PREDICTION OF SKIN PERMEABILITY OF DRUGS - COMPARISON OF HUMAN AND HAIRLESS RAT SKIN

被引:117
作者
MORIMOTO, Y
HATANAKA, T
SUGIBAYASHI, K
OMIYA, H
机构
[1] JOSAI UNIV,LIFE SCI RES CTR,SAKADO,SAITAMA 35002,JAPAN
[2] KITASATO UNIV,SCH MED,DEPT SURG,SAGAMIHARA,KANAGAWA 228,JAPAN
关键词
D O I
10.1111/j.2042-7158.1992.tb05484.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Relationships between skin permeability and physicochemical properties of drugs were examined to establish a predictive method for the steady-state permeation rate of drugs through human skin. Human skin permeation properties fell into two categories: one in which the permeability coefficient is correlated to the partition coefficient, revealed with lipophilic drugs. and the other in which the permeability coefficients are almost constant. shown with hydrophilic drugs. The stratum corneum, the main barrier in skin, could be considered as a membrane with two parallel permeation pathways: lipid and pore pathways. and an equation for predicting the steady-state permeation rate of drugs was derived. The skin permeabilities of drugs for man were compared with those for hairless rat. The species difference in skin permeability found was suggested to be due to the difference in skin permeation pathways, since lipid content and water uptake of the stratum corneum varied between human and hairless rat skin.
引用
收藏
页码:634 / 639
页数:6
相关论文
共 25 条
[1]  
Adeyeye CM, 1990, ANAL PROFILES DRUG S, V19, P123, DOI DOI 10.1016/S0099-5428(08)60366-4
[2]  
Baker R., 1987, CONTROLLED RELEASE B
[3]   SKIN PERMEABILITY IN-VIVO - COMPARISON IN RAT, RABBIT, PIG AND MAN [J].
BARTEK, MJ ;
LABUDDE, JA ;
MAIBACH, HI .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1972, 58 (03) :114-&
[4]   CUTANEOUS BARRIERS [J].
BLANK, IH .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1965, 45 (04) :249-&
[5]   METHODS FOR INVITRO PERCUTANEOUS-ABSORPTION STUDIES .2. ANIMAL-MODELS FOR HUMAN-SKIN [J].
BRONAUGH, RL ;
STEWART, RF ;
CONGDON, ER .
TOXICOLOGY AND APPLIED PHARMACOLOGY, 1982, 62 (03) :481-488
[6]   METHODS FOR INVITRO PERCUTANEOUS-ABSORPTION STUDIES .3. HYDROPHOBIC COMPOUNDS [J].
BRONAUGH, RL ;
STEWART, RF .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1984, 73 (09) :1255-1258
[7]   THE EFFECTS OF PH AND CHEMICAL ENHANCERS ON THE PERCUTANEOUS-ABSORPTION OF INDOMETHACIN [J].
CHIANG, CH ;
LAI, JS ;
YANG, KH .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1991, 17 (01) :91-111
[8]   PERMEATION OF HAIRLESS MOUSE SKIN .1. EXPERIMENTAL METHODS AND COMPARISON WITH HUMAN EPIDERMAL PERMEATION BY ALKANOLS [J].
DURRHEIM, H ;
FLYNN, GL ;
HIGUCHI, WI ;
BEHL, CR .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1980, 69 (07) :781-786
[9]   PERMEATION OF HAIRLESS MOUSE SKIN .2. MEMBRANE SECTIONING TECHNIQUES AND INFLUENCE ON ALKANOL PERMEABILITIES [J].
FLYNN, GL ;
DURRHEIM, H ;
HIGUCHI, WI .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1981, 70 (01) :52-56
[10]   PREDICTION OF SKIN PERMEABILITY OF DRUGS .1. COMPARISON WITH ARTIFICIAL MEMBRANE [J].
HATANAKA, T ;
INUMA, M ;
SUGIBAYASHI, K ;
MORIMOTO, Y .
CHEMICAL & PHARMACEUTICAL BULLETIN, 1990, 38 (12) :3452-3459