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A Retrospective Biopharmaceutical Analysis of800 Approved Oral Drug Products: Are Drug Properties of Solid Dispersions and Lipid-Based Formulations Distinctive?
- Source :
- Journal of pharmaceutical sciences. 109(11)
- Publication Year :
- 2020
-
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 display1 rule-of-5 violation versus Others, over 55% of LBF drugs exceeded the reported melting point guide of150 °C, while 24% of SD drugs contained10 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.
- Subjects :
- Drug
Bioavailability
media_common.quotation_subject
Pharmaceutical Science
Biological Availability
02 engineering and technology
030226 pharmacology & pharmacy
Polar surface area
03 medical and health sciences
0302 clinical medicine
Drug-like property(s)
Lipid-based formulation(s)
Retrospective analysis
Statistical analysis
Solid dispersion(s)
media_common
Retrospective Studies
Biological Products
Chemistry
021001 nanoscience & nanotechnology
Combinatorial chemistry
Lipids
Drug delivery systems
Biopharmaceutical
Poorly water-soluble drug(s)
Formulation
Pharmaceutical Preparations
Solubility
Lipophilicity
0210 nano-technology
Amorphous solid dispersion(s) (ASD)
Oral retinoid
Subjects
Details
- ISSN :
- 15206017
- Volume :
- 109
- Issue :
- 11
- Database :
- OpenAIRE
- Journal :
- Journal of pharmaceutical sciences
- Accession number :
- edsair.doi.dedup.....cefe5c6817789104437bf3c4506cd823