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固体分散物

固体分散体(英语:solid dispersion)系指难溶性药物分子胶体状态、微晶或无定型状态分散在另一种水溶性材料中,或分散在难溶性、肠溶性材料中呈固体状态。

难溶性药物的生物利用度往往不高,而药物的吸收速率又取决于溶出速率,溶出速度随分散度的提高而提高,固体分散体中的载体多为水溶性,故制成固体分散体后可以明显改善难溶性药物的生物利用度。

载体

载体材料的性质对固体分散体的性质有很大影响,载体材料应该具有无毒、无致癌性、不影响药物稳定性、不与药物发生化学变化、不影响药物的药效与含量监测等基本性质。

常用的固体分散体载体材料可以分为三大类:水溶性载体材料,包括聚乙二醇(PEG)、聚维酮(PVP)、表面活性剂、有机酸、糖与醇等;难溶性载体材料,包括纤维素、聚丙烯酸树脂等;肠溶性载体材料,包括纤维素类和聚丙烯酸树脂类。

制备

固体分散体的制备常用的方法有熔融法、溶剂法、溶剂-熔融法、溶剂喷雾冷冻干燥法、研磨法等。

  • 熔融法系指将药物与载体材料混合熔融后迅速冷却成固体,再将该固体在一定温度下放置使成为易碎物,例如滴丸,该法适合对热稳定的药物和难溶于有机溶剂、熔点低的载体材料如PEG、枸橼酸
  • 溶剂法亦称为共沉淀法,系指将药物和载体共溶于有机溶剂中挥干溶剂,使药物与载体材料同时析出,经干燥即得到药物与载体材料混合成的固体分散体,该法适合于易挥发、热不稳定、易溶于有机溶剂的药物和载体材料。

参见

滴丸剂 生物利用度

外部链接

固体分散体水溶性载体研究新进展 (中医药传播网页面存档备份,存于互联网档案馆))

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固体分散物
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