Premium
Sex and Food Influence on Intestinal Absorption of Ketoprofen Gastroresistant Formulation
Author(s) -
Magallanes Laura,
Lorier Marianela,
Ibarra Manuel,
Guevara Natalia,
Vázquez Marta,
Fagiolino Pietro
Publication year - 2015
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.208
Subject(s) - medicine , ketoprofen , confidence interval , crossover study , absorption (acoustics) , pharmacokinetics , oral administration , gastroenterology , pharmacology , physics , alternative medicine , pathology , acoustics , placebo
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. C max , AUC, C max /AUC, and k el 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 C max /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 (T 0 ), with a longer T 0 after food intake (5.5 vs 2.5 hours). Also, a significant difference between the medians of T max was found ( P < .01), being 7.0 hours after food coadministration and 4.0 hours under fasting administration, but this difference disappeared once T 0 was subtracted from T max . C max /AUC, which is related to drug absorption rate, showed significant differences between sexes. Men showed higher ( P =.006) C max /AUC means (0.468 ± 0.094 vs 0.361 ± 0.087 h −1 . T max 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.