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Abstract
Glibenclamide (GLB) is a second-generation sulfonylurea oral hypoglycemic agent used in the treatment of non-insulin dependent diabetes mellitus. The use of this drug is limited due to its poor dissolution and pharmacokinetic profile. In order to nullify these drawbacks, GLB oral thin films were prepared and evaluated to study the influence of preparatory conditions on the physicochemical properties by using Scanning Electron Microscopy (SEM), Fourier Transform Infra-red Spectroscopy (FTIR) and Differential Scanning Calorimetric (DSC). The surface pH of the GLB thin film was found to be in the range of 6.50 ± 0.10 and it is non-irritant to mucosal lining of the oral cavity. The results of the SEM analysis showed uniform surface morphology with homogenous distribution of GLB pure drug in PVP matrix. The in vitro drug release profile at pH 5.0 and 7.5 revealed sustained release patterns for a period of 8 h. The GLB oral thin film showed an enhanced in vivo insulin release profiles as compared to pure GLB drug. Thus, the results of the present study revealed that, the prepared GLB oral thin film can be used as alternative strategy to deliver glibenclamide for diabetes mellitus as it showed a significant role in increasing in vitro dissolution and in vivo insulin release profiles.
Highlights
Glibenclamide (GLB) is a long-acting oral anti hyperglycemic agent used in the treatment of type II diabetes, closely related to sulfa drugs [1]
GLB acts through stimulating the insulin release from pancreatic β-cells by binding highaffinity receptors that are present in the K/ATP channels in β-cells of plasma membranes and it increases the sensitivity of peripheral tissue to insulin [2]
The results of the present study showed the enhanced insulin release properties of GLB thin film, when compared to GLB pure drug at the selected dose and route of administration (Figure 6)
Summary
Glibenclamide (GLB) is a long-acting oral anti hyperglycemic agent used in the treatment of type II diabetes (noninsulin-dependent diabetes), closely related to sulfa drugs [1]. Being a class II drug (it has high permeability and poor water solubility), the rate of drug dissolution is most certainly the principal limitation to its oral absorption [3,4]. The GLB showed to have a low oral bioavailability (40-45%), short biological half-life (3-5 h), and undergoes oxidative hepatic first-pass metabolism to yield metabolites having no hypoglycemic activity [6]. All these factors contributed to glucose variability and other gastric side effects viz., nausea, vomiting, anorexia and increased appetite [6,7]
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