塞来昔布固体分散体的制备及溶出度研究

Preparation and Dissolution of Celecoxib Solid Dispersions

目的采用溶剂挥干法制备塞来昔布固体分散体来改善其体外溶出度。方法以羟丙甲基纤维素(HPMC),聚乙烯吡咯烷酮K30 (PVPK30),泊洛沙姆188 (F68)为载体,筛选最适合塞来昔布固体分散体的材料。结果 HPMC作为载体时,塞来昔布:HPMC=1∶5时,溶出速率改善最大,在10 min内溶出度达到90%以上,是原料药溶出速率的6倍。结论在HPMC,PVPK30,泊洛沙姆188 (F68) 3种载体中,HPMC改善塞来昔布的溶出度效果较好。适合作为塞来昔布固体分散体的载体。

Objective To prepare the eeleeoxib solid dispersion by solvent evaporation method and to improve its dissolution in vitro. Methods HPMC, PVPK 30 and poloxamer 188 （ F68 ） were used as carriers to screen the most suitable material for celecoxib solid dispersion. Results When HPMC was used as a carrier and celecoxib ： HPMC = 1 ： 5, the dissolution rate improved most, and the dissolution rate reached more than 90% within 10 minutes, which was 5 times higher than the dissolution rate of the drug substance. Conclusion HPMC, PVPK30 and poloxamer 188 （F68） all can improve the dissolution of celecoxib. HPMC was especially suitable as a carrier for a solid dispersion of celecoxib.