pRED, Pharma Research and Early Development, Pharmaceutical and Analytical R&D, Hoffmann-La Roche, Nutley, New Jersey, USA.
J Pharm Sci. 2013 Mar;102(3):960-6. doi: 10.1002/jps.23424. Epub 2012 Dec 26.
The binding constants (K(b)s) of 17 aryl propionic acid derivatives (APADs) and related compounds with polyvinylpyrrolidone (PVP K30) and vinylpyrrolidone-vinyl acetate copolymer (Kollidon VA64) in aqueous media were determined by affinity capillary electrophoreses (ACE). The K(b)s of APAD to polymers increase with octanol-water partition coefficients of the compounds. Kollidon VA64 is a stronger binder than PVP K30 to APAD compounds. The K(b)s are greater at pH 4 than at pH 9. Both hydrophobic interaction and hydrogen bonding may be involved. However, hydrophobic interaction appears to be dominant. The ACE method is simple and fast, which could be used to study drug-polymer interaction in aqueous media.
采用亲和毛细管电泳法（ACE）测定了 17 种芳基丙酸衍生物（APAD）及其相关化合物与聚乙烯吡咯烷酮（PVP K30）和乙烯基吡咯烷酮-醋酸乙烯酯共聚物（共聚维酮 Kollidon VA64）在水相中的结合常数（K(b)s）。APAD 与聚合物的 K(b)s 随化合物的辛醇-水分配系数增大而增大。共聚维酮 Kollidon VA64 与 APAD 化合物的结合能力强于聚乙烯吡咯烷酮 K30。在 pH 4 时的 K(b)s 大于在 pH 9 时的 K(b)s。氢键和疏水相互作用可能都参与其中，但疏水相互作用似乎占主导地位。ACE 法简单快速，可用于研究水相中的药物-聚合物相互作用。
