Document Detail

Use of sorption promoters to increase systemic absorption of coumarin from transdermal drug delivery systems.
MedLine Citation:
PMID:  3245850     Owner:  NLM     Status:  MEDLINE    
In previous communications it was shown that coumarin is transdermally well absorbed. Increasing the application area for a coumarin ointment from 5 cm2 to 30 cm2, the absolute bioavailability increases from 8.6% to 66%. Using a transdermal drug delivery system (TDDS) based on an elastomer matrix, the absolute bioavailability was 21.9%. By selecting a proper sorption promoter (Labrafil), the absolute bioavailability increased to 71%. No correlation was found between tlag, flux or amount permeated obtained from ex vivo flux measurements, and the in vivo parameters Cmax and AUC. Whereas the bioavailability of a large area application of coumarin ointment is practically the same as with a small TDDS, the latter one is preferred to maintain a therapeutic concentration over a 24 h or 48 h period.
W A Ritschel; J K Barkhaus
Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  38     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1988 Dec 
Date Detail:
Created Date:  1989-06-02     Completed Date:  1989-06-02     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  1774-7     Citation Subset:  IM    
Division of Pharmaceutics and Drug Delivery Systems, University of Cincinnati Medical Center, OH.
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MeSH Terms
Administration, Cutaneous
Biological Availability
Coumarins / administration & dosage,  pharmacokinetics*
Drug Compounding
Rats, Inbred Strains
Skin Absorption
Reg. No./Substance:

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