A retrospective biopharmaceutical analysis of >800 approved oral drug products: Are drug properties of solid dispersions and lipid-based formulations distinctive?

Show simple item record

dc.contributor.author Bennett-Lenane, Harriet
dc.contributor.author O'Shea, Joseph P.
dc.contributor.author O'Driscoll, Caitriona M.
dc.contributor.author Griffin, Brendan T.
dc.date.accessioned 2020-09-10T07:31:49Z
dc.date.available 2020-09-10T07:31:49Z
dc.date.issued 2020-08-19
dc.identifier.citation Bennett-Lenane, H., O'Shea, J. P., O'Driscoll, C. M. and Griffin, B. T. (2020) 'A retrospective biopharmaceutical analysis of >800 approved oral drug products: Are drug properties of solid dispersions and lipid-based formulations distinctive?', Journal of Pharmaceutical Sciences. doi: 10.1016/j.xphs.2020.08.008 en
dc.identifier.issn 0022-3549
dc.identifier.uri http://hdl.handle.net/10468/10498
dc.identifier.doi 10.1016/j.xphs.2020.08.008 en
dc.description.abstract Increasing numbers of poorly water soluble drugs in development has intensified need for bio-enabling formulations including Lipid-Based Formulations (LBF) and Solid Dispersions (SD). Resultantly, a data-driven approach is required to increase formulation development efficiency. This review provides a retrospective analysis of molecular and biopharmaceutical properties of drugs commercialised as LBFs or SDs. A comprehensive stepwise statistical analysis of LBF and SD drug properties was conducted and compared to drugs not commercialised via either technology (Others), aiming to identify key predictors of successful formulation development. This review demonstrates LBF and SD drugs differ significantly in molecular weight, polar surface area, rotatable bonds and hydrogen bond acceptor count. Meanwhile, LBF and SD drugs display significantly different aqueous solubility, lipophilicity, size, molecular flexibility, hydrogen bonding capacity and rule-of-5 violations versus Others. LBF and SDs were 3 and 5 times more likely to display >1 rule-of-5 violation versus Others, over 55% of LBF drugs exceeded the reported melting point guide of 10 Hydrogen Bond Acceptors. Overall, by focusing on successfully commercialised drugs, this review provides improved understanding of links between drug properties and successful SD/LBF approaches, providing a framework for guiding pharmaceutical development on formulation approaches. en
dc.description.sponsorship Irish Research Council (Post Graduate Scholarship Project Number: GOIPG/2018/883) en
dc.format.mimetype application/pdf en
dc.language.iso en en
dc.publisher Elsevier Inc. en
dc.rights © 2020, American Pharmacists Association®. Published by Elsevier Inc. All rights reserved. This manuscript version is made available under the CC BY-NC-ND 4.0 license. en
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/ en
dc.subject Solid dispersion(s) en
dc.subject Lipid-based formulation(s) en
dc.subject Poorly water-soluble drug(s) en
dc.subject Formulation en
dc.subject Drug-like property(s) en
dc.subject Amorphous solid dispersion(s) (ASD) en
dc.subject Bioavailability en
dc.subject Drug delivery systems en
dc.title A retrospective biopharmaceutical analysis of >800 approved oral drug products: Are drug properties of solid dispersions and lipid-based formulations distinctive? en
dc.type Article (peer-reviewed) en
dc.internal.authorcontactother Brendan Griffin, Pharmacy, University College Cork, Cork, Ireland. +353-21-490-3000 Email: brendan.griffin@ucc.ie en
dc.internal.availability Full text available en
dc.check.info Access to this article is restricted until 12 months after publication by request of the publisher. en
dc.check.date 2021-08-19
dc.date.updated 2020-09-10T07:19:28Z
dc.description.version Accepted Version en
dc.internal.rssid 536050961
dc.internal.pmid 32822721
dc.contributor.funder Irish Research Council en
dc.description.status Peer reviewed en
dc.identifier.journaltitle Journal of Pharmaceutical Sciences en
dc.internal.copyrightchecked Yes
dc.internal.licenseacceptance Yes en
dc.internal.IRISemailaddress brendan.griffin@ucc.ie en
dc.internal.bibliocheck In press. Check vol / issue / page range. Amend citation as necessary. en
dc.identifier.eissn 1520-6017


Files in this item

This item appears in the following Collection(s)

Show simple item record

© 2020, American Pharmacists Association®. Published by Elsevier Inc. All rights reserved. This manuscript version is made available under the CC BY-NC-ND 4.0 license. Except where otherwise noted, this item's license is described as © 2020, American Pharmacists Association®. Published by Elsevier Inc. All rights reserved. This manuscript version is made available under the CC BY-NC-ND 4.0 license.
This website uses cookies. By using this website, you consent to the use of cookies in accordance with the UCC Privacy and Cookies Statement. For more information about cookies and how you can disable them, visit our Privacy and Cookies statement