OBJECTIVE:To prepare icaritin-poloxamer 188 solid dispersions in order to increase the dissolution rate of icaritin. METHODS:With poloxamer 188 as the carrier,melting method was used to prepare solid dispersions. By comparing the in vitro dissolution rates,the effects of the content of poloxamer 188(the ratios of icaritin to poloxamer 188 were 5∶1,3∶1,2∶1,1∶1,1∶3,1∶5,1∶7,1∶9,1∶11,1∶13,1∶15,1∶17,1∶19,1∶27 and 1∶31),melting temperature(60,70 and 80 ℃)and cooling tem-perature(-20,0 and 20 ℃)on the dissolution rate of icaritin in the solid dispersions were investigated,and the in vitro dissolu-tion rates of icaritin in its active pharmaceutical ingredient,physical mixture and solid dispersions were compared to confirm the for-mation of the solid dispersions. RESULTS:The dissolution rate of icaritin in the prepared solid dispersions increased to some extent as the proportion of the carrier increased. When the ratio of icaritin to the carrier was 1∶17-1∶27,the dissolution rate of icaritin at 120 min was above 90%. Where melting temperature and cooling temperature were respectively determined as 60 ℃ and 0 ℃ after comprehensive comparison,the dissolution rate of icaritin in the solid dispersions was 1.5 times as much as that in the physical mix-ture at 30 min. CONCLUSIONS:The prepared solid dispersion has a significantly higher dissolution rate of icaritin.%目的：制备淫羊藿素-泊洛沙姆188固体分散体以提高淫羊藿素的溶出度。方法：以泊洛沙姆188为载体，采用熔融法制备固体分散体。通过体外溶出度比较，考察了载体泊洛沙姆188的用量（淫羊藿素-泊洛沙姆188质量之比为5∶1、3∶1、2∶1、1∶1、1∶3、1∶5、1∶7、1∶9、1∶11、1∶13、1∶15、1∶17、1∶19、1∶27、1∶31）、熔融温度（60、70、80℃）、冷却温度（－20、0、20℃）对固体分散体中淫羊藿溶出度的影响；同时比较了淫羊藿素原料药及其物理混合物、固体分散体的体外溶出度以证实固体分散体的形成。结果：所制固体分散体的淫羊藿素溶出度在一定程度上随载体比例增加而增加，当淫羊藿素与载体之比为1∶17～1∶27时淫羊藿素在120 min时的溶出度均在90％以上；熔融温度、冷却温度经综合分析后分别确定为60、0℃；在溶出30 min时，固体分散体的溶出度是物理混合物的1.5倍。结论：制备的固体分散体显著提高了淫羊藿素的溶出度。
展开▼
