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β-环糊精衍生物增溶药物分子能显著提高药物的理化性质,可解决药物制作中遇到的诸多困难,为药物新制剂,新剂型的发展提供了有效手段。荧光光谱能够表征分子之间的相互作用,同时能够在较大范围内检测药物分子的浓度。测定了普拉洛芬(PRA)在甲基-β-环糊精(Me-beta-CD)溶液中的荧光光谱及相溶解度图,结果表明甲基-β-环糊精与普拉洛芬形成1∶1包络物,包络物属于AL型。包络平衡常数为2.0665l/mol,且在45mmol/L的甲基-β-环糊精溶液中,普拉洛芬的溶解度增加42倍,达到2.22mg/mL。同时计算机模拟表明,普拉洛芬的芳环端是由大口倾斜进入Me-beta-CD的空腔,包络作用以范德华力为主,分子间没有明显的氢键作用。
β-Cyclodextrin derivatives solubilizing drug molecules can significantly improve the physical and chemical properties of the drug, which can solve many difficulties encountered in drug production and provide an effective means for the development of new drugs and new dosage forms. Fluorescence spectroscopy can characterize the interaction between molecules and at the same time detect the concentration of drug molecules in a wide range. The fluorescence spectra and phase solubility of pranoprofen (PRA) in methyl-β-cyclodextrin (Me-beta-CD) solution were measured and the results showed that methyl-β-cyclodextrin and pranoprofen The formation of 1: 1 envelope, the envelope belongs to the AL type. The equilibrium constant of the envelop was 2.0665l / mol, and the solubility of pranoprofen increased 42-fold to 2.22mg / mL in the 45mmol / L methyl-β-cyclodextrin solution. At the same time, computer simulation shows that the aromatic ring end of pranoprofen is inclined into the cavity of Me-beta-CD by the largemouth mouth, and the enveloping effect is dominated by van der Waals forces. There is no obvious hydrogen bonding between molecules.