IVIVC in oral absorption for fenofibrate immediate release tablets using a dissolution/permeation system.
The usefulness of a dissolution/permeation (D/P) system to predict the in vivo performance of solid dosage forms containing the poorly soluble drug, fenofibrate, was studied. Biorelevant dissolution media simulating the fasted and fed state conditions of the human gastrointestinal tract were used in order to simulate the effect of food on the absorption of fenofibrate. Moreover, the results obtained from the D/P system were correlated with pharmacokinetic parameters obtained following in vivo studies in rats. The in vitro parameter (amount permeated in the D/P system) reflected well the in vivo performance in rats in terms of AUC and C(max) of fenofibric acid. This study thus demonstrates the potential of the D/P system as valuable tool for absorption screening of dosage forms for poorly soluble drugs.
Department of Pharmaceutical Technology and Biopharmaceutics, Johannes Gutenberg-University, Staudinger Weg 5, 55099 Mainz, Germany.
Philipp
P
Buch
Peter
P
Langguth
Makoto
M
Kataoka
Shinji
S
Yamashita
D000042:Absorption; D000284:Administration, Oral; D000818:Animals; D018938:Caco-2 Cells; D002626:Chemistry, Pharmaceutical / Q000295:instrumentation* / Q000379:methods*; D011345:Fenofibrate / Q000097:blood / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics*; D006801:Humans; D000960:Hypolipidemic Agents / Q000097:blood / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics*; D008297:Male; D010539:Permeability; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013607:Tablets / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics
D000960:Hypolipidemic Agents; D013607:Tablets; D011345:Fenofibrate