Kinetics of degradation and oil solubility of ester prodrugs of a model dipeptide (Gly-Phe)

SW Larsen, M Ankersen, C Larsen

Index: Larsen, Susan Weng; Ankersen, Michael; Larsen, Claus European Journal of Pharmaceutical Sciences, 2004 , vol. 22, # 5 p. 399 - 408

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Citation Number: 25

Abstract

Oil-based depot formulations may constitute a future delivery method for small peptides. Thus, a requirement is attainment of sufficient oil solubility for such active compounds. A model dipeptide (Gly-Phe) has been converted into lipophilic prodrugs by esterification at the C-terminal carboxylic acid group. The decomposition kinetics of octyl ester of Gly-Phe (IV) has been investigated at pH 7.4 (37° C) and IV was shown to degrade by first-order ...