Evaluation of drug load and polymer by using a 96-well plate vacuum dry system for amorphous solid dispersion drug delivery.

AAPS PharmSciTech
Po-Chang ChiangRyan Hart

Abstract

It is well recognized that poor dissolution rate and solubility of drug candidates are key limiting factors for oral bioavailability. While numerous technologies have been developed to enhance solubility of the drug candidates, poor water solubility continuously remains a challenge for drug delivery. Among those technologies, amorphous solid dispersions (SD) have been successfully employed to enhance both dissolution rate and solubility of poorly water-soluble drugs. This research reports a high-throughput screening technology developed by utilizing a 96-well plate system to identify optimal drug load and polymer using a solvent casting approach. A minimal amount of drug was required to evaluate optimal drug load in three different polymers with respect to solubility improvement and solid-state stability of the amorphous drug-polymer system. Validation of this method was demonstrated with three marketed drugs as well as with one internal compound. Scale up of the internal compound SD by spray drying further confirmed the validity of this method, and its quality was comparable to a larger scale process. Here, we demonstrate that our system is highly efficient, cost-effective, and robust to evaluate the feasibility of spray dryin...Continue Reading

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Citations

Apr 27, 2013·International Journal of Pharmaceutics·Qingyan HuHarpreet Sandhu
Jul 23, 2013·International Journal of Pharmaceutics·Paul T WhitesideClive J Roberts
Jul 16, 2015·Journal of Pharmaceutical Sciences·Yan He, Chris Ho
Feb 12, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Nicole WyttenbachSusanne Page
Jul 23, 2015·International Journal of Pharmaceutics·Kentaro NaganeHiromitsu Yamamoto
Mar 31, 2015·Journal of Materials Science. Materials in Medicine·Junjie YuanYouzhuan Xie
Feb 19, 2015·Therapeutic Delivery·Ann NewmanRobert Wenslow
May 31, 2016·Journal of Pharmaceutical Sciences·Po-Chang ChiangLaurent Salphati
Jul 2, 2014·Analytical Chemistry·Joana RomãoJonas Baltrusaitis
May 10, 2017·International Journal of Molecular Sciences·Luyuan ChenJie Gao
May 20, 2017·Pharmaceutical Research·Khadijah EduengChristel A S Bergström
Sep 20, 2017·AAPS PharmSciTech·Siyuan Huang, Robert O Williams
Oct 12, 2018·Pharmaceutical Development and Technology·Aymeric OussetKalliopi Dodou
May 15, 2019·Pharmaceutics·Ann-Christin JacobsenAnnette Bauer-Brandl
May 7, 2019·Pharmaceutical Development and Technology·Sadegh Poozesh, Seid Mahdi Jafari
Sep 3, 2019·Chemical & Pharmaceutical Bulletin·Satoshi TanidaYuichi Tozuka
Nov 27, 2020·Advanced Drug Delivery Reviews·Rahul UpadhyaAdam J Gormley

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