【作者】 张勇；

【导师】 潘见；

【作者基本信息】 合肥工业大学 ， 农产品加工与贮藏， 2003， 硕士

【摘要】 天然产物有效成分是制药的重要原料，黄酮类活性成分更是天然药物研究的热点。文献报道的黄酮类化合物晶体的结构、溶解度、光谱特性等物化参数往往存在显著差异，已制约药物开发利用。葛根素就是一例。汇集国内外报道的葛根素物性数据，颇为分散，已影响到葛根素原料药标准的完善。本文运用显微观察、红外、热重、差热、X射线粉末衍射等现代分析手段，确认了葛根素的三种晶体与一种非晶态的存在，其熔点变化范围为182～211℃；8℃下在水中溶解度随晶型的增大而下降，范围在3.29～3.66mg／ml；与用普通溶剂结晶相比，发现采用超临界CO₂结晶所得葛根素的溶剂残留最少、与中国药典中的标准红外光谱最为接近、品质更优。基于氢键结合与介电常数理论分析，实验考察葛根素在不同溶剂系统中溶解度的变化，结果表明：葛根素溶解度和溶剂的介电常数有关，其介电需量DR大致在35左右；通过介电需量选择70％异丙醇作为制剂溶剂，其粘度和溶解度优于现用的50％丙二醇。更多还原

【Abstract】 With the research and development of natural products, their active compounds, especially flavonoids had been the focus of drug raw material R&D. But it was reported that structure, solubility and spectrum of crystal flavonoids were different, which had baffled the application of drug, such as puerarin. Determination data of puerarin in recent years showed in disorder, so it had great effect on drug quality standard.With the help of modern instruments, there were three crystalline forms and one non-crystalline form from magnified pictures, infrared spectrum, DSC, TGA and X-ray powder diffraction; The melting point of puerarin ranged from 182 to 211 ℃; The solubility descended while size of crystal increased, which ranged from 3.29mg/ml to 3.66mg/ml in 8℃; Compared with normal solvents, crystal from super critical fluid extraction had the fewest residue solvents; best quality and shape; and only SCFE crystal IR spectrum was the most similar with the standard IR spectrum in Chinese Pharmacopoeia than other crystals.From the theory of hydrogen bond and dielectric constant, the solubility of puerarin in different solvents and mixed solvents had been explained. Final results showed the solubility of puerarin was related with dielectric requirement which was 35. Because of low viscidity and high solubility, 70% isopropanol and water had been selected as the solvent of puerarin injection rather than 50% 1,2-propandiol and water.更多还原