Solubility of amlodipine besylate in binary mixtures of polyethylene glycol 400 + water at various temperatures: Measurement and modelling

Behboudi, Elmira; Soleymani, Jafar; Martínez, Fleming; Jouyban, Abolghasem

doi:10.1016/j.molliq.2021.118394

Cited by 12 publications

(7 citation statements)

References 41 publications

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“…The non-randomness factors of α12, α13 and α23 for NRTL were considered 0.4, 0.4 and 0.04, respectively. The r and q values for each component (drug and mono-solvents) for data fitting with UNIQUAC were respectively 20.55196 and 16.30338 for AMB [16], 2.1281 and 1.9483 for ethanol [28] and 16.0904 and 14.04 for PEG 400 [29]. The results demonstrated that the cosolevency models with MRD% < 7.0% show better prediction power compared with activity coefficient models with MRD% > 10.0%.…”

Section: For These Equations Fus Hmentioning

confidence: 95%

“…The non-aqueous mixed solvents such as PEG 400 + ethanol could be used in soft gelatin capsule formulations. A comprehensive literature search shows that up to now the solubility of AMB studied in PEG 400 + water [16], acetonitrile + water [17], n-propanol/isopropanol + water [18], ethanol/propane-1,2-diol + water [19], polyvinyl pyrrolidone [20] and supercritical carbon dioxide [21].…”

Section: Introductionmentioning

confidence: 99%

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Amlodipine besylate solubility in polyethylene glycol 400 + ethanol at different temperatures: Thermodynamic analysis and data modeling

Sayad

Moradi

Jafari

et al. 2023

Preprint

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In the present study, the solubility values of amlodipine besylate (AMB) in the binary mixtures of polyethylene glycol 400 and ethanol were determined using the shake-flask method at 293.2 to 313.2 K under atmospheric pressure (≈ 85 kPa) and correlated to some cosolvency and activity coefficient models. The accuracy of each model was marked by the mean relative deviations (MRD%) of the back-calculated solubility data. Also, the apparent thermodynamic properties of AMB dissolution were computed by the van't Hoff and Gibbs equations.

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Section: For These Equations Fus Hmentioning

confidence: 95%

Section: Introductionmentioning

confidence: 99%

Amlodipine besylate solubility in polyethylene glycol 400 + ethanol at different temperatures: Thermodynamic analysis and data modeling

Sayad

Moradi

Jafari

et al. 2023

Preprint

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“…An enthalpy-entropy compensation analysis is utilized, as previously reported [ 38 ], to examine the solvation behavior of FXT (3) in binary mixtures of {PEG 400 (1) + H 2 O (2)}. The weighted graphs of Δ sol H ° vs. Δ sol G ° were created for this analysis at T hm = 308 K [ 39 , 40 ].…”

Section: Methodsmentioning

confidence: 99%

“…PEG 400 has been examined as a potential solubilizer/cosolvent for the solubilization of several weakly soluble pharmacological molecules, such as lornoxicam, tenoxicam, dihydropyrimidine derivative, ferulic acid, pterostilbene, amlodipine besylate, and mesalazine [ 34 , 35 , 36 , 37 , 38 , 39 , 40 ]. The solubility data and thermodynamic parameters of FXT (3) in binary {PEG 400 (1) + H 2 O (2)} mixtures at various temperatures (298.2–318.2 K) and fixed atmospheric pressure (101.1 kPa) are not reported in the literature.…”

Section: Introductionmentioning

confidence: 99%

Solubility and Thermodynamic Properties of Febuxostat in Various (PEG 400 + Water) Mixtures

et al. 2022

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The solubility of the poorly soluble medicine febuxostat (FXT) (3) in various {polyethylene glycol 400 (PEG 400) (1) + water (H2O) (2)} mixtures has been examined at 298.2–318.2 K and 101.1 kPa. FXT solubility was measured using an isothermal method and correlated with “van’t Hoff, Apelblat, Buchowski–Ksiazczak λh, Yalkowsky–Roseman, Jouyban–Acree, and Jouyban–Acree-van’t Hoff models”. FXT mole fraction solubility was enhanced via an increase in temperature and PEG 400 mass fraction in {(PEG 400 (1) + H2O (2)} mixtures. Neat PEG 400 showed the highest mole fraction solubility of FXT (3.11 × 10–2 at 318.2 K), while neat H2O had the lowest (1.91 × 10–7 at 298.2 K). The overall error value was less than 6.0 % for each computational model, indicating good correlations. Based on the positive values of apparent standard enthalpies (46.72–70.30 kJ mol−1) and apparent standard entropies (106.4–118.5 J mol−1 K−1), the dissolution of FXT was “endothermic and entropy-driven” in all {PEG 400 (1) + H2O (2)} mixtures examined. The main mechanism for FXT solvation in {PEG 400 (1) + H2O (2)} mixtures was discovered to be an enthalpy-driven process. In comparison to FXT-H2O, FXT-PEG 400 showed the strongest molecular interactions. In conclusion, these results suggested that PEG 400 has considerable potential for solubilizing a poorly soluble FXT in H2O.

