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

Felipe J O Varum, Hamid A Merchant, Abdul W Basit

Research output: Contribution to journalReview article

62 Citations (Scopus)

Abstract

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. Multiple-unit 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.

LanguageEnglish
Pages26-36
Number of pages11
JournalInternational Journal of Pharmaceutics
Volume395
Issue number1-2
Early online date28 May 2010
DOIs
Publication statusPublished - 16 Aug 2010
Externally publishedYes

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Gastrointestinal Transit
Gastrointestinal Agents
Dosage Forms
Pharmaceutical Preparations
Gastrointestinal Tract
Pharmacokinetics

Cite this

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title = "Oral modified-release formulations in motion: the relationship between gastrointestinal transit and drug absorption",
abstract = "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. Multiple-unit 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.",
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Oral modified-release formulations in motion : the relationship between gastrointestinal transit and drug absorption. / Varum, Felipe J O; Merchant, Hamid A; Basit, Abdul W.

In: International Journal of Pharmaceutics, Vol. 395, No. 1-2, 16.08.2010, p. 26-36.

Research output: Contribution to journalReview article

TY - JOUR

T1 - Oral modified-release formulations in motion

T2 - International Journal of Pharmaceutics

AU - Varum, Felipe J O

AU - Merchant, Hamid A

AU - Basit, Abdul W

N1 - Copyright (c) 2010. Published by Elsevier B.V.

PY - 2010/8/16

Y1 - 2010/8/16

N2 - 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. Multiple-unit 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.

AB - 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. Multiple-unit 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.

KW - Administration, Oral

KW - Biological Availability

KW - Chemistry, Pharmaceutical

KW - Delayed-Action Preparations

KW - Drinking

KW - Drug Administration Schedule

KW - Eating

KW - Feeding Behavior

KW - Gastrointestinal Transit

KW - Humans

KW - Intestinal Absorption

KW - Pharmacokinetics

KW - Tablets, Enteric-Coated

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DO - 10.1016/j.ijpharm.2010.04.046

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JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

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