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

Solubilities of tricyclic acyclovir derivatives in buffered aqueous solutions of hydroxypropyl- Delta *b-cyclodextrin (HP- Delta *b-CD) at pH 5.5 and 7.0 were determined at 25 and 37 ?C. Complexation of these compounds with HP- Delta *b-CD resulted in a noticeable increase of their solubility; never...

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Published inJournal of thermal analysis and calorimetry Vol. 101; no. 2; pp. 555 - 560
Main Authors Zielenkiewicz, Wojciech, Kozbial, Malgorzata, Golankiewicz, Bozenna, Poznanski, Jaroslaw
Format Journal Article
LanguageEnglish
Published 01.08.2010
Subjects
Aqueous solutions
Buffers
Calorimetry
Complexation
Derivatives
Differential scanning calorimetry
Extinction
Solubility
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Summary:Solubilities of tricyclic acyclovir derivatives in buffered aqueous solutions of hydroxypropyl- Delta *b-cyclodextrin (HP- Delta *b-CD) at pH 5.5 and 7.0 were determined at 25 and 37 ?C. Complexation of these compounds with HP- Delta *b-CD resulted in a noticeable increase of their solubility; nevertheless it was limited to tricyclic derivatives of acyclovir carrying an aryl substituent. Combination of 1H NMR and DSC techniques demonstrated the existence of inclusion complexes between acyclovir derivatives and HP- Delta *b-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 ?C and molar extinction coefficients in aqueous buffered solutions were also determined for all studied compounds.
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ISSN:1388-6150
DOI:10.1007/s10973-010-0847-0