Development and Evaluation of Glyburide Fast Dissolving Tablets Using Solid Dispersion Technique

Abstract

Glyburide is a poorly water-soluble oral hypoglycemic agent, with problems of variable bioavailability and bio-inequivalence related to its poor water-solubility. This work investigated the possibility of developing glyburide tablets, allowing fast, reproducible, and complete drug dissolution, by using drug solid dispersion in polyethylene glycol. Phase-solubility studies were performed to investigate the drug-carrier interactions in solution, whereas differential scanning calorimetry, X-ray powder diffraction, and infrared spectroscopy were used to characterize the solid state of solid dispersions. The effects of several variables related to both solid dispersion preparation (cofusion or coevaporation technique, drug-to-carrier ratio, polyethylene glycol molecular weight) and tablet production (direct compression or previous wet-granulation, tablet hardness, drug, and solid dispersion particle size) on drug dissolution behavior were investigated. Tablets obtained by direct compression, with a hardness of 7-9 Kp, and containing larger sized solid dispersions (20-35 mesh, i.e., 850-500 microm) of micronized glyburide in polyethylene glycol 6000 prepared by the cofusion method gave the best results, with a 135% increase in drug dissolution efficiency at 60 min in comparison with a reference tablet formulation containing the pure micronized drug. Moreover, the glyburide dissolution profile from the newly developed tablets was clearly better than those from various commercial tablets at the same drug dosage.

Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques.

“…The DSC thermograms of gliclazide, PVP K30 and SD are shown in Figure 1. The sharp melting endotherm of pure gliclazide appeared at 168.9 o C, whereas small endotherm was observed in solid dispersions at 160.0 o C prepared with PVP K30, indicated the decreased intensity of crystalline nature [14]. It may be due to that the drug molecules were dispersed in the PVP.…”

Formulating Taste Masked Orally Disintegrating Tablets of a Bitter Drug Ibuprofen

“…The powder is passed till it forms a heap and touches the tip of the funnel. The radius was measured and angle of repose was calculated by using the above formula 5,6 . From the results in Table 1, it is evident that the drug has very poor flow properties, as the compressibility index, Hausner's ratio and Angle of repose values are high.…”

Micellar Solubilization of Some Poorly Soluble Antidiabetic Drugs: A Technical Note

“…Improvement in the solubility of glyburide by solid dispersion technique has been reported (18). Ammar et al (19) have shown that the association of water soluble polymers with glimepiridecyclodextrin systems leads to great enhancement in the dissolution rate of the drug.…”