Oral pharmaceutical formulation in the form of a plurality of microcapsules for prolonged release of active principle(s) with low solubility

可延长释放低溶解度活性成分的多微囊形式的口服药物制剂

Abstract

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-formingpolymer (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 behaviour 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.
本发明涉及延长释放低溶解度活性成分(AP)的微囊,这些微囊由包含AP的囊心以及包裹囊心的用于控制AP释放的聚合物层构成。本发明的目的在于,包含低溶解度AP的这些口服微囊应当具有厚度足以确保可控的渗透性并且在工业上可重复的包膜。所述目的通过本发明的微囊来达到,这些微囊的平均直径小于1000微米,并且其包膜含有在胃肠道液中不溶的成膜聚合物(P1);水溶性聚合物(P2);增塑剂(PL);和任选的润滑表面活性剂(TA);其特征在于,它们的包膜相对于它们的总质量为至少3%干重/干重,并且它们的囊心含有低溶解度AP和增溶剂(聚氧乙烯化氢化蓖麻油),该增溶剂赋予含有增溶剂的囊心这样的特性,即裸露的(未涂覆的)囊心在给定溶解试验TD中的性质如下:在小于2小时的时间释放80%的AP。本发明还涉及所述微囊在盖仑制剂中的用途。

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