EXTRACTION COEFFICIENTS AND FACILITATED TRANSPORT - THE EFFECT OF ABSORPTION ENHANCERS

被引:4
作者
IRWIN, WJ
SMITH, JC
机构
[1] Drug Development Research Group, Pharmaceutical Sciences Institute, Aston University, Birmingham, B4 7ET, Aston Triangle
关键词
AZONE; ENHANCER; EXTRACTION COEFFICIENT; FACILITATED TRANSPORT; PERCUTANEOUS ABSORPTION; PARTITIONING; SALICYLIC ACID; PH;
D O I
10.1016/0378-5173(91)90353-P
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A theoretical model of the extraction coefficients of weak acids has been developed to account for the variation in partition dependent upon pK(a) using the partition coefficients of the ionised and unionised species (P(i), P(u)). The effect of these variables on the plots of both the extraction ratios and the relative changes, as indicated by the ratio of these coefficients, is illustrated. The model has been applied to the distribution of salicylic acid, as a function of pH, between an aqueous phase and isopropyl myristate containing tertiary amide enhancers of percutaneous absorption. The extraction coefficients determined are consistent with the model and show that ion-pairing between the ion and enhancer need not be invoked to explain the behaviour of the system.
引用
收藏
页码:151 / 159
页数:9
相关论文
共 24 条
[1]   STUDIES ON BASE STRENGTHS OF N,N-DISUBSTITUTED AMIDES [J].
ADELMAN, RL .
JOURNAL OF ORGANIC CHEMISTRY, 1964, 29 (07) :1837-&
[2]  
Albert A., 1984, DETERMINATION IONISA
[3]   INTERFACIAL TRANSFER STUDIED WITH A ROTATING DIFFUSION CELL [J].
ALBERY, WJ ;
BURKE, JF ;
LEFFLER, EB ;
HADGRAFT, J .
JOURNAL OF THE CHEMICAL SOCIETY-FARADAY TRANSACTIONS I, 1976, 72 :1618-1626
[4]   FACILITATED PERCUTANEOUS-ABSORPTION - A MODEL SYSTEM [J].
BARKER, N ;
HADGRAFT, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1981, 8 (03) :193-202
[5]  
BARKER N, 1984, J CHEM SOC CHEM COMM, V77, P97
[6]  
Barry, 1983, DERMATOLOGICAL FORMU
[7]   PREPARATION OF BUFFER SYSTEMS OF CONSTANT IONIC STRENGTH [J].
ELVING, PJ ;
MARKOWITZ, JM ;
ROSENTHAL, I .
ANALYTICAL CHEMISTRY, 1956, 28 (07) :1179-1180
[8]   ESTIMATION OF DIFFUSION-COEFFICIENTS USING THE ROTATING DIFFUSION CELL [J].
GUY, RH ;
FLEMING, R .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1979, 3 (2-3) :143-149
[9]   FACILITATED TRANSPORT OF SODIUM-SALICYLATE ACROSS AN ARTIFICIAL LIPID-MEMBRANE BY AZONE [J].
HADGRAFT, J ;
WALTERS, KA ;
WOTTON, PK .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1985, 37 (10) :725-727
[10]  
Hadgraft J., 1989, DRUGS PHARM SCI, V35