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 mum to 15 mum and 90 volume-% of the particles (D90) ranging from about 14 mum to 30 mum, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles.