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  • 1985-1989  (2)
  • 1
    ISSN: 1573-904X
    Keywords: Progabide ; reversed phase ; high-performance liquid chromatography (HPLC) ; plasma ; analysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A reversed-phase high-performance liquid chromatography (HPLC) assay procedure for Progabide, its active acid metabolite (PGA), and its hydrolytic degradation product (SL79.182) has been developed. This highly specific technique has allowed the simultaneous determination of these drugs in aqueous samples, and when coupled with a single and easy extraction step, spiked plasma samples could also be analyzed. The method had a sensitivity of about 30, 45, and 100 ng/ml for Progabide, SL79.182, and PGA, respectively.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-904X
    Keywords: Progabide ; metabolic derivatives ; stability ; solubility
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The stability–pH profile of the γ-aminobutyric acid prodrug, Progabide, was found to be bell shaped, with maximum stability occurring at pH 6 to 7 with a t 1/2 of 126 min. Of its metabolic derivatives, the deamidated product PGA degraded in a similar fashion to Progabide, whereas the hydrolytic degradation product SL79.182 was, as expected, a stable compound. Progabide behaved as a typical weak base, with its solubility increasing with a decrease in pH. SL79.182 behaved as a typical phenolic weak acid, with its solubility increasing with an increase in pH. Both compounds displayed low intrinsic solubilities of 14.5 × 10−5 M for Progabide and 33.4 × 10−6 M for SL79.182. An increase in temperature resulted in an increase in the solubility but a decrease in the stability of Progabide. The data obtained indicate that the gastric pH and gastric emptying rate will have a profound effect on the oral bioavailability of Progabide.
    Type of Medium: Electronic Resource
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