| Literature DB >> 27648957 |
Katarina Bukara1, Laurent Schueller2, Jan Rosier2, Mark A Martens2, Tinne Daems2, Loes Verheyden2, Siemon Eelen2, Michiel Van Speybroeck2, Cristian Libanati3, Johan A Martens4, Guy Van Den Mooter5, Françoise Frérart6, Koen Jolling7, Marjan De Gieter7, Branko Bugarski8, Filip Kiekens9.
Abstract
Formulating poorly water soluble drugs using ordered mesoporous silica materials is an emerging approach to tackle solubility-related bioavailability problems. The current study was conducted to assess the bioavailability-enhancing potential of ordered mesoporous silica in man. In this open-label, randomized, two-way cross-over study, 12 overnight fasted healthy volunteers received a single dose of fenofibrate formulated with ordered mesoporous silica or a marketed product based on micronized fenofibrate. Plasma concentrations of fenofibric acid, the pharmacologically active metabolite of fenofibrate, were monitored up to 96h post-dose. The rate (Cmax/dose increased by 77%; tmax reduced by 0.75h) and extent of absorption (AUC0-24h/dose increased by 54%) of fenofibrate were significantly enhanced following administration of the ordered mesoporous silica based formulation. The results of this study serve as a proof of concept in man for this novel formulation approach.Entities:
Keywords: Absorption; Bioavailability; Fenofibrate; Ordered mesoporous silica; Solubility
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Year: 2016 PMID： 27648957 DOI： 10.1016/j.ejpb.2016.08.020
Source DB: PubMed Journal: Eur J Pharm Biopharm ISSN： 0939-6411 Impact factor: 5.571