title: Improving the solubility of ampelopsin by solid dispersions and inclusion complexes.
abstract: The aim of this study was to increase the solubility of ampelopsin (AMP) in water by two systems: solid dispersions with polyethylene glycol 6000 (PEG 6000) or polyvinylpyrrolidone K-30 (PVP K30) and inclusion complexes with beta-cyclodextrin (BCD) and hydroxypropyl-beta-cyclodextrin (HPBCD). The interaction of AMP with the hydrophilic polymers was evaluated by differential scanning calorimetry (DSC), Fourier transformation-infrared spectroscopy (FTIR), scanning electron microscopy (SEM). The results from DSC, FTIR and SEC analyses of solid dispersions and inclusion complexes showed that AMP might exist as an amorphous state or as a solid solution. On the other hand, the SEM images of the physical mixtures revealed that to some extent the drug was present in a crystalline form. The influence of various factors (pH, temperature, type of polymer, ration of the drug to polymer) on the solubility and dissolution rate of the drug were also evaluated. The solubility and dissolution rates of AMP were significantly increased by solid dispersions and cyclodextrin complexes as well as their physical mixtures. The improvement of solubility using polymers was in the following order: HPBCD approximately BCD>PVP K30>PEG 6000.
authors.affiliation: School of Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, PR China.
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Ruan
authors.forename: Bo-Yang
authors.initials: BY
authors.lastname: Yu
authors.forename: Guang-Miao
authors.initials: GM
authors.lastname: Fu
authors.forename: Dan-Ni
authors.initials: DN
authors.lastname: Zhu
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002152:Calorimetry, Differential Scanning / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D005419:Flavonoids / Q000737:chemistry* / Q000302:isolation & purification / Q000493:pharmacokinetics; D006860:Hydrogen Bonding; D006863:Hydrogen-Ion Concentration; D008855:Microscopy, Electron, Scanning / Q000379:methods; D011092:Polyethylene Glycols / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D012996:Solutions / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D014867:Water / Q000737:chemistry; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D005419:Flavonoids; D012996:Solutions; D047392:beta-Cyclodextrins; D014867:Water; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C106407:ampelopsin; D011092:Polyethylene Glycols; D011205:Povidone; C031215:betadex