Solubility and thermodynamics of apremilast in different mono solvents: Determination, correlation and molecular interactions

Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Faiyaz Shakeel, Nazrul Haq, Fars K. Alanazi, Ibrahim A. Alsarra The solubility data of recently launched poorly soluble antipsoriatic drug apremilast (APM) in any mono solvent or cosolvent mixtures with respect to temperature are not available in literature. Hence, in this research work, the solubility of APM in twelve different mono solvents namely “water, methanol, ethanol, isopropanol (IPA), ethylene glycol (EG), propylene glycol (PG), 1-butanol, 2-butanol, ethyl acetate (EA), dimethyl sulfoxide (DMSO), polyethylene glycol-400 (PEG-400) and Transcutol®” was determined at temperatures “T =298.2K to 318.2K” and pressure “p =0.1 MPa”. Eexperimental solubilities of APM in mole fraction were determined by a static equilibrium method using high performance liquid chromatography at 254nm. Experimental solubilities of APM in mole fraction were correlated well with “Van’t Hoff and Apelblat models”. The solubilities of APM in mole fraction were recorded highest in DMSO (9.91×10−2), followed by EA (2.54×10−2), Transcutol (2.51×10−2), PEG-400 (2.16×10−2),PG (4.01×10−3), EG (1.61×10−3), IPA (4.96×10−4), 1-butanol (4.18×10−4), 2-butanol (3.91×10−4), methanol (2.25×10−4), ethanol (2.20×10−4) and water (1.29×10−6) at “T =318.2K” and similar results were also obtained at each temperature evaluated. The molecular interac...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research