Abstract
PENETRATION ENHANCEMENT OF METFORMIN HCL BY USING MIXED SURFACTANTS AS GRANULATING AGENT

Omar Y. Mady, Ebtessam A. Essa, Ahmed A. Donia and Adam A. Al-Shoubki*

ABSTRACT

The aim of this study is enhancement the permeability of metformin HCl drug by using an industrial granulation technique. Span 60, as a surfactant used in food industry, was used as a granulating agent. That is because it has low melting point and at the same time it is solid at room temperature. After formation of the drug granules, a constant volume of tween 80 was added while stirring to induce a hydrophilic character to the granule surface. The granulation of the drug led to decreasing the bulk density in comparing to the pure drug. In addition, the flow characters and compressibility of the drug granules (micromeritics characters) are markedly improved. For examine the penetration enhancing effect of the used surfactants, non-everted intestinal sac technique was used. The results showed increasing the apparent permeability of the drug granulated by span 60 with Tween 80 comparing to the drug alone. That is may be due to inhibition the activity of P-gp. In addition, the presence of span 60 and tween 80 may be provide the suitable HLP value, which improved the drug permeation and consequently bioavailability. This technique could be suggested to solve the permeability problem of class III.

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