Preparation and characterization of emulsified solid dispersions containing docetaxel |
| |
Authors: | Ying Chen Qiongzhi Shi Zhiyu Chen Jianling Zheng Hengjun Xu Jiazhi Li Hong Liu |
| |
Institution: | (1) Laboratorium voor Farmacotechnologie en Biofarmacie, K. U. Leuven, Campus Gasthuisberg O+N Herestraat 49, 3000 Leuven, Belgium;(2) Laboratorium voor Analytische Chemie en Medicinale Fysicochemie, K. U. Leuven, Van Evenstraat 4, 3000 Leuven, Belgium |
| |
Abstract: | An emulsified solid dispersion of docetaxel was prepared and characterized in vitro. In contrast to conventional solid dispersions, emulsifying pharmaceutical excipients and hydroxypropyl methylcellulose (HPMC)
as a supersaturation promoter were introduced into the PEG6000-based solid dispersion to further improve its solubilizing
capability. The solubility, dissolution in vitro and stability of the prepared emulsified solid dispersions were studied taking into consideration of the effects of different
emulsifying excipients, preparation methods and the media. Results of the emulsified solid dispersion of docetaxel showed
that the solubility and dissolution at 2 h were 34.2- and 12.7-fold higher than the crude powder. The type of emulsifying
excipient used had a significant influence on the dissolution of the emulsified solid dispersion. The dissolution of the emulsified
solid dispersion prepared by the solvent-melting method or the solvent method was higher than the melting method. There were
no apparent differences among the dissolution media utilized. The status of the drug in the emulsified solid dispersion was
observed in an amorphous or a molecular dispersion state by differential thermal analysis and powder Xray diffraction. In
conclusion, the incorporation of emulsifying pharmaceutical excipients and HPMC with polymers into a solid dispersion could
be a new and useful tool to greatly increase the solubility and dissolution of poorly water-soluble drugs. |
| |
Keywords: | |
本文献已被 PubMed SpringerLink 等数据库收录! |
|