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

来源：

JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY | 2010年 / 101卷 / 02期

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

页码：555 / 560

页数：6

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