Document Detail

Percutaneous absorption of valproic acid and its plasma concentration after application of ointment.
MedLine Citation:
PMID:  3126287     Owner:  NLM     Status:  MEDLINE    
In order to develop a percutaneous (p.c.) dosage form of valproic acid (VPA), ointments containing VPA and both VPA and its calcium salt (VPA-Ca) were prepared. The p.c. absorption was studied by determining the plasma concentrations of VPA in rabbits following application of either ointment. In addition, the in vitro penetration study with excised full-thickness rabbit skin was done to evaluate the pharmaceutical availability. VPA was readily and rapidly absorbed through the skin from the gel ointment. The plasma concentrations of VPA higher than 30 micrograms/ml were maintained for 6 h after application of 5% VPA.5% VPA-Ca gel ointment, and for 4 h after application of 5% VPA ointment. The bioavailability of VPA following dosing of both ointment was above 97%. The in vitro penetration rate through the skin and skin/solvent partition coefficient were significantly lower with 5% VPA.5% VPA-Ca solution than with 5% VPA, suggesting the slower penetration of VPA from the 5% VPA.5% VPA-Ca. A small difference was observed in the release rate of drugs from these ointments. The present results demonstrated the pharmaceutical effectiveness of the VPA.VPA-Ca ointment for seizure disorders.
T Ogiso; Y Ito; M Iwaki; Y Yamamoto; T Yamahata
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmacobio-dynamics     Volume:  10     ISSN:  0386-846X     ISO Abbreviation:  J. Pharmacobio-dyn.     Publication Date:  1987 Oct 
Date Detail:
Created Date:  1988-04-18     Completed Date:  1988-04-18     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  7901854     Medline TA:  J Pharmacobiodyn     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  537-42     Citation Subset:  IM    
Faculty of Pharmaceutical Sciences, Kinki University, Higashi-Osaka, Japan.
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MeSH Terms
Biological Availability
Injections, Intravenous
Skin Absorption*
Valproic Acid / administration & dosage,  blood,  pharmacokinetics*
Reg. No./Substance:
0/Ointments; 99-66-1/Valproic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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