Cheng S W, Shanker R, Lindenbaum S
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence 66045.
Pharm Res. 1990 Aug;7(8):856-62. doi: 10.1023/a:1015969017395.
The distribution of chlorpromazine (CPZ) between aqueous buffer solutions and 1-octanol was studied over a wide range of pH, buffer concentration, and temperature. A mathematical model was developed to simulate the distribution profiles. It is assumed that only monomers of CPZ exist in the organic phase, whereas in the aqueous phase, association equilibria were assumed to occur. The model predicted the formation of dimers and no higher aggregates over most of the concentration range covered in this study. Thermodynamic parameters for the partition equilibria were evaluated from the equilibrium partition coefficients measured as a function of temperature. Positive values of delta H and delta S were obtained for the transfer of CPZ from the aqueous to the organic phase. The process is entropy controlled indicative of a hydrophobic interaction between CPZ and the aqueous solvent.
在较宽的pH值、缓冲液浓度和温度范围内，研究了氯丙嗪（CPZ）在水性缓冲溶液和1-辛醇之间的分配情况。建立了一个数学模型来模拟分配曲线。假设在有机相中仅存在CPZ单体，而在水相中，假定发生缔合平衡。该模型预测在本研究涵盖的大部分浓度范围内会形成二聚体，且不会形成更高的聚集体。根据作为温度函数测量的平衡分配系数评估分配平衡的热力学参数。CPZ从水相转移到有机相时获得了正值的ΔH和ΔS。该过程由熵控制，表明CPZ与水性溶剂之间存在疏水相互作用。
