公开(公告)号：US08669265B2

公开(公告)日：2014-03-11

申请号：US13900647

申请日：2013-05-23

Applicant: Hetero Research Foundation

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Thungathurthy Srinivas Rao

IPC: A61K31/517

CPC classification number: C07D239/94

Abstract: The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 μm to 15 μm and 90 volume-% of the particles (D90) ranging from about 14 μm to 30 μm, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles.

Abstract translation: 本发明提供了一种新颖稳定的埃洛替尼游离碱的水合形式及其制备方法。 本发明还提供了一种制备基本上不含多晶型物B的盐酸埃罗替尼结晶多晶型物的方法。本发明还涉及平均粒径（D50）为约4μm至15μm和90体积％的盐酸埃罗替尼结晶颗粒， 约14μm至30μm的颗粒（D90）的百分比，制造所述结晶颗粒的方法，以及包含所述结晶颗粒的药物组合物。