胆酸-羟丙基-β-环糊精包合物的物相鉴别及体外鼻黏膜渗透评价  

Characterization and in vitro permeation of nasal mucosa evaluation of inclusion complex of cholic acid-hydroxypropyl-β-cyclodextrin

作　　者：苏柘僮[1] 杨明[1] 吴品江[1] 许润春[1] 高亚男[1] 杨争[2] 

机构地区：[1]成都中医药大学,四川成都610075 [2]四川大学,四川成都610064

出　　处：《中草药》2009年第6期878-882,共5页Chinese Traditional and Herbal Drugs

摘　　要：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 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 HP-β-CD on cholic acid, the studies of in vitro permeation of nasal mucosa was performed. Results Phase solubility curve was AL type, K=564.30 L/tool, and the characterization demonstrates 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 eholic acid- HP-β-CD.

关 键 词：胆酸-羟丙基-β-环糊精包合物 物相鉴别 体外鼻黏膜渗透试验 

分 类 号：R286.02[医药卫生—中药学]