Method for preparing a solid dispersion, solid dispersion obtained thereby and use thereof
申请人:King Saud University
公开号:EP2649989A1
公开(公告)日:2013-10-16
The present invention relates to a method for preparing a solid dispersion, comprising the steps:
a.1) melting of a mixture of at least one drug, at least one carrier and at least one acid, at least one carbonate and/or at least one bicarbonate and optinally at least one surfactant under effervescence of CO2;
or
a.2) melting of at least one of the constituents of the mixture according to step a.1) and adding the remaining constituents in arbitrary order under effervescence of CO2 wherein either the at least one acid or the at least one bicarbonate and/or the at least one carbonate has/ have to be added last;
b) solidifying the mixture obtained in step a.1 or a.2), preferably by cooling and optionally drying;
c) comminuting the mixture obtained in step b).
a solid dispersion prepared thereby, a pharmaceutical composition containing the solid dispersion as well as the use of the solid dispersion for enhancing the water solubility of drugs.
本发明涉及一种制备固体分散体的方法,包括以下步骤
a.1) 将至少一种药物、至少一种载体和至少一种酸、至少一种碳酸盐和/或至少一种碳酸氢盐以及可选的至少一种表面活性剂的混合物在二氧化碳的气泡作用下熔化;
或
a.2) 熔化步骤 a.1) 所述混合物中的至少一种成分,然后在二氧化碳气泡作用下按任意顺序加入其余成分,其中至少一种酸或至少一种碳酸氢盐和/或至少一种碳酸盐必须最后加入;
b) 将在步骤 a.1 或 a.2) 中得到的混合物固化,最好是通过冷却,也可选择干燥;
c) 粉碎在步骤 b) 中得到的混合物。
由此制备的固体分散体、含有该固体分散体的药物组合物以及该固体分散体在提高药物水溶性方面的用途。