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Adsorption and co-adsorption; promising approaches for enhancement of glibenclamide dissolution

Research Authors
Mahmoud A. Younis, Hesham M. Tawfeek
Research Department
Research Journal
4th international conference of pharmaceutical sciences, faculty of pharmacy, Future university, Egypt
Research Publisher
NULL
Research Rank
4
Research Vol
NULL
Research Website
NULL
Research Year
2017
Research Abstract

Glibenclamide (GLC) is a potent oral hypoglycemic drug widely-used in the treatment of type II diabetes mellitus. It is practically-insoluble in water which hindering its dissolution at the gastric pH hence, lowering its absorption and oral bioavailability (45% only. The aim of this work was to improve such dissolution via formulation of adsorbates and co-adsorbates to enhance the oral bioavailability of GLC. This will enable its use at a lower dose to minimize the cost and possible side effects. Adsorption of drug onto different adsorbents including Laponite RD, Laponite FP, Neusilin US2, Aerosil 200 and Florite R was studied and Langmuir adsorption isotherms were constructed. Moreover, the effect of surfactant addition on the adsorption process was studied also using different concentrations of different surfactants namely; Tween 80, Pluronic F-127 and Pluronic F-68. Laponite RD as an adsorbent and Pluronic F-68 as a surfactant showed the best results and therefore, they were used in the formulation of adsorbates and co-adsorbates. Adsorbates of drug with Laponite RD were prepared in different weight ratios using two different techniques; physical mixing and solvent evaporation technique. Co-adsorbates of drug with pluronic F-68 and Laponite RD were prepared in different weight ratios by solvent evaporation technique. The prepared systems were tested for their drug content and in-vitro dissolution rate. The results showed marked enhancement of GLC in-vitro dissolution rate compared with untreated GLC which would be promising in further incorporation of the optimized formulation into several dosage forms with enhanced bioavailability.