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


METHODS
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).


CONCLUSIONS
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.
Zhang
Jing-Ying
JY
Department of Pharmaceutics, Shenyang Pharmaceutical University and Shenyang, PR China.
Fang
Liang
L
Tan
Zhe
Z
Wu
Jian
J
He
Zhong-Gui
ZG
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005079:Excipients / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D000077239:Meloxicam; D010539:Permeability; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption; D013843:Thiazines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013844:Thiazoles / Q000008:administration & dosage / Q000493:pharmacokinetics*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D013843:Thiazines; D013844:Thiazoles; D000077239:Meloxicam