Oral modified-release formulations in motion: The relationship between gastrointestinal transit and drug absorption

被引：76
作者：
Varum, Felipe J. O. [1 ]
Merchant, Hamid A. [1 ]
Basit, Abdul W. [1 ]
机构：
[1] Univ London, Sch Pharm, London WC1N 1AX, England
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2010年 / 395卷 / 1-2期
关键词：
Controlled release; Delayed release; Colonic delivery; Enteric coatings; Multiparticulates; Multiple-units; Single-units; Gamma scintigraphy; Gastrointestinal transit; Biopharmaceutics; Bioavailability; Pharmacokinetics; PHARMACEUTICAL DOSAGE FORMS; SMALL-INTESTINAL TRANSIT; POLYETHYLENE-GLYCOL; 400; IN-VIVO PERFORMANCE; GAMMA-SCINTIGRAPHY; CROHNS-DISEASE; COLONIC DELIVERY; HEALTHY-SUBJECTS; MULTIPLE-UNITS; SINGLE-UNIT;
D O I：
10.1016/j.ijpharm.2010.04.046
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Oral modified-release dosage forms can be designed with the aim of achieving specific pharmacokinetic profiles, delivering to specific gut localities or reducing the number of drug administrations. Multipleunit systems, such as pellets, beads or granules, often claim superiority to single-unit modified-release formulations in terms of predictability and reproducibility of behaviour in the gastrointestinal tract. This is an oversimplification and in this review we discuss the effect of the highly variable gastrointestinal transit on the bioperformance of multiple-unit dosage forms, relative to their single-unit counterparts. We examine the sometimes contradictory literature in this area and highlight specific case studies which demonstrate the effect of intestinal transit on dosage form performance and drug absorption. (C) 2010 Published by Elsevier B.V.
引用
收藏
页码：26 / 36
页数：11
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