The preparation and characterization of sorafenib solid dispersion

SHAN Xingjie; YAN Zhankuan; YU Chaofeng; LI Chuanjun

doi:10.3969/j.issn.1006-0111.2016.04.009

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Objective To prepare sorafenib (SFN)/mesoporous silica solid dispersion (SD) and investigate characteristics in vitro and in vivo. Methods The SD was prepared by solvent evaporation method; the optimal ratio of SFN to mesoporous 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 c_max of SD group was 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.

The preparation and characterization of sorafenib solid dispersion

Jiang Su Heng Rui Medicine Co., Ltd., Lianyungang 222047, China

Received Date: 2015-09-09

Rev Recd Date: 2016-01-14

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Abstract: Objective To prepare sorafenib (SFN)/mesoporous silica solid dispersion (SD) and investigate characteristics in vitro and in vivo. Methods The SD was prepared by solvent evaporation method; the optimal ratio of SFN to mesoporous 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 c_max of SD group was 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.

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The preparation and characterization of sorafenib solid dispersion

doi: 10.3969/j.issn.1006-0111.2016.04.009

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