申请人:——
公开号:US20040176328A1
公开(公告)日:2004-09-09
A solid phannaceutical composition comprising a water-soluble bioactive material and an encapsulating material which is present in the composition in the form of continuous solid phase, and in which solid particles of the bioactive material are dispersed and encapsulated in the continuous solid phase of the encapsulating material, wherein each of the bioactive material and the encapsulating material is normally a solid at room temperature and the melting point of the encapsulating material is lower than the melting point of the bioactive material, the bioactive material being preferably a bisphosphonate, most preferably alendronate, and the encapsulating material includes an enhancer, preferably a mono- or di-glyceride, or an encapsulating surfactant, preferably, a polyoxyethylene/polyoxypropylene block copolymer having surface active properties, and a process for preparing the composition in which solid particles of the bioactive material are mixed with and dispersed in the encapsulating material which is in molten (liquid) form; and cooling the molten form of the encapsulating material to form a solid pharmaceutical composition having the solid particles of the bioactive material dispersed and encapsulated in a continuous solid phase of the encapsulating material.
一种固体药物组合物,包括水溶性生物活性材料和封装材料,封装材料以连续固相的形式存在于组合物中,其中生物活性材料的固体颗粒分散并封装在封装材料的连续固相中,其中生物活性材料和封装材料在室温下通常都是固体,封装材料的熔点低于生物活性材料的熔点、生物活性材料最好是双膦酸盐,最好是阿仑膦酸盐,包封材料包括增强剂,最好是单甘油酯或双甘油酯,或包封表面活性剂,最好是具有表面活性的聚氧乙烯/聚氧丙烯嵌段共聚物,以及制备该组合物的工艺,其中生物活性材料的固体颗粒与处于熔融(液体)状态的包封材料混合并分散在包封材料中;冷却封装材料的熔融状态,形成固体药物组合物,其中生物活性材料的固体颗粒分散并封装在封装材料的连续固相中。