A combined approach to control valproic acid release via novel delivery system of valpromide: A kinetic and pharmacokinetic study

Abraham Rubinstein, Meir Bialer*, Michael Friedman, Itamar Raz, Oded Abramsky

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

The kinetics of two novel controlled release formulations of valpromide (VPD; designed hereafter as VPDCR1 and VPDCR2) were studied in vitro and were found to follow the Hixson-Crowell cube root law model with a threefold difference between the two valpromide release rate constants. After oral administration of VPDCR1, VPDCR2 and a commercially available standard VPD formulation (Depamide®) to six healthy subjects, valpromide was found to be a prodrug of valproic acid (VPA). Serum levels of valproic acid were monitored, and the pharmacokinetics of VPA and the absorption characteristics of VPDCR1, VPDCR2 and Depamide® were analyzed comparatively. Results from this study suggest that sustained release dosage forms of valpromide have certain advantages over sustained release formulations of valproic acid.

Original languageEnglish
Pages (from-to)33-38
Number of pages6
JournalJournal of Controlled Release
Volume4
Issue number1
DOIs
StatePublished - Jun 1986

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