发明授权
- 专利标题: Method for assessing absorption properties of low solubility compounds
- 专利标题(中): 评估低溶解度化合物吸收性能的方法
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申请号: US12224449申请日: 2007-02-27
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公开(公告)号: US08175815B2公开(公告)日: 2012-05-08
- 发明人: Alex Avdeef , Manfred Kansy
- 申请人: Alex Avdeef , Manfred Kansy
- 申请人地址: CH Basel US MA Woburn
- 专利权人: F. Hoffmann-La Roche AG,pION Inc.
- 当前专利权人: F. Hoffmann-La Roche AG,pION Inc.
- 当前专利权人地址: CH Basel US MA Woburn
- 代理机构: Mintz Levin Cohn Ferris Glovsky and Popeo PC
- 国际申请: PCT/CH2007/000097 WO 20070227
- 国际公布: WO2007/098625 WO 20070907
- 主分类号: G01N31/00
- IPC分类号: G01N31/00 ; C08B11/20
摘要:
The invention deals with a method for the assessment of the effect of excipients, pH and combinations thereof on the predicted absorption properties of low solubility compounds, comprising the step of assessing a change in a flux function for a combination of a low solubility compound and an excipient at at least one predefined pH value. The method allows a fast, accurate, and economic evaluation of an excipient being capable of optimizing the absorption of drug molecules, i.e. low solubility compounds. Furthermore, animal experiments can be excluded and use of compounds can be reduced in such evaluation. Thus, screening for future formulation efficacy (pH and excipient effects on solubility and permeability) of drug candidates can be justified, since the method is fast, compound-sparing, cost-effective, and reasonably accurate.
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