DM-β-CD对盐酸二氢埃托啡离体鼻黏膜渗透的影响

Transnasal absorption of dihydroetorphine hydrochloride by DM-β-CD

目的:考察不同条件下二甲基-β-环糊精(DM--βCD)对盐酸二氢埃托啡促渗作用的影响。方法:采用透皮实验用扩散池装置用于透黏膜实验,HPLC法测定黏膜渗透药量,分别考察DM-β-CD的质量浓度和加入方式对渗透的影响。结果:DM-β-CD的质量浓度与黏膜渗透率不呈线性关系,DM-β-CD的加入方式对黏膜渗透速率有较强的影响。结论:促渗剂质量浓度为10 mg.mL-1,以超声包合法制备DM-β-CD和盐酸二氢埃托啡的包合物,可使渗透速率达到最大。

Objective：To assess the effects of dimethyl-β-cyclodextrin （DM-β-CD） on the transnasal penetration of dihydroetorphine hydrochloride （DHE）. Methods： A transport of dihydroetorphine through nasal mucosa was mimicked using diffusion cells in vitro. The concentration of DHE was measured by HPLC. Relationship of concentration and adding procedure of DM-β-CD with the nasal penetration of DHE was verified. Results：A non-linearity of DM-β-CD concentration with the cumulative penetration rate of DHE was confirmed. The adding procedure of DM-β-CD significantly impacted the nasal penetration rate of DHE. Conclusion：The maximal nasal penetration rate of DHE was achieved when DM-β-CD was in a concentration of 10 mg·mL^-1 and included with DHE by uhrasonication.