烟酰胺乳膏剂的制备处方研究

Study on ointment formulation design of nicotinamide

烟酰胺是一种吡啶衍生物,经皮给药后可发挥抑制黑色素转移、抗自由基氧化,抗炎和增强皮肤屏障等多种作用。但其酰胺结构易被氧化产生烟酸,造成皮肤刺激性,引发皮肤不良反应。本研究通过水相乳化法将烟酰胺制备成油包水(W/O)型乳膏剂,增加烟酰胺的稳定性及用药便捷性,并以外观均一性、涂布延展性、离心稳定性以及耐寒耐热性的综合评分作为考察指标,对油相/水相比例、乳化剂以及辅助乳化剂的用量进行单因素影响试验及正交设计,筛选得到制备烟酰胺乳膏剂的最佳处方。优选处方下,油相/水相的质量比例为6∶4,乳化剂Span-60与辅助乳化剂Tween-80的质量分数分别为1%及0.5%。根据优选处方制备得到的烟酰胺乳膏剂稳定性良好,常温(25℃)下可稳定保存3个月。该研究为其后期进一步应用奠定了物质基础。

Nicotinamide is a kind of pyridine derivative,which has various pharmacological effects such as inhibition of melanic transmission,anti-free radical,anti-aging,anti-inflammatory and enhancement of skin barrier after transdermal administration.However,due to its structure of amide,nicotinamide could be oxidized to nicotinic acid,which could cause dermal irritation and side effects.Thus,water-in-oil(W/O)ointment was prepared to enhance stability and compliance of nicotinamide.In this investigation,comprehensive scoring of homogeneity,extensibility,centrifugal stability and cold/heat resistance was set as the evaluation indicator to obtain the optimal proportion of oil phase,emulsifier and coemulsifier through single-factor experiment and orthogonal screening.under the optimal formulation.Span-60 and Tween-80 were used as emulsifier and coemulsifier respectively with the mass percentage of 1%,and the weight ratio of oil to water was 6∶4.Under the selected formulation,storage stability of ointment remained in 3 months under 25℃,which provides the basis for practical application.