A comparative pharmacokinetic study of valpromide and valproic acid after intravenous administration in humans

Meir Bialer; Abraham Rubinstein; Joseph Dubrovsky; Itamar Raz; Oded Abramsky

doi:10.1016/0378-5173(85)90219-4

A comparative pharmacokinetic study of valpromide and valproic acid after intravenous administration in humans

Meir Bialer^*
, Abraham Rubinstein
, Joseph Dubrovsky
, Itamar Raz
, Oded Abramsky

^*Corresponding author for this work

School of Pharmacy

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

Abstract

The pharmacokinetics of valpromide and valproic acid were investigated comparatively in 6 healthy subjects after intravenous administration of the two drugs. Valpromide was very rapidly and almost completely biotransformed to valproic acid (f_m = 81.2 ± 10.5%; mean ± S.D.; n = 6). Relative to valproic acid valpromide has a very short half-life (0.84 ± 0.33 h) a high-clearance value (70 ± 30.5 l/h) and a large volume of distribution (V_β = 75.3 ± 12.7 l). The results of this study showed that there was no significant difference between the biotransformation of valpromide to valproic acid after intravenous administration and that obtained after oral administration of valpromide. Therefore, in humans, valpromide appears to be a prodrug of valproic acid after intravenous as well as oral administration.

Original language	English
Pages (from-to)	25-33
Number of pages	9
Journal	International Journal of Pharmaceutics
Volume	23
Issue number	1
DOIs	https://doi.org/10.1016/0378-5173(85)90219-4
State	Published - Jan 1985

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title = "A comparative pharmacokinetic study of valpromide and valproic acid after intravenous administration in humans",

abstract = "The pharmacokinetics of valpromide and valproic acid were investigated comparatively in 6 healthy subjects after intravenous administration of the two drugs. Valpromide was very rapidly and almost completely biotransformed to valproic acid (fm = 81.2 ± 10.5\%; mean ± S.D.; n = 6). Relative to valproic acid valpromide has a very short half-life (0.84 ± 0.33 h) a high-clearance value (70 ± 30.5 l/h) and a large volume of distribution (Vβ = 75.3 ± 12.7 l). The results of this study showed that there was no significant difference between the biotransformation of valpromide to valproic acid after intravenous administration and that obtained after oral administration of valpromide. Therefore, in humans, valpromide appears to be a prodrug of valproic acid after intravenous as well as oral administration.",

author = "Meir Bialer and Abraham Rubinstein and Joseph Dubrovsky and Itamar Raz and Oded Abramsky",

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AU - Bialer, Meir

AU - Rubinstein, Abraham

AU - Dubrovsky, Joseph

AU - Raz, Itamar

AU - Abramsky, Oded

PY - 1985/1

Y1 - 1985/1

N2 - The pharmacokinetics of valpromide and valproic acid were investigated comparatively in 6 healthy subjects after intravenous administration of the two drugs. Valpromide was very rapidly and almost completely biotransformed to valproic acid (fm = 81.2 ± 10.5%; mean ± S.D.; n = 6). Relative to valproic acid valpromide has a very short half-life (0.84 ± 0.33 h) a high-clearance value (70 ± 30.5 l/h) and a large volume of distribution (Vβ = 75.3 ± 12.7 l). The results of this study showed that there was no significant difference between the biotransformation of valpromide to valproic acid after intravenous administration and that obtained after oral administration of valpromide. Therefore, in humans, valpromide appears to be a prodrug of valproic acid after intravenous as well as oral administration.

AB - The pharmacokinetics of valpromide and valproic acid were investigated comparatively in 6 healthy subjects after intravenous administration of the two drugs. Valpromide was very rapidly and almost completely biotransformed to valproic acid (fm = 81.2 ± 10.5%; mean ± S.D.; n = 6). Relative to valproic acid valpromide has a very short half-life (0.84 ± 0.33 h) a high-clearance value (70 ± 30.5 l/h) and a large volume of distribution (Vβ = 75.3 ± 12.7 l). The results of this study showed that there was no significant difference between the biotransformation of valpromide to valproic acid after intravenous administration and that obtained after oral administration of valpromide. Therefore, in humans, valpromide appears to be a prodrug of valproic acid after intravenous as well as oral administration.

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A comparative pharmacokinetic study of valpromide and valproic acid after intravenous administration in humans

Abstract

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