Solubility of Diflunisal in Supercritical Carbon Dioxide

Coimbra, Patrícia; Fernandes, Daniel; Gil, M.H.; Sousa, Hermínio C. de

doi:10.1021/je800384h

Cited by 29 publications

(14 citation statements)

References 43 publications

(79 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The highest deviations (13.7% and 13.4%) were observed at lower pressure (10 MPa) and when comparing with data measured by Pauchon et al [41] and Wagner et al [43], respectively. These results, together with solubility data previously published for different solid solutes at different temperature, pressure and solubility ranges [27][28][29][30][31][32][33][34][35] and using the same apparatus and experimental procedures, confirm the accuracy of the measurements reported in the present work.…”

Section: Resultssupporting

confidence: 91%

“…Experimental equilibrium solubility data of ATRA in scCO 2 were measured using a static analytical method and accordingly to the methodology previously described in the literature [27][28][29][30][31][32][33][34][35]. Briefly, it consists in a high pressure stainless steel equilibrium cell with sapphire windows connected to a six-port sampling valve, which is further connected to a known volume sampling loop followed by a glass trap (collector for the scCO 2 solubilized solute with known volume) and a stainless steel balloon (with calibrated volume to quantify the solvent).…”

Section: Solubility Determination 221 Apparatus and Proceduresmentioning

confidence: 99%

See 1 more Smart Citation

Solubility of all-trans retinoic acid in supercritical carbon dioxide

Rosa

Marceneiro

Braga

et al. 2015

The Journal of Supercritical Fluids

View full text Add to dashboard Cite

All-trans retinoic acid (ATRA) is a derivative of retinol (or vitamin A) presenting similar benefits but considerable lower adverse toxicity, mainly in cases of high or long-term therapeutic doses. ATRA showed to be effective in the treatment and/or chemoprevention of several epithelial and hematological malignancies and diverse dermatological and eye diseases however, its low solubility in aqueous media and photosensitivity hinder its wider usage by the conventional administration methods. Supercritical fluids technologies are being widely used to enhance the in vivo bioactivity of this type of drugs both by improving their dissolution rate (using particle size reduction processes) and/or by controlling their release into the media after incorporation into solid polymeric/inorganic matrices (using supercritical impregnation/foaming processes). In both cases the solubility of the drug in the supercritical fluid (usually scCO 2) is required for process optimization purposes. Therefore, in this work the solubility of ATRA in scCO 2 was measured at different isotherms (308.2, 318.2 and 328.2 K) and pressures that ranged from 10 up to 30 MPa using a static analytical method. Solubility data were correlated using three commonly used density-based models, namely the Bartle, Chrastil and Méndez-Santiago-Teja models. The solubility of ATRA in scCO 2 was found to be between 1.52 × 10 −6 and 1.84 × 10 −5 in terms of ATRA mole fraction and between 7.50 × 10 −3 and 1.07 × 10 −1 in terms of amount of solid solute per unit of volume of scCO 2. Fairly good correlation agreement was obtained with all the applied models being the lowest deviations obtained with the Chrastil model. ATRA particles obtained after scCO 2 processing (dissolution in scCO 2 followed by re-precipitation) were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared (FTIR) and in vitro dissolution studies. The results showed that the processed particles maintained their chemical structure and presented enhanced dissolution in aqueous media (PBS:ethanol, 80:20, v/v) when compared with commercial (non-processed) ATRA.

show abstract

Section: Resultssupporting

confidence: 91%

Section: Solubility Determination 221 Apparatus and Proceduresmentioning

confidence: 99%

Solubility of all-trans retinoic acid in supercritical carbon dioxide

Rosa

Marceneiro

Braga

et al. 2015

The Journal of Supercritical Fluids

View full text Add to dashboard Cite

show abstract

“…The major problem with the formation of pure IND and mixed IND-PLA particles is the solubility of IND in supercritical CO 2 which seems to be much lower that of KET and NAP. 15,16 We could not generate enough pure IND particles with our lowthroughput setup to properly analyze the properties of these particles. The addition of PLA to IND in the extractor increased the solubility of IND so that we were at least able to record infrared spectra of the mixed IND-PLA particles in the aerosol phase after particle formation.…”

Section: Discussionmentioning

confidence: 99%

Phase Behavior of Ketoprofen−Poly(lactic acid) Drug Particles Formed by Rapid Expansion of Supercritical Solutions

