A NOVEL HYDRATED FORM OF ERLOTINIB FREE BASE AND A PROCESS FOR PREPARATION OF ERLOTINIB HYDROCHLORIDE POLYMORPH FORM A SUBSTANTIALLY FREE OF POLYMORPH FORM B

摘要

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.