1985
DOI: 10.1002/bdd.2510060406
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Pharmacokinetic evaluation of novel sustained‐release dosage forms of valproic acid in humans

Abstract: Five new sustained-release dosage forms of valproic acid (VPA) were developed. The new sustained-release formulations were administered to six healthy subjects for comparison with a standard tablet and an i.v. preparation of the drug. Three of the formulations exhibited a more prolonged and uniform absorption rate and yielded more sustained serum levels after ingestion. These three formulations maintained serum therapeutic levels of VPA for 24 h after a single oral administration of 1 g, and were bioequivalent… Show more

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Cited by 23 publications
(4 citation statements)
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“…12 After oral administration of 900 mg valpromide (tablet or solution), no or very low plasma valpromide concentrations could be detected in humans, but valproate was consistently detected in plasma. 13 The absorption rate of valproate after oral administration of valpromide enteric-coated tablet is slower than after oral administration of valproate sodium enteric-coated tablets, but similar after oral administration of sustained release forms of valproate sodium 14 After a therapeutic dose, serum valproate levels peak at 6 ]/10 hours following valpromide ingestion, whereas serum valproate levels peak at 2 ]/ 4 hours following ingestion of valproate sodium regular-release forms. 15 The delayed increase of serum valproate levels in our three cases is consistent with the pharmacokinetic profile of valpromide.…”
Section: Discussionmentioning
confidence: 99%
“…12 After oral administration of 900 mg valpromide (tablet or solution), no or very low plasma valpromide concentrations could be detected in humans, but valproate was consistently detected in plasma. 13 The absorption rate of valproate after oral administration of valpromide enteric-coated tablet is slower than after oral administration of valproate sodium enteric-coated tablets, but similar after oral administration of sustained release forms of valproate sodium 14 After a therapeutic dose, serum valproate levels peak at 6 ]/10 hours following valpromide ingestion, whereas serum valproate levels peak at 2 ]/ 4 hours following ingestion of valproate sodium regular-release forms. 15 The delayed increase of serum valproate levels in our three cases is consistent with the pharmacokinetic profile of valpromide.…”
Section: Discussionmentioning
confidence: 99%
“…The first published report concerned 5 new sustained release valproic acid formulations, administered to 6 healthy volunteers in comparison with a standard tablet and an intravenous preparation (Bialer et al 1985). Three of the formulations exhibited prolonged and uniform absorption rates and yielded serum concentrations which were sustained within the therapeutic range (50 to 100 mg!…”
Section: Valproic Acidmentioning
confidence: 98%
“…The biotransformation was complete in the case of the ethyl, trichloroethyl, propyl, butyl and hexyl derivatives of valproate, but was only partial in the case of the isobutyl, isoamyl and valproyl derivatives. Due to the rapid conversion of the prodrugs to the parent drug, the valproate plasma levels obtained after administration of the prodrugs peaked 6-26 rain after dosing, and did not yield a sustained release profile in vivo [28]. Of the eight monoesters of valproate only propylvalproate demonstrated anticonvulsant activity.…”
Section: Monoester Prodrugs Of Valproic Acidmentioning
confidence: 99%