Preformulation and pharmacokinetic studies on antalarmin: a novel stress inhibitor

Journal of Pharmaceutical Sciences
Ritesh SanghviSamuel H Yalkowsky

Abstract

The preformulation, solubilization and pharmacokinetic evaluation of antalarmin, a stress inhibitor, have been conducted. Antalarmin has a poor water solubility of less than 1 microg/mL and is weakly basic with an experimentally determined pK(a) of 5.0. Multiple solubilization approaches including pH-control either alone or in combination with cosolvents, surfactants and complexing agents have been investigated. The applicability of lipid-based systems has also been explored. Four formulations, each with a targeted drug loading capacity of 100 mg/mL, show potential for oral administration. Three of these formulations are aqueous solutions (10% ethanol + 40% propylene glycol; 20% cremophor EL; 20% sulfobutylether-beta-cyclodextrin) each buffered at pH 1. The fourth formulation is a lipid-based formulation comprising of 20% oleic acid, 40% cremophor EL and 40% Labrasol. No precipitation was observed following dilution of the four formulations with water and enzyme free simulated gastric fluid. However, only the lipid-based formulation successfully resisted drug precipitation following dilution with enzyme free simulated intestinal fluid. Pharmacokinetic analysis conducted in rats revealed that the 20% cremophor EL solution formul...Continue Reading

References

Aug 1, 1981·Journal of Pharmaceutical Sciences·S H Yalkowsky
Dec 6, 2000·Advanced Drug Delivery Reviews·M J Lawrence, G D Rees
Aug 8, 2001·International Journal of Pharmaceutics·N JainS H Yalkowsky
Dec 14, 2002·International Journal of Pharmaceutics·Y V Rama PrasadKanji Takada
Dec 31, 2003·International Journal of Pharmaceutics·Hemant N JoshiAbu T M Serajuddin
Dec 1, 2004·Journal of Pharmaceutical Sciences·Yingqing RanSamuel H Yalkowsky
Mar 24, 2005·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Xianyi ShaXiaoling Fang
Jul 4, 2006·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Colin W Pouton
Dec 6, 2006·International Journal of Pharmaceutics·Ritesh SanghviSamuel H Yalkowsky
Jan 18, 2007·Journal of Agricultural and Food Chemistry·Chen Zhang, Kenneth S Suslick
Mar 3, 2007·Nature Reviews. Drug Discovery·Christopher J H PorterWilliam N Charman
Jul 10, 2007·Advanced Drug Delivery Reviews·David J Hauss

❮ Previous
Next ❯

Citations

Feb 12, 2014·Journal of Pharmaceutical Sciences·Cordula StillhartMartin Kuentz
Apr 19, 2011·International Journal of Pharmaceutics·Alexei MerzlikineTakashi Mano
Feb 7, 2013·Pharmacological Reviews·Hywel D WilliamsChristopher J H Porter
Feb 6, 2019·Advances in Pharmacological Sciences·Mervin Chávez-CastilloJoselyn Rojas-Quintero

❮ 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

Proceedings of the National Academy of Sciences of the United States of America
J GulyasJ Rivier
Progress in Neuro-psychopharmacology & Biological Psychiatry
Daniel J Lodge, Andrew J Lawrence
Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]
A R ZampronioGlória E P Souza
© 2022 Meta ULC. All rights reserved