The physicochemical characteristics of freeze-dried scutellarin-cyclodextrin tetracomponent complexes.
In an effort to improve the solubility of the insoluble drug scutellarin, a novel complexation of scutellarin with beta-cyclodextrin (beta-CD) was studied. Tetracomponent freeze-dried complex was prepared with scutellarin, beta-CD, Hydroxypropyl Methylcellulose (HPMC), and triethanolamine. To confirm complex formation, complex was characterized by Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction, and differential scanning calorimetry (DSC). Phase-solubility analysis suggested the soluble complexes having 1:1 stoichiometry. The beta-CD solubilization of scutellarin could be improved significantly by combining water-soluble polymer and pH adjuster. Comparing the binary, ternary solid systems with tetrary systems, tetracomponent freeze-dried complex showed the best effect of solubilization. A maximal solubility of scutellarin (23.65 mg/ml) was achieved with tetracomponent freeze-dried complex, up to 148-fold increase over scutellarin solubility in water, and the solubility of scutellarin is 15.35 microg/ml (up to 6-fold) in simulated gastric fluid.
Cao
Feng
F
Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. China.
Guo
Jianxin
J
Ping
Qineng
Q
D047310:Apigenin / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D004983:Ethanolamines / Q000737:chemistry*; D005612:Freeze Drying; D005750:Gastric Juice / Q000737:chemistry; D005965:Glucuronates / Q000737:chemistry*; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry; D033362:Powder Diffraction; D011759:Pyrrolidines / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000737:chemistry*
D004983:Ethanolamines; D005965:Glucuronates; D011145:Polyvinyls; D011759:Pyrrolidines; D047392:beta-Cyclodextrins; C505150:poly(N-vinylpyrrolidine); D014867:Water; C484876:scutellarin; D065347:Hypromellose Derivatives; D047310:Apigenin; D008747:Methylcellulose; C009546:triethanolamine; C020283:diethanolamine; C031215:betadex