The Physicochemical Characteristics of Freeze-Dried Scutellarin-Cyclodextrin Tetracomponent Complexes |
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Authors: | Feng Cao Jianxin Guo Qineng Ping |
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Affiliation: | Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. China |
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Abstract: | ABSTRACTIn an effort to improve the solubility of the insoluble drug scutellarin, a novel complexation of scutellarin with β-cyclodextrin (β-CD) was studied. Tetracomponent freeze-dried complex was prepared with scutellarin, β-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 β-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 ug/ml (up to 6-fold) in simulated gastric fluid. |
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Keywords: | KEYWORDS Scutellarin β-cyclodextrin Tetracomponent complexes Fourier transform infrared spectroscopy Powder X-ray diffraction Differential scanning calorimetry Phase solubility Solubility |
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