Capsaicin and nonivamide as novel skin permeation enhancers for indomethacin

被引：38
作者：
Fang, JY
Fang, CL
Hong, CT
Chen, HY
Lin, TY
Wei, HM
机构：
[1] Taipei Med Coll, Grad Inst Pharmaceut Sci, Taipei, Taiwan
[2] Taipei Municipal Wan Fang Hosp, Res Ctr Clin Pharm, Taipei, Taiwan
[3] Taipei Med Coll, Dept Pathol, Taipei, Taiwan
[4] Taipei Municipal Wan Fang Hosp, Dept Neurol, Taipei, Taiwan
来源：
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2001年 / 12卷 / 03期
关键词：
indomethacin; capsaicin; nonivamide; skin permeation; enhancer; ultrasound;
D O I：
10.1016/S0928-0987(00)00118-4
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The study was conducted in vitro to investigate the changes of indomethacin transdermal permeation pretreated by capsaicin and nonivamide, two compounds chemically similar to Atone. The combined effect of low frequency ultrasound (20 kHz) and enhancers on the indomethacin permeation was also evaluated. The experimental data demonstrated that capsaicin and nonivamide significantly enhanced the flux of indomethacin across nude mouse skin. Enhancement effects of both analogues were very similar and depended predominantly on the concentration tested. Histological examination coupled with visual scores indicated the safety of capsaicin and nonivamide on skin structure. Simultaneous application of ultrasound and enhancers significantly increased skin permeation of indomethacin compared with either ultrasound or enhancers alone. Better effect was obtained by the combination with capsaicin than nonivamide. (C) 2001 Elsevier Science B.V. All rights reserved.
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收藏
页码：195 / 203
页数：9
相关论文
共 29 条
[1]   HYPOTENSIVE AND ANTINOCICEPTIVE EFFECTS OF ETHER-LINKED AND RELATIVELY NON-PUNGENT ANALOGS OF N-NONANOYL VANILLYLAMIDE [J].
CHEN, IJ ;
YANG, JM ;
YEH, JL ;
WU, BN ;
LO, YC ;
CHEN, SJ .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1992, 27 (03) :187-192
[2]   EFFECT OF TOPICAL APPLICATION WITH CAPSAICIN ON SKIN-RESPONSES TO BRADYKININ AND HISTAMINE IN MAN [J].
CRIMI, N ;
POLOSA, R ;
MACCARRONE, C ;
PALERMO, B ;
PALERMO, F ;
MISTRETTA, A .
CLINICAL AND EXPERIMENTAL ALLERGY, 1992, 22 (10) :933-939
[3]   HEAT AND MECHANICAL HYPERALGESIA INDUCED BY CAPSAICIN - CROSS MODALITY THRESHOLD MODULATION IN HUMAN C-NOCICEPTORS [J].
CULP, WJ ;
OCHOA, J ;
CLINE, M ;
DOTSON, R .
BRAIN, 1989, 112 :1317-1331
[4]   The effects of Azone and capsaicin on the permeation of naproxen through human skin [J].
Degim, IT ;
Uslu, A ;
Hadgraft, J ;
Atay, T ;
Akay, C ;
Cevheroglu, S .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1999, 179 (01) :21-25
[5]   In vitro permeation study of capsaicin and its synthetic derivatives from ointment bases using various skin types [J].
Fang, JY ;
Wu, PC ;
Huang, YB ;
Tsai, YH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1995, 126 (1-2) :119-128
[6]   In vivo percutaneous absorption of capsaicin, nonivamide and sodium nonivamide acetate from ointment bases: Skin erythema test and non-invasive surface recovery technique in humans [J].
Fang, JY ;
Wu, PC ;
Huang, YB ;
Tsai, YH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1996, 131 (02) :143-151
[7]   In vivo percutaneous absorption of capsaicin, nonivamide and sodium nonivamide acetate from ointment bases: Pharmacokinetic analysis in rabbits [J].
Fang, JY ;
Wu, PC ;
Huang, YB ;
Tsai, YH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1996, 128 (1-2) :169-177
[8]  
Fang JY, 1997, DRUG DEVELOP RES, V40, P56, DOI 10.1002/(SICI)1098-2299(199701)40:1<56::AID-DDR6>3.0.CO
[9]  
2-S
[10]   Effect of low frequency ultrasound on the in vitro percutaneous absorption of clobetasol 17-propionate [J].
Fang, JY ;
Fang, CL ;
Sung, KC ;
Chen, HY .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1999, 191 (01) :33-42
123