The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations

Research output: Contribution to journalJournal articlepeer-review

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The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations. / Khan, Jamal; Rades, Thomas; Boyd, Ben.

In: Pharmaceutical Research, Vol. 33, No. 3, 03.2016, p. 548-62.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Khan, J, Rades, T & Boyd, B 2016, 'The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations', Pharmaceutical Research, vol. 33, no. 3, pp. 548-62. https://doi.org/10.1007/s11095-015-1829-5

APA

Khan, J., Rades, T., & Boyd, B. (2016). The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations. Pharmaceutical Research, 33(3), 548-62. https://doi.org/10.1007/s11095-015-1829-5

Vancouver

Khan J, Rades T, Boyd B. The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations. Pharmaceutical Research. 2016 Mar;33(3):548-62. https://doi.org/10.1007/s11095-015-1829-5

Author

Khan, Jamal ; Rades, Thomas ; Boyd, Ben. / The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations. In: Pharmaceutical Research. 2016 ; Vol. 33, No. 3. pp. 548-62.

Bibtex

@article{cdd3f82acb284530ae5325e1ddd217cc,
title = "The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations",
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 = "Biological Availability, Chemistry, Pharmaceutical, Digestion, Humans, Intestine, Small, Lipids, Pharmaceutical Preparations, Solubility, Water, Journal Article, Research Support, Non-U.S. Gov't, Review",
author = "Jamal Khan and Thomas Rades and Ben Boyd",
year = "2016",
month = mar,
doi = "10.1007/s11095-015-1829-5",
language = "English",
volume = "33",
pages = "548--62",
journal = "Pharmaceutical Research",
issn = "0724-8741",
publisher = "Springer",
number = "3",

}

RIS

TY - JOUR

T1 - The Precipitation Behavior of Poorly Water-Soluble Drugs with an Emphasis on the Digestion of Lipid Based Formulations

AU - Khan, Jamal

AU - Rades, Thomas

AU - Boyd, Ben

PY - 2016/3

Y1 - 2016/3

N2 - 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.

AB - 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.

KW - Biological Availability

KW - Chemistry, Pharmaceutical

KW - Digestion

KW - Humans

KW - Intestine, Small

KW - Lipids

KW - Pharmaceutical Preparations

KW - Solubility

KW - Water

KW - Journal Article

KW - Research Support, Non-U.S. Gov't

KW - Review

U2 - 10.1007/s11095-015-1829-5

DO - 10.1007/s11095-015-1829-5

M3 - Journal article

C2 - 26597939

VL - 33

SP - 548

EP - 562

JO - Pharmaceutical Research

JF - Pharmaceutical Research

SN - 0724-8741

IS - 3

ER -

ID: 169414363