title: Preparation and characterization of emulsified solid dispersions containing docetaxel.
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.
authors.affiliation: Department of Pharmacy, Wuhan General Hospital of Guangzhou Command, Wuhan 430070, China. cysci@yahoo.com.cn
authors.forename: Ying
authors.initials: Y
authors.lastname: Chen
authors.forename: Qiongzhi
authors.initials: Q
authors.lastname: Shi
authors.forename: Zhiyu
authors.initials: Z
authors.lastname: Chen
authors.forename: Jianling
authors.initials: J
authors.lastname: Zheng
authors.forename: Hengjun
authors.initials: H
authors.lastname: Xu
authors.forename: Jiazhi
authors.initials: J
authors.lastname: Li
authors.forename: Hong
authors.initials: H
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D000077143:Docetaxel; D004339:Drug Compounding; D004355:Drug Stability; D045703:Emulsifying Agents / Q000737:chemistry*; D004655:Emulsions; D005079:Excipients / Q000737:chemistry*; D006358:Hot Temperature; D057927:Hydrophobic and Hydrophilic Interactions; D065347:Hypromellose Derivatives; D007700:Kinetics; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D033362:Powder Diffraction; D012995:Solubility; D043823:Taxoids / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D045703:Emulsifying Agents; D004655:Emulsions; D005079:Excipients; D043823:Taxoids; D000077143:Docetaxel; D065347:Hypromellose Derivatives; D008747:Methylcellulose