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New hydrate, anhydrous and solvate crystal forms of zolpidem hemitartrate, useful for treating insomnia in patients
New hydrate, anhydrous and solvate crystal forms of zolpidem hemitartrate, useful for treating insomnia in patients
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机译:半酒石酸唑吡坦的新型水合物,无水和溶剂化物晶体形式,可用于治疗患者的失眠
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摘要
New hydrate, anhydrous and solvate crystal forms of zolpidem hemitartrate are disclosed. The following compounds are claimed: a zolpidem hemitartrate hydrate; a zolpidem hemitartrate monohydrate; a zolpidem hemitartrate dihydrate; a zolpidem hemitartrate trihydrate; a zolpidem hemitartrate tetrahydrate; a zolpidem hemitartrate solvate; a zolpidem hemitartrate anhydrous; an anhydrous zolpidem hemitartrate Form C; a zolpidem hemitartrate Form C, characterized by an X-ray powder diffraction pattern having peaks at about 7.3, 9.5, 17.8, and 23.8 +-0.2 degrees 2-theta; a zolpidem hemitartrate with not more than 1% water content; a zolpidem hemitartrate Form D monohydrate; a zolpidem hemitartrate Form D, characterized by a water content of 2.3-2.7wt.%; a zolpidem hemitartrate Form D hemiethanolate; a zolpidem hemitartrate Form D, characterized by an X-ray powder diffraction pattern having peaks at about 7.1, 9.5, 14.1, 19.6 and 24.5 +-0.2 degrees 2-theta; a zolpidem hemitartrate Form E dihydrate; a zolpidem hemitartrate Form E trihydrate; a zolpidem hemitartrate Form E tetrahydrate; a zolpidem hemitartrate Form E, characterized by a water content of 5.0-8.5wt.%; a zolpidem hemitartrate Form E, characterized by an X-ray powder diffraction pattern having peaks at about 5.2, 7.9, 10.4, 17.2, 18.0 and 18.8 +-0.2 degrees 2-theta; a zolpidem hemitartrate Form F methanolate; a zolpidem hemitartrate Form F, characterized by a methanol content of about 5.5wt.%; a zolpidem hemitartrate Form F, characterized by an X-ray powder diffraction pattern having peaks at about 7.6 and 18.0 +-0.2 degrees 2-theta; a zolpidem hemitartrate Form G solvate; a zolpidem hemitartrate Form G, characterized by an X-ray powder diffraction pattern having peaks at about 6.8 +-0.2 degrees 2-theta; a zolpidem hemitartrate Form H, characterized by an X-ray powder diffraction pattern having peaks at about 7.7, 17.4, 18.0 and 24.3 +-0.2 degrees 2-theta; a zolpidem hemitartrate Form L dihydrate; a zolpidem hemitartrate Form L, characterized by a water content of about 4.3wt.%; a zolpidem hemitartrate Form L, characterized by an X-ray powder diffraction pattern having peaks at about 6.8, 9.7, 17.3, 19.6, and 21.1 +-0.2 degrees 2-theta. Independent claims are also included for: (1) a method for synthesizing zolpidem hemitartrate, comprising: (a) forming a zolpidic acid halide from zolpidic acid; (b) reacting zolpidem acid halide with dimethyl amine, to form zolpidem base; (c) forming zolpidem hemitartrate salt from the zolpidem base; (2) a process for preparing zolpidem hemitartrate Form C comprising: (a) exposing zolpidem hemitartrate Form A to vapors of isopropyl alcohol; or (b) heating zolpidem hemitartrate to 70-150[deg]C to convert zolpidem hemitartrate to Form C; (3) a process for preparing zolpidem hemitartrate Form D comprising: (a) exposing zolpidem hemitartrate Form A to water vapor at a relative humidity from 60-100%; (b) exposing Form C to water vapor at a relative humidity of about 100%; (c) exposing zolpidem hemitartrate Form A or Form C to vapors of ethanol; (d) forming a slurry of zolpidem hemitartrate Form A in ethyl acetate, acetone, or isopropanol; (4) a process for preparing zolpidem hemitartrate Form C comprising forming a slurry of zolpidem hemitartrate Form A in isopropanol; (5) a process for preparing zolpidem hemitartrate Form D comprising granulating zolpidem hemitartrate Form A in butanol; (6) a process for preparing zolpidem hemitartrate Form E comprising: (a) exposing a solid form of zolpidem hemitartrate to water vapor at a relative humidity of about 100%; (b) forming a slurry of a solid form of zolpidem hemitartrate in water; or (c) granulating a solid form of zolpidem hemitartrate in water; (7) a process for preparing zolpidem hemitartrate Form F comprising exposing a solid form of zolpidem hemitartrate to vapors of methanol; (8) a process for preparing zolpidem hemitartrate Form G comprising: (a) exposing zolpidem hemitartrate Form A to vapors of ethyl acetate; (b) forming a slurry of zolpidem hemitartrate Form C in ethanol or methanol; or (c) granulating zolpidem hemitartrate Form C in ethanol or methanol; (9) a process for preparing zolpidem hemitartrate Form H comprising: (a) slurrying zolpidem hemitartrate Form A in ethanol or methanol; or (b) granulating zolpidem hemitartrate Form A in ethanol or methanol; (10) a process for preparing zolpidem hemitartrate Form L comprising: (a) dissolving zolpidem hemitartrate in a solvent mixture of methanol and water; (b) precipitating zolpidem hemitartrate from the solvent mixture; and (c) isolating zolpidem hemitartrate; (11) zolpidem hemitartrate having particles up to about 200 or 50 microns in size; (12) micronized zolpidem hemitartrate Form A having particles up to about 200 microns in size as measured by laser diffraction and an x-ray diffraction pattern having a peak at about 8.6+-0.2 degrees 2-theta. ACTIVITY : Somnogenic; hypnotic. MECHANISM OF ACTION : None given in the source material.
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