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Evaluation of aspartame as a co-former in the preparation of co-amorphous formulations of dipyridamole using spray drying.
Int J Pharm
December 2024
Pharmaceutical and Molecular Biotechnology Research Centre, South East Technological University, Waterford, Ireland; SSPC, The Research Ireland Centre for Pharmaceuticals, South East Technological University, Waterford, Ireland. Electronic address:
Article Synopsis
- Co-amorphous systems (CAMs) can improve the solubility of poorly water-soluble drugs, but challenges like a limited number of co-formers and lab-scale preparation techniques exist.
- This study uses aspartame and dipyridamole to create CAMs through spray drying, showing that AspPhe has better solid-state properties and physical stability than individual amino acids.
- Molecular interactions analyzed by Hirshfeld Surface analysis and FT-IR spectroscopy demonstrate that hydrogen bond interactions significantly enhance the stability of the DPM-AspPhe co-amorphous system, while crystallization rates are affected by temperature and humidity.
Exploring novel dilazep derivatives as hENT1 inhibitors and potentially covalent molecular tools.
Purinergic Signal
June 2024
Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.
The human equilibrative nucleoside transporter 1 (SLC29A1, hENT1) is a solute carrier that modulates the passive transport of nucleosides and nucleobases, such as adenosine. This nucleoside regulates various physiological processes, such as vasodilation and -constriction, neurotransmission and immune defense. Marketed drugs such as dilazep and dipyridamole have proven useful in cardiovascular afflictions, but the application of hENT1 inhibitors can be beneficial in a number of other diseases.
View Article and Find Full Text PDFThe Therapeutic Target of IBD and the Mechanism of Dipyridamole in Treating IBD Explored by Geo Gene Chips, Network Pharmacology, and Molecular Docking.
Endocr Metab Immune Disord Drug Targets
May 2024
Department of Pharmacy, Guangzhou Women and Children's Medical Center, Guangzhou Medical University, Guangzhou, China.
Background And Aims: Inflammatory Bowel Disease (IBD) is a refractory disease with repeated attacks, and there is no accurate treatment target at present. Dipyridamole, a phosphodiesterase (PDE) inhibitor, has been proven to be an effective treatment for IBD in a pilot study. This study explored the therapeutic target of IBD and the pharmacological mechanism of dipyridamole for the treatment of IBD.
View Article and Find Full Text PDFQuantitative myocardial perfusion in liver transplantation candidates: Poorly metabolized caffeine inhibition of vasodilatory stress.
J Nucl Cardiol
August 2024
Martin Bucksbaum Distinguished University Chair, Weatherhead PET Center for Preventing and Reversing Atherosclerosis, McGovern Medical School, University of Texas, Houston, USA. Electronic address:
Background: Data on cardiac positron emission tomography (PET) in liver transplantation (LT) candidates are limited with no prior study accounting for poorly metabolized caffeine reducing stress perfusion.
Method: Consecutive LT candidates (n = 114) undergoing cardiac rest/stress PET were instructed to abstain from caffeine for 2 days extended to 5 and 7 days. Due to persistently high prevalence of measurable blood caffeine after 5-day caffeine abstinence, dipyridamole (n = 41) initially used was changed to dobutamine (n = 73).
Sorbitol Destroyed Intestinal Microfold Cells (M Cells) Development through Inhibition of PDE4-Mediated RANKL Expression.
Mediators Inflamm
May 2024
Department of Gastroenterology, Guangzhou Women and Children's Medical Center, Guangzhou Medical University, Guangzhou, China.
Objective: Microfold cells (M cells) are specific intestinal epithelial cells for monitoring and transcytosis of antigens, microorganisms, and pathogens in the intestine. However, the mechanism for M-cell development remained elusive.
Materials And Methods: Real-time polymerase chain reaction, immunofluorescence, and western blotting were performed to analyze the effect of sorbitol-regulated M-cell differentiation and , and luciferase and chromatin Immunoprecipitation were used to reveal the mechanism through which sorbitol-modulated M-cell differentiation.
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