蛇床子素β-环糊精包合物分散片研制-药剂学专业论文.docxVIP

Study on the Osthol-β-CD inclusion compound dispersible tabletAbstractObjective: In this paper, the osthol-β-cyclodextrin(Ost-β-CD) inclusion complex was prepared for improving its solubility. The Ost-β-CD inclusion complex as raw material was mixed with appropriate excipients to make dispersible tablet by optimizing the formulation.The formulation composition, preparation technology, absorption mechanism as well as pharmacokinetics were investigated in order to obtain a safe and effective formulation of osthol.Methods: (1)The Ost-β-CD inclusion complex was manufactured by saturated water solution method．The content，the solubility and the dissolution of osthol weredetermined by UV. Inclusion complex was characterized by the means of FT-IR spectroscopy, thermogravimetric analysis and X-ray diffraction (XRD).Taking the content of osthol as the inspection index, the Ost-β-CD inclusion complex was examined under intense light and high temperature and humidity.(2) The orthogonaldesign was applied to obtain the optimal formulation with the hardness ，weight,disintegration time and dissolution of tablets as indicators.At the same time, the quality standard and stability of best prescription were investigated. (3) The Caco-2 cell monolayer model was cultivated to investigate the uptake and the transport mechanisms of the osthol, Ost-β-CD inclusion complex and inclusion complex dispersible tablet across the membranes. The relative factors for enchancing the absoption of drug carriers, including time, temperature, drug concentration, accelerators and inhibitors were also investigated. The differences between the osthol and its preparations in transport of membranes were explored.(4) In situ circulation method was used to determine the absorption characteristic at different segments, and with different concentrations. (5)The blood concentration of osthol in rat was assayed by HPLC．Pharmacokineticsparameters were calculated by 3P97 program.Results:（1）The formation of t