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Journal of Chinese Integrative Medicine ›› 2006, Vol. 4 ›› Issue (1): 68-72.doi: 10.3736/jcim20060118

• Original Experimental Research • Previous Articles     Next Articles

Percutaneous absorption of aconitine and mesaconitine in extracts of Radix Aconitum kusnezoffii

Zhi-min Liu, Xin Niu, Xue-zhi Yang, Shu-dong Niu   

  1. Department of Functional Experiment, School of Preclinical Medicine, Beijing University of Traditional Chinese Medicine, Beijing 100029, China
  • Online:2006-01-20 Published:2006-01-15

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Objective

This study was conducted to evaluate the percutaneous absorption of aconitine and mesaconitine in extracts of Radix Aconitum kusnezoffii.

Methods

The extracts of Radix Aconitum kusnezoffii were collected by using Franz diffusion cells after permeation through the skin of rats. Then rate