Effect of PEG400 Concentration in Receiving Solution on Drug Transdermal Test in Vitro

Zi-xuan DU; Yi-bo WANG; Li-li GAO; Xing-bin YIN; Chang-hai QU; Xin FENG; Jian NI

doi:10.13422/j.cnki.syfjx.20181803

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Effect of PEG400 Concentration in Receiving Solution on Drug Transdermal Test in Vitro

Pharmacy and Processing | 更新时间：2021-02-09

- Effect of PEG400 Concentration in Receiving Solution on Drug Transdermal Test in Vitro
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 25, Issue 1, Pages: 196-200(2019)
- 作者机构：
  
  1.北京中医药大学　中药学院，北京　 100102
  2.首都医科大学附属北京妇产医院，北京　 100026
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.20181803
  CLC： R22;R283.6;R284;R94;R285;P575.2
- Received：01 May 2018，
  
  Published Online：29 June 2018，
  
  Published：05 January 2019
- 稿件说明：
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Zi-xuan DU, Yi-bo WANG, Li-li GAO, et al. Effect of PEG400 Concentration in Receiving Solution on Drug Transdermal Test in Vitro[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(1): 196-200.
DOI：

Zi-xuan DU, Yi-bo WANG, Li-li GAO, et al. Effect of PEG400 Concentration in Receiving Solution on Drug Transdermal Test in Vitro[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(1): 196-200. DOI： 10.13422/j.cnki.syfjx.20181803.

摘要

目的：

考察接受液中不同体积分数聚乙二醇（PEG）400对药物体外透皮试验的影响。

方法：

选择5-氟尿嘧啶为模型药物，通过配制不同体积分数的PEG400磷酸盐缓冲液（PBS）作为接受液，接收室不加药，大鼠皮肤按正常操作条件处理12 h，后续用PBS置换出含PEG400的接受液，加药测定药物透皮吸收情况并计算相关透皮参数；采用扫描电镜观察离体大鼠皮肤在经含PEG400的接受液处理12 h后皮肤角质层形态变化。

结果：

体积分数为10%，15%和40%的PEG400-PBS组未影响相关药物透皮参数，体积分数为20%和30%的PEG400-PBS组的药物稳态透皮速率和累积透过量均明显高于PBS组（

0.01，

0.05）；扫描电镜结果显示，当PEG400体积分数

20%时，正常皮肤表面的褶皱逐渐消失，并伴有脱落的鳞片状物，同时30%PEG400-PBS组和40%PEG400-PBS组皮肤极度皱缩。

结论：

大鼠皮肤体外透皮试验中，接受液中PEG400用量应控制在20%以下。

Abstract

Objective:

To investigate the effect of varying concentrations of polyethylene glycol(PEG)400 in receiving solution on

in vitro

transdermal test of drugs.

Method:

5-Fluorouracil(5-FU) was selected as a model drug

by preparing different concentrations of PEG400-phosphate buffer solution(PBS) as the receiving solution

the receiving chamber did not add drug

the excised rat skins were treated with various additives for 12 h

then replaced by PBS and added the saturated model drug into the donor compartment to determine the transdermal parameters of the drug.Meanwhile

scanning electron microscopy(SEM) was employed to monitor the effect of PEG400 with different concentration on the stratum corneum of rat skin.

Result:

The 10%

15% and 40%PEG400-PBS groups had no significant effect on

in vitro

transdermal absorption parameters of the 5-FU.The steady transdermal rate and cumulative penetration rate of the drug in 20% and 30% PEG400-PBS groups were significantly higher than that in the PBS group(

0.01

0.05). SEM indicated that wrinkle of the intact rat skin gradually disappeared and a number of flakes were desquamated from the skin when the concentration of PEG400 was above 20% in receiving solution.Meanwhile

30% PEG400-PBS group and 40% PEG400-PBS group were extremely wrinkled.

Conclusion:

In the rat skin transdermal test

the concentration of PEG400 in receiving solution should be controlled below 20%.

关键词

Keywords

references

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