Haste Makes Waste: The Interplay Between Dissolution and Precipitation of Supersaturating Formulations

The AAPS Journal
Dajun D Sun, Ping I Lee

Abstract

Contrary to the early philosophy of supersaturating formulation design for oral solid dosage forms, current evidence shows that an exceedingly high rate of supersaturation generation could result in a suboptimal in vitro dissolution profile and subsequently could reduce the in vivo oral bioavailability of amorphous solid dispersions. In this commentary, we outline recent research efforts on the specific effects of the rate and extent of supersaturation generation on the overall kinetic solubility profiles of supersaturating formulations. Additional insights into an appropriate definition of sink versus nonsink dissolution conditions and the solubility advantage of amorphous pharmaceuticals are also highlighted. The interplay between dissolution and precipitation kinetics should be carefully considered in designing a suitable supersaturating formulation to best improve the dissolution behavior and oral bioavailability of poorly water-soluble drugs.

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Citations

Aug 5, 2016·Expert Opinion on Drug Delivery·Sophia Yui Kau FongMartin Brandl
Nov 20, 2016·Drug Delivery and Translational Research·Emilia SawickiNeeltje Steeghs
Jan 8, 2021·International Journal of Pharmaceutics: X·Christian LuebbertGabriele Sadowski
Mar 30, 2021·International Journal of Pharmaceutics·Mario A Cano-VegaRodolfo Pinal
Jun 22, 2021·International Journal of Pharmaceutics: X·Afroditi KapouraniPanagiotis Barmpalexis
Jul 4, 2021·International Journal of Pharmaceutics·Giovanna C R M Schver, Ping I Lee
Dec 7, 2019·Molecular Pharmaceutics·Peter J SkrdlaPhilip C Dell'Orco
Aug 23, 2021·International Journal of Pharmaceutics·Nikola PešićDjordje Medarević
Oct 2, 2021·AAPS PharmSciTech·Gayathri Ramachandran, M S Sudheesh

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