Poor water solubility of new chemical entities is considered as one of the main obstacles in drug development, as it usually leads to low bioavailability after administration. To overcome these problems, the selection of the appropriate formulation technology needs to be based on the physicochemical properties of the drug and introduced in the early stages of drug research.
One example of the new potential drug substance with poor solubility is DK-I-60-3, deuterated pyrazoloquinolinone, designed for the treatment of various neuropsychiatric ...
... formulations in rats, two to three-fold
bioavailability enhancement was observed in plasma and investigated organs, including the brain.
Keywords: pyrazoloquinolinones; nanocrystals; wet media milling; fasted/fed bioavailability
1. Introduction
The emerging trends in the combinatorial chemistry and design ...
... observed in plasma and investigated organs, including the brain.
Copyright: © 2021 by the authors.
Licensee MDPI, Basel, Switzerland.
Keywords: pyrazoloquinolinones; nanocrystals; wet media milling; fasted/fed bioavailability
1. Introduction
This article is an open access article
The emerging trends in ...
... beneficial. Additionally, it can provide a commercial advantage and prevent costly
reformulation later in the product lifecycle [11].
Deuterated pyrazoloquinolinones are investigated as non-benzodiazepine ligands to
interact with α6β2/3γ2 subunit of GABAA receptors with improved metabolic stability to
retard ...
Jelena R. Mitrović , Branka Divović-Matović, Daniel E. Knutson, Jelena B. Ðoković, Aleksandar Kremenović, Vladimir D. Dobričić, Danijela V. Randjelović, Ivana Pantelić, James M. Cook, Miroslav M. Savić, Snežana D. Savić. "Overcoming the Low Oral Bioavailability of Deuterated Pyrazoloquinolinone Ligand DK-I-60-3 by Nanonization: A Knowledge-Based Approach" in Pharmaceutics, MDPI, Basel, Switzerland (2021). https://doi.org/10.3390/pharmaceutics13081188
