Effect of Cyclodextrin Derivatives on Indomethacin Stability in Aqueous Solution View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1990-05

AUTHORS

Thomas Backensfeld, Bernd W. Müller, Michael Wiese, Joachim K. Seydel

ABSTRACT

The effect of various cyclodextrins (CD) and cyclodextrin derivatives on indomethacin stability in phosphate buffer, pH 7.4, was investigated. The influence of CD-ring size, type of substituent, degree of substitution, substitution pattern, and influence of CD concentration were monitored. The indomethacin complex in solution was studied by 1H-NMR spectroscopy to develop a molecular inclusion model. The most favorable ring size for the stabilization of indomethacin was the beta-CD. The beta-CD derivatives inhibited the hydrolysis of indomethacin more effectively than the parent CD. Among the studied CD derivatives, those with lipophilic substituents, such as ethyl or methyl, were superior to those with hydrophilic substitutents. The more hydroxyl groups of the glucose moiety are substituted, the better is the stabilizing effect. Further, the p-chlorobenzoic part of the indomethacin molecule is included in the CD channel. More... »

PAGES

484-490

Identifiers

URI

http://scigraph.springernature.com/pub.10.1023/a:1015860531565

DOI

http://dx.doi.org/10.1023/a:1015860531565

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1012490579

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/2367316


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