Meyer J D, Manning M C
Center for Pharmaceutical Biotechnology, School of Pharmacy, University of Colorado Health Sciences Center, Denver 80262, USA.
Pharm Res. 1998 Feb;15(2):188-93. doi: 10.1023/a:1011998014474.
The high aqueous solubility of ionic compounds can be attributed to the ease of solvation of the counter ions. Replacement of the counter ions with ionic detergents dramatically alters the solubility properties of the molecule. Not only does the aqueous solubility drop precipitously, but the solubility in organic phases increases as well. Consequently, the partition coefficient changes by orders of magnitude. This ion pairing phenomenon, which we term hydrophobic ion pairing (HIP), has been extended to polyelectrolytes, such as proteins and polynucleotides. These materials form HIP complexes that dissolve in a range of organic solvents, often with retention of native structure and enzymatic activity. The HIP process has been used to purify protein mixtures, conduct enzymatic reactions in nonaqueous environments, increase structural stability, enhance bioavailability, and prepare new dosage forms.
离子化合物的高水溶性可归因于抗衡离子易于溶剂化。用离子型去污剂取代抗衡离子会显著改变分子的溶解性。不仅水溶性急剧下降，而且在有机相中的溶解度也会增加。因此，分配系数会发生几个数量级的变化。这种离子对现象，我们称之为疏水离子对（HIP），已扩展到聚电解质，如蛋白质和多核苷酸。这些物质形成可溶解在一系列有机溶剂中的HIP复合物，通常保留天然结构和酶活性。HIP过程已用于纯化蛋白质混合物、在非水环境中进行酶促反应、提高结构稳定性、增强生物利用度以及制备新剂型。
