| Biopharmaceutical aspects of tolfenamic acid. | |
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MedLine Citation:
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PMID: 7816776 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The pharmacokinetics of tolfenamic acid is well described by a two-compartment model with relatively short half-lives (T/2 beta 1-2 hours) and tolfenamic acid is highly protein-bound with small volumes of distribution. It is cleared relatively fast (150-200 ml/min), mainly by hepatic metabolism and the metabolites are renally cleared as glucuronic acid conjugates. The peroral absorption is good and the peroral bioavailability is about 75%, as first pass metabolism accounts for about 20%. Tolfenamic acid shows linear pharmacokinetics and during multiple dosage regimen, i.e. thrice daily, no accumulation beyond the second dose is observed. The bioavailability in dependence of age and disease has been studied and only in the case of severe liver or kidney impairment, a change in dosage regimen seems warranted. The development of different formulations will be outlined, mainly on rectal delivery, on sustained release and rapid release oral formulations, on topical ointment, and on parenteral delivery. The problems with tolfenamic acid in pharmaceutical formulation caused mainly by poor solubility will be discussed. Formulations ready for the market now or very soon are Clotam capsules (tablets). Clotam retard tablets, Clotam suppositories, and Clotam oral suspension, whereas rapid tablets, topical ointments, and parenteral formulations need further development to be ready for marketing in the years to come. |
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Authors:
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S B Pedersen |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Pharmacology & toxicology Volume: 75 Suppl 2 ISSN: 0901-9928 ISO Abbreviation: Pharmacol. Toxicol. Publication Date: 1994 |
Date Detail:
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Created Date: 1995-02-06 Completed Date: 1995-02-06 Revised Date: 2005-11-17 |
Medline Journal Info:
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Nlm Unique ID: 8702180 Medline TA: Pharmacol Toxicol Country: DENMARK |
Other Details:
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Languages: eng Pagination: 22-32 Citation Subset: IM |
Affiliation:
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A/S GEA Farmaceutisk Fabrik, Biochemical Department, Hvidovre, Denmark. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Absorption Aging / metabolism Anthranilic Acids / pharmacokinetics* Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics* Arthritis, Rheumatoid / metabolism Biological Availability Dosage Forms Drug Administration Routes Half-Life Humans Liver Cirrhosis / metabolism Migraine Disorders / metabolism |
| Chemical | |
Reg. No./Substance:
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0/Anthranilic Acids; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Dosage Forms; 13710-19-5/tolfenamic acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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