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THE EFFECT OF FOOD ON THE BIOAVAILABILITY OF IBUPROFEN AND FLURBIPROFEN FROM SUSTAINED RELEASE FORMULATIONS
Author(s) -
Pargal Anisha,
Kelkar Medha G.,
Nayak P. Jagadeesh
Publication year - 1996
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199608)17:6<511::aid-bdd969>3.0.co;2-y
Subject(s) - postprandial , bioavailability , cmax , ibuprofen , flurbiprofen , chemistry , meal , plasma concentration , area under the curve , capsule , pharmacokinetics , zoology , pharmacology , medicine , food science , biology , insulin , botany
The effect of food on the plasma concentration–time profile of sustained release dosage forms of ibuprofen and flurbiprofen has been investigated in healthy Asian Indian volunteers, in two separate studies. In study 1, 20 volunteers were administered a single 200 mg multiple‐unit sustained release capsule of flurbiprofen (Froben SR ™ ), after an overnight fast or a heavy vegetarian breakfast. Food produced a statistically significant increase in the mean (±SE) maximal plasma concentration ( C max ) and area under the plasma concentration–time curve (AUC 0–48 . C max (±SE) increased from 9·88± 0·48 mg L −1 (fasting) to 11·36±0·88 mg L −1 (postprandial) and AUC 0–48 (±SE) increased from 120·78±9·64 mg h L −1 (fasting) to 149·73±12·24 mg h L −1 (postprandial). The mean (±SE) time to peak ( t max ) was also significantly delayed from 3·85±0·27 h to 8·70±0·89 h. In study 2, 18 volunteers were administered a single 800 mg erodible sustained release matrix tablet of ibuprofen (Brufen Retard ™ ), after an overnight fast or along with a heavy vegetarian breakfast. The formulation exhibited multiple peaks ( n ≥2) on the plasma concentration–time curve. Although food did not affect the bioavailability of this formulation, there was a statistically significant increase in the mean (±SE) concentration of the first peak ( C peak1 ) from 14·21±1·38 mg L −1 (fasting) to 20·14±1·38 mg L −1 (with food). The time at which C peak1 was reached was not influenced by the intake of food. Results indicate that while qualitative changes in the plasma concentration versus time curves are primarily influenced by the nature of the formulation and the type of meal, bioavailability is influenced by the absorption characteristics of the drug as well. Thus, despite a significant increase in peak plasma concentrations of both drugs with a meal, the bioavailability of flurbiprofen alone was enhanced.