EFFECT OF D-LIMONENE ON THE TRANSDERMAL PERMEATION OF NIFEDIPINE AND DOMPERIDONE

被引:24
作者
CALPENA, AC [1 ]
LAUROBA, J [1 ]
SURIOL, M [1 ]
OBACH, R [1 ]
DOMENECH, J [1 ]
机构
[1] UNIV BARCELONA,SCH PHARM,PHARMACOKINET & BIOPHARMACEUT LAB,BARCELONA,SPAIN
关键词
DOMPERIDONE; NIFEDIPINE; TRANSDERMAL PENETRATION; RAT SKIN; HUMAN SKIN; ENHANCER; D-LIMONENE;
D O I
10.1016/0378-5173(94)90098-1
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
The aim of this research is to study the profile of transdermal permeation of nifedipine and domperidone. Permeation studies were carried out using the skin of hairless rat and human skin as a membrane mounted in a permeation system in vitro. The influence of the type of skin used and the presence of d-limonene on the transdermal penetration of these drugs were studied. The drugs studied permeate approx. 3 times faster through rat skin than through human skin. The type of skin has no influence on the lag time. d-limonene increases the values of the permeability constant (K-p), flux (J) and lag time (T-l) for both drugs, but not the lag time for domperidone when human skin is used. The effect of the enhancer on the enhancement index (EI) of domperidone varies with the type of skin used (EI = 15.7 (rat skin) and EI = 7.7 (human skin)). When human skin is used, although penetration is increased by d-limonene, the concentration Values predicted at steady state are below therapeutic levels for both studied drugs.
引用
收藏
页码:179 / 186
页数:8
相关论文
共 18 条
[1]
BERBA J, 1990, AM PHARM, V11, P33
[2]
BLANES C, 1990, EUR J DRUG METAB PH, P410
[3]
CLEARLY GW, 1984, MED APPLICATIONS CON, P212
[4]
A COMPARATIVE INVITRO STUDY OF TRANSDERMAL ABSORPTION OF A SERIES OF CALCIUM-CHANNEL ANTAGONISTS [J].
DIEZ, I ;
COLOM, H ;
MORENO, J ;
OBACH, R ;
PERAIRE, C ;
DOMENECH, J .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1991, 80 (10) :931-934
[5]
ESTER RC, 1992, CLIN PHARMAOCKINET, V23, P235
[6]
THERMODYNAMIC STUDY ON ENHANCEMENT OF PERCUTANEOUS PENETRATION OF DRUGS BY AZONE [J].
ITO, Y ;
OGISO, T ;
IWAKI, M .
JOURNAL OF PHARMACOBIO-DYNAMICS, 1988, 11 (11) :749-757
[7]
EFFICACY OF CLONIDINE AS TRANSDERMAL THERAPEUTIC SYSTEM - THE INTERNATIONAL CLINICAL-TRIAL EXPERIENCE [J].
LOWENTHAL, DT ;
SARIS, S ;
PARAN, E ;
CRISTAL, N ;
SHARIF, K ;
BIES, C ;
FAGAN, T .
AMERICAN HEART JOURNAL, 1986, 112 (04) :893-900
[8]
OKAMOTO H, 1986, INT J PHARM, V30, P35, DOI 10.1016/0378-5173(86)90133-X
[9]
SCHMITT LG, 1986, ARCH OTOLARYNGOL, V112, P88
[10]
TESTING OF CONTROLLED-RELEASE TRANSDERMAL DOSAGE FORMS - PRODUCT DEVELOPMENT AND CLINICAL-TRIALS [J].
SHAW, JE ;
PREVO, ME ;
AMKRAUT, AA .
ARCHIVES OF DERMATOLOGY, 1987, 123 (11) :1548-1556