Enhancement of aqueous solubility of tricyclic acyclovir derivatives by their complexation with hydroxypropyl-β-cyclodextrin

被引:20
|
作者
Zielenkiewicz, Wojciech [1 ]
Kozbial, Malgorzata [1 ]
Golankiewicz, Bozenna [2 ]
Poznanski, Jaroslaw [1 ]
机构
[1] Polish Acad Sci, Inst Phys Chem, PL-01224 Warsaw, Poland
[2] Polish Acad Sci, Inst Bioorgan Chem, PL-61704 Poznan, Poland
关键词
Acyclovir derivatives; Hydroxypropyl-beta-cyclodextrin; Solubility enhancement; ANTIVIRAL ACTIVITY; ANALOGS;
D O I
10.1007/s10973-010-0847-0
中图分类号
O414.1 [热力学];
学科分类号
摘要
Solubilities of tricyclic acyclovir derivatives in buffered aqueous solutions of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) at pH 5.5 and 7.0 were determined at 25 and 37 A degrees C. Complexation of these compounds with HP-beta-CD resulted in a noticeable increase of their solubility; nevertheless it was limited to tricyclic derivatives of acyclovir carrying an aryl substituent. Combination of H-1 NMR and DSC techniques demonstrated the existence of inclusion complexes between acyclovir derivatives and HP-beta-CD. The stability constants, estimated using the Higuchi-Connors method, were found in the range of 10-100 M-1. Additionally, the pK (a) values at 25 A degrees C and molar extinction coefficients in aqueous buffered solutions were also determined for all studied compounds.
引用
收藏
页码:555 / 560
页数:6
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