Physicochemical characterization of gliclazide–macrogol solid dispersion and tablets based on optimized dispersion

Khattab, Ibrahim; Nada, Aly; Zaghloul, Abdel-Azim

doi:10.3109/03639040903578734

Cited by 19 publications

(16 citation statements)

References 21 publications

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“…Six tablets of each formulation were placed one in each vessel containing 900 mL of the test medium. Samples (2 mL) were withdrawn at predetermined time points (10,20,30,45,60, and 120 min), and the volume withdrawn was taken into consideration when calculating the percentage release of GLZ or Na-GLZ in the remaining volume of test medium. Filtration of samples was performed in situ via resident probes to which polyethylene filters were connected and designed to be left in the dissolution vessel for the duration of the test.…”

Section: Dissolution Testsmentioning

confidence: 99%

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Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

El-Sabawi¹,

Hamdan²

2014

Dissolution Technol.

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Gliclazide is a hypoglycemic agent exhibiting to some extent inadequate and variable absorption as a consequence of poor aqueous solubility and slow dissolution rates. A sodium salt of gliclazide was prepared and investigated for solubility and dissolution properties in comparison to untreated gliclazide. The salt was formed by adding equimolar amounts of gliclazide and sodium hydroxide in an aqueous-ethanolic phase. To confirm salt formation, sodium gliclazide was fully characterized by spectroscopy, differential scanning calorimetry, and potentiometric titration. Furthermore, solubility and in vitro dissolution studies of formulated tablets were performed at pH values of 1.2, 4.5, and 6.8. Sodium gliclazide demonstrated a significant increase in solubility at pH values of 4.5 and 6.8. The most apparent increase was achieved in unbuffered distilled water with a 235-fold higher solubility. Moreover, sodium gliclazide showed an enhancement in the dissolution rate in all tested media, but most significantly at pH 4.5 and 6.8. The highest difference (60%) in dissolution rate between gliclazide and its sodium salt was obtained at pH 6.8 at 30 min.The sodium salt of gliclazide presents improved solubility and drug dissolution, therefore limiting the possibility of variable absorption and improving the onset of action with potential enhancement in its overall bioavailability.

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Section: Dissolution Testsmentioning

confidence: 99%

“…One approach involves the preparation of solid dispersions of GLZ with hydrophilic carriers such as polyethylene glycols through applying different methodologies including fusion techniques (9)(10)(11)(12), cogrinding methods (13), solvent melting, and solvent evaporation methods (14).…”

Section: Introductionmentioning

confidence: 99%

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

El-Sabawi¹,

Hamdan²

2014

Dissolution Technol.

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“…4,5) The pH-dependent solubility of GLZ was suggested to be a relevant factor for its slow absorption in the gastrointestinal tract (GIT). 6,7) To improve its availability, modified-release (MR) tablets of the drug were formulated with a hydrophilic matrix to obtain a more consistent and less pH-dependent release profile of the active pharmaceutical ingredient over a 24 h period. 8,9) The formulation can be administered before, during or after meals.…”

mentioning

confidence: 99%

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Bezerra

Pinto

Cabral

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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Gliclazide (GLZ) is a second generation hypoglycemic drug used for the treatment of Type 2 diabetes mellitus. The low solubility of GLZ has been described as the rate limiting step for drug dissolution and absorption, thus a prediction of its in vivo behavior based on a discriminative dissolution test should lead to a relevant in vitro-in vivo correlation (IVIVC). The aim of this study was to develop a dissolution method for GLZ modified-release (MR) tablets using an United States Pharmacopeia (USP) apparatus 3 through its evaluation by an IVIVC analysis. Various dissolution parameters were evaluated to establish an in vitro method for GLZ tablets. The final dissolution conditions, referred to as method 3, utilized a 400 µm mesh and 30 dips per minute over a total period of 10 h that included 1h in HCl media (pH 1.2), 2h in acetate buffer solution (pH 4.5), 1 h in phosphate buffer solution (PBS; pH 5.8), 5h in PBS (pH 6.8) and finally 1h in PBS (pH 7.2). The calculated point-to-point IVIVC (R 2 0.9970) was significantly greater than other methods. The robustness of method 3 suggests it could be applied to pharmaceutical equivalence studies and for quality control analyses of GLZ.

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“…Various grades of polyethylene glycol (PEG) have been tried for solubility enhancement, and the effect of the molecular weight of PEG on drug release has also been reported in similar studies. [4] The effect of PEG20000 on the solubility and drug release of ACY from the resulting SDs were evaluated using a wide spectrum of advanced characterization techniques.…”

Section: Introductionmentioning

confidence: 99%

Mechanistic insights into acyclovir-polyethylene glycol 20000 binary dispersions

Krishnamoorthy

Parasuraman

Gunasunderi

et al. 2016

Int J Pharma Investig

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Objective:The objective of this study is to provide a mechanistic insight into solubility enhancement and dissolution of acyclovir (ACY) by polyethylene glycol20000 (PEG20000).Materials and Methods:Solid dispersions with differing ratios of drug (ACY) and carrier (PEG20000) were prepared and evaluated by phase solubility, in vitro release studies, kinetic analysis, in situ perfusion, and in vitro permeation studies. Solid state characterization was also done by Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared spectroscopy (FT-IR) analysis and surface morphology was assessed by Polarizing Microscopic Image (PMI) analysis, Scanning Electron Microscopy (SEM), Atomic Force Microscopy (AFM), and Nuclear Magnetic Resonance (NMR) analysis.Results:Thermodynamic parameters proved the solubilization effect of carrier. The aqueous solubility and dissolution of ACY were increased in all samples. Formation of solid solution, crystallinity reduction, and absence of interaction between drug and carrier was proved by XRD, DSC, and FTIR analysis. The particle size reduction and change in surface morphology were confirmed by SEM and AFM and analysis. The permeation coefficient and amount of drug diffused was higher in samples as compared to ACY. The stability was high in dispersions, and it was proved by NMR analysis.Conclusion:The mechanical insights into the enhancement of solubility and dissolution could be used as a platform to improve the aqueous solubility for other poor water soluble drugs.

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Physicochemical characterization of gliclazide–macrogol solid dispersion and tablets based on optimized dispersion

Abstract: It was thus concluded that SD formulations of GLC can be successfully used to design a solid dosage form of the drug, which would have significant advantages over the current marketed tablets.

Cited by 19 publications

References 21 publications

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Mechanistic insights into acyclovir-polyethylene glycol 20000 binary dispersions

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