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Abstract

Evaluation Of Stereoselective Dissolution Of Racemic Ketoprofen From Formulations Containing Chiral Excipients

Author(s): K Valliappan, K Kannan, R Manavalan, C Muralidharan

The dissolution characteristics of ketoprofen enantiomers from matrices containing chiral excipients sodium alginate, β-cyclodextrin and hydroxypropylmethylcellulose under three different pH values (pH 1.5,4.6 and 7.4) in aqueous environment were determined. An achiral excipient, Eudragit RL 100, was used to generate a control dissolution profile. This study demonstrates that release of ketoprofen enantiomers from formulation containing hydroxypropylmethylcellulose matrix at pH 7.4 is stereoselective and statistically significant. It is observed that the release of S-ketoprofen (eutomer) was faster than the R-ketoprofen (distomer). Further, it indicates that the differential release is pH-dependent. The research implication is that by choosing the appropriate chiral excipient and other formulation conditions one can deliberately manipulate the release of a specific enantiomer from a racemic therapeutic. This intended stereospecific retardation/acceleration in the release of enantiomers could be exploited for the design of stereoselective drug delivery systems.

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