天津农学院学报 ›› 2020, Vol. 27 ›› Issue (1): 76-81.doi: 10.19640/j.cnki.jtau.2020.01.017

• 研究与简报 • 上一篇    下一篇

烟酰胺乳膏剂的制备处方研究

洪静a, 刘黎瑶a,b,通信作者, 王庆奎b   

  1. 天津农学院 a. 基础科学学院,b. 天津市水产生态及养殖重点实验室,天津300384
  • 收稿日期:2019-04-22 发布日期:2020-04-01
  • 通讯作者: 刘黎瑶(1988-),女,讲师,博士,主要从事药物制剂方面的研究。E-mail: llymeilin@163.com。
  • 作者简介:洪静(1996-),女,本科在读,主要从事药物制剂方面的研究。E-mail:753348752@qq.com。
  • 基金资助:
    天津市教委科研计划项目(2017KJ181); 天津市水产产业技术体系创新团队项目(ITTFRS2017004); 国家自然科学基金面上项目(31170442)

Study on ointment formulation design of nicotinamide

HONG Jinga, LIU Li-yaoa,b,Corresponding Author, WANG Qing-kuib   

  1. Tianjin Agricultural University a. College of Basic Science, b. Tianjin Key Lab of Aquatic Ecology and Aquaculture, Tianjin 300384, China
  • Received:2019-04-22 Published:2020-04-01

摘要: 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。

关键词: 烟酰胺, 乳膏剂, 单因素影响试验, 正交设计, 处方筛选

Abstract: 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.

Key words: nicotinamide, ointment, single-factor experiment, orthogonal screening, formulation optimization

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