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

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

doi:10.1016/j.ijpharm.2010.04.046

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 journal › Review article › peer-review

93 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.

Original language	English
Pages (from-to)	26-36
Number of pages	11
Journal	International Journal of Pharmaceutics
Volume	395
Issue number	1-2
Early online date	28 May 2010
DOIs	https://doi.org/10.1016/j.ijpharm.2010.04.046
Publication status	Published - 16 Aug 2010
Externally published	Yes

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10.1016/j.ijpharm.2010.04.046

93 Citations
1 Chapter

Basic Pharmacokinetics
Merchant, H., 13 Jan 2022, Biopharmaceutics: From Fundamentals to Industrial Practice. Batchelor, H. (ed.). 1st ed. Chichester, UK: John Wiley & Sons, Ltd, p. 9-29 21 p. (Advances in Pharmaceutical Technology).
Research output: Chapter in Book/Report/Conference proceeding › Chapter › peer-review

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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author = "Varum, {Felipe J O} and Merchant, {Hamid A} and Basit, {Abdul W}",

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language = "English",

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T2 - the relationship between gastrointestinal transit and drug absorption

AU - Varum, Felipe J O

AU - Merchant, Hamid A

AU - Basit, Abdul W

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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

U2 - 10.1016/j.ijpharm.2010.04.046

DO - 10.1016/j.ijpharm.2010.04.046

M3 - Review article

C2 - 20546855

VL - 395

SP - 26

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JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

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

Abstract

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Research output

Basic Pharmacokinetics

Cite this