Document Detail


Human plasma concentrations of R, S, and racemic flurbiprofen given as a toothpaste.
MedLine Citation:
PMID:  8809639     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Flurbiprofen, an arylpropionic acid (APA) class nonsteroidal antiinflammatory drug (NSAID), is commercially available only as the racemic mixture, although its pharmacologic effect has been credited primarily to the S isomer. In humans, the bioavailability of racemic flurbiprofen absorbed from the oral cavity has been studied measuring the total concentration of S- and R-flurbiprofen, and the pharmacokinetics of S- and R-flurbiprofen have been studied after oral administration of racemic flurbiprofen. In this study, the plasma concentrations of S-flurbiprofen and to some extent R-flurbiprofen were studied after brushing with a toothpaste containing different mixtures of S- and R-flurbiprofen. The toothpaste formulations contained 1% racemic (50:50), eutectic (14:86), 1%, 0.5%, and 0.25% (5:95) R- to S-flurbiprofen. Both S- and R-flurbiprofen were rapidly absorbed, with a time to reach maximum concentration (tmax) of 1.2 to 1.4 hours. Based on the AUC, the amount of S-flurbiprofen absorbed increased proportionally when given as the 0.25% (5:95) preparation to the 0.5% (5:95) mixture but did not increase significantly above the 0.5% (5:95) mixture when given as 1% (5:95) R- to S-flurbiprofen. This suggests that dose-proportional absorption of S-flurbiprofen is not maintained at higher concentrations. The elimination of S-flurbiprofen appears to be variable and prolonged after this mode of administration, as observed from plasma concentrations. Further controlled and more prolonged studies of S- and R-flurbiprofen are needed to confirm these observations.
Authors:
S C Forland; W J Wechter; S Witchwoot; K H Clifford; R L Arnett; R E Cutler
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  36     ISSN:  0091-2700     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  1996 Jun 
Date Detail:
Created Date:  1996-12-06     Completed Date:  1996-12-06     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  546-53     Citation Subset:  IM    
Affiliation:
Medical Center, Loma Linda University, California 92354, USA.
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MeSH Terms
Descriptor/Qualifier:
Adult
Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
Area Under Curve
Flurbiprofen / pharmacokinetics*
Half-Life
Humans
Male
Mouth / metabolism*
Stereoisomerism
Toothpaste
Chemical
Reg. No./Substance:
0/Anti-Inflammatory Agents, Non-Steroidal; 0/Toothpaste; 5104-49-4/Flurbiprofen

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


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