Development and evaluation of glibenclamide floating tablet with optimum release

作者：Essa Ebtessam A^*; Elkotb Fatma E; Eldin Esmat E Zin; El Maghraby Gamal M

来源：JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2015, 27: 28-36.

DOI：10.1016/j.jddst.2015.04.002

• Gastroretentive
• Absorption window
• Carbopol
• Poloxamer
• Solid dispersion

Glibenclamide is a poorly soluble drug with narrow absorption The strategy of this work was to enhance the dissolution rate of Glibenclamide by solid dispersion (SD) technique with optimum formulation being developed as floating tablets. Binary SDs of drug and poloxamer 407 were prepared at different ratios. Ternary dispersion was prepared by the addition of sodium bicarbonate as third component. For floating tablets, a series of floating formulations was prepared using HPMC k4 (F1), HPMC k15 (F2) and combination of both with Carbopol (F3), using ternary solid dispersion as the drug matrix. Effect of matrix type was studied, F4 and F5 were prepared using the same floating matrix as F3 but drug was either binary poloxamer SD or physically mixed with bicarbonate. Unprocessed drug in floating matrix was used as control. All SDs increased drug dissolution rate, with ternary mixture showing the highest dissolution efficiency reflecting synergism between poloxamer and sodium bicarbonate. Solid state characterization showed evidences of decreased drug crystalline structure. F3 showed the best floating behavior. Considering floating behavior together with the release pattern, F3 was the optimum formulation. Overall, employing drug as ternary SD with optimum dissolution can provide flexibility in developing controlled release floating system.

• 出版日期2015-6