
这是一系列论文中的第二篇，这些论文报告了一系列阴离子药物（双氯芬酸，水杨酸）从液晶凝胶中的释放和运输，并最终报告了它们在透皮给药中的应用。前一篇论文[菲茨帕特里克，D.，Corish，J.，2005.阴离子药物化合物从液晶凝胶中透皮释放特性的研究。第一部分.通过非速率限制膜被动释放。Int. J. Pharm. 301，226-236]研究了通过非速率限制膜的被动释放曲线：在此，我们报道了对用于阴离子化合物的经皮递送的合适的模型增强剂（苄基二甲基十二烷基溴化铵）的研究。所呈现的结果揭示了离子配对和缓冲的重要作用，类似于Nolan，L.M.A.，Corish，J.，科里根，O.I.，菲茨帕特里克博士，2003.离子电渗和化学增强药物输送。第一部分.穿过人造膜。Int. J. Pharm. 12，41-55。还研究了溶媒的制备方法。结果表明，药物与增强剂的离子配对降低了可用于从液晶凝胶运输到水性受体介质中的药物的量。这种降低与药物浓度与增强剂浓度的比率直接相关。缓冲载体在一定程度上抑制离子对的形成。还发现溶剂制备影响离子对缔合的程度。发现将类似电荷的增强剂（油酸）包含到药物中不会阻碍药物从凝胶中扩散。
This is the second in a series of papers that report on the release and transport of a range of anionic drugs (diclofenac, salicylic acid) from liquid crystalline gels and ultimately on their use in transdermal delivery. The previous paper [Fitzpatrick, D., Corish, J., 2005. Release characteristics of anionic drug compounds from liquid crystalline gels for transdermal delivery. Part I. Passive release across non-rate limiting membranes. Int. J. Pharm. 301, 226–236] investigated passive release profiles across a non-rate-limiting membrane: here we report on the search for a suitable model enhancer (benzyl dimethyldodecyl ammonium bromide) for the transdermal delivery of anionic compounds. The results presented reveal a significant role for ion pairing and for buffering, analogous to those found in the investigations of cationic species (salbutamol) by Nolan, L.M.A., Corish, J., Corrigan, O.I., Fitzpatrick, D., 2003. Iontophoretic and chemical enhancement of drug delivery. Part I. Across artificial membranes. Int. J. Pharm. 12, 41–55. The method of vehicle preparation is also investigated. It is shown that ion pairing of the drug with the enhancer decreases the amount of drug available for transport from the liquid crystalline gels into aqueous receptor media. This decrease is directly related to the ratio of the concentration of drug to that of the enhancer. Buffering the vehicle inhibits the ion-pair formation to some extent. Vehicle preparation was also found to influence the degree of ion-pair association. The inclusion of a similarly charged enhancer (oleic acid) to the drug was found not to impede the diffusion of the drug from the gels.