Solubility of E2050 at various pH: a case in which apparent solubility is affected by the amount of excess solid

Journal of Pharmaceutical Sciences
Zeren WangWilliam J Lambert

Abstract

The solubility of E2050, supplied as a dihydrochloride salt, in aqueous solutions at different pHs was studied. Two pK(a)s controlling the equilibrium between the various protonated species were determined. The solubility-pH profile of E2050 is expected to be high in acidic solutions because protonated species are formed and to be low in alkaline conditions due to the formation of hydrophobic free base. The solubility is also affected by chloride ion, a common ion for this drug substance. Two solubility products (K(sp)) were determined corresponding to the solubility of di-HCl salt and mono-HCl salt. Based on the pK(a)s (3.10 and 7.71), the solubility products with chloride (2.92 and 3.77 as corresponding pK(sp)), and the solubility of free base (2 x 10(-5) M), the solubility in solutions with different pH and different levels of chloride ion can be predicted. The prediction of the solubility change during the dilution of E2050 parenteral formulations by saline was also demonstrated. Furthermore, the present study presents an interesting example in which an apparent solubility can be different if varying (excess) amounts of salt are added to the solution. In this case, excess chloride ion suppresses the solubility in the pH reg...Continue Reading

References

May 1, 1948·Journal of the American Chemical Society·R H STOKES, R A ROBINSON

❮ Previous
Next ❯

Citations

Jan 30, 2008·Journal of Pharmaceutical Sciences·Amit KokateBhaskara R Jasti
Jul 3, 2007·Advanced Drug Delivery Reviews·Jochem Alsenz, Manfred Kansy
Oct 24, 2006·Drug Discovery Today·Shobha N BhattacharJames A Wesley
Jul 12, 2016·Journal of Pharmaceutical Sciences·Rodrigo Cristofoletti, Jennifer B Dressman
Feb 6, 2017·Journal of Pharmaceutical Sciences·Yan HeEdward Orton
Apr 11, 2017·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Alex Avdeef
Sep 1, 2005·Pharmaceutical Research·Kohsaku KawakamiYasuo Ida
Feb 7, 2013·Pharmacological Reviews·Hywel D WilliamsChristopher J H Porter
Sep 13, 2019·Drug Development and Industrial Pharmacy·Ardita VeseliAlbin Kristl
May 1, 2010·Pharmaceutical Development and Technology·Sharad B MurdandeRobin H Bogner

❮ 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.

© 2021 Meta ULC. All rights reserved