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Oral pharmaceutical formulation in the form of a plurality of microcapsules for prolonged release of active principle(s) with slow solubility
专利权人:
Florence Guimberteau
发明人:
Florence Guimberteau,Catherine Castan,Rémi Meyrueix
申请号:
US10522252
公开号:
US08652523B2
申请日:
2003.07.28
申请国别(地区):
US
年份:
2014
代理人:
摘要:
The invention concerns microcapsules with prolonged release of active principles with low solubility, consisting of a core containing the active principle and coated with a polymer layer which controls the release of the active principle. The aim is that said oral microcapsules containing hardly soluble active principles, should have a coating film of sufficient thickness to ensure controlled permeability and should be adapted to industrial reproduction. This is achieved by the inventive microcapsules of mean diameter less than 1000 microns, and whereof the coating film contains a film-forming polymer (P1) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA). Said microcapsules are characterized in that their coating films represents at least 3% p/p of dry matter, relative to their total weight and their core contains a hardly soluble active principle and a solubilizing agent (polyoxyethylene hydrogenated castor oil) which provides the core wherein it is contained with properties such that the behavior of the exposed core (non-coated) in a given dissolving test (TD), is as follows: release of 80% of active principle in less than two hours. The invention also concerns the use of such microcapsules in galenic formulation.
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