Enabling Technologies to Improve Oral Bioavailability of Poorly Soluble Compounds by Amorphous Solid

来源 :第二届全国生物颗粒学术研讨会、第三届国际工业药学和临床药学研讨会暨第一届岭南国际药学大会 | 被引量 : 0次 | 上传用户:wfdzdb
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  The interest in Amorphous Solid Dispersions (ASDs) as a means of improving solubility of Active Pharmaceutical Ingredients (APIs) is still strong as highlighted by many recently approved market products.Unlike crystalline APIs which solubilities and dissolution rates are reduced due to high lattice energy barriers, the amorphous phase has high apparent solubility, good dissolution rates and bioavailability.In an amorphous solid dispersion the API is at the molecular level dispersed in a polymer matrix.The mobility of the API molecules must be low enough to ensure that it will be unlikely that crystallization nuclei are formed.Making use of the amorphous phase of your drug rather than crystalline forms could shift your drug from a class 2 (or 4) into a class 1 (or 3) drug according to the biopharmaceutical classification system.In this presentation, the techniques for making ASD by spray drying and hot melt extrusion will be thoroughly discussed.
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