载硝酸益康唑和曲安奈德的o/w型凝胶的研制和质量评价

Preparation and Quality Evaluation of o/w Gel Loaded with Econazole Nitrate and Triamcinolone Acetonide

采用正交试验,以外观性状、离心稳定性、黏度、流动性、p H值和药物晶体析出情况为评价指标,筛选含硝酸益康唑(1)和曲安奈德(2)的o/w型凝胶处方。所得优化处方为:1,2-丙二醇用量30%,95%乙醇用量18%,卡波姆用量1.5%,油/水相比例25∶75。3批优化凝胶中1和2的平均含量为(100.1±0.3)%和(99.9±0.5)%,平均黏度(37.8±0.6)Pa·s,p H值为5.3±0.3。以离体猪皮肤为屏障考察自制品与市售乳膏(派瑞松)的体外经皮渗透行为。结果显示,两种制剂中1的渗透行为无显著差异。初步稳定性考察结果表明,样品在30℃、相对湿度65%环境放置6个月,性状、p H值、含量无明显改变。

The formulation of oil-in-water gel loaded with econazole nitrate（1） and triamcinolone acetonide（2） were optimized by orthogonal design with appearance, centrifugal stability, viscosity, flowability, p H value and drug crystal precipitation as indexes. The optimal formulation was as follows： the amounts of 1,2-propylene glycol, 95%ethanol and carbomer were 30%, 18% and 1.5%, and the ratio of oil phase to aqueous phase was 25∶75. The mean contents of 1 and 2, viscosity and p H value of the optimal product were（100.1±0.3）%,（99.9±0.5）%,（37.8±0.6）Pa·s and 5.3±0.3, respectively. The transdermal behaviors of the self-made product and commercial cream（Pevisone） were investigated with excised pig skin as a barrier. The results showed that the transdermal behavior of 1 in the above two preparations had no significant difference. The results of preliminary stability test showed that the appearance, p H value, drug contents of the product stored at 30 ℃ and 65% relative humidity for 6 months had no significant changes.