离子对和化学增强剂对美洛昔康经皮传递的影响。

Influence of ion-pairing and chemical enhancers on the transdermal delivery of meloxicam.

机构信息

Department of Pharmaceutics, Shenyang Pharmaceutical University and Shenyang, PR China.

出版信息

Drug Dev Ind Pharm. 2009 Jun;35(6):663-70. doi: 10.1080/03639040802578111.

DOI:10.1080/03639040802578111

PMID:19259875

Abstract

PURPOSE

To investigate the influence of ion pairing and chemical enhancers on the transdermal delivery of meloxicam.

METHOD

We examined the increased permeation of meloxicam produced by ion pair formation with six organic bases, diethylamine, triethylamine, ethanolamine, diethanolamine, triethanolamine, and N-(2'-hydroxyethanol)-piperidine, and four normal permeation enhancers, oleic acid, menthol, azone, and N-methyl-2-pyrrolidone. The cumulative permeation was markedly increased in the presence of either a counter ion or chemical enhancers. In particular, we proved the formation of a meloxicam/amine ion-pair in solution by (13)C-NMR (nuclear magnetic resonance).

RESULTS AND CONCLUSION

The cumulative permeation was markedly increased in the presence of either a counter ion or chemical enhancers. These results suggest that the degree of enhancement possibly depends on the structure and hydrophilicity of the counter ions.

摘要

目的

研究离子对和化学增溶剂对美洛昔康经皮传递的影响。

方法

我们考察了与 6 种有机碱（二乙胺、三乙胺、乙醇胺、二乙醇胺、三乙醇胺和 N-（2'-羟乙基）-哌啶）以及 4 种普通渗透促进剂（油酸、薄荷醇、氮酮和 N-甲基-2-吡咯烷酮）形成离子对后美洛昔康渗透的增加情况。在存在反离子或化学增溶剂的情况下，累积渗透明显增加。特别是，我们通过（13）C-NMR（核磁共振）证明了溶液中美洛昔康/胺离子对的形成。