2010

View full text Add to dashboard Cite

The present contribution investigates whether it is possible to form stable amorphous particles of ketoprofen-poly(lactic acid), naproxen-poly(lactic acid), and indomethacin-poly(lactic acid). Amorphization and micronization of these poorly water-soluble drugs offer a combined way to improve the solubility and enhance the dissolution rate. The particles were formed by pulsed rapid expansion of supercritical CO(2) solutions and characterized in the aerosol phase with rapid-scan infrared spectroscopy and after collection with scanning electron microscopy and X-ray diffraction. None of the three drug-poly(lactic acid) mixtures showed long-term stability on the order of weeks against the reversion from the amorphous to the crystalline state. Ketoprofen was the only drug that formed mixed amorphous particles with at least short-term stability. The long-term products turned out to be submicrometer- to micrometer-sized particles with a crystalline drug core and an amorphous poly(lactic acid) shell. Moreover, we found that the poly(lactic acid) coating stabilizes the particles against agglomeration.

show abstract

“…Muitos compostos ativos apresentam pouca solubilidade em água e sua incorporação é dificultada em tais dispositivos (Coimbra et al, 2008).…”

Section: Introductionunclassified

Efeito Do Uso De Etanol Como Cossolvente Na Impregnação Supercrítica De Cetoprofeno Em Filmes De Quitosana-Xantana

Veiga¹,

Braga²,

Sousa³

et al. 2015

Anais Do XX Congresso Brasileiro De Engenharia Química

View full text Add to dashboard Cite

RESUMO -Filmes de quitosana-xantana (Q-X) apresentam grande potencial na cicatrização de lesões dérmicas, auxiliando no tratamento e na diminuição da dor. Estes filmes podem ser associados a um anti-inflamatório com efeito analgésico como o cetoprofeno. Neste contexto, o presente trabalho teve por objetivo verificar a incorporação de cetoprofeno em filmes de Q-X por impregnação supercrítica com CO 2 . Os experimentos foram realizados de acordo com um planejamento experimental 2 3 , variando a temperatura (40 e 50°C), a pressão de operação (150 e 300 bar) e a presença do cossolvente etanol. A análise da incorporação de cetoprofeno foi realizada através da liberação deste em solução de PBS por 24 h (37°C, 100 rpm) e quantificação por espectrofotometria a 260 nm. Foram obtidos resultados para a incorporação entre 1,6 e 20,0 mg/g de filme. A adição de etanol e o aumento da pressão de operação resultaram no aumento da incorporação, enquanto que a temperatura não teve efeito significativo na impregnação. Os resultados obtidos demonstram a viabilidade de impregnação de cetoprofeno em filmes de Q-X utilizando o método de impregnação supercrítica. INTRODUÇÃOA incorporação de fármacos em dispositivos formados por polímeros biocompatíveis tem recebido atenção crescente nos últimos anos na área farmacêutica (Duarte et al., 2006). Muitos compostos ativos apresentam pouca solubilidade em água e sua incorporação é dificultada em tais dispositivos (Coimbra et al., 2008).As tecnologias envolvendo fluido supercrítico têm sido cada vez mais aplicadas na formação de dispositivos, polimerização, intumescimento e impregnação de polímeros. O interesse no uso dessas tecnologias é atribuído aos efeitos substanciais destes fluidos em polímeros, tais como a diminuição da temperatura de transição vítrea (efeito plastificante) e o seu intumescimento reversível (Kikik e Vecchione, 2003). Os processos de impregnação utilizando fluidos supercríticos são viáveis quando oÁrea temática: Engenharia de Materiais e Nanotecnologia 1

show abstract

Solubility of Diflunisal in Supercritical Carbon Dioxide

Cited by 29 publications

References 43 publications

Solubility of all-trans retinoic acid in supercritical carbon dioxide

Solubility of all-trans retinoic acid in supercritical carbon dioxide

Phase Behavior of Ketoprofen−Poly(lactic acid) Drug Particles Formed by Rapid Expansion of Supercritical Solutions

Efeito Do Uso De Etanol Como Cossolvente Na Impregnação Supercrítica De Cetoprofeno Em Filmes De Quitosana-Xantana

Contact Info

Product

Resources

About