51. Preparation, physicochemical characterization and in vitro dissolution studies of azithromycin-cyclodextrin inclusion complexes
- Author
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Li-sheng Wang, Mei-rong Zhao, Ya-jing Wang, Hua-wen Liu, and Hua Yang
- Subjects
chemistry.chemical_classification ,Aqueous solution ,Chromatography ,Cyclodextrin ,Scanning electron microscope ,02 engineering and technology ,General Chemistry ,Polymer ,021001 nanoscience & nanotechnology ,Condensed Matter Physics ,030226 pharmacology & pharmacy ,03 medical and health sciences ,0302 clinical medicine ,chemistry ,Solubility ,Fourier transform infrared spectroscopy ,0210 nano-technology ,Spectroscopy ,Dissolution ,Food Science ,Nuclear chemistry - Abstract
To improve the water solubility of hydroxypropyl-β-cyclodextrin(HP-β-CD, 500–800 mg/mL), a novel hydroxypropyl-β-cyclodextrin polymer (HP-β-CDP) was firstly synthesized and characterized by Fourier Transform Infrared spectroscopy (FT-IR), Nuclear magnetic resonance (1H-NMR), and X-ray diffraction spectroscopy (XRD) comprehensively. The solubility of HP-β-CDP was determined as 40.2 g/mL, which is about 46.6 times more than HP-β-CD. The inclusion complexes were prepared with HP-β-CD and HP-β-CDP by saturated solution method to improve the solubility and in vitro release behavior of insoluble drug AZM. The formulation was optimized by orthogonal design with three factors and three levels L9 (34). Solubility, FT-IR, XRD and scanning electron microscope investigations demonstrated that both HP-β-CD and HP-β-CDP effectively formed the inclusion complex. The resultant HP-β-CDP complex presented an increased AZM solubility (628.5 ± 0.25 μg/mL) than HP-β-CD (311.3 ± 0.26 μg/mL) compared with AZM (34.2 ± 0.30 μg/mL) in water. The in vitro accumulative release studies revealed that more than 90 % of AZM could be released from HP-β-CDP inclusion complex within 1 h, which is far more than free AZM (27.5 %) and HP-β-CD inclusion complex (46.5 %). The studies indicated that HP-β-CDP with better water solubility could improve remarkably the solubility and release properties of AZM than HP-β-CD.
- Published
- 2016