Measurements, Thermodynamic Modeling, and a Hydrogen Bonding Study on the Solubilities of Metoprolol Succinate in Organic Solvents

Shen, Jian; Liang, Xianrui; Liang, H.

doi:10.3390/molecules23102469

Cited by 12 publications

(7 citation statements)

References 35 publications

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“…These findings revealed that the experimental solubility data for FBX were in good accord with the published values [1,9]. Table 1 summarizes the findings, which show that the solubility of FBX increased considerably with increasing temperature in all mono solvents examined (p < 0.05) and was in good agreement with prior research [16][17][18] (1.14 × 10 −6 ) at 318.2 K. Since PEG-400 has the maximum solubility of FBX compared to the other mono solvents tested, it may be the optimal solvent for FBX solubility.…”

Section: Measured Solubility Data Of Fbxsupporting

confidence: 87%

“…The obtained suspensions were vortexed for 10 min. All of the samples were shaken at 100 rpm for 72 h in a "WiseBath ® WSB Shaking Water Bath (Model WSB-18/30/-45, Daihan Scientific Co., Ltd., Seoul, Korea)" [16,17]. Each sample was obtained, filtered, and centrifuged at 5000 rpm for 30 min after equilibrium was reached (equilibrium time = 72 h).…”

Section: Fbx Solubility Measurementmentioning

confidence: 99%

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Solubility and Thermodynamic Data of Febuxostat in Various Mono Solvents at Different Temperatures

et al. 2022

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This study examines the solubility and thermodynamics of febuxostat (FBX) in a variety of mono solvents, including “water, methanol (MeOH), ethanol (EtOH), isopropanol (IPA), 1-butanol (1-BuOH), 2-butanol (2-BuOH), ethylene glycol (EG), propylene glycol (PG), polyethylene glycol-400 (PEG-400), ethyl acetate (EA), Transcutol-HP (THP), and dimethyl sulfoxide (DMSO)” at 298.2–318.2 K and 101.1 kPa. The solubility of FBX was determined using a shake flask method and correlated with “van’t Hoff, Buchowski-Ksiazczak λh, and Apelblat models”. The overall error values for van’t Hoff, Buchowski-Ksiazczak λh, and Apelblat models was recorded to be 1.60, 2.86, and 1.14%, respectively. The maximum mole fraction solubility of FBX was 3.06 × 10−2 in PEG-400 at 318.2 K, however the least one was 1.97 × 10−7 in water at 298.2 K. The FBX solubility increased with temperature and the order followed in different mono solvents was PEG-400 (3.06 × 10−2) > THP (1.70 × 10−2) > 2-BuOH (1.38 × 10−2) > 1-BuOH (1.37 × 10−2) > IPA (1.10 × 10−2) > EtOH (8.37 × 10−3) > EA (8.31 × 10−3) > DMSO (7.35 × 10−3) > MeOH (3.26 × 10−3) > PG (1.88 × 10−3) > EG (1.31 × 10−3) > water (1.14 × 10−6) at 318.2 K. Compared to the other combinations of FBX and mono solvents, FBX-PEG-400 had the strongest solute-solvent interactions. The apparent thermodynamic analysis revealed that FBX dissolution was “endothermic and entropy-driven” in all mono solvents investigated. Based on these findings, PEG-400 appears to be the optimal co-solvent for FBX solubility.

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Section: Measured Solubility Data Of Fbxsupporting

confidence: 87%

Section: Fbx Solubility Measurementmentioning

confidence: 99%

Solubility and Thermodynamic Data of Febuxostat in Various Mono Solvents at Different Temperatures

et al. 2022

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“…Comparing the melting enthalpies of pure crystalline MS with that of MS in the filament revealed a reduction in the melting enthalpy from 178.7 to 68.1 J/g (total weight). The melting enthalpy of pure crystalline MS is in agreement with that reported in the literature [ 71 ]. Reduced melting enthalpies in the filament are in part attributable to concentration reduction from 100% in the raw materials to 40% MS and 20% PEG1500 in the filament.…”

Section: Resultssupporting

confidence: 90%

Independent Tailoring of Dose and Drug Release via a Modularized Product Design Concept for Mass Customization

et al. 2020

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Independent individualization of multiple product attributes, such as dose and drug release, is a crucial overarching requirement of pharmaceutical products for individualized therapy as is the unified integration of individualized product design with the processes and production that drive patient access to such therapy. Individualization intrinsically demands a marked increase in the number of product variants to suit smaller, more stratified patient populations. One established design strategy to provide enhanced product variety is product modularization. Despite existing customized and/or modular product design concepts, multifunctional individualization in an integrated manner is still strikingly absent in pharma. Consequently, this study aims to demonstrate multifunctional individualization through a modular product design capable of providing an increased variety of release profiles independent of dose and dosage form size. To further exhibit that increased product variety is attainable even with a low degree of product modularity, the modular design was based upon a fixed target dosage form size of approximately 200 mm3 comprising two modules, approximately 100 mm3 each. Each module contained a melt-extruded and molded formulation of 40% w/w metoprolol succinate in a PEG1500 and Kollidon® VA64 erodible hydrophilic matrix surrounded by polylactic acid and/or polyvinyl acetate as additional release rate-controlling polymers. Drug release testing confirmed the generation of predictable, combined drug release kinetics for dosage forms, independent of dose, based on a product’s constituent modules and enhanced product variety through a minimum of six dosage form release profiles from only three module variants. Based on these initial results, the potential of the reconfigurable modular product design concept is discussed for unified integration into a pharmaceutical mass customization/mass personalization context.

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“…The Apelblat model, which is a commonly applied semi-empirical correlation model, , correlates the mole fraction solubility data and the absolute temperature in pure solvents, derived from the Clausius–Clapeyron equation, can be expressed as: where A , B , and C are model parameters of the equation. A and B represent the nonideality of the change of the activity coefficient in the actual solution, while C denotes the effect of temperature on the fusion enthalpy.…”

Section: Thermodynamic and Correlating Modelsmentioning

confidence: 99%

Solubility Measurement and Data Correlation of Pyrimethamine in 13 Pure Solvents at Temperatures from 278.15 to 318.15 K

et al. 2021

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The solubility of PMN in 13 organic solvents (methanol, ethanol, n-propanol, isopropanol, n-butanol, sec-butanol, isobutanol, acetone, acetonitrile, methyl acetate, ethyl acetate, n-propyl acetate, and isopropyl acetate) was determined by the gravimetric method over the temperatures ranging from 278.15 to 318.15 K at 0.1 MPa. The solubility of all selected solvents increases with increasing temperature; however, the change in methanol is substantially more than that in other solvents. Four models, including the modified Apelblat equation, the λh equation, the NRTL, and the van't Hoff equation, were applied to correlate the experimental solubility data, which showed that a relative deviation is less than 3% with the four models. In addition, a KAT-LSER model was employed to quantitatively evaluate and describe the solvent effect, which indicate that the hydrogen bonding basicity of solvents has a greater effect on the solubility of PMN.

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Measurements, Thermodynamic Modeling, and a Hydrogen Bonding Study on the Solubilities of Metoprolol Succinate in Organic Solvents

Cited by 12 publications

References 35 publications

Solubility and Thermodynamic Data of Febuxostat in Various Mono Solvents at Different Temperatures

Solubility and Thermodynamic Data of Febuxostat in Various Mono Solvents at Different Temperatures

Independent Tailoring of Dose and Drug Release via a Modularized Product Design Concept for Mass Customization

Solubility Measurement and Data Correlation of Pyrimethamine in 13 Pure Solvents at Temperatures from 278.15 to 318.15 K

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