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Aqueous systems for the preparation of lipid-based pharmaceutical compounds; compositions, procedures and uses thereof
专利权人:
JINA PHARMACEUTICALS INC.
发明人:
ALI, Shoukath,AHMAD, Moghis,AHMAD, Ateeq,SHEIKH, Saifuddin,AHMAD, Imran
申请号:
ES07873522
公开号:
ES2617747T3
申请日:
2007.10.10
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A process without organic solvents for the preparation of a lipid formulation of an active compound, said process comprising: a) preparing a suspension comprising at least one active compound and at least one lipid in a first aqueous medium at a pH between about pH 4 , 0 and pH 8.0, wherein said preparation of said suspension comprises a process consisting of: i) providing: 1) a first aqueous medium consisting of water or water having a buffer dissolved therein, 2) at least one active compound partially soluble in water or insoluble in water, 3) at least one phospholipid and at least one lipid selected from the group consisting of cholesterol or cholesterol sulfate and salts thereof, cholesterol hemisuccinate and salts thereof, cholesterol phosphate and salts thereof; and 4) one or more cryoprotectants; ii) adding to said first aqueous medium at least one active compound and at least one lipid; and iii) mixing said first aqueous medium, said at least one active compound, and said at least one lipid to form a suspension; b) treating said suspension to form a compound-lipid suspension, comprising compound-lipid complexes having a defined particle size; c) lyophilizing said lipid-compound suspension comprising compound-lipid complexes having a defined particle size in the presence of one or more cryoprotectants to form a lyophilized material; and d) reconstituting said lyophilized material with a second aqueous medium to obtain a lipid formulation of an active compound, said lipid formulation comprising a suspension of compound-lipid complexes of defined particle size, said defined particle size having a lower average particle size at 5 micrometersUn procedimiento sin disolventes orgánicos para la preparación de una formulación lipídica de un compuesto activo, comprendiendo dicho procedimiento: a) preparar una suspensión que comprende al menos un compuesto activo y al menos un lípido en un primer medio acuoso a un pH entre aproximadamente pH 4,0 y pH 8,0, en el que dic
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