Physicochemical properties of the binary system glibenclamide and polyethylene glycol 4000 |
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Authors: | Bartsch S E Griesser U J |
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Institution: | (1) Institute of Pharmacy, Department of Pharmaceutical Technology, University of Innsbruck, Innrain 52, A-6020 Innsbruck, Austria;(2) Institute of Pharmacy, Ph. Technology, University of Innsbruck, Innrain 52, 6020 Innsbruck, Austria |
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Abstract: | Solid dispersions of the antidiabetic drug glibenclamide and polyethylene glycol 4000 (macrogol 4000) were prepared by the
melting method in order to increase the solubility of this poorly water-soluble compound. The temperature/composition phase
diagram of the components was analyzed by hot-stage microscopy and differential scanning calorimetry, showing a monotectic.
Polarized light hot stage microscopy and X-ray-powder diffraction confirmed, that glibenclamide is mainly present in a non-crystalline
state after melting and solidifying of a 10% (w/w) mixture, which results in an enhanced solubility compared to physical mixtures. The solubility and dissolution rate of the
drug increases clearly with decreasing drug/polymer ratio. Moreover, it was observed for the first time that a drug could
crystallize as whiskers at the surface of aged solid dispersion particles. Besides relaxation phenomena, this crystallization
mechanism may be responsible for a deterioration of liberation properties and bioavailability of solid dispersion based drug
products with increasing storage time.
This revised version was published online in July 2006 with corrections to the Cover Date. |
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Keywords: | glibenclamide solubility thermal analysis solid dispersions binary phase diagram dissolution crystal whiskers physical mixtures polyethylene glycol |
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