title: Sex and Food Influence on Intestinal Absorption of Ketoprofen Gastroresistant Formulation.
abstract: Sixteen healthy volunteers (8 women and 8 men) participated in a 2-period, 2-treatment crossover study. A delayed-release gastroresistant formulation of ketoprofen was administered under fasting and fed conditions. Cmax , AUC, Cmax /AUC, and kel obtained after food coadministration did not differ from those calculated under fasting administration. Ninety-five percent confidence intervals for fed/fasting geometric mean ratio of Cmax /AUC and AUC were 0.80-1.14 and 0.80-1.23, respectively. A significant difference (P < .01) was found between lag-time medians (T0 ), with a longer T0 after food intake (5.5 vs 2.5 hours). Also, a significant difference between the medians of Tmax was found (P < .01), being 7.0 hours after food coadministration and 4.0 hours under fasting administration, but this difference disappeared once T0 was subtracted from Tmax . Cmax /AUC, which is related to drug absorption rate, showed significant differences between sexes. Men showed higher (P =.006) Cmax /AUC means (0.468 ± 0.094 vs 0.361 ± 0.087 h(-1) . Tmax was also significantly different (P < .05), being 4.0 (3.0-5.0) hours for men and 8.0 (5.0-10.0) hours for women. In conclusion, men showed a faster intestinal absorption rate with earlier time-to-peak plasma concentration of ketoprofen. Food coadministration extended the gastric residence time of formulation but exerted no effect on its intestinal absorption pattern.
authors.affiliation: Department of Pharmaceutical Sciences Faculty of Chemistry & Bioavailability and Bioequivalence Centre for Medicine Evaluation, Universidad de la República, Montevideo, Uruguay.
authors.forename: Laura
authors.initials: L
authors.lastname: Magallanes
authors.affiliation: Department of Pharmaceutical Sciences Faculty of Chemistry & Bioavailability and Bioequivalence Centre for Medicine Evaluation, Universidad de la República, Montevideo, Uruguay.
authors.forename: Marianela
authors.initials: M
authors.lastname: Lorier
authors.affiliation: Department of Pharmaceutical Sciences Faculty of Chemistry & Bioavailability and Bioequivalence Centre for Medicine Evaluation, Universidad de la República, Montevideo, Uruguay.
authors.forename: Manuel
authors.initials: M
authors.lastname: Ibarra
authors.affiliation: Department of Pharmaceutical Sciences Faculty of Chemistry & Bioavailability and Bioequivalence Centre for Medicine Evaluation, Universidad de la República, Montevideo, Uruguay.
authors.forename: Natalia
authors.initials: N
authors.lastname: Guevara
authors.affiliation: Department of Pharmaceutical Sciences Faculty of Chemistry & Bioavailability and Bioequivalence Centre for Medicine Evaluation, Universidad de la República, Montevideo, Uruguay.
authors.forename: Marta
authors.initials: M
authors.lastname: Vázquez
authors.affiliation: Department of Pharmaceutical Sciences Faculty of Chemistry & Bioavailability and Bioequivalence Centre for Medicine Evaluation, Universidad de la República, Montevideo, Uruguay.
authors.forename: Pietro
authors.initials: P
authors.lastname: Fagiolino
mesh_terms: D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D019540:Area Under Curve; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D005260:Female; D018565:Food-Drug Interactions; D006801:Humans; D007408:Intestinal Absorption; D007660:Ketoprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008297:Male; D012737:Sex Factors; D055815:Young Adult
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D007660:Ketoprofen
keywords: gastrointestinal transit; ketoprofen delayed-release gastroresistant formulation; sex and food influence on ketoprofen absorption