Solubility and thermodynamic function of apremilast in different (Transcutol + water) cosolvent mixtures: Measurement, correlation and molecular interactions

Shakeel, Faiyaz; Haq, Nazrul; Alanazi, Fars K.

doi:10.1016/j.jiec.2017.07.002

Cited by 16 publications

(12 citation statements)

References 34 publications

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“…The binary combination of methanol and ethanol (80:20%, v/v) was utilized as the mobile phase for FFA estimation. The solubility of FFA in the mole fraction (x e ) was determined using its standard formulate, described previously [12,13].…”

Section: Ffa Solubility Determinationmentioning

confidence: 99%

“…The solvation behavior of FFA in mixed solvent systems and pure solvents was investigated using enthalpy-entropy compensation analysis [12,32]. Such analysis was carried out by plotting the weighted graphs of ∆ sol H • vs. ∆ sol G • at T hm = 308 K [12].…”

Section: Enthalpy-entropy Compensation Analysismentioning

confidence: 99%

“…where J i = model coefficient of Equation (12) and was predicted using no-intercept regression analysis [41]. The correlation between the experimental and Jouyban-Acree model solubilities of FFA was performed in terms of RMSD.…”

Section: Computational Modelingmentioning

confidence: 99%

“…The commonly used cosolvents for solubility enhancement are ethanol, propylene glycol and polyethylene glycol 400 (PEG 400) [6,9]. However, Carbitol [also known as Transcutol or 2-(2-ethoxyethoxy) ethanol] has also been reported as a potent cosolvent in the solubility enhancement of various poorly-soluble drugs in addition to its complete miscibility with water [10][11][12]. The efficiency of Carbitol had been investigated in the solubilization of different, poorly water-soluble compounds in literature [10][11][12][13][14][15].…”

Section: Introductionmentioning

confidence: 99%

“…However, Carbitol [also known as Transcutol or 2-(2-ethoxyethoxy) ethanol] has also been reported as a potent cosolvent in the solubility enhancement of various poorly-soluble drugs in addition to its complete miscibility with water [10][11][12]. The efficiency of Carbitol had been investigated in the solubilization of different, poorly water-soluble compounds in literature [10][11][12][13][14][15]. The solubility of FFA in water, light mineral oil and polyethylene glycol 400 (PEG 400) at T = 295.2 K, T = 305.2 K and T = 298.2 K, respectively, has been reported elsewhere [3,[16][17][18].…”

Section: Introductionmentioning

confidence: 99%

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Solubilization, Hansen Solubility Parameters, Solution Thermodynamics and Solvation Behavior of Flufenamic Acid in (Carbitol + Water) Mixtures

Shakeel

Alshehri

2020

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The solubilization, solution thermodynamics, solvation behavior and Hansen solubility parameters (HSPs) of an anti-inflammatory medicine flufenamic acid (FFA) in various Carbitol + water mixtures were evaluated in this study. The experimental solubility of FFA in mole fraction (xe) was measured at T = 298.2–318.2 K and p = 0.1 MPa using a static equilibrium method. The xe values of FFA in various Carbitol + water mixtures were correlated with van’t Hoff, Apelblat, Yalkowsky–Roseman, Jouyban–Acree and Jouyban–Acree–van’t Hoff models. All the studied models showed good correlation with mean error values of less than 2%. The xe value of FFA was found to increase significantly with the increase in temperature and Carbitol mass fraction in all Carbitol + water mixtures evaluated. The maximum and minimum xe values of FFA were recorded in pure Carbitol (2.81 × 10−1) at T = 318.2 K and pure water (5.80 × 10−7) at T = 298.2 K, respectively. Moreover, the HSP of FFA was found to be more closed with that of pure Carbitol, indicating the maximum solubility of FFA in pure Carbitol. The estimated values of activity coefficients showed higher molecular interactions in FFA–Carbitol combinations compared with FFA–water combinations. Thermodynamic studies indicated an endothermic and entropy-driven dissolution of FFA in all Carbitol + water mixtures. The solvation behavior of FFA was observed as enthalpy driven in all Carbitol + water combinations evaluated.

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Section: Ffa Solubility Determinationmentioning

confidence: 99%