1. Macromolecular prodrugs: X. Kinetics of fenoprofen release from PHEA-fenoprofen conjugate.
- Author
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van der Merwe T, Boneschans B, Zorc B, Breytenbach J, and Zovko M
- Subjects
- Chromatography, High Pressure Liquid, Hydrogen-Ion Concentration, Kinetics, Solubility, Anti-Inflammatory Agents, Non-Steroidal chemistry, Fenoprofen chemistry, Polyhydroxyethyl Methacrylate analogs & derivatives, Polyhydroxyethyl Methacrylate chemistry, Prodrugs chemistry
- Abstract
The kinetics of fenoprofen release from poly[alpha,beta-(N-2-hydroxyethyl-DL-aspartamide)]-fenoprofen conjugate (PHEA-Fen) in aqueous buffer solutions (pH 10 and 1.1), simulated gastric (SGF) and intestinal fluids (SIF) was studied. In borate buffer pH 10, the following rate constants were obtained: k=0.2659 (t=60 degrees C) and k=0.0177 h(-1) (t=37 degrees C) and in glycine buffer solution pH 1.1 k=0.0036 h(-1). In SGF and SIF fenoprofen release did not occur in significant extend within 12 h. The hydrolysis of the ester bond between the polymeric carrier and fenoprofen followed the pseudo first-order kinetics, with activation energy indicative for the breakage of a sigma bond (E(a)=100.6 kJ mol(-1)). The concentration of the released fenoprofen was determined by high performance liquid chromatography (HPLC).
- Published
- 2002
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