Micronization of drugs using supercritical carbon dioxide

Kerč, Janez; Srčič, Stanko; Knez, Željko; Senčar-Božič, Petra

doi:10.1016/s0378-5173(99)00063-0

Cited by 160 publications

(67 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…In detail, as the solubility of pure FEL at 37°C was found to be 0.53 mg/L, the binary system containing PVP of 90% (w/w) corresponds to a FEL solubility about 30 times higher. Similar behaviour, especially for FEL, has been observed by Kerč et al [14]. Micronized FEL and PEG mixtures appear to have higher solubility (3.00 mg/L) than crystalline FEL (0.26 mg/L).…”

Section: Solubility In Water At 37°csupporting

confidence: 66%

“…There is a consideration if the interactions affect the solubility directly or through the mechanism of particle size reduction as mentioned by Kerč [14]. As the solubility is a physicochemical constant, it cannot be modified by only the particle size reduction.…”

Section: Drug Particle Size Evaluationmentioning

confidence: 99%

“…FEL is a dihydropyridine practically insoluble in water [14], but highly permeable, while its dissolution rate is the limiting factor for its bioavailability. Nevertheless, the dissolution profile of dihydropyridines is not always representative of their bioavailability due to the fact that several surfactants are used in the dissolution medium in order to achieve sink conditions.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone

Karavas

Ktistis

Xenakis

et al. 2006

European Journal of Pharmaceutics and Biopharmaceutics

138

View full text Add to dashboard Cite

Solid dispersion systems are widely investigated for the dissolution enhancement of poorly water soluble drugs. Nevertheless, very limited commercial use has been achieved due to the poor predictability of such systems caused by the lack of a basic understanding of the dissolution optimization mechanism. In the present study an investigation of the release mechanism is performed for solid dispersion systems composed by polyvinylpyrrolidone (PVP) and felodipine (FEL), based on a correlation of their hydrophilicity with the intensity of interactions. The existing interactions were evaluated by using NMR and UV spectroscopy while molecular simulation techniques were also enabled. It was found that the interactions that take place correspond to the creation of hydrogen bonds. The correlation between the intensity of interactions and the concentration of PVP in the matrix showed a sigmoid function. The interactions are impressively increased for polymer concentration exceeding 75% (w/w). This phenomenon was well explained by using the molecular simulation technique. A similar sigmoid pattern was found for the function between dissolution profiles and polymer concentration in the matrix, indicating that the intensity of interactions promotes the dissolution enhancement. Investigation of the solubility and the particle size distribution of FEL in the binary system appeared to have similar behaviour indicating that the interactions affect the release profile through these two factors. The hydrophilicity of PVP does not significantly affect this enhancement as the contact angle was found to be linear to PVP concentration. Microscopic observation of the dissolution behaviour showed that FEL remains in fine dispersion in aqueous solution, verifying the release mechanism.

show abstract

Section: Solubility In Water At 37°csupporting

confidence: 66%

Section: Drug Particle Size Evaluationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone

Karavas

Ktistis

Xenakis

et al. 2006

European Journal of Pharmaceutics and Biopharmaceutics

138

View full text Add to dashboard Cite

show abstract

“…Physical modifications, such as particle size reduction of amorphous 60 synthesis, often aim to increase the surface area, solubility and wettability of the drug particles. Different proposed strategies are those based on the 61 formulation of solid mixtures or matrix dispersions (Rasenack and Müller, 2004;Kerc et al, 1999;Elvira et al, 2004). Poorly water soluble crystalline drugs 62 are preferentially formulated as molecular dispersions in porous matrices.…”

Section: Introduction 28mentioning

confidence: 99%

Hybrid aerogel preparations as drug delivery matrices for low water-solubility drugs

Veres

López‐Periago

Lázár

et al. 2015

International Journal of Pharmaceutics

View full text Add to dashboard Cite

“…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: 94%

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

View full text Add to dashboard Cite

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.

show abstract

Micronization of drugs using supercritical carbon dioxide

Cited by 160 publications

References 8 publications

Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone

Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone

Hybrid aerogel preparations as drug delivery matrices for low water-solubility drugs

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

Contact Info

Product

Resources

About