Document Detail


The bioavailability of diclofenac from enteric coated products in healthy volunteers with normal and artificially decreased gastric acidity.
MedLine Citation:
PMID:  7888605     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The relative bioavailability of four monolithic enteric coated (MEC) diclofenac products was compared in 16 healthy volunteers. Only one generic product was fully bioequivalent with the reference product Voltaren with regard to AUC, Cmax, and tlag. Two products showed significant differences in tlag. In a second experiment with eight volunteers the influence of increased gastric pH (ranitidine treatment) on the two mutually most differing products was studied. They showed equivalence in AUC, but not in Cmax. Analysis of tlag suggests that the product with the low tlag disintegrates within the non-acid stomach, whereas the product with the long tlag passes the non-acid stomach intact. Several in vitro dissolution tests were conducted. The European Pharmacopeia test did not detect any differences between the products. At pH 5, both with and without mechanical stress, only the product with the shortest tlag released diclofenac. The in vivo results were best predicted by the in vitro dissolution tests performed at several fixed pH values with mechanical stress.
Authors:
M E Van Gelderen; M Olling; D M Barends; J Meulenbelt; P Salomons; A G Rauws
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Publication Detail:
Type:  Clinical Trial; Controlled Clinical Trial; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biopharmaceutics & drug disposition     Volume:  15     ISSN:  0142-2782     ISO Abbreviation:  Biopharm Drug Dispos     Publication Date:  1994 Dec 
Date Detail:
Created Date:  1995-04-17     Completed Date:  1995-04-17     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7911226     Medline TA:  Biopharm Drug Dispos     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  775-88     Citation Subset:  IM    
Affiliation:
National Institute of Public Health and Environmental Protection, Bilthoven, The Netherlands.
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MeSH Terms
Descriptor/Qualifier:
Adolescent
Adult
Biological Availability
Diclofenac / administration & dosage,  blood,  pharmacokinetics*
Female
Gastric Acid / physiology*
Humans
Hydrogen-Ion Concentration
Male
Quality Control
Solubility
Spectrophotometry, Ultraviolet
Tablets, Enteric-Coated
Chemical
Reg. No./Substance:
0/Tablets, Enteric-Coated; 15307-86-5/Diclofenac

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


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