Influence of excipients on solubility and dissolution of pharmaceuticals

International Journal of Pharmaceutics
Raphael PausYuanhui Ji

Abstract

In this work, solubilities and dissolution profiles of the active pharmaceutical ingredients (APIs) indomethacin and naproxen were measured in water in the presence of one excipient out of polyethylene glycol (PEG) 2000, 6000 and 12000, polyvinylpyrrolidone (PVP) K 25 and mannitol. It was found that the solubility of indomethacin and naproxen was increased with an addition of the selected excipients, which was also predicted by the perturbed-chain statistical associating fluid theory (PC-SAFT). The two-step chemical-potential-gradient model was applied to investigate the dissolution mechanism of indomethacin and naproxen in water in the presence of the excipient. It was found that the dissolution mechanisms of indomethacin and naproxen were changed by the presence of excipients. Although the solubility of the API was increased by the addition of excipients, the dissolution rate of the API was decreased in some cases. This was mainly due to the combination of the molecular interactions between the API and the polymer with the influence of the excipients on the kinetic part (rate constant of the surface reaction or diffusion of the API or both) of API dissolution as function of PEG molar mass as well as of the API type. Based upo...Continue Reading

References

Jan 1, 1981·Journal of Pharmaceutical Sciences·K G MooneyV J Stella
Jan 1, 1981·Journal of Pharmaceutical Sciences·K G MooneyV J Stella
Apr 1, 1981·Journal of Pharmaceutical Sciences·D E Cadwallader, D K Madan
Jun 1, 1997·Journal of Pharmaceutical Sciences·L P de AlmeidaM Figueiredo
Jan 7, 1999·Drug Development and Industrial Pharmacy·M C Tros de IlarduyaM C Martínez-Ohárriz
Apr 12, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·P Costa, J M Sousa Lobo
Dec 31, 2003·International Journal of Pharmaceutics·Hemant N JoshiAbu T M Serajuddin
Jan 17, 2007·Journal of Pharmaceutical and Biomedical Analysis·Jianmei D KochlingEda Ross Montgomery
Mar 14, 2009·Journal of Pharmaceutical Sciences·Feelly Ruether, Gabriele Sadowski
Apr 11, 2009·Journal of Controlled Release : Official Journal of the Controlled Release Society·Maike WindbergsPeter Kleinebudde
Jun 27, 2012·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Sofia A PapadimitriouDimitrios N Bikiaris
May 30, 2014·Molecular Pharmaceutics·Anke PrudicGabriele Sadowski
Oct 9, 2014·Molecular Pharmaceutics·Anke PrudicGabriele Sadowski
Feb 27, 2015·Pharmaceutical Research·Yuanhui JiGabriele Sadowski
Mar 21, 2015·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Anke PrudicGabriele Sadowski
Jun 29, 2015·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Anke PrudicGabriele Sadowski

❮ Previous
Next ❯

Citations

Dec 25, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·David P ElderRené Holm
Jul 15, 2015·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Raphael PausYuanhui Ji
Jan 31, 2017·International Journal of Pharmaceutics·Sirima SoodvilaiPraneet Opanasopit
Feb 18, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Christian LuebbertGabriele Sadowski
Jan 7, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Daniel M WaldenJyotika Varshney
Oct 20, 2018·Molecular Pharmaceutics·Christian LuebbertGabriele Sadowski
Oct 21, 2017·Molecular Pharmaceutics·Kristin LehmkemperGabriele Sadowski

❮ 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

Pharmaceutical Development and Technology
Stefania BaldursdottirJukka Rantanen
European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Anke PrudicGabriele Sadowski
© 2022 Meta ULC. All rights reserved