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Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles
专利权人:
Catherine Castan;Rémi Meyrueix;Gérard Soula;Valérie Legrand
发明人:
Valérie Legrand,Catherine Castan,Rémi Meyrueix,Gérard Soula
申请号:
US10826690
公开号:
US08101209B2
申请日:
2004.04.19
申请国别(地区):
US
年份:
2012
代理人:
摘要:
The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system comprises of microcapsules (200 to 600 μm) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5. These microcapsules have a dissolution behavior in vitro such that, at a constant pH of 1.4, a latency phase of between 1 and 5 hours is observed, followed by a release of the AP, and such that the change from pH 1.4 to pH 6.8 results in a release of the AP without a latency period in vitro.
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中国工程科技知识中心
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