Title: Evaluation of Hydroxyethyl Esters of Mefenamic Acid and Diclofenac as Prodrugs
Abstract: Hydroxyethyl esters of diclofenac and mefenamic acid were prepared with the aim of obtaining enzymatically labile prodrugs, and their stability was evaluated in aqueous buffer solutions of pH 7.4, 1 N HCl, and also in human plasma. The hydrolytic degradation of diclofenac ester in aqueous buffer solutions was slow, as shown by t1/2 values greater than 22 hr, while rapid enzymatic hydrolysis occurred in the plasma (t1/2 = 1.12 hr). However, the mefenamic acid ester showed a relatively higher stability in buffer solutions (t1/2 greater than 38 hr at pH 10) as well as in the plasma (t1/2 = 7.28 hr) compared with the diclofenac ester. Therefore, the mefenamic acid ester would not be considered suitable as a prodrug.
Publication Year: 1997
Publication Date: 1997-01-01
Language: en
Type: article
Indexed In: ['crossref']
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Cited By Count: 10
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