May 23 2022




Active ingredient: ibuprofen

Food does not seem to exert an important action on the absorption and effect of ibuprofen[1].

Overall, results of experimental studies on NSAIDs in laboratory animals show that fasting increases gastric side effects of these drugs, while foods increase damage in the small intestine, although this has not been verified in humans[2].

The possible effects of food on the modification of gastric damage caused by anti-inflammatory are complex, since the amount and composition of food can substantially modify the response.

Usually, food delayed the peak plasma level (Tmax) and, therefore, the onset of action, without affecting the total bioavailability.

This fact can be important when the time lapsed until effect starts is relevant, especially when a quick relief is expected.

The effect of food on plasma concentration of sustained release ibuprofen has been investigated after fasting overnight or with a heavy vegetarian breakfast. The formulation presented multiple peaks in the plasma concentration curve over time. Although food did not affect bioavailability of ibuprofen[3], there was a significant increase in mean drug concentration. The results seemed to indicate that the qualitative changes in the plasma concentration were mainly influenced by the nature of the formulation and type of food, while bioavailability would be influenced by absorption features of the drug[4].

In experimental trials, Cmax and AUC of ibuprofen increased significantly after one or more doses of Coca-Cola, indicating a higher degree of absorption of ibuprofen[5]. For this reason, daily dose and frequency of dosing of ibuprofen should be reduced when administered with this beverage.

It has conducted a study which concluded that tamarind's fruit extract significantly increases the bioavailability of ibuprofen[6].

Data from a study in healthy volunteers about the chiral inversion of the R to L ibuprofen suggest a reduction in analgesic efficacy when the antiinflammatory is taken after a meal[7].

The effect of food on bioavailability of sustained release forms lacks any relevance[8].

References:

1: Marasanapalle VP, Crison JR, Ma J, Li X, Jasti BR. Investigation of some factors contributing to negative food effects. Biopharm Drug Dispos. 2009 Mar;30(2):71-80. doi: 10.1002/bdd.647.
2: Rainsford KD, Bjarnason I. NSAIDs: take with food or after fasting? J Pharm Pharmacol. 2012 Apr;64(4):465-9. doi: 10.1111/j.2042-7158.2011.01406.x.
3: Pargal A, Kelkar MG, Nayak PJ. The effect of food on the bioavailability of ibuprofen and flurbiprofen from sustained release formulations. Biopharm Drug Dispos. 1996 Aug;17(6):511-9. .
4: Bushra R, Aslam N. An overview of clinical pharmacology of Ibuprofen. Oman Med J. 2010 Jul;25(3):155-1661. doi: 10.5001/omj.2010.49.
5: Kondal A, Garg SK. Influence of acidic beverage (Coca-Cola) on pharmacokinetics of ibuprofen in healthy rabbits. Indian J Exp Biol. 2003 Nov;41(11):1322-4.
6: Garba M, Yakasai IA, Bakare MT, Munir HY. Effect of Tamarindus indica. L on the bioavailability of ibuprofen in healthy human volunteers. Eur J Drug Metab Pharmacokinet. 2003 Jul-Sep;28(3):179-84.
7: Siemon D, de Vries JX, Stötzer F, Walter-Sack I, Dietl R. . Fasting and postprandial disposition of R(-)- and S(+)-ibuprofen following oral administration of racemic drug in healthy individuals. Eur J Med Res. 1997 May 28;2(5):215-9.
8:: Borin MT, Khare S, Beihn RM, Jay M. The effect of food on gastrointestinal (GI) transit of sustained-release ibuprofen tablets as evaluated by gamma scintigraphy. Pharm Res. 1990 Mar;7(3):304-7.