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AssigneeHetero Drugs Limited
InventorsBandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
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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.
A hydrated crystalline form of erlotinib free base having water content in the range of about 1-10% by weight, characterized by peaks in the powder X-ray diffraction pattern having 26 angle positions at about 6.4, 7.4, 11.2, 12.8, 14.5, 16.3, 18.2, 20.0, 20.5, 21.9, 22.3, 23.3, 23.5, 24.6, 27.6 and 30.0-0.2 degrees.
A process for preparation of erlotinib hydrochloride crystalline polymorph form A substantially free of polymorph form B, which comprises adding hydrochloric acid to a solution of erlotinib free base in a solvent or a mixture of solvents selected from isopropyl acetate and methyl isobutyl ketone, and isolating erlotinib hydrochloride crystalline polymorph form A substantially free of polymorph B from the solution.
Erlotinib hydrochloride crystalline polymorph form A characterized by peaks in the powder X-ray diffraction pattern having 26 angle positions at about 5.75, 9.88, 11.40, 18.97, 22.84, 23.65, 24.29, 24.75, 25.56 and 29.37±0.2 degrees and by the absence of a peak at about 6.26±0.2 degrees.
Crystalline particles of erlotinib hydrochloride having mean particle size (D90) ranging from about 4 μm to 15 μm and 90 volume-% of the particles (D90) ranging from about 14 μm to 30 μm.
A pharmaceutical composition comprising 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, and one or more pharmaceutically inert excipients.
A pharmaceutical composition comprising erlotinib hydrochloride crystalline polymorph form A characterized by peaks in the powder X-ray diffraction pattern having 29 angle positions at about 5.75, 9.88, 11.40, 18.97, 22.84, 23.65, 24.29, 24.75, 25.56 and 29.37±0.2 degrees and by the absence of a peak at about 6.26±0.2 degrees, and one or more pharmaceutically inert excipients.
Dependencies are inferred from the claim text.