Tags

Type your tag names separated by a space and hit enter

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.EJ

Abstract

The effects of preceding food intake on the plasma concentrations of R(-)-ibuprofen and the pharmacologically active enantiomer S(+)-ibuprofen were investigated in healthy subjects. A single oral dose of 400 mg racemic ibuprofen was administered either fasting or following a standardized meal. As compared to fasting administration postprandial drug intake resulted in a clear reduction of R(-) and S(+)- ibuprofen plasma concentrations mainly during the initial three hours. The ratio of S(+)/R(-)-ibuprofen postprandially was increased for Cmax and AUC o-tmax as well as for AUC o-infinity. These data are compatible with a meal-induced enhancement of chiral inversion of R(-) to S(+)-ibuprofen. The significant reduction of plasma concentrations of ibuprofen mainly during the initial three hours suggests that the analgesic efficacy is diminished when the drug is taken after a meal. This may to a slight extent be compensated for by a small increase of the metabolic inversion of the R(-)-enantiomer into the active S(+)-form of the drug.

Authors+Show Affiliations

Abteilung Klinische Pharmakologie der Medizinischen Klinik und Poliklinik der Universität Heidelberg, Heidelberg, Germany.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

9153347

Citation

Siemon, D, et al. "Fasting and Postprandial Disposition of R(-)- and S(+)-ibuprofen Following Oral Administration of Racemic Drug in Healthy Individuals." European Journal of Medical Research, vol. 2, no. 5, 1997, pp. 215-9.
Siemon D, de Vries JX, Stötzer F, et al. Fasting and postprandial disposition of R(-)- and S(+)-ibuprofen following oral administration of racemic drug in healthy individuals. Eur J Med Res. 1997;2(5):215-9.
Siemon, D., de Vries, J. X., Stötzer, F., Walter-Sack, I., & Dietl, R. (1997). Fasting and postprandial disposition of R(-)- and S(+)-ibuprofen following oral administration of racemic drug in healthy individuals. European Journal of Medical Research, 2(5), 215-9.
Siemon D, et al. 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. PubMed PMID: 9153347.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fasting and postprandial disposition of R(-)- and S(+)-ibuprofen following oral administration of racemic drug in healthy individuals. AU - Siemon,D, AU - de Vries,J X, AU - Stötzer,F, AU - Walter-Sack,I, AU - Dietl,R, PY - 1997/5/28/pubmed PY - 1997/5/28/medline PY - 1997/5/28/entrez SP - 215 EP - 9 JF - European journal of medical research JO - Eur J Med Res VL - 2 IS - 5 N2 - The effects of preceding food intake on the plasma concentrations of R(-)-ibuprofen and the pharmacologically active enantiomer S(+)-ibuprofen were investigated in healthy subjects. A single oral dose of 400 mg racemic ibuprofen was administered either fasting or following a standardized meal. As compared to fasting administration postprandial drug intake resulted in a clear reduction of R(-) and S(+)- ibuprofen plasma concentrations mainly during the initial three hours. The ratio of S(+)/R(-)-ibuprofen postprandially was increased for Cmax and AUC o-tmax as well as for AUC o-infinity. These data are compatible with a meal-induced enhancement of chiral inversion of R(-) to S(+)-ibuprofen. The significant reduction of plasma concentrations of ibuprofen mainly during the initial three hours suggests that the analgesic efficacy is diminished when the drug is taken after a meal. This may to a slight extent be compensated for by a small increase of the metabolic inversion of the R(-)-enantiomer into the active S(+)-form of the drug. SN - 0949-2321 UR - https://www.unboundmedicine.com/medline/citation/9153347/Fasting_and_postprandial_disposition_of_R_____and_S_+__ibuprofen_following_oral_administration_of_racemic_drug_in_healthy_individuals_ DB - PRIME DP - Unbound Medicine ER -