| Human plasma concentrations of R, S, and racemic flurbiprofen given as a toothpaste. | |
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MedLine Citation:
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PMID: 8809639 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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S C Forland; W J Wechter; S Witchwoot; K H Clifford; R L Arnett; R E Cutler |
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Publication Detail:
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Type: Comparative Study; Journal Article |
Journal Detail:
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Title: Journal of clinical pharmacology Volume: 36 ISSN: 0091-2700 ISO Abbreviation: J Clin Pharmacol Publication Date: 1996 Jun |
Date Detail:
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Created Date: 1996-12-06 Completed Date: 1996-12-06 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0366372 Medline TA: J Clin Pharmacol Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 546-53 Citation Subset: IM |
Affiliation:
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Medical Center, Loma Linda University, California 92354, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adult Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics* Area Under Curve Flurbiprofen / pharmacokinetics* Half-Life Humans Male Mouth / metabolism* Stereoisomerism Toothpaste |
| Chemical | |
Reg. No./Substance:
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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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