艾拉莫德醇质体凝胶的制备及其经皮渗透特性研究

金银秀, 陶雪芬, 王玉新, 张明涛, 王金朝, 周逸轩, 杨芳芳, 罗俊杰

中国药学杂志 ›› 2020, Vol. 55 ›› Issue (21) : 1807-1811.

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中国药学杂志 ›› 2020, Vol. 55 ›› Issue (21) : 1807-1811. DOI: 10.11669/cpj.2020.21.010
论著

艾拉莫德醇质体凝胶的制备及其经皮渗透特性研究

  • 金银秀1, 陶雪芬1, 王玉新1, 张明涛1, 王金朝2, 周逸轩1, 杨芳芳1, 罗俊杰1
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Preparation and Transdermal Permeation of Iguratimod Ethosomal Gel in Vitro

  • JIN Yin-xiu1, TAO Xue-fen1, WANG Yu-xin1, ZHANG Ming-tao1, WANG Jin-zhao2, ZHOU Yi-xuan1, YANG Fang-fang1, LUO Jun-jie1
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摘要

目的 研究艾拉莫德醇质体最佳制备工艺,并考察其制剂性能和体外经皮渗透特性。方法 采用注入法制备艾拉莫德醇质体,利用正交设计优化处方,并对其形态、粒径和包封率等理化性质进行表征,以卡波姆为基质制备醇质体凝胶。采用透皮扩散试验仪,小鼠离体皮肤进行体外经皮渗透试验,并计算药物经皮渗透量。结果 按优选处方制备的艾拉莫德醇质体外观为淡蓝色,平均粒径为(97.60±5.9)nm,包封率为(95.39±1.06)%。艾拉莫德醇质体凝胶剂24 h的累积经皮渗透量为51.15 μg·cm-2,是普通凝胶剂的3.43倍。结论 所得的艾拉莫德醇质体粒径大小适宜,包封率高,醇质体凝胶制备工艺简单,质量可控,能促进艾拉莫德的经皮渗透。

Abstract

OBJECTIVE To optimize the preparation technology of iguratimod ethosomal and evaluate its preparations performance and characteristics of the in vitro transdermal penetration. METHODS The iguratimod ethosomes were prepared with injection method. The formulation and the preparation method of ethosomes were optimized by orthogonal experiment. Their physicochemical properties including particle size, morphology and encapsulation efficiency were characterized,and the carbomer was added as the base for the preparation of the ethosomal gel. The penetration of iguratimod ethosomal gel through mouse skin were performed by Franz′s cell. The cumulative penetration amount was calculated. RESULTS The color of iguratimod ethosome prepared under optimum conditions was light blue, the sizes were (97.60±5.9) nm. The entrapment efficiency of iguratimod in ethosomes was (95.39±1.06)%. Accumulative permeation amount of iguratimod ethosomal gel within 24 h was 51.15 μg·cm-2, which was about 3.43 times of normal gel. CONCLUSION The iguratimod ethosomes have a suitable size, a high entrapment efficiency and the gel is feasible in preparation technique, controllable in quality and can improve transdermal penetration of iguratimod.

关键词

艾拉莫德 / 醇质体 / 凝胶剂 / 经皮渗透

Key words

iguratimod / ethosomal / gel / transdermal permeation

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导出引用
金银秀, 陶雪芬, 王玉新, 张明涛, 王金朝, 周逸轩, 杨芳芳, 罗俊杰. 艾拉莫德醇质体凝胶的制备及其经皮渗透特性研究[J]. 中国药学杂志, 2020, 55(21): 1807-1811 https://doi.org/10.11669/cpj.2020.21.010
JIN Yin-xiu, TAO Xue-fen, WANG Yu-xin, ZHANG Ming-tao, WANG Jin-zhao, ZHOU Yi-xuan, YANG Fang-fang, LUO Jun-jie. Preparation and Transdermal Permeation of Iguratimod Ethosomal Gel in Vitro[J]. Chinese Pharmaceutical Journal, 2020, 55(21): 1807-1811 https://doi.org/10.11669/cpj.2020.21.010
中图分类号: R944   

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基金

浙江省大学生科技创新活动计划暨新苗人才计划资助(2018R477007);台州职业技术学院2018年度重点课题资助(2018ZD03)
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