Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man

被引：88

作者：

Bukara, Katarina ^{[1
,2
]}

Schueller, Laurent ^{[3
]}

Rosier, Jan ^{[3
]}

Martens, Mark A. ^{[3
]}

Daems, Tinne ^{[3
]}

Verheyden, Loes ^{[3
]}

Eelen, Siemon ^{[3
]}

Van Speybroeck, Michiel ^{[3
]}

Libanati, Cristian ^{[4
]}

Martens, Johan A. ^{[5
]}

Van Den Mooter, Guy ^{[6
]}

Frerart, Francoise ^{[7
]}

Jolling, Koen ^{[8
]}

De Gieter, Marjan ^{[8
]}

Bugarski, Branko ^{[2
]}

Kiekens, Filip ^{[1
]}

机构：

[1] Univ Antwerp, Lab Pharmaceut Technol & Biopharm, Univ Pl 1, B-2610 Antwerp, Belgium

[2] Univ Belgrade, Fac Technol & Met, Dept Chem Engn, Belgrade, Serbia

[3] Formac Pharmaceut NV, Gaston Geenslaan 1, B-3001 Heverlee, Belgium

[4] WR Grace & Co, Incubator Technol, 7500 Grace Dr, Columbia, MD 21044 USA

[5] Katholieke Univ Leuven, Ctr Surface Chem & Catalysis, Kasteelpk Arenberg 23, B-3001 Heverlee, Belgium

[6] Katholieke Univ Leuven, O&N2, Lab Pharmacotechnol & Biopharm, Herestr 49,Box 921, B-3000 Leuven, Belgium

[7] SGS Lab Simon SA, Vieux Chemin Poete 10, B-1301 Bierges Wavre, Belgium

[8] SGS Belgium NV, Intercity Business Pk,Gen Wittelaan 19, B-2800 Mechelen, Belgium

来源：

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | 2016年 / 108卷

关键词：

Ordered mesoporous silica; Solubility; Absorption; Bioavailability; Fenofibrate; ORAL BIOAVAILABILITY; ITRACONAZOLE; FENOFIBRATE; ABSORPTION; RELEASE;

D O I：

10.1016/j.ejpb.2016.08.020

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 96 h post-dose. The rate (C-max/dose increased by 77%; t(max) reduced by 0.75 h) and extent of absorption (AUC(0-24h)/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. (C) 2016 Elsevier B.V. All rights reserved.

引用

页码：220 / 225

页数：6

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