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 ...
... s were
performed in triplicate, and the concentration of DK-I-60-3 in samples was analyzed by the
LC-MS/MS method.
Solubility of Nanocrystals
Solubility of nanocrystals in formulations F5, F6, and F8, corresponding suspensions
(S5, S6, and S8) was determined at 37 ◦C. A total of 300 µL of the sample ...
... variations in DK-I-60-3 absorption. Similar observations of
the role of nanocrystals in the mitigation of interindividual differences were confirmed in
the case of itraconasole nanosuspensions [32]. More balanced absorption after nanocrystals
could be a consequence of small and uniformed particle size, causing ...
... three times higher after nanocrystals re-
gardless of food intake (Figure 7). Significant differences in plasma AUC following dif-
ferent treatments (p < 0.05, ANOVA) proved the increased extent of absorption following
nanocrystal administration. Although results of the nanocrystals’ solubility (Figure 6b) ...
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
