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Type: Journal article
Title: The precipitation behavior of poorly water-soluble drugs with an emphasis on the digestion of lipid based formulations
Author: Khan, J.
Rades, T.
Boyd, B.
Citation: Pharmaceutical Research, 2016; 33(3):548-562
Publisher: Springer
Issue Date: 2016
ISSN: 0724-8741
Statement of
Jamal Khan, Thomas Rades, Ben Boyd
Abstract: An increasing number of newly discovered drugs are poorly water-soluble and the use of natural and synthetic lipids to improve the oral bioavailability of these drugs by utilizing the digestion pathway in-vivo has proved an effective formulation strategy. The mechanisms responsible for lipid digestion and drug solubilisation during gastrointestinal transit have been explored in detail, but the implications of drug precipitation beyond the potential adverse effect on bioavailability have received attention only in recent years. Specifically, these implications are that different solid forms of drug on precipitation may affect the total amount of drug absorbed in-vivo through their different physico-chemical properties, and the possibility that the dynamic environment of the small intestine may afford re-dissolution of precipitated drug if present in a high-energy form. This review describes the events that lead to drug precipitation during the dispersion and digestion of lipid based formulations, common methods used to inhibit precipitation, as well as conventional and newly emerging characterization techniques for studying the solid state form of the precipitated drug. Moreover, selected case studies are discussed where drug precipitation has ensued from the digestion of lipid based formulations, as well as the apparent link between drug ionisability and altered solid forms on precipitation, culminating in a discussion about the importance of the solid form on precipitation with relevance to the total drug absorbed.
Keywords: Digestion; lipids; lipolysis; poorly water-soluble drugs; precipitation; solid state
Rights: © Springer Science+Business Media New York 2015
DOI: 10.1007/s11095-015-1829-5
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