Lipids in the Stomach – Implications for the Evaluation of Food Effects on Oral Drug Absorption

Autor: Mirko Koziolek, Frédéric Carrière, Christopher J.H. Porter
Přispěvatelé: Enzymologie interfaciale et de physiologie de la lipolyse (EIPL), Centre National de la Recherche Scientifique (CNRS)-Aix Marseille Université (AMU), Bioénergétique et Ingénierie des Protéines (BIP ), Aix Marseille Université (AMU)-Centre National de la Recherche Scientifique (CNRS), Monash Institute of Pharmaceutical Science
Jazyk: angličtina
Rok vydání: 2018
Předmět:
0301 basic medicine
Drug
Absorption (pharmacology)
Gastric lipolysis
in vitro digestion
media_common.quotation_subject
Pharmaceutical Science
Administration
Oral
Biological Availability
Pharmacology
030226 pharmacology & pharmacy
lipids
03 medical and health sciences
Food-Drug Interactions
0302 clinical medicine
Pharmacotherapy
food effect
Medicine
Humans
Pharmacology (medical)
Gastric lipase
media_common
Gastric Absorption
Gastrointestinal tract
milk
Gastric Juice
business.industry
Stomach
Organic Chemistry
digestive
oral
and skin physiology
Lipase
Hydrogen-Ion Concentration
biorelevant dissolution
[SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences
human gastric lipase
Dietary Fats
3. Good health
Bioavailability
Drug Liberation
030104 developmental biology
medicine.anatomical_structure
Gastric Mucosa
Molecular Medicine
lipids (amino acids
peptides
and proteins)
business
Lipid digestion
Biotechnology
Zdroj: Pharmaceutical Research
Pharmaceutical Research, American Association of Pharmaceutical Scientists, 2018, 35 (3), ⟨10.1007/s11095-017-2289-x⟩
Pharmaceutical Research, 2018, 35 (3), ⟨10.1007/s11095-017-2289-x⟩
ISSN: 0724-8741
1573-904X
DOI: 10.1007/s11095-017-2289-x⟩
Popis: International audience; Food effects on oral drug bioavailability can have significant impact on the provision of safe and reliable oral pharmacotherapy. A mechanistic understanding of the events that contribute to the occurrence of food effects is therefore critical. An increased oral bioavailability is often seen for poorly water-soluble drugs after co-administration with lipids, including lipids in food, and is commonly explained by the ability of lipids to enhance drug solubility in intestinal luminal fluids. In contrast, the impact of lipids on drug solubilisation in the stomach has received less attention. This is in spite of the fact that lipid digestion is initiated in the stomach by human gastric lipase and that gastric events also initiate emulsification of lipids in the gastrointestinal tract. The stomach therefore acts to ‘pre-process’ lipids for subsequent events in the intestine and may significantly affect downstream events at intestinal drug absorption sites. In this article, the mechanisms by which lipids are processed in the stomach are reviewed and the potential impact of these processes on drug absorption discussed. Attention is also focused on in vitro methods that are used to assess gastric processing of lipids and their application to better understand food effects on drug release and absorption.
Databáze: OpenAIRE
Externí odkaz: