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Polymorph 1 of bilastine, process for preparing thereof, its antihistaminic and antiallergic use and pharmaceutical preparation containing it
专利权人:
FAES FARMA; S.A.
发明人:
ORJALES VENERO AURELIO,BORDELL MARTIN MARAVILLAS,CANAL MORI GONZALO,BLANCO FUENTE HAYDEE,LUCERO DE PABLO MARIA LUISA,RUBIO ROYO VICTOR,MOSQUERA PESTANA RAMON,LUCERO DE PABLO MARIA
申请号:
SK50202004
公开号:
SK288052B6
申请日:
2002.04.19
申请国别(地区):
SK
年份:
2013
代理人:
摘要:
Polymorph 1 of bilastine of the formula (I), which the X-ray crystallographic analysis has the following crystal parameters: crystallographic system: monoclinic; spatial group: P2(1)/c; crystal size: 0.56 x 0.45 x 0.24 mm; cell dimension: a = 2.338 (5) alpha = 90ø, b = 0.8829 (17) nm beta = 90ø, c = 1.259 (2) nm gamma = 90ø; volume 2.6 nm3; Z, calculated density 4, 1.1.84 mg m-3. A process for preparing the polymorph that consists in heating the raw bilastine or polymorphs 2 and 3 of bilastine or a mixture thereof in a solvent selected from short chained alcohols, preferably isopropylic alcohol and n-butanol, acetone and mixtures thereof. The polymorph 1 of bilastine is suitable for antihistaminic and antiallergic use. A pharmaceutical preparation containing this polymorph.Polymorph 1 of bilastine of the formula (I), which the X-ray crystallographic analysis has the following crystal parameters: crystallographic system: monoclinic; spatial group: P2(1)/c; crystal size: 0.56 x 0.45 x 0.24 mm; cell dimension: a = 2.338 (5) alpha = 90ř, b = 0.8829 (17) nm beta = 90ř, c = 1.259 (2) nm gamma = 90ř; volume 2.6 nm3; Z, calculated density 4, 1.1.84 mg m-3. A process for preparing the polymorph that consists in heating the raw bilastine or polymorphs 2 and 3 of bilastine or a mixture thereof in a solvent selected from short chained alcohols, preferably isopropylic alcohol and n-butanol, acetone and mixtures thereof. The polymorph 1 of bilastine is suitable for antihistaminic and antiallergic use. A pharmaceutical preparation containing this polymorph.
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