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    Substantially Pure and a Stable Crystalline Form of Bosentan
    2.
    发明申请
    Substantially Pure and a Stable Crystalline Form of Bosentan 审中-公开
    波斯坦的基本纯度和稳定的结晶形式

    公开(公告)号：US20110021547A1

    公开(公告)日：2011-01-27

    申请号：US12864571

    申请日：2009-01-22

    申请人： Girish Dixit ,  Nandkumar Gaikwad ,  Hima Prasad Naidu ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    发明人： Girish Dixit ,  Nandkumar Gaikwad ,  Hima Prasad Naidu ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    IPC分类号： A61K31/513 ,  C07D403/04

    CPC分类号： C07D403/04

    摘要： Described is a highly stable crystalline form of bosentan having a water content in the range of about 3-4% by weight, based on the total weight of the bosentan, (bosentan crystalline form A5), a process for preparation thereof, and pharmaceutical compositions comprising the bosentan crystalline form A5. Provided also herein is a bosentan impurity, p-tert-butyl-N[6-hydroxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide (deshydroxyethyl bosentan impurity), and process for preparing and isolating thereof. Further provided are highly pure bosentan or a pharmaceutically acceptable salt thereof substantially free of deshydroxyethyl bosentan and bosentan dimer impurities, process for the preparation thereof, and pharmaceutical compositions comprising solid particles of highly pure bosentan or a pharmaceutically acceptable salt thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 300 microns.

    摘要翻译： 描述了基于波生坦总重量（波生坦结晶形式A5），其制备方法和药物组合物的水含量在约3-4重量％范围内的波生坦的高度稳定的结晶形式 包括波生坦晶体A5。 本文还提供了一种波生坦杂质，对叔丁基-N [6-羟基-5-（2-甲氧基苯氧基）-2-（2-嘧啶基）-4-嘧啶基]苯磺酰胺（脱羟乙基波生坦杂质），和 制备和分离。 还提供了高纯度的波生坦或其药学上可接受的盐，其基本上不含脱羟基乙基波生坦和波生坦二聚体杂质，其制备方法以及包含高纯度波生坦固体颗粒或其药学上可接受的盐的药物组合物，其中90体积％ 的颗粒（D90）具有小于约300微米的尺寸。