Fast-Dissolving Tablets of Glyburide Based on Ternary Solid Dispersions with PEG 6000 and Surfactants

Cirri, Marzia; Maestrelli, Francesca; Corti, Giovanna; Mura, Paola; Valleri, Maurizio

doi:10.1080/10717540601067802

Cited by 26 publications

(11 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Therefore, preparing solid dispersions of a poorly soluble drug with water-soluble polymers is a promising method for improving the dissolution characteristics and bioavailability of the drug (11). In recent years, the binary and ternary solid dispersions were prepared to enhance the dissolution of poorly soluble drugs to improve oral absorption of these drugs (12)(13)(14). Many water-soluble carriers have been employed for preparing solid dispersions, such as polyethylene glycols, polyvinylpyrrolidone (15), mannitol, hydroxypropyl methylcellulose (16), poloxamer (17), etc.…”

Section: Introductionmentioning

confidence: 99%

Preparation and In Vitro Evaluation of Solid Dispersions of Total Flavones of Hippophae rhamnoides L.

Xie

Yuan

et al. 2009

AAPS PharmSciTech

View full text Add to dashboard Cite

The purpose of this study was to enhance the dissolution of total flavones of Hippophae rhamnoides L. (TFH) by solid dispersions consisting of the drug and a polymeric carrier, poloxamer 188 (PXM). The solvent evaporation method was used to prepare solid dispersions. A 3(2) full-factorial design approach was used for optimization wherein the amount of solvent (X(1)) and the drug-to-polymer ratio (X(2)) were selected as independent variables and the percentage of TFH dissolved in 10 min (Q(10)) was selected as the dependent variable. Multiple linear regression analysis revealed that a suitable level of (1) and X(2) was required for obtaining higher dissolution of TFH from PXM solid dispersions. Solid dispersions were characterized by differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy, and dissolution tests. Characterization studies revealed that solid dispersion of TFH-PXM showed enhancement of TFH dissolution due to the conversion of TFH into a less crystalline and/or amorphous form. In conclusion, dissolution enhancement of TFH was obtained by preparing its solid dispersions in PXM using solvent method.

show abstract

Section: Introductionmentioning

confidence: 99%

Preparation and In Vitro Evaluation of Solid Dispersions of Total Flavones of Hippophae rhamnoides L.

Xie

Yuan

et al. 2009

AAPS PharmSciTech

View full text Add to dashboard Cite

show abstract

“…Most of the previous reports about the use of different formulative strategies to improve the dissolution properties of GLI [18,53,10,61,11,12,3,58,33,47] do not provide data about the actual consequent improvement of in vivo bioavailability and therapeutic efficacy of the drug from such formulations. On the other hand, an increase in GLI bioavailability has been reported for its solid dispersions in Gelucire or PEG 6000 with respect to a commercial formulation (Daonil tablets (Hoechst)), but without any effect on the duration of the antiglycemic action [52].…”

Section: In Vivo Studies Of Anti-glycemic Effect Of Gli-loaded Slnmentioning

confidence: 99%

“…Stabilized SLN containing lecithin alone showed a good EE% of 70.3 ± 5.2, while, unexpectedly, a clearly lower EE% value (19.6 ± 4.8) was found for those with PEG coating, despite their similar dimensions and stability properties. The lower entrapment efficiency of SLN7L could be attributed to the possible solubilizing and wetting effects of PEG toward GLI [4,11], which could produce a hydrophilic environment around the drug, thus reducing its affinity for the SLN lipid core, and/or favoring some drug losing during the SLN formation. It was also checked that the EE% values of both these SLN formulations remained almost unchanged after 2 h in acidic medium.…”

Section: Improvement Of Sln Stability In Gastrointestinal (Gi) Conditmentioning

confidence: 99%

“…The very poor water-solubility of the drug is responsible for its limited and variable oral bioavailability [34], as well as for problems of nonbio-equivalence among its different commercial tablets [6]. Therefore, various approaches have been applied over the last years aimed at improving the solubility and dissolution properties of glibenclamide, including formation of binary [52,53] or ternary [11] solid dispersions in hydrophilic polymers, complexation with cyclodextrins [18,10], combined use of cyclodextrins and polymers [61,12], formulation as liquid SMEDDS [3] or solid SMEDDS [33], or even as microparticles [35] or nanoparticles [58,47].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Development of solid lipid nanoparticles as carriers for improving oral bioavailability of glibenclamide

Gonçalves

Maestrelli

Mannelli

et al. 2016

European Journal of Pharmaceutics and Biopharmaceutics

View full text Add to dashboard Cite

a b s t r a c tA solid lipid nanoparticle (SLN) formulation was developed with the aim of improving the oral bioavailability and the therapeutic effectiveness of glibenclamide (GLI), a poorly water-soluble drug used in the treatment of type 2 diabetes. The SLN was prepared using different lipid components (Precirol Ò and Compritol Ò) and preparation procedures. Precirol-based SLN, obtained with the emulsion of solvent evaporation technique gave the best results and was selected for drug loading. Addition of lecithin to the SLN core or PEG coating was effective in increasing the nanoparticles stability in simulated gastric solution. Both such formulations were stable after one month storage at 5 ± 3°C, exhibited the absence of in vitro cytotoxicity, and presented a similar in vitro prolonged-release, reaching 100% release after 24 h. The lecithin-containing GLI-loaded SLN formulation, selected for in vivo studies in virtue of its higher EE% than the PEG-coated formulation (70.3% vs 19.6%), showed a significantly stronger hypoglycemic effect with respect to the drug alone, in terms of both shorter onset time and longer duration of the effect. These positive results indicated that the proposed SLN approach was successful in improving GLI oral bioavailability, confirming its potential as an effective delivery system for a suitable therapy of diabetes.

show abstract

“…The very low aqueous solubility of GLY gives rise to problems of poor and variable bioavailability and bio-inequivalence of its commercial dosage forms [15]. Several methods have been exploited to improve the solubility and dissolution properties of orally administered GLY, including drug amorphization [16], complexation with cyclodextrins [17], or solid dispersion in hydrophilic carriers [18][19][20]. As an alternative to these methods, we evaluated the effectiveness of the ME formulation approach to adequately increase the apparent solubility of this drug, and consequently its bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Mixture experiment methods in the development and optimization of microemulsion formulations

Furlanetto

Cirri

Piepel

et al. 2011

Journal of Pharmaceutical and Biomedical Analysis

View full text Add to dashboard Cite

Fast-Dissolving Tablets of Glyburide Based on Ternary Solid Dispersions with PEG 6000 and Surfactants

Cited by 26 publications

References 29 publications

Preparation and In Vitro Evaluation of Solid Dispersions of Total Flavones of Hippophae rhamnoides L.

Preparation and In Vitro Evaluation of Solid Dispersions of Total Flavones of Hippophae rhamnoides L.

Development of solid lipid nanoparticles as carriers for improving oral bioavailability of glibenclamide

Mixture experiment methods in the development and optimization of microemulsion formulations

Contact Info

Product

Resources

About