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Microparticulate oral galenic form for the delayed and controlled release of pharmaceutical active ingredients
专利权人:
Flamel Ireland Limited
发明人:
LEGRAND, Valérie,CASTAN, Catherine,MEYRUEIX, Rémi,SOULA, Gérard
申请号:
ES02800645
公开号:
ES2661723T3
申请日:
2002.10.09
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Microparticulate oral galenic form of delayed and controlled release of at least one active principle, with the exclusion of peridopril, this active principle having an in vivo absorption window essentially limited to the upper parts of the gastrointestinal tract, this oral galenic form comprising microcapsules " reservoir "containing at least one active ingredient with the exclusion of perindopril, these microcapsules being of the type constituted by particles of active principle each coated with at least one coating film, and characterized by the fact that this coating film is consisting of a composite material: - comprising: at least one hydrophilic polymer A bearing ionized groups at neutral pH, and at least one hydrophobic compound B selected from the group consisting of: - vegetable waxes taken alone or in mixtures with each other; - hydrogenated vegetable oils taken alone or in admixture with each other; preferably selected from the group comprising: hydrogenated cottonseed oil, hydrogenated soybean oil, hydrogenated palm oil and all mixtures with each other; - diesters of glycerol and at least one fatty acid, preferably benzene acid, taken alone or in mixtures with each other; - triesters of glycerol and at least one fatty acid, preferably behenic acid, taken alone or in mixtures with each other; - and representing a mass fraction (% by weight with respect to the total mass of the microcapsules) <;= 40: ∗ because said microcapsules have a diameter between 200 and 800 microns, preferably between 200 and 600 microns; ∗ because the B / A weight ratio is between 0.5 and 1.5; ∗ because the release of the active substance from said microcapsules is controlled by two different activation mechanisms, one being based on a variation of pH and the other allowing the release of the active substance, at the end of a predetermined time of permanence in the stomach, with an in vitro dissolution behavior, carried out according to the indications of the European Pharmacopo
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