The preparation and characterization of sorafenib solid dispersion
10.3969/j.issn.1006-0111.2016.04.009
- VernacularTitle:索拉非尼固体分散体的制备及性质研究
- Author:
Xingjie SHAN
1
;
Zhankuan YAN
;
Chaofeng YU
;
Chuanjun LI
Author Information
1. 江苏恒瑞医药股份有限公司
- Keywords:
sorafenib;
mesoporous silica;
solid dispersion;
dissolution;
stability;
bioavailability
- From:
Journal of Pharmaceutical Practice
2016;34(4):320-323,342
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare sorafenib (SFN )/mesoporous silica solid dispersion (SD) and investigate characteris-tics in vitro and in vivo .Methods The SD was prepared by solvent evaporation method ;the optimal ratio of SFN to meso-porous silica was determined by examining the dissolution of formula ,the drug state and physical stability of SD were examined by DSC and XRD ;the surface morphology was characterized by electron microscope ;the pharmacokinetics of SD was studied for the solid dispersion which compared with SFN powders in vivo study using rats .Results SFN raw drug was crystalline and its dissolution was <10% ;the dissolution of SD increased with an increase in amount of mesoporous silica ;when the ratio of SFN to mesoporous silica was 1∶5 ,drug in SD was non-crystalline state and the dissolution was >90% .The physical state and dissolution of SFN in SD were hardly changed during the six months accelerated test .The cmax of SD groupwas 1 .8 times that of powder group ,relative bioavailability was 175% .Conclusion The physical stability of self-preparing solid dispersions is good ,the dissolution and oral absorption are improved by solid dispersion .
