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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

Dissolution curves of glibenclamide powder and typical glibenclamide formulations comprising various fractions of HPMCE5 (H), PEG6000 (P), and Poloxamer407 (X), prepared by supercritical fluid solvent-antisolvent techniques method (10 mg). A fixed 1:10 weight ratio of glibenclamide to the carrier system was used in all experiments. Each formulation is represented as a three-letter code with numbers indicating the amount of each component in the mixture.
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Figure 5: Dissolution curves of glibenclamide powder and typical glibenclamide formulations comprising various fractions of HPMCE5 (H), PEG6000 (P), and Poloxamer407 (X), prepared by supercritical fluid solvent-antisolvent techniques method (10 mg). A fixed 1:10 weight ratio of glibenclamide to the carrier system was used in all experiments. Each formulation is represented as a three-letter code with numbers indicating the amount of each component in the mixture.

Mentions: Comparison of the dissolution profiles of pure GLIB, GLIB- carriers physical mixture, and GLIB formulations prepared by SE and SCF-SAS techniques are shown in Figs 4 and 5, respectively. The dissolution rate of GLIB in pH 9.5 phosphate buffer solution was very low with about 19% ± 0.98% dissolving at the end of 45 min. As shown in both figures, the dissolution rate of GLIB was significantly higher (p<0.01) from all GLIB formulations, as compared to pure GLIB or the GLIB-carriers physical mixture. Where only about 19% of GLIB powder was dissolved within 45 min the extent of drug dissolution during the same time period ranged from about 50-81% and 89-100% for GLIB formulations prepared by SE and SCF-SAS techniques, 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)

Dissolution curves of glibenclamide powder and typical glibenclamide formulations comprising various fractions of HPMCE5 (H), PEG6000 (P), and Poloxamer407 (X), prepared by supercritical fluid solvent-antisolvent techniques method (10 mg). A fixed 1:10 weight ratio of glibenclamide to the carrier system was used in all experiments. Each formulation is represented as a three-letter code with numbers indicating the amount of each component in the mixture.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 5: Dissolution curves of glibenclamide powder and typical glibenclamide formulations comprising various fractions of HPMCE5 (H), PEG6000 (P), and Poloxamer407 (X), prepared by supercritical fluid solvent-antisolvent techniques method (10 mg). A fixed 1:10 weight ratio of glibenclamide to the carrier system was used in all experiments. Each formulation is represented as a three-letter code with numbers indicating the amount of each component in the mixture.
Mentions: Comparison of the dissolution profiles of pure GLIB, GLIB- carriers physical mixture, and GLIB formulations prepared by SE and SCF-SAS techniques are shown in Figs 4 and 5, respectively. The dissolution rate of GLIB in pH 9.5 phosphate buffer solution was very low with about 19% ± 0.98% dissolving at the end of 45 min. As shown in both figures, the dissolution rate of GLIB was significantly higher (p<0.01) from all GLIB formulations, as compared to pure GLIB or the GLIB-carriers physical mixture. Where only about 19% of GLIB powder was dissolved within 45 min the extent of drug dissolution during the same time period ranged from about 50-81% and 89-100% for GLIB formulations prepared by SE and SCF-SAS techniques, 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