Effect of penetration enhancers on flurbiprofen permeation through rat skin

被引:45
作者
Chi, SC
Park, ES
Kim, H
机构
[1] College of Pharmacy, Sung Kyun Kwan University, Suwon
关键词
flurbiprofen; skin permeation; fatty acids; urea; pharmacokinetics;
D O I
10.1016/0378-5173(95)04137-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
To increase the skin permeation rate of flurbiprofen, fatty acids and urea were added in propylene glycol vehicle containing 1% flurbiprofen. The enhancing effects of these compounds on the skin permeation of flurbiprofen were evaluated using Keshary-Chien diffusion cells fitted with excised rat skins. Unsaturated fatty acids increased the skin permeation rate of flurbiprofen 6.5-17.5 fold compared to the control vehicle without enhancer, while saturated fatty acids did not show any significant increase. Although the addition of urea in the vehicle decreased the skin permeation rate of flurbiprofen, the mixture of oleic acid and urea showed a significantly higher permeation rate than oleic acid alone. It was coincident with the results obtained with the plasma concentrations of flurbiprofen determined after the transdermal application of propylene glycol vehicle containing them. AUC and C-max of the vehicle containing the mixture were increased 2.3 and 2.5 fold, respectively, whereas each parameter of the vehicle containing oleic acid only was increased 1.7 fold compared to those of the control vehicle.
引用
收藏
页码:267 / 274
页数:8
相关论文
共 28 条
[1]   ABSORPTION THROUGH HUMAN-SKIN OF IBUPROFEN AND FLURBIPROFEN - EFFECT OF DOSE VARIATION, DEPOSITED DRUG FILMS, OCCLUSION AND THE PENETRATION ENHANCER N-METHYL-2-PYRROLIDONE [J].
AKHTER, SA ;
BARRY, BW .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1985, 37 (01) :27-37
[2]   ENHANCEMENT OF NALOXONE PENETRATION THROUGH HUMAN-SKIN INVITRO USING FATTY-ACIDS, FATTY ALCOHOLS, SURFACTANTS, SULFOXIDES AND AMIDES [J].
AUNGST, BJ ;
ROGERS, NJ ;
SHEFTER, E .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1986, 33 (1-3) :225-234
[3]  
BARRY B W, 1987, Journal of Controlled Release, V6, P85, DOI 10.1016/0168-3659(87)90066-6
[4]  
Barry B.W., 1983, DERMATOLOGICAL FORMU, P49
[5]   THE INFLUENCE OF UREA ON PERCUTANEOUS-ABSORPTION [J].
BEASTALL, J ;
GUY, RH ;
HADGRAFT, J ;
WILDING, I .
PHARMACEUTICAL RESEARCH, 1986, 3 (05) :294-297
[6]   FLURBIPROFEN - REVIEW OF ITS PHARMACOLOGICAL PROPERTIES AND THERAPEUTIC USE IN RHEUMATIC DISEASES [J].
BROGDEN, RN ;
HEEL, RC ;
SPEIGHT, TM ;
AVERY, GS .
DRUGS, 1979, 18 (06) :417-438
[7]  
Buyuktimkin Nadir, 1993, Pharmaceutical Research (New York), V10, pS241
[8]   HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC ANALYSIS OF FLURBIPROFEN IN RAT PLASMA [J].
CHI, SC ;
KIM, H ;
LEE, SC .
ANALYTICAL LETTERS, 1994, 27 (02) :377-389
[9]   EFFECT OF FATTY-ACIDS AND ALCOHOLS ON THE PENETRATION OF ACYCLOVIR ACROSS HUMAN-SKIN INVITRO [J].
COOPER, ER ;
MERRITT, EW ;
SMITH, RL .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1985, 74 (06) :688-689
[10]   INCREASED SKIN PERMEABILITY FOR LIPOPHILIC MOLECULES [J].
COOPER, ER .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1984, 73 (08) :1153-1156