盐酸特比萘芬二元醇质体的制备及体外评价  

Preparation and evaluation in vitro of terbinafine hydrochloride binary ethosomes

作　　者：何一鸣[1] 何卓儒 朱秀城 胡雪艳[1] 孙英英[1] 邓红[1] 张蜀[1] 

机构地区：[1]广东药学院药物研究所/广东省药物新剂型重点实验室,广东广州510006

出　　处：《广东药学院学报》2015年第2期139-144,共6页Academic Journal of Guangdong College of Pharmacy

摘　　要：目的制备盐酸特比萘芬二元醇质体并进行体外评价。方法采用乙醇注入-超声法制备二元醇质体;以粒径、Zeta电位和包封率为评价指标,通过正交试验优化处方;采用改良Franz扩散池对不同脂质体进行体外皮肤渗透试验。结果最优处方为:药物质量分数为0.5‰,药脂比为1∶5(g∶g),二元醇相体积分数为30%,乙醇-丙二醇体积比为7∶3;以优选的处方制备的二元醇质体粒径为(36.2±1.0)nm、Zeta电位为(-23.22±2.02)m V、包封率为(97.61±0.09)%,表皮真皮层滞留量最高为(23.18±2.38)μg/cm2。结论所选工艺合理可行,可用于制备盐酸特比萘芬二元醇质体,二元醇质体增加盐酸特比萘芬在表皮真皮层滞留量。Objective To prepare and evaluate in vitro terbinafine hydrochloride binary ethosomes. Methods Terbinafine hydrochloride binary ethosomes were prepared by ethanol injection method. The formation was optimized by orthogonal design with particle size,Zeta potential and entrapment efficiency as indexes. The percutaneous permeation of different kinds of terbinafine hydrochloride liposomes were determined by Franz diffusion cells. Results Optimal formation was as follows：the mass fraction of drug was 0.5%e; the ratio of drug to lecithin was 1：5 （g：g） ;the volume fraction of diol phase was 30% （ethanol：propylene glycol= 7 ：3）. The mean particle size, Zeta potential, and encapsulation efficiency were （ 36.2± 1.0） nm, （ - 23.22 ±2.02 ） mV, and （ 97.61 ± 0.09 ） %, respectively. The maximum in vitro epidermal-dermal retention amount at 24 h was （23. 18±2.38） p^g/em：. Conclusion The optimized formulation was reasonable,and it could be used for the preparation of terbinafine hydrochloride binary ethosomes, which significantly improved the epidermal-dermal retention.

关 键 词：盐酸特比萘芬 二元醇质体 皮肤滞留 

分 类 号：R943[医药卫生—药剂学]