PARTITIONING AND THERMODYNAMICS OF DIPYRIDAMOLE IN THE N-OCTANOL BUFFER AND LIPOSOME SYSTEMS

被引:27
作者
BETAGERI, GV
DIPALI, SR
机构
[1] Department of Pharmacol Sciences, School of Pharmacy, Auburn University, Auburn, Alabama
关键词
D O I
10.1111/j.2042-7158.1993.tb05627.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The thermodynamics of partitioning (K) of dipyridamole has been determined in n-octanol/buffer and liposome-buffer systems at pH 7.4. Dimyristoylphosphatidylcholine (DMPC) and dipalmitoylphosphatidylcholine (DPPC) were used to prepare multilamellar liposomes. Partitioning of dipyridamole did not depend on the amount of n-octanol employed, however, partitioning was dependent upon the quantity, of DMPC employed to prepare liposomes. Plots of log K vs 1/T were linear in the n-octanol and liposome systems. Partitioning was generally greater in liposomes than In the n-octanol/buffer system. Among liposomes, the partitioning was greater in DMPC liposomes at all temperatures. The values of enthalpy (AH) and entropy (AS) were positive in both the n-octanol and liposome systems. These values were lower in DMPC liposomes and were comparable in the n-octanol and DPPC liposomes. Thus, the interaction of dipyridamole depends on the rigidity of lipid bilayers and liposomes constitute a more selective partitioning system than the n-octanol/buffer system.
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收藏
页码:931 / 933
页数:3
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