Melting point depression by using supercritical CO2 for a novel melt dispersion micronization process

Dohrn, Ralf; Bertakis, Evangelos; Behrend, Olaf; Voutsas, Epaminondas; Tassios, Dimitrios P.

doi:10.1016/j.molliq.2006.08.026

Cited by 40 publications

(22 citation statements)

References 9 publications

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“…The first melting point consists on the appearance of the first drop of liquid in the presence of solid and gas phases by means of temperature or pressure raises. The second method considers the formation of the first solids from fluid phase(s) as equilibrium criteria [8][9][10][11][12]. Some apparatus have been alternatively developed with slight modifications of the melting or freezing methods with successful results such as the modified capillary method [13,14].…”

Section: Introductionmentioning

confidence: 99%

An enhanced “first freezing point” method for solid–liquid–gas equilibrium measurements in binary systems

González-Arias

Verónico-Sánchez

Elizalde-Solis

et al. 2015

The Journal of Supercritical Fluids

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Section: Introductionmentioning

confidence: 99%

An enhanced “first freezing point” method for solid–liquid–gas equilibrium measurements in binary systems

González-Arias

Verónico-Sánchez

Elizalde-Solis

et al. 2015

The Journal of Supercritical Fluids

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“…The modification of the physicochemical property of the molecule, the use of supercritical fluid processes, surfactants, solubilizers, and novel excipients are some of the approaches used to improve solubility of poorly soluble drug molecules (1,(3)(4)(5). Modification of the physicochemical property of a molecule includes the reduction of the particle size to increase the surface area through micronization and nanosuspensions as well as crystal engineering to decrease the crystallinity through the formation of solid dispersions (1,6).…”

Section: Introductionmentioning

confidence: 99%

A Menthol-Based Solid Dispersion Technique for Enhanced Solubility and Dissolution of Sulfamethoxazole from an Oral Tablet Matrix

Choonara

Kumar

et al. 2014

AAPS PharmSciTech

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Abstract. A menthol-based solid dispersion was designed to improve the intrinsic solubility of the poorly soluble sulfamethoxazole-a class II drug molecule of Biopharmaceutics Classification System (BCS) displaying widespread antibacterial activity. Solid dispersions of menthol and sulfamethoxazole were compressed with hydroxypropyl methylcellulose (HPMC) into suitable sulfamethoxazole-loaded matrix tablets for oral drug delivery. The sulfamethoxazole-loaded solid dispersions and compressed tablets were characterized for their physicochemical and physicomechanical properties such as changes in crystallinity, melting point, molecular transitions, and textural analysis for critical analysis of their effects on the solubility and dissolution of sulfamethoxazole. The formulations were further evaluated for swelling, degradation, solubility, and in vitro drug release behavior. In vitro drug release from the sulfamethoxazole-loaded matrix tablets displayed a minimum and maximum fractional release of 0.714 and 0.970, respectively. The tablets further displayed different release rate profiles over the study periods of 12, 16, 48, and 56 h which were attributed to the varying concentrations of menthol within each formulation. Menthol was determined as a suitable hydrophilic carrier for sulfamethoxazole since it functioned as a solubilizing and release-retarding agent for improving the solubility and dissolution of sulfamethoxazole as well as controlling the rate at which it was released.

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“…These results are consistent with those of a previous study demonstrating that the melting point of solid substances can be significantly reduced by using supercritical fluids that are highly soluble in the molten substance. 20 The CO 2 gas used in this experiment was significantly soluble in molten fenofibrate under high pressure, 21,22 leading to the decreased melting point of fenofibrate observed in this study.…”

Section: Phase Behavior Studymentioning

confidence: 70%

Enhancement of the dissolution rate and bioavailability of fenofibrate by a melt-adsorption method using supercritical carbon dioxide

Ho¹,

Cho²,

Kim³

et al. 2012

IJN

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Background: The aim of this study was to enhance the bioavailability of fenofibrate, a poorly water-soluble drug, using a melt-adsorption method with supercritical CO 2 . Methods: Fenofibrate was loaded onto Neusilin ® UFL2 at different weight ratios of fenofibrate to Neusilin UFL2 by melt-adsorption using supercritical CO 2 . For comparison, fenofibrate-loaded Neusilin UFL2 was prepared by solvent evaporation and hot melt-adsorption methods. The fenofibrate formulations prepared were characterized by differential scanning calorimetry, powder x-ray diffractometry, specific surface area, pore size distribution, scanning electron microscopy, and energy-dispersive x-ray spectrometry. In vitro dissolution and in vivo bioavailability were also investigated. Results: Fenofibrate was distributed into the pores of Neusilin UFL2 and showed reduced crystal formation following adsorption. Supercritical CO 2 facilitated the introduction of fenofibrate into the pores of Neusilin UFL2. Compared with raw fenofibrate, fenofibrate from the prepared powders showed a significantly increased dissolution rate and better bioavailability. In particular, the area under the drug concentration-time curve and maximal serum concentration of the powders prepared using supercritical CO 2 were 4.62-fold and 4.52-fold greater than the corresponding values for raw fenofibrate. Conclusion: The results of this study highlight the usefulness of the melt-adsorption method using supercritical CO 2 for improving the bioavailability of fenofibrate.

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Melting point depression by using supercritical CO2 for a novel melt dispersion micronization process

Cited by 40 publications

References 9 publications

An enhanced “first freezing point” method for solid–liquid–gas equilibrium measurements in binary systems

An enhanced “first freezing point” method for solid–liquid–gas equilibrium measurements in binary systems

A Menthol-Based Solid Dispersion Technique for Enhanced Solubility and Dissolution of Sulfamethoxazole from an Oral Tablet Matrix

Enhancement of the dissolution rate and bioavailability of fenofibrate by a melt-adsorption method using supercritical carbon dioxide

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