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目的通过羟丙基-β-环糊精包合胆酸,对包合物进行物相鉴别,提高胆酸的鼻黏膜渗透性。方法采用相溶解度法、扫描电子显微镜法(SEM)、傅立叶变换红外光谱法(FT-IR)、差示扫描量热法(DSC)、核磁共振波谱法(NMR)对包合物进行物相鉴别;采用体外鼻黏膜渗透试验评价羟丙基-β-环糊精对胆酸鼻黏膜渗透性影响。结果物相鉴别证明包合物形成,相溶解度曲线为AL型,包合常数K=564.30 L/mol;采用羊鼻黏膜进行渗透试验,胆酸-羟丙基-β-环糊精包合物的渗透系数和稳态流量分别为胆酸的1.46、144倍。结论采用羟丙基-β-环糊精包合胆酸,形成了胆酸-羟丙基-β-环糊精包合物,并能提高胆酸鼻黏膜渗透性。
Objective Inclusion of cholic acid by hydroxypropyl-β-cyclodextrin, inclusion complex phase identification, improve the permeability of bile acids nasal mucosa. Methods The phases of inclusions were identified by phase-solubility method, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and nuclear magnetic resonance spectroscopy ; In vitro nasal mucosal permeability test evaluation of hydroxypropyl-β-cyclodextrin on the permeability of bile acid nasal mucosa. Results The phase identification proved that the inclusion complex was formed, the phase solubility curve was AL type, and the inclusion constant was K = 564.30 L / mol. The sheep’s nasal mucosa was used for osmotic test. The inclusion complex of cholic acid-hydroxypropyl-β-cyclodextrin The permeability coefficient and steady-state flowrate were 1.46 and 144 times that of cholic acid respectively. Conclusion Hydroxypropyl-β-cyclodextrin inclusion of bile acid, the formation of bile acid - hydroxypropyl-β-cyclodextrin inclusion complex, and can improve the permeability of bile acid nasal mucosa.