Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery

Bioorganic & Medicinal Chemistry Letters
Sonali S Bharate, Ram A Vishwakarma

Abstract

An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates. Despite of the availability of multiple solubility estimation methods, none of the reported method involves simplified fixed protocol for diverse set of compounds. Therefore, a simple and medium-throughput solubility estimation protocol is highly desirable during lead optimization stage. The present work introduces a rapid method for assessment of thermodynamic equilibrium solubility of compounds in aqueous media using 96-well microplate. The developed protocol is straightforward to set up and takes advantage of the sensitivity of UV spectroscopy. The compound, in stock solution in methanol, is introduced in microgram quantities into microplate wells followed by drying at an ambient temperature. Microplates were shaken upon addition of test media and the supernatant was analyzed by UV method. A plot of absorbance versus concentration of a sample provides saturation point, which is thermodynamic equilibrium solubility of a sample. The established protocol was validated using a large panel of commercially available drugs and with conventional miniaturized shake flask met...Continue Reading

References

Mar 29, 2001·Journal of Pharmacological and Toxicological Methods·C A Lipinski
Dec 10, 2002·Combinatorial Chemistry & High Throughput Screening·Teng-Man ChenChegnyue Zhu
Jun 30, 2007·Advanced Drug Delivery Reviews·J B DressmanC Reppas
Mar 29, 2013·Expert Opinion on Drug Delivery·Sonali S Bharate, Ram A Vishwakarma
Dec 1, 2004·Drug Discovery Today. Technologies·Christopher A Lipinski

❮ Previous
Next ❯

Citations

Aug 2, 2016·European Journal of Medicinal Chemistry·Rammohan R YadavSandip B Bharate
Jul 17, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Vikas KumarRam A Vishwakarma
Jun 9, 2015·Chemical Communications : Chem Comm·Anyanee Kamkaew, Kevin Burgess
Apr 22, 2015·Organic & Biomolecular Chemistry·Baljinder SinghRam A Vishwakarma
Sep 13, 2019·Drug Development and Industrial Pharmacy·Ardita VeseliAlbin Kristl
Dec 20, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yukang MaoHuicai Huang
Jan 27, 2018·Journal of Medicinal Chemistry·Sandip B BharateRam A Vishwakarma
Aug 14, 2018·Bioconjugate Chemistry·Zhengyang JiangKevin Burgess

❮ 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

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Bruno BardPierre-Alain Carrupt
© 2022 Meta ULC. All rights reserved