Abstract
Background: The aim was to determine the effect of feeding on chiral inversion of Ibuprofen isomers. Method: Six healthy volunteers participated in a two-treatment crossover study where a single dose of Ibuprofen racemate was given. One stage consisted in an 8-hour interval of fasting, while in the other, the drug was administered with a solution of saccharose and a standard food intake regimen was implemented.
Highlights
MethodsMaterials and Methods a) Subjects and study design Six healthy Caucasian volunteers (3 women and3 men) between 22 and 31 years old with mean body weight of 61 and 92 kg, respectively, were enrolled in a two-treatment (fasting and fed), two-period (first and second week) and two-sequence (fasting-fed and fedfasting) crossover study where a single dose of 600 mg of Ibuprofen was given.An immediate release formulation was selected for a rapid drug release, avoiding any possible excipient-related interference with drug pancreatic secretion, important to achieve the aim of the study
Clearance of R-ibuprofen increased following the and pharmacodynamic properties.[4],[5] These drugs ingestion of saccharose and food, the increased are clinically administered as a racemic mixture though bioavailability of S-ibuprofen due to R-to-S chiral inversion its anti-inflammatory activity is attributed almost entirely overrode its increased clearance
One of the possible metabolism might be explained by the supplementary amount of drug molecules that reaches the enter ocytes through pancreatic/intestinal juice secretion following the ingestion of food
Summary
Materials and Methods a) Subjects and study design Six healthy Caucasian volunteers (3 women and3 men) between 22 and 31 years old with mean body weight of 61 and 92 kg, respectively, were enrolled in a two-treatment (fasting and fed), two-period (first and second week) and two-sequence (fasting-fed and fedfasting) crossover study where a single dose of 600 mg of Ibuprofen was given.An immediate release formulation was selected for a rapid drug release, avoiding any possible excipient-related interference with drug pancreatic secretion, important to achieve the aim of the study. 3 men) between 22 and 31 years old with mean body weight of 61 and 92 kg, respectively, were enrolled in a two-treatment (fasting and fed), two-period (first and second week) and two-sequence (fasting-fed and fedfasting) crossover study where a single dose of 600 mg of Ibuprofen was given. The study was carried out administering the Ibuprofen capsule with only 200 mL of water at one period (Fasting stage) and with 20 g of saccharose in 200 mL of water at the other period (Fed stage). For the Fasting stage, fasting was prolonged throughout the whole 8-hour study. Subjects maintained an eight-hour overnight fasting period before each stage but were given a light breakfast three hours before drug administration in order to disrupt the prolonged fasting and ensure the safety of the volunteers. The present study distinguishes from previously reported ones due to this absolute fasting stage that allows a purer comparison between fed and fasting conditions
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