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“…There are numerous publications regarding studies of the dissolution of a number of active substances in various mixed solvents: meloxicam in mixtures ethylene glycol -water and PG -ethanol [17]; mesalazine in ternary systems ethanol -PG -water [18]; nicotinamide in mixtures water -ethanol and water -PG [19]; caffeine in mixtures N-MP -PG [20]; lifitegrast in mixed solvents containing DME, glycerin, PEG 400, PG and water [21]; carvedilol in the ternary system water -choline chloride -PG [22]; paracetamol in mixed solvents water -ethanol and water -PG [23]; ketoconazole in mixtures ethanol -PG [24]; acetaminophen in mixed solvents containing ethanol, PG and water [25]; curcumin in four mixed solvents: water -ethanol, water -n-propanol, water -isopropyl alcohol, water -PG [26]; sodium phenytoin in mixed solvents PG -water [27]; sulfapyridine in mixed solvents water -PG [28] and sulfadiazine in binary mixtures PEG 400 -water [29]; deferiprone in mixed solvents water -ethylene glycol, water -PG and water -PEG 400 [30]; amlodipine besylate in mixed solvents PEG 400 -water [31]; fluphenazine decanoate in aqueous solutions of PEG 400 or PEG 600 [32].…”

Section: Introductionmentioning

confidence: 99%

Influence of physicochemical properties and structure of mixed solvents propylene glycol – macrogol 400 on their in vitro release

Bezuglaya

Krasnopyorova

Liapunova

et al. 2023

SR: PS

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Aim. To study the density and dynamic viscosity of the mixed solvents propylene glycol (PG) – macrogol 400 (M400), to calculate their excess values and excess activation parameters of viscous flow, to evaluate the features of the structure of the mixed solvents and its influence on the in vitro release of PG and M400. Materials and methods. The mixed solvents PG - M400 were studied over the entire concentration range at temperatures from 293.15 to 313.15 K. The density and dynamic viscosity were determined, and the excess density, excess dynamic viscosity, activation parameters of viscous flow, and excess activation parameters of viscous flow were calculated. The in vitro release of PG and M400 from the mixed solvents was studied using vertical diffusion cells. The content of PG and M400 in the receptor medium was determined by gas chromatography using validated analytical procedures. The release rate, cumulative content, percentage of released PG or M400, coefficients of correlation and coefficients of determination were calculated. Results. The isotherms of excess density and excess dynamic viscosity of the mixed solvents PG-M400 pass through a maximum. The enthalpy makes the main contribution to the free activation energy of the viscous flow. The excess free energy is positive and has small values; the values of the excess entropy and excess enthalpy are negative, and the isotherms have the minimum at PG concentrations of 70‑75mol %. The release parameters of M400 are greater in binary mixtures where the M400 structure predominates. At PG content of ~75 mol %, the release parameters for PG and M400 are identical. With the increase in PG content above 75 mol %, when the PG structure predominates in the system, the release parameters of PG increase dramatically, and the release parameters of M400 decrease sharply. Conclusions. The structure of the binary system PG – M400 depends on its composition. Based on the isotherms of excess activation of viscous flow, it is possible to differentiate the areas where the structure of PG or the structure of M400 dominates, or the mixed structure of the binary solvent prevails. The in vitro release parameters for PG and M400 depend on the structure of the mixed solvents. The greatest difference in the release parameters of PG and M400 was observed in the area where the structure of PG dominates

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Solubility of amlodipine besylate in binary mixtures of polyethylene glycol 400 + water at various temperatures: Measurement and modelling

Cited by 12 publications

References 41 publications

Amlodipine besylate solubility in polyethylene glycol 400 + ethanol at different temperatures: Thermodynamic analysis and data modeling

Amlodipine besylate solubility in polyethylene glycol 400 + ethanol at different temperatures: Thermodynamic analysis and data modeling

Solubility and Thermodynamic Properties of Febuxostat in Various (PEG 400 + Water) Mixtures

Influence of physicochemical properties and structure of mixed solvents propylene glycol – macrogol 400 on their in vitro release

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