Solution-mediated phase transformation: significance during dissolution and implications for bioavailability

Journal of Pharmaceutical Sciences
Kristyn Greco, Robin Bogner

Abstract

Solubility improvement of poorly soluble drug compounds is a key approach to ensuring the successful development of many new drugs. Methods used to improve the solubility of drug compounds include forming a salt, cocrystal, or amorphous solid. These methods of improving solubility can often lead to a phenomenon called solution-mediated phase transformation, a phase change that is facilitated through exposure to solution. Solution-mediated phase transformation occurs in three steps: dissolution to create a supersaturated solution followed by nucleation of less soluble phase and the growth of that phase. When the growth of the less soluble phase occurs on the surface of the metastable solid, this phenomenon can cause a marked decrease in dissolution rate during in vitro dissolution evaluation, and ultimately in vivo. Therefore, transformation to a less soluble solid during dissolution is an important aspect to consider when evaluating approaches to increase the solubility of a poorly soluble drug. Identification of solution-mediated phase transformation during dissolution is reviewed for powder dissolution, rotating disk method, and channel flow-through apparatus. Types of solution-mediated phase transformation are described in t...Continue Reading

References

Sep 1, 1975·Journal of Pharmaceutical Sciences·A C Shah, K G Nelson
May 1, 1991·Journal of Pharmaceutical Sciences·W W Young, R Suryanarayanan
May 1, 1986·Journal of Pharmaceutical Sciences·J H de SmidtD J Crommelin
Oct 1, 1986·Chemical & Pharmaceutical Bulletin·E FukuokaS Yamamura
Jan 1, 1981·Journal of Pharmaceutical Sciences·K G MooneyV J Stella
Feb 1, 1980·Chemical & Pharmaceutical Bulletin·T MaedaT Noguchi
Jan 1, 1997·Journal of Pharmaceutical Sciences·B C Hancock, G Zografi
Mar 1, 1997·Journal of Pharmaceutical Sciences·V AndronisG Zografi
Jul 7, 1999·Journal of Pharmaceutical Sciences·N Rodríguez-Hornedo, D Murphy
Oct 9, 1999·Journal of Pharmaceutical Sciences·T KristmundsdóttirH Thormar
Dec 22, 1999·Angewandte Chemie·J BernsteinJ O Henck
Dec 22, 1999·International Journal of Pharmaceutics·Y KobayashiK Yamamoto
Feb 25, 2000·Journal of Pharmaceutical Sciences·J JinnoG L Amidon
Apr 18, 2000·International Journal of Pharmaceutics·G L EngelL L Winneroski
Jun 7, 2000·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·C Leuner, J Dressman
May 23, 2001·Advanced Drug Delivery Reviews·J Siepmann, N A Peppas
Jan 5, 2002·International Journal of Pharmaceutics·Duncan Q M Craig
Sep 25, 2002·International Journal of Pharmaceutics·D MurphyN Rodríguez-Hornedo
Dec 13, 2002·Drug Development and Industrial Pharmacy·Giovanni Filippo PalmieriSante Martelli
Dec 18, 2002·Journal of Pharmaceutical Sciences·Patrick A AnquetilIan W Hunter
Jan 18, 2003·Journal of Pharmaceutical Sciences·Wei SunMarylee Z Southard
Jan 6, 2004·Journal of Pharmaceutical Sciences·N Rodríguez-Hornedo, D Murphy
Jul 6, 2004·International Journal of Pharmaceutics·J KukuraF J Muzzio
Jul 14, 2004·Critical Reviews in Therapeutic Drug Carrier Systems·Aditya Mohan KaushalArvind Kumar Bansal
Jul 21, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·Jaap van der Weerd, Sergei G Kazarian
Nov 24, 2004·Pharmaceutical Research·Piyush GuptaArvind K Bansal
Feb 24, 2005·International Journal of Pharmaceutics·Jennifer L BaxterFernando J Muzzio
Mar 17, 2005·Journal of Pharmaceutical Sciences·Madhu Pudipeddi, Abu T M Serajuddin
Mar 22, 2005·International Journal of Pharmaceutics·Hirofumi TakeuchiYoshiaki Kawashima
Jul 30, 2005·Journal of Pharmaceutical Sciences·Jaap van der Weerd, Sergei G Kazarian
Sep 2, 2005·Journal of Pharmaceutical Sciences·Shoufeng LiAbu T M Serajuddin
Jun 6, 2006·Molecular Pharmaceutics·Naír Rodríguez-HornedoChristopher J Falkiewicz
Jul 13, 2006·Pharmaceutical Research·Daniel P McNamaraAeri Park
Aug 8, 2006·Journal of Pharmaceutical Sciences·Jaakko AaltonenJukka Rantanen
Jul 10, 2007·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Garima Chawla, Arvind K Bansal

❮ Previous
Next ❯

Citations

Sep 4, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Annika SarnesLeena Peltonen
Jun 4, 2013·International Journal of Pharmaceutics·Irena TomaszewskaNikoletta Fotaki
Dec 7, 2002·Lung Cancer : Journal of the International Association for the Study of Lung Cancer·Robert Pirker
Jul 2, 2014·Drug Development and Industrial Pharmacy·Marique AucampJosias Hamman
Feb 18, 2016·Journal of Pharmaceutical Sciences·Alfred C F RumondorFilippos Kesisoglou
Jan 18, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Johan P BoetkerBen Boyd
Nov 5, 2015·Drug Development and Industrial Pharmacy·Jiannan LuMichael A Repka
Dec 26, 2015·International Journal of Pharmaceutics·Marnus MilneMarique Elizabeth Aucamp
Nov 20, 2012·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Ning QiaoMingzhong Li
Apr 15, 2015·Advanced Drug Delivery Reviews·Amrit PaudelJukka Rantanen
Nov 12, 2013·The Journal of Pharmacy and Pharmacology·Elina TurunenPekka Jarho
Mar 4, 2015·AAPS PharmSciTech·Marnus MilneMarique Aucamp
Aug 5, 2016·Expert Opinion on Drug Delivery·Sophia Yui Kau FongMartin Brandl
Oct 28, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Jenniffer I Arenas-GarcíaHerbert Höpfl
Aug 12, 2014·Molecular Pharmaceutics·Yi Gao, Kenneth W Olsen
Mar 21, 2018·Pharmaceutical Development and Technology·Shahram EmamiMohammadreza Siahi-Shadbad
Nov 7, 2018·BioImpacts : BI·Shahram EmamiMohammad Barzegar-Jalali
Apr 21, 2018·Chemical Science·Qingying ZengAllan S Myerson
Jun 21, 2016·Chemical & Pharmaceutical Bulletin·Ken-Ichi IzutsuEtsuo Yonemochi
May 8, 2013·Angewandte Chemie·Kira B LandenbergerAdam J Matzger
Sep 25, 2018·Molecular Pharmaceutics·Dunja NovakovicClare J Strachan

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

International Journal of Pharmaceutics
Ranjit ThakuriaN Rodríguez-Hornedo
European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Ning QiaoMingzhong Li
International Journal of Pharmaceutics
David P ElderHeidi Lopez de Diego
© 2021 Meta ULC. All rights reserved