IN-VIVO EVALUATION OF INDOMETHACIN/CYCLODEXTRIN COMPLEXES - GASTROINTESTINAL TOLERANCE AND DERMAL ANTIINFLAMMATORY ACTIVITY

被引:40
作者
LIN, SZ
WOUESSIDJEWE, D
POELMAN, MC
DUCHENE, D
机构
[1] UNIV PARIS 11,FAC PHARM,PHYSICOCHIM PHARMACOTECH BIOPHARMAC LAB,CNRS,URA 1218,F-92290 CHATENAY MALABRY,FRANCE
[2] UNIV PARIS 05,FAC PHARM,DEPT DERMOPHARM,F-75006 PARIS,FRANCE
关键词
INDOMETHACIN; BETA-CYCLODEXTRIN; HYDROXYPROPYL-BETA-CYCLODEXTRIN; INCLUSION; GASTROINTESTINAL TOLERANCE; ANTIINFLAMMATORY ACTIVITY; DERMAL ROUTE;
D O I
10.1016/0378-5173(94)90276-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Inclusion complexes of indomethacin in beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin were prepared and evaluated in vivo. With respect to the gastrointestinal tolerance assessed in the rat, it appears that the inclusion of indomethacin in these cyclodextrins results in a decrease in its irritation power, confirming that this undesirable effect has at least a local origin. With respect to the dermal anti-inflammatory activity assessed on healthy volunteers by the methyl nicotinate test, the results seem to demonstrate that inclusions in either of the cyclodextrins investigated have a higher activity than free indomethacin.
引用
收藏
页码:63 / 67
页数:5
相关论文
共 12 条
[1]  
AMMOURY N, 1990, THESIS U PARIS SUD
[2]   EFFECT OF CYCLODEXTRIN DERIVATIVES ON INDOMETHACIN STABILITY IN AQUEOUS-SOLUTION [J].
BACKENSFELD, T ;
MULLER, BW ;
WIESE, M ;
SEYDEL, JK .
PHARMACEUTICAL RESEARCH, 1990, 7 (05) :484-490
[3]  
BIANCHI PG, 1987, ALIMENT PHARM THERAP, V1, P5405
[4]  
DJAHANGUIRI B, 1969, SCAND J GASTROENTERO, V4, P265
[5]  
HAMADA Y, 1975, CHEM PHARM BULL, V23, P1205
[6]   INDOMETHACIN AND CYCLODEXTRIN COMPLEXES [J].
LIN, SZ ;
WOUESSIDJEWE, D ;
POELMAN, MC ;
DUCHENE, D .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1991, 69 (03) :211-219
[7]  
LIN SZ, 1993, THESIS U PARIS SUD
[8]  
LIN SZ, 1992, 6TH INT S CYCL CHIC, P522
[9]  
MULLER BW, 1990, PHARMACEUT RES, V7, pS107
[10]   ASSESSMENT OF TOPICAL NON-STEROIDAL ANTI-INFLAMMATORY DRUGS [J].
POELMAN, MC ;
PIOT, B ;
GUYON, F ;
DERONI, M ;
LEVEQUE, JL .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1989, 41 (10) :720-722