The objective of this study was to develop and optimize the gliclazide extended-release formulations by using simultaneously combination of two hydrophilic polymers: HPMC K 15M and sodium alginate as retardant. D-Optimal mixture design was employed to evaluate the effect of HPMC (X(1)), lactose (X(2)), and sodium alginate (X(3)) concentrations on the release rate of gliclazide from the matrices...

The poorly water soluble antidiabetic drug gliclazide was selected to study the effect of excipients on dissolution rate enhancement. Ordered mixtures of micronized gliclazide with lactose, mannitol, sorbitol, maltitol and sodium chloride were prepared by manual shaking of glass vials containing the drug and excipient(s). Different water soluble excipients, addition of surfactant and superdisin...

Previous studies showed associations between variants in TCF7L2 gene and the therapeutic response to sulfonylureas. All sulfonylureas stimulate insulin secretion by the closure of ATP-sensitive potassium (KATP) channel. The aim of the present study was to compare TCF7L2 genotype specific effect of gliclazide binding to KATP channel A-site (Group 1) with sulfonylureas binding to AB-site (Group 2...

BACKGROUND Increased oxidative stress is involved in the pathogenesis of diabetic nephropathy and neuropathy. Angiotensin II is a know factor in the pathogenesis of diabetic complications. The protective effects of ACEIs is known in diabetic nephropathy. Thus, Angiotensin receptor antagonists may have the same role. In this study, possible antidiabetic effect of Telmisartan and its tissues anti...

An in vivo study has been conducted to observe the effects of caffeine on the hypoglycemic activity of gliclazide and metformin HCI in rats. For this, healthy rats weighing about 250±25 g were used and the blood sugar levels were measured after administration of a drug alone and in combination. Diabetes was induced in rats by administration of alloxan at a dose of 40 mg/kg body weight. Drugs we...

Among sulfonylureas, gliclazide is prescribed to 80% of the diabetic population and mainly metabolized by CYP2C9 in Caucasians. Our data shows that the orientation of the substrate is changed and therefore, the site of oxidation with respect to heme-Fe is altered in *2. This leads to an altered metabolic pathway in *2 and it is a rate limiting step in gliclazide metabolism. Our results also sho...

Gliclazide is an oral hypoglycaemic agent used for the treatment of non-insulin dependent diabetes mellitus T2DM. has low solubility in stomach and poor absorption bioavailability. The pH-dependent gliclazide influences intra- inter-subject variability. purpose this study was to develop, optimize evaluate pH-sensitive nanoparticles (NPs) based on Eudragit® S100 polymer delivery (GLZ) attempt im...