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Solid dispersions of water-insol. drugs - comprising coherent crystals of drug in water-soluble matrix
Solid dispersions of water-insol. drugs - comprising coherent crystals of drug in water-soluble matrix
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机译：水溶胶的固体分散体。药物-在水溶性基质中包含药物的相干晶体
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摘要
New solid dispersions comprise a water-insoluble drug (I) in a water-soluble crystalline matrix (II), where (I) has a solubility of up to 0.01% in H2O at 37 deg.C. The dispersions contain more than 5 wt.% of (I) in coherent crystalline form. New crystalline porous drug structures have a BET surface area of 1-15 m2/g and a pore vol. of 20-95% (by Hg porosimetry), where the drug has a water-solubility of up to 0.01% at 37 deg.C. USE/ADVANTAGE - The prods. are esp. useful for oral admin. of dihydropyridine-type Ca antagonists, e.g. nifedipine, diethyl 4-(2,1,3-benzoxadiazol-4-yl) -1,4-dihydro -2,6-dimethyl-3,5-pyridine dicarboxylate (Ia) and 3-isopropyl 5-methyl 4-(2,1,3-benzodioxazol-4-yl) -1,4-dihydro-2,6-dimethyl -3,5-dicarboxylate (Ib). They provide controlled release without impaired bioavailability.
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