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A_L 型,包合常数K =564.30L/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、1.44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 To improve the permeation of nasal mucosa by preparing the cholic acid-hydroxypropyl-β-cyclodextrin(HP-β-CD) and characterize the inclusion complex.Methods The inclusion complex was characterized by using phase solubility,scanning electron microscope(SEM),Fourier transform-infrared(FT-IR),differential scanning calorimetry(DSC),and superconducting NMR;In an effort to investigate the effect of HPβ-CD on cholic acid,the studies of in vitro permeation of nasal mucosa was performed.Results Phase solubility curve was A_L type,K =564.30L/mol,and the characterization de-monstrates the formation of inclusion complex;The permeability coefficients and steady state fluxes through ovine and porcine nasal mucosa were enhanced by the formation of inclusion complex with HP-β-CD about 1.46 and 1.44 times of the uncomplexed cholic acid,respectively.Conclusion The inclusion complex is formed and it could increase the permeability of nasal mucosa by preparing the cholic acid-HP-β-CD.