Design amorphous solid dispersions with optimal physical stability and dissolution performance

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:xgz521521
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  With the extensive adoption of combinatorial chemistry and high throughput screening by the pharmaceutical industry, a large percentage (>50%) of selected drug candidates are poorly water-soluble, which presents a critical hurdle for the pre-clinical and clinical assessments,and commercial drug product development.As the last resort for drug delivery, drug-polymer solid dispersion technology, in particular, stabilized amorphous solid dispersion technology,has been demonstrated as a highly effective and versatile technology for oral delivery of these poorly water-soluble compounds.As a thermodynamically unstable system, the drug-polymer interaction, stabilization mechanism for amorphous drugs, phase behavior of the drug-polymer binary system, dissolution behavior, etc., have been drawing continuous research interests over the past two decades.While knowledge is accumulating, potential risks still persist and deserve further investigation.In this presentation, an overview of the current understanding about solid dispersion technology will be discussed;more importantly,examples will be used to illustrate several critical risks, such as drug-polymer mixing homogeneity, effect of water on the physical stability, and in vivo pharmacokinetic performance, etc.Potential strategies to develop solid dispersions with satisfactory physical stability and in vivo performance will be proposed.
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