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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

FTIR spectra of (A) HPMCE5, (B) PEG6000, (C) poloxamer407, (D) glibenclamide powder, (E) glibenclamide solid dispersion (H6P4X0), prepared by SE method, and (F) glibenclamide solid dispersion (H6P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method.
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Figure 1: FTIR spectra of (A) HPMCE5, (B) PEG6000, (C) poloxamer407, (D) glibenclamide powder, (E) glibenclamide solid dispersion (H6P4X0), prepared by SE method, and (F) glibenclamide solid dispersion (H6P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method.

Mentions: The formulations prepared were evaluated for physical characterization viz. FTIR, DSC, and XRD. Pure GLIB and carrier blends were also run as control. The FTIR spectrum of GLIB powder (Fig. 1) showed characteristic amide peaks at 3367, 3315, 1716 cm-1, urea N-H stretching vibrations at 1277, 1618 and 1525 cm-1 and SO2 stretching vibration at 1342 and 1159 cm-1. Figs (1e and 1f) illustrate the IR spectra of typical GLIB formulations prepared by SE and SCF-based processing, respectively. The characteristic bands of the drug at 3315, 1716, 1618, 1342, and about 111-1155 cm-1 were also apparent in the spectra with decreased intensity.


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)

FTIR spectra of (A) HPMCE5, (B) PEG6000, (C) poloxamer407, (D) glibenclamide powder, (E) glibenclamide solid dispersion (H6P4X0), prepared by SE method, and (F) glibenclamide solid dispersion (H6P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 1: FTIR spectra of (A) HPMCE5, (B) PEG6000, (C) poloxamer407, (D) glibenclamide powder, (E) glibenclamide solid dispersion (H6P4X0), prepared by SE method, and (F) glibenclamide solid dispersion (H6P3.5X0.5), prepared by supercritical fluid solvent-antisolvent techniques method.
Mentions: The formulations prepared were evaluated for physical characterization viz. FTIR, DSC, and XRD. Pure GLIB and carrier blends were also run as control. The FTIR spectrum of GLIB powder (Fig. 1) showed characteristic amide peaks at 3367, 3315, 1716 cm-1, urea N-H stretching vibrations at 1277, 1618 and 1525 cm-1 and SO2 stretching vibration at 1342 and 1159 cm-1. Figs (1e and 1f) illustrate the IR spectra of typical GLIB formulations prepared by SE and SCF-based processing, respectively. The characteristic bands of the drug at 3315, 1716, 1618, 1342, and about 111-1155 cm-1 were also apparent in the spectra with decreased intensity.

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