特比萘芬乳凝胶的制备及质量评价

目的:制备特比萘芬乳凝胶并对其质量进行评价。方法:以溶解度为指标筛选乳化剂和油相,以不同微乳体系的三元相图筛选油相、乳化剂和助乳化剂的用量,采用直接溶胀法制备乳凝胶,并对其含量、体外经皮渗透性、皮肤刺激性、稳定性进行考察。结果:乳凝胶的最优处方(100 g)为丙二醇辛酸酯14.0 g、聚氧乙烯-35-蓖麻油40.0 g、丙二醇2.0 g。制备的特比萘芬乳凝胶含量合格,12 h的体外累积渗透量为(1 283.7±33.5)μg/cm2,皮肤刺激反应评分24 h为0.1、48 h为0(无刺激),稳定性各项指标无明显变化。结论:该制剂制备处方合理,质量可控。

Preparation and Quality Evaluation of Terbinafine Microemulsion-based Gel

OBJECTIVE： To prepare Terbinafine microemulsion-based gel, and to evaluate the quality of it. METHODS： The emulsifier and oil phase were selected with solubility as index. Ternary phase diagrams of different microemulsion system was used to select the amount of oil, emulsifier and co-emulsifier. Direct swelling method was used to prepare microemulsion-based gel; the content, in vitro percutaneous permeation, skin irritation and stability were all investigated. RESULTS： The optimized formulation （100 g） included propylene glycol dicaprylate 14.0 g, polyoxyethylene-35-castor oil 40.0 g and propylene glycol 2.0 g. The pre- pared Terbinafine microemulsion-based gel was qualified in quality; 12 h accumulative permeation was （1283.7±33.5）μg/cm2 in vitro; 24 h skin irritation score was 0.1 and 48 h skin irritation score was 0 （no irritation） ; no obvious change was found in stabili- ty. CONCLUSIONS： The preparation formulation is reasonable and it is controllable in quality.