Solubilization, Hansen solubility parameters and apparent thermodynamic parameters of Osimertinib in (propylene glycol + water) cosolvent mixtures

Author:

Shakeel Faiyaz1,Anwer Md. Khalid2,Haq Nazrul1,Alsarra Ibrahim A.1

Affiliation:

1. Department of Pharmaceutics , College of Pharmacy, King Saud University , Riyadh , Saudi Arabia

2. Department of Pharmaceutics , College of Pharmacy, Prince Sattam Bin Abdulaziz University , Al-Kharj , Saudi Arabia

Abstract

Abstract The solubilization, Hansen solubility parameters (HSPs) and apparent thermodynamic parameters of a novel anticancer medicine osimertinib (OMT) in binary propylene glycol (P) + water (W) cosolvent mixtures were evaluated. The mole fraction solubility (x e) of OMT in various (P + W) cosolvent mixtures including neat P and neat W was determined at T = 298.2–318.2 K and p = 0.1 MPa by applying a saturation shake flask method. HSPs of OMT, neat P, neat W and (P + W) cosolvent compositions free of OMT were also estimated. The x e values of OMT were regressed with Van’t Hoff, modified Apelblat, Yalkowsky-Roseman, Jouyban-Acree and Jouyban-Acree-Van’t Hoff models with an average errors of <3.0 %. The highest and lowest x e value of OMT was estimated in neat P (2.70 × 10−3 at T = 318.2 K) and neat W (1.81 × 10−5 at T = 298.2 K), respectively. Moreover, HSP of OMT was found to be closed with that of neat P. The solubility of OMT was found to be increased significantly with an increase in temperature and P mass fraction in all (P + W) cosolvent compositions including neat P and neat W. The results of activity coefficients suggested higher molecular interactions in OMT-P combination compared with OMT-W combination. The results of thermodynamic studies indicated an endothermic and entropy-driven dissolution of OMT in all (P + W) cosolvent compositions including neat P and neat W.

Publisher

Walter de Gruyter GmbH

Subject

Physical and Theoretical Chemistry

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