Influence of sodium lauryl sulphate on the in vitro percutaneous absorption of compounds with different lipophilicity

被引:31
作者
BorrasBlasco, J [1 ]
Lopez, A [1 ]
Morant, MJ [1 ]
DiezSales, O [1 ]
HerraezDominguez, M [1 ]
机构
[1] UNIV VALENCIA,FAC FARM,DEPT PHARM & PHARMACEUT TECHNOL,E-46010 VALENCIA,SPAIN
关键词
percutaneous absorption; sodium lauryl sulphate; lipophilicity; enhancement;
D O I
10.1016/S0928-0987(96)00184-4
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effects of sodium lauryl sulphate (SLS) at different concentrations on the ''in vitro'' percutaneous absorption of a number of compounds (5-fluorouracil, antipyrine, pentoxifylline, salicylamide, 4-ethylaniline, 4-n-butylaniline and indomethacin) with a wide range of lipophilicity values (log P-OCT from -0.95 to 4.42) through rat skin were analysed. After pretreatment of the skin with SLS (1% and 5%, w/w) the permeability coefficients increased only for compounds having a log P-OCT < 3 (5-fluorouracil, antipyrine, pentoxifylline, salicylamide and 4-ethylaniline). The enhancement ratios show that the greater the enhancer effect observed, the lower the lipophilicity value of the penetrant. An empirical hyperbolic equation between enhancement ratios and partitioning values was established. This equation makes it possible to determine the enhancement ratio for a compound with a known P-OCT when the membrane has been pretreated with SLS (1%, w/w). In conclusion, the effect of SLS as an enhancer depends on the lipophilicity value of the penetrant and seems similar in this aspect to other enhancers such as Laurocapram.
引用
收藏
页码:15 / 22
页数:8
相关论文
共 32 条
[1]  
Akaike H., 1976, MATH SCI, V14, P5
[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]  
Babhair S. A., 1984, ANAL PROFILES DRUG S, V13, P521
[4]  
BLAKEHASKINS JC, 1986, J SOC COSMET CHEM, V37, P199
[5]   EFFECT OF N-ALKYL-AZOCYCLOHEPTAN-2-ONES INCLUDING AZONE ON THE THERMAL-BEHAVIOR OF HUMAN STRATUM-CORNEUM [J].
BOUWSTRA, JA ;
PESCHIER, LJC ;
BRUSSEE, J ;
BODDE, HE .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 52 (01) :47-54
[6]   EFFECT OF SURFACTANTS ON PERCUTANEOUS ABSORPTION OF NAPROXEN .1. COMPARISONS OF RABBIT, RAT, AND HUMAN EXCISED SKIN [J].
CHOWHAN, ZT ;
PRITCHARD, R .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1978, 67 (09) :1272-1274
[7]   A mechanistic investigation of the in vitro human skin permeation enhancing effect of Atone(R) [J].
DiezSales, O ;
Watkinson, AC ;
HerraezDominguez, M ;
Javaloyes, C ;
Hadgraft, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1996, 129 (1-2) :33-40
[8]   A MODELISTIC APPROACH SHOWING THE IMPORTANCE OF THE STAGNANT AQUEOUS LAYERS IN INVITRO DIFFUSION STUDIES, AND INVITRO-INVIVO CORRELATIONS [J].
DIEZSALES, O ;
COPOVI, A ;
CASABO, VG ;
HERRAEZ, M .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1991, 77 (01) :1-11
[9]  
DIEZSALES O, 1993, PREDICTION PERCUTANE, V3, P68
[10]  
DIEZSALES O, 1991, EUR J DRUG METAB PH, V16, P441