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Dissolution enhancement of glibenclamide by solid dispersion: solvent evaporation versus a supercritical fluid-based solvent -antisolvent technique.

Tabbakhian M, Hasanzadeh F, Tavakoli N, Jamshidian Z - Res Pharm Sci (2014 Sep-Oct)

Bottom Line: A D-optimal mixture design was used to investigate the effects of different ratios of HPMCE5 (50-100%), PEG6000 (0-40%), and Poloxamer407 (0-20%) on drug dissolution from different solid dispersion (SD) formulations prepared by SE.The model generated according to the results of the D-optimal mixture design indicated that GLIB formulations comprising HPMC (50%-60%), PEG (34-40%), and poloxamer (6-10%) had enhanced dissolution performances.As compared to SE method, the SCF-SAS technique produced formulations of higher dissolution performances, likely due to the effects of solution and the supercritical CO2 (SC-CO2) on enhanced plasticization of polymers and thus increased diffusion of the drug into the polymer matrix.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Novel Drug Delivery Systems Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.

ABSTRACT
Glibenclamide (GLIB) is a poorly soluble drug with formulation-dependent bioavailability. Therefore, we attempted in this study to improve GLIB dissolution rate by preparing drug solid dispersions by solvent evaporation (SE) and supercritical fluid solvent-antisolvent techniques (SCF-SAS). A D-optimal mixture design was used to investigate the effects of different ratios of HPMCE5 (50-100%), PEG6000 (0-40%), and Poloxamer407 (0-20%) on drug dissolution from different solid dispersion (SD) formulations prepared by SE. The ratios of carriers used in SCF-SAS method were HPMCE5 (fixed at 60%), PEG6000 (20-40%), and Poloxamer407 (0-20%). A constant drug: carrier weight ratio of 1:10 was used in all experiments. The SDs obtained were physically characterized and subjected to the dissolution study. The major GLIB bands in FTIR spectra were indicative of drug integrity. The reduced intensity and the fewer number of peaks observed in X-ray diffractograms (XRD) of GLIB formulations was the indicative of at least partial transformation of crystalline to amorphous GLIB. This change and/or dilution of drug in much higher amounts of carriers present caused disappearance of distinctive endothermic peaks in differential scanning calorimetry thermograms of GLIB formulations. The model generated according to the results of the D-optimal mixture design indicated that GLIB formulations comprising HPMC (50%-60%), PEG (34-40%), and poloxamer (6-10%) had enhanced dissolution performances. As compared to SE method, the SCF-SAS technique produced formulations of higher dissolution performances, likely due to the effects of solution and the supercritical CO2 (SC-CO2) on enhanced plasticization of polymers and thus increased diffusion of the drug into the polymer matrix.

No MeSH data available.


Related in: MedlinePlus

Differential scanning calorimetry curves of (a) glibenclamide, (b) glibenclamide solid dispersion (H5P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method, (c) carrier physical mixture (H6P3X1 and (d) glibenclamide solid dispersion (H6P4X0), prepared by SE method.
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Figure 2: Differential scanning calorimetry curves of (a) glibenclamide, (b) glibenclamide solid dispersion (H5P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method, (c) carrier physical mixture (H6P3X1 and (d) glibenclamide solid dispersion (H6P4X0), prepared by SE method.

Mentions: The DSC thermogram of GLIB indicates the onset of endothermic peak at around 165 °C, corresponding to the melting of drug (Fig. 2a), however, no distinctive endothermic peak appeared in the thermograms of GLIB-SCF and GLIB-SE formulations and the GLIB carriers physical mixture (Figs 2b, 2d, and 2c, respectively)


Dissolution enhancement of glibenclamide by solid dispersion: solvent evaporation versus a supercritical fluid-based solvent -antisolvent technique.

Tabbakhian M, Hasanzadeh F, Tavakoli N, Jamshidian Z - Res Pharm Sci (2014 Sep-Oct)

Differential scanning calorimetry curves of (a) glibenclamide, (b) glibenclamide solid dispersion (H5P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method, (c) carrier physical mixture (H6P3X1 and (d) glibenclamide solid dispersion (H6P4X0), prepared by SE method.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4318002&req=5

Figure 2: Differential scanning calorimetry curves of (a) glibenclamide, (b) glibenclamide solid dispersion (H5P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method, (c) carrier physical mixture (H6P3X1 and (d) glibenclamide solid dispersion (H6P4X0), prepared by SE method.
Mentions: The DSC thermogram of GLIB indicates the onset of endothermic peak at around 165 °C, corresponding to the melting of drug (Fig. 2a), however, no distinctive endothermic peak appeared in the thermograms of GLIB-SCF and GLIB-SE formulations and the GLIB carriers physical mixture (Figs 2b, 2d, and 2c, respectively)

Bottom Line: A D-optimal mixture design was used to investigate the effects of different ratios of HPMCE5 (50-100%), PEG6000 (0-40%), and Poloxamer407 (0-20%) on drug dissolution from different solid dispersion (SD) formulations prepared by SE.The model generated according to the results of the D-optimal mixture design indicated that GLIB formulations comprising HPMC (50%-60%), PEG (34-40%), and poloxamer (6-10%) had enhanced dissolution performances.As compared to SE method, the SCF-SAS technique produced formulations of higher dissolution performances, likely due to the effects of solution and the supercritical CO2 (SC-CO2) on enhanced plasticization of polymers and thus increased diffusion of the drug into the polymer matrix.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Novel Drug Delivery Systems Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.

ABSTRACT
Glibenclamide (GLIB) is a poorly soluble drug with formulation-dependent bioavailability. Therefore, we attempted in this study to improve GLIB dissolution rate by preparing drug solid dispersions by solvent evaporation (SE) and supercritical fluid solvent-antisolvent techniques (SCF-SAS). A D-optimal mixture design was used to investigate the effects of different ratios of HPMCE5 (50-100%), PEG6000 (0-40%), and Poloxamer407 (0-20%) on drug dissolution from different solid dispersion (SD) formulations prepared by SE. The ratios of carriers used in SCF-SAS method were HPMCE5 (fixed at 60%), PEG6000 (20-40%), and Poloxamer407 (0-20%). A constant drug: carrier weight ratio of 1:10 was used in all experiments. The SDs obtained were physically characterized and subjected to the dissolution study. The major GLIB bands in FTIR spectra were indicative of drug integrity. The reduced intensity and the fewer number of peaks observed in X-ray diffractograms (XRD) of GLIB formulations was the indicative of at least partial transformation of crystalline to amorphous GLIB. This change and/or dilution of drug in much higher amounts of carriers present caused disappearance of distinctive endothermic peaks in differential scanning calorimetry thermograms of GLIB formulations. The model generated according to the results of the D-optimal mixture design indicated that GLIB formulations comprising HPMC (50%-60%), PEG (34-40%), and poloxamer (6-10%) had enhanced dissolution performances. As compared to SE method, the SCF-SAS technique produced formulations of higher dissolution performances, likely due to the effects of solution and the supercritical CO2 (SC-CO2) on enhanced plasticization of polymers and thus increased diffusion of the drug into the polymer matrix.

No MeSH data available.


Related in: MedlinePlus