Approaches to increase mechanistic understanding and aid in the selection of precipitation inhibitors for supersaturating formulations – a PEARRL review
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Authors
Koehl, Niklas
Tsakiridou, Georgia
Nair, Anita
Holm, Rene
Dressman, Jennifer
Saal, Christoph
Author (Corporation)
Publication date
05/2018
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Type
01A - Journal article
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Parent work
Journal of Pharmacy and Pharmacology
Special issue
DOI of the original publication
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Volume
71
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Publisher / Publishing institution
Wiley
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Abstract
Objectives
Supersaturating formulations hold great promise for delivery of poorly soluble active pharmaceutical ingredients (APIs). To profit from supersaturating formulations, precipitation is hindered with precipitation inhibitors (PIs), maintaining drug concentrations for as long as possible. This review provides a brief overview of supersaturation and precipitation, focusing on precipitation inhibition. Trial‐and‐error PI selection will be examined alongside established PI screening techniques. Primarily, however, this review will focus on recent advances that utilise advanced analytical techniques to increase mechanistic understanding of PI action and systematic PI selection.
Key findings
Advances in mechanistic understanding have been made possible by the use of analytical tools such as spectroscopy, microscopy and mathematical and molecular modelling, which have been reviewed herein. Using these techniques, PI selection can be guided by molecular rationale. However, more work is required to see widespread application of such an approach for PI selection.
Summary
Precipitation inhibitors are becoming increasingly important in enabling formulations. Trial‐and‐error approaches have seen success thus far. However, it is essential to learn more about the mode of action of PIs if the most optimal formulations are to be realised. Robust analytical tools, and the knowledge of where and how they can be applied, will be essential in this endeavour.
Keywords
controlled ans sustained release systems, development of novel analytical techniques, dosage from design and characterisation, pharmaceutical analysis, pharmaceutics and drug discovery
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ISBN
ISSN
0022-3573
2042-7158
2042-7158
Language
English
Created during FHNW affiliation
Yes
Strategic action fields FHNW
Publication status
Published
Review
Peer review of the complete publication
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Citation
PRICE, Daniel J., Felix DITZINGER, Niklas KOEHL, Sandra JANKOVIC, Georgia TSAKIRIDOU, Anita NAIR, Rene HOLM, Martin KUENTZ, Jennifer DRESSMAN und Christoph SAAL, 2018. Approaches to increase mechanistic understanding and aid in the selection of precipitation inhibitors for supersaturating formulations – a PEARRL review. Journal of Pharmacy and Pharmacology. Mai 2018. Bd. 71. DOI 10.1111/jphp.12927. Verfügbar unter: http://hdl.handle.net/11654/27323