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    • 2. 发明申请
    • MEDICAMENT THAT IS INTENDED FOR ORAL ADMINISTRATION, COMPRISING A CYCLOOXYGENASE-2 INHIBITOR, AND PREPARATION METHOD THEREOF
    • 专门用于口服给药的药物,包含CYCLOOXYGENASE-2抑制剂及其制备方法
    • WO2006077334A3
    • 2007-04-12
    • PCT/FR2006000144
    • 2006-01-23
    • VETOQUINOLMOREAU MARINETTEOSTY NICOLAS
    • MOREAU MARINETTEOSTY NICOLAS
    • A61K9/50
    • A61K9/5078
    • The invention relates to a medicament which is intended for oral administration, which comprises a cyclooxygenase-2 inhibitor and which has improved bioavailability, and to a method of preparing said medicament. The inventive medicament comprises an agglomerate based on inert solid particles based on at least one excipient, said agglomerate comprising a cyclooxygenase-2 inhibitor and at least one hydrophilic polymer. According to the invention, the agglomerate comprises a spray which is applied to the aforementioned particles, consisting of a solution or suspension of micronized grains of the inhibitor in said polymer(s), in order to agglomerate said particles. The inventive method essentially comprises the following steps, namely: (i) the preparation of a sprayable liquid that is based on the micronized grains of said inhibitor in solution or in suspension in at least one hydrophilic polymer; and (ii) the spraying of the liquid onto the solid particles, in order to obtain the agglomerate by means of wet granulation, said agglomerate comprising the grain solution or suspension spray.
    • 本发明涉及旨在用于口服给药的药物,其包含环氧合酶-2抑制剂并且其具有改善的生物利用度,以及制备所述药物的方法。 本发明的药物包含基于至少一种赋形剂的基于惰性固体颗粒的附聚物,所述附聚物包含环加氧酶-2抑制剂和至少一种亲水性聚合物。 根据本发明,附聚物包括施加到上述颗粒的喷雾,由在所述聚合物中的抑制剂的微粉化颗粒的溶液或悬浮液组成,以使所述颗粒附聚。 本发明的方法基本上包括以下步骤,即:(i)制备基于所述抑制剂在溶液中或悬浮于至少一种亲水性聚合物中的微粉化颗粒的可喷雾液体; 和(ii)将液体喷射到固体颗粒上,以便通过湿法制粒获得附聚物,所述附聚物包含谷物溶液或悬浮液喷雾。