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. 2023 Nov 7;25(6):103.
doi: 10.1208/s12248-023-00865-8.

Drug Dissolution in Oral Drug Absorption: Workshop Report

Kimberly Raines  1 , Payal Agarwal  1 , Patrick Augustijns  2 , Alaadin Alayoubi  1 , Lucas Attia  3 , Annette Bauer-Brandl  4 , Martin Brandl  4 , Parnali Chatterjee  1 , Hansong Chen  1 , Yuly Chiang Yu  5 , Carrie Coutant  6 , Ana Luisa Coutinho  5 , David Curran  7 , Jennifer Dressman  8 , Bryan Ericksen  1 , Leah Falade  1 , Yi Gao  9 , Zongming Gao  10 , Debasis Ghosh  1 , Tapash Ghosh  1 , Anitha Govada  1 , Elizabeth Gray  1 , Ruiqiong Guo  11 , Dana Hammell  5 , Andre Hermans  12 , Rohit Jaini  13 , Hanlin Li  14 , Haritha Mandula  1 , Shuaiqian Men  5 , Johanna Milsmann  15 , Huong Moldthan  1 , Rebecca Moody  1 , Dana E Moseson  16 , Anette Müllertz  17 , Roshni Patel  5 , Kalpana Paudel  1 , Christos Reppas  18 , Rajesh Savkur  1 , Kerstin Schaefer  15 , Abu Serajuddin  19 , Lynne S Taylor  20 , Rutu Valapil  5 , Kevin Wei  1 , Werner Weitschies  21 , Shinji Yamashita  22 , James E Polli  23
Affiliations

Drug Dissolution in Oral Drug Absorption: Workshop Report

Kimberly Raines et al. AAPS J. .

Abstract

The in-person workshop "Drug Dissolution in Oral Drug Absorption" was held on May 23-24, 2023, in Baltimore, MD, USA. The workshop was organized into lectures and breakout sessions. Three common topics that were re-visited by various lecturers were amorphous solid dispersions (ASDs), dissolution/permeation interplay, and in vitro methods to predict in vivo biopharmaceutics performance and risk. Topics that repeatedly surfaced across breakout sessions were the following: (1) meaning and assessment of "dissolved drug," particularly of poorly water soluble drug in colloidal environments (e.g., fed conditions, ASDs); (2) potential limitations of a test that employs sink conditions for a poorly water soluble drug; (3) non-compendial methods (e.g., two-stage or multi-stage method, dissolution/permeation methods); (4) non-compendial conditions (e.g., apex vessels, non-sink conditions); and (5) potential benefit of having both a quality control method for batch release and a biopredictive/biorelevant method for biowaiver or bridging scenarios. An identified obstacle to non-compendial methods is the uncertainty of global regulatory acceptance of such methods.

Keywords: absorption; amorphous; dissolution; food; permeability; solubility.

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References

    1. Kramer SF, Flynn GL. Solubility of organic hydrochlorides. J Pharm Sci. 1972;61(12):1896–904. https://doi.org/10.1002/jps.2600611203 . - DOI - PubMed
    1. Singh S, Parikh T, Sandhu HK, Shah NH, Malick AW, Singhal D, et al. Supersolubilization and amorphization of a model basic drug, haloperidol, by interaction with weak acids. Pharm Res. 2013;30(6):1561–73. https://doi.org/10.1007/s11095-013-0994-7 . - DOI - PubMed
    1. Parikh T, Sandhu HK, Talele TT, Serajuddin AT. Characterization of solid dispersion of itraconazole prepared by solubilization in concentrated aqueous solutions of weak organic acids and drying. Pharm Res. 2016;33(6):1456–71. https://doi.org/10.1007/s11095-016-1890-8 . - DOI - PubMed
    1. Parikh T, Serajuddin ATM. Development of fast-dissolving amorphous solid dispersion of itraconazole by melt extrusion of its mixture with weak organic carboxylic acid and polymer. Pharm Res. 2018;35(7):127. https://doi.org/10.1007/s11095-018-2407-4 . - DOI - PubMed
    1. Tho I, Liepold B, Rosenberg J, Maegerlein M, Brandl M, Fricker G. Formation of nano/micro-dispersions with improved dissolution properties upon dispersion of ritonavir melt extrudate in aqueous media. Eur J Pharm Sci. 2010;40(1):25–32. https://doi.org/10.1016/j.ejps.2010.02.003 . - DOI - PubMed

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