摘要:
The present invention relates to a process for manufacturing a pulverous preparation of a (sub)micron-sized biologically active compound comprising the steps of: (1) dissolving a biologically active compound under elevated pressure in a compressed gas, liquid or supercritical fluid containing a surface modifier; or in compressed dimethylether optionally containing a surface modifier; (2a) rapidly expanding the compressed solution of step (1) thereby precipitating the dissolved compound; or (2b) spraying the compressed solution of step (1) into an antisolvant phase optionally containing a surface modifier under vacuum, atmospheric pressure or elevated pressure; and (3) optionally converting the antisolvant phase of step (2b) into a pulverous preparation using conventional powder processing techniques. With the process according to the present invention formation of aggregations or flocculations of particles dissolved in the supercritical solution is prevented; moreover, the addition of cosolvents is not required, thus increasing the stabilisation of the suspension on an industrial scale.
摘要:
The present invention relates to a process for manufacturing a pulverous preparation of a (sub)micron-sized biologically active compound comprising the steps of: (1) dissolving a biologically active compound under elevated pressure in a compressed gas, liquid or supercritical fluid containing a surface modifier; or in compressed dimethylether optionally containing a surface modifier; (2a) rapidly expanding the compressed solution of step (1) thereby precipitating the dissolved compound; or (2b) spraying the compressed solution of step (1) into an antisolvant phase optionally containing a surface modifier under vacuum, atmospheric pressure or elevated pressure; and (3) optionally converting the antisolvant phase of step (2b) into a pulverous preparation using conventional powder processing techniques. With the process according to the present invention formation of aggregations or flocculations of particles dissolved in the supercritical solution is prevented; moreover, the addition of cosolvents is not required, thus increasing the stabilisation of the suspension on an industrial scale.
摘要:
The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride and can be used as medicament for the treatment of hyperproliferative disorders.