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Solubilization of a novel antitumor drug ribociclib in water and ten different organic solvents at different temperatures.

Authors:
Ramadan Al-Shdefat Mohammad Hailat Osama Y Alshogran

Drug Dev Ind Pharm 2022 Jan 21;48(1):12-20. Epub 2022 Jun 21.

Department of Clinical Pharmacy, Faculty of Pharmacy, University of Science and Technology, Irbid, Jordan.

Objective: This study reports new solubility and physicochemical data for ribociclib (RCB) in water and ten organic solvents including "methanol (MeOH), ethanol (EtOH), isopropyl alcohol (IPA), n-butanol (n-BuOH), propylene glycol (PG), polyethylene glycol-400 (PEG-400), acetone, ethyl acetate (EA), Transcutol-HP (THP), and dimethyl sulfoxide (DMSO)" at 293.2-313.2 K and 101.1 kPa.

Significance: The obtained data are useful for the industrial applications of RCB.

Methods: The solubility of RCB was measured and regressed using "van't Hoff, Buchowski-Ksiazczak , the modified Apelblat, and Jouyban models."

Results: The overall deviations of <4.0% were recorded for all four models. The maximum mole fraction solubility of RCB was 2.66 × 10 in PEG-400 at 313.2 K, however, the lowest one was in the water. The RCB solubility increased with temperature and the order followed in the water and ten different organic solvents was PEG-400 (2.66 × 10) > THP (1.00 × 10) > PG (5.39 × 10) > DMSO (5.00 × 10) > n-BuOH (3.23 × 10) > acetone (3.11 × 10) > IPA (1.58 × 10) > EA (1.41 × 10) > EtOH (1.37 × 10) > MeOH (8.10 × 10) > water (2.38 × 10) at 313.2 K. The maximum solute-solvent interactions were found in RCB-PEG-400 in comparison with other combination of RCB and solvents. "Apparent thermodynamic analysis" indicated an "endothermic and entropy-driven dissolution" of RCB in water and ten organic solvents.

Conclusions: Based on all these data and observations, PEG-400 can be used as the best co-solvent for RCB solubilization.

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http://dx.doi.org/10.1080/03639045.2022.2089161DOI Listing
January 2022

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