基于相同载体体系的中药成分自乳化制剂的制备及其体外透皮吸收特性考察

梁静娴; 吕邵娃; 朱婷; 关显桐; 武元群; 李永吉; 李英鹏

doi:10.13422/j.cnki.syfjx.20190315

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基于相同载体体系的中药成分自乳化制剂的制备及其体外透皮吸收特性考察

药剂与炮制 | 更新时间：2021-02-09

- 基于相同载体体系的中药成分自乳化制剂的制备及其体外透皮吸收特性考察
- Preparation of Self-emulsifying Preparations of Chinese Medicinal Ingredients Based on Identical Carrier System and Investigation of Their Transdermal Absorption Characteristics in Vitro
- 中国实验方剂学杂志 2019年25卷第11期页码：121-126
- 作者机构：
  
  1.黑龙江中医药大学，哈尔滨　 150040；
  2.天津中医药大学，天津　 300193
- 作者简介：
  
  梁静娴，在读硕士，从事中药药剂学研究，E-mail：642317280@qq.com
  李永吉，博士，教授，从事中药传统剂型、新型给药系统研究，E-mail：liyongji2009@163.com；
  李英鹏，博士，讲师，从事中药药剂学研究，E-mail：li_ying _ peng@hotmail.com
- 基金信息：
  
  国家自然科学基金青年项目(81703710);天津市自然科学基金项目(17JCYBJC41800);国家自然科学基金面上项目(81671411)
- DOI：10.13422/j.cnki.syfjx.20190315
  中图分类号： R22; R94; R28; C37
- 收稿日期：2018-08-03，
  
  网络出版日期：2018-11-16，
  
  纸质出版日期：2019-06-05
- 稿件说明：
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梁静娴, 吕邵娃, 朱婷, 等. 基于相同载体体系的中药成分自乳化制剂的制备及其体外透皮吸收特性考察[J]. 中国实验方剂学杂志, 2019,25(11):121-126.

Jing-xian LIANG, Shao-wa LYU, Ting ZHU, et al. Preparation of Self-emulsifying Preparations of Chinese Medicinal Ingredients Based on Identical Carrier System and Investigation of Their Transdermal Absorption Characteristics in Vitro[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(11): 121-126.
梁静娴, 吕邵娃, 朱婷, 等. 基于相同载体体系的中药成分自乳化制剂的制备及其体外透皮吸收特性考察[J]. 中国实验方剂学杂志, 2019,25(11):121-126. DOI： 10.13422/j.cnki.syfjx.20190315.

Jing-xian LIANG, Shao-wa LYU, Ting ZHU, et al. Preparation of Self-emulsifying Preparations of Chinese Medicinal Ingredients Based on Identical Carrier System and Investigation of Their Transdermal Absorption Characteristics in Vitro[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(11): 121-126. DOI： 10.13422/j.cnki.syfjx.20190315.

摘要

目的：

制备同时适合于黄芩素、黄连素及大蒜素3种中药成分的自乳化载体体系，并考察这3种自乳化制剂的体外透皮吸收效果。

方法：

采用饱和溶解度法、伪三元相图法、正交试验筛选最佳的空白处方组成及基质用量。以Franz扩散池和离体大鼠皮肤进行体外透皮吸收试验，采用HPLC分别测定3种自乳化制剂中黄芩素、黄连素及大蒜素的累积透皮渗透量，并分别与黄芩素散剂、黄连素散剂及大蒜素散剂进行比较。

结果：

最佳处方为油酸乙酯-聚氧乙烯氢化蓖麻油40-聚乙二醇400载体体系，所形成的自乳化制剂粒径适宜，其微观形态呈较规整的球形。透皮吸收10 h，黄芩素、黄连素及大蒜素3种自乳化制剂的药物透皮速率分别为6.898 6，7.600 4，190.040 μg·cm

－2

·h

－1

，累积透皮渗透量分别为71.38，85.54，1 795.16 μg·cm

－2

。

结论：

成功制备了不同种类中药成分均能使用的自乳化载体体系，且该自乳化制剂的体外透皮吸收效果良好，可为后续中药复方自乳化制剂的制备及其透皮给药吸收研究提供实验依据。

Abstract

Objective:

To prepare self-emulsifying carrier system which was suitable for three Chinese medicinal ingredients(baicalein

berberine and allicin)

and investigate transdermal absorption effect

in vitro

of these three self-emulsifying preparations.

Method:

The optimum formulation and dosage were screened by the saturated solubility method

pseudo-ternary phase diagram method and orthogonal experiment.Transdermal absorption test

in vitro

was carried out with excised rats skin and Franz diffusion cell.The cumulative penetration amounts of baicalein

berberine and allicin in the identical self-emulsifying system were determined by HPLC and compared with baicalein powder

berberine powder and allicin powder

respectively.

Result:

The optimum formulation was ethyl oleate-cremophor RH40-polyethylene glycol(PEG)400.The self-emulsifying preparation had a suitable particle size with a relatively regular spherical shape.At 10 h of transdermal absorption

the transdermal rates of baicalein

berberine and allicin in identical self-emulsifying system were 6.898 6

7.600 4

190.040 μg·cm

-2

·h

-1

the cumulative penetration amounts of them were 71.38

85.54

1 795.16 μg·cm

-2

respectively.

Conclusion:

The self-emulsifying carrier system is prepared successfully

which can be used by different kinds of Chinese medicinal ingredients

and the transdermal absorption effect

in vitro

of these self-emulsifying preparations is good

which can provide experimental basis for the preparation and transdermal absorption of self-emulsifying preparation of Chinese herbal compound.

关键词

Keywords

references

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