Evaluation of some Methods for Preparing Gliclazide-&amp;#946-Cyclodextrin Inclusion Complexes

Sapkal, Nidhi; Kilor, Vaishali; Bhursari, K P; Daud, A S

doi:10.4314/tjpr.v6i4.14667

Cited by 38 publications

(31 citation statements)

References 14 publications

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“…Another approach that has been investigated extensively is the complexation of poorly water-soluble drugs with cyclodextrins, which was found to improve the aqueous solubility of such drugs (15)(16)(17)(18)(19). Enhanced GLZ dissolution was also achieved via formulation of ordered mixtures of the hydrophobic drug with water-soluble carriers of larger particle size such as mannitol and lactose (7).…”

Section: Introductionmentioning

confidence: 99%

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: Introductionmentioning

confidence: 99%

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

El-Sabawi¹,

Hamdan²

2014

Dissolution Technol.

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“…The solvent evaporation, melt adsorption, fusion, spray drying, spray freezing, spray congealing, melt extrusion, and supercritical fluid precipitation are the techniques reported for the preparation of solid dispersions. There is report on improvement of solubility of gliclazide using cyclodextrin inclusion complex approach [5]. In the present work, fusion and solvent evaporation techniques were used to prepare gliclazide solid dispersions.…”

Section: Introductionmentioning

confidence: 99%

Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques.

Shavi

Kumar

Usha

et al. 2010

Int. J. Drug Delivery

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Abstract:Gliclazide is practically insoluble in water and its bioavailability is limited by dissolution rate. To enhance the dissolution rate and bioavailability the present study was aimed to formulate solid dispersions using different water soluble polymers such as polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000) using fusion method and polyvinyl pyrrolidone K-30 (PVP K 30) by solvent evaporation method. The interaction of gliclazide with the hydrophilic polymers was studied by Differential Scanning Calorimetry (DSC), Fourier Transformation-Infrared Spectroscopy (FTIR) and X-Ray diffraction analysis. Solid dispersions were characterized for physicochemical properties like drug content, surface morphology and dissolution studies. Various factors like type of polymer and ratio of the drug to polymer on the solubility and dissolution rate of the drug were also evaluated. Pharmacokinetic studies of optimized formulation were compared with pure drug and marketed formulation in wistar rats. The dissolution of the pure drug and solid dispersion prepared with PVP K 30 (1:1) showed 38.3 + 4.5 % and 95 + 5.2 % release respectively within 30 min. Peak plasma concentration of pure drug, solid dispersion (PVP K 30) and marketed formulation was found to be 8.76 + 2.5, 16.04 + 5.5 and 9.24 + 3.6 μg/ml respectively, from these results it was observed that there is two fold increase in peak plasma concentration compared to pure drug. Solid dispersion is an effective technique in increasing solubility, dissolution rate and bioavailability of the poorly soluble drugs.

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“…Complexation of gliclazide with β-cyclodextrin and the characterization of the resulting complex has been reported [6,7,8]. Complexation of gliclazide with β-cyclodextrin-hydroxypropyl methylcellulose enhanced its hypoglycemic activity has been reported [9].…”

Section: Introductionmentioning

confidence: 99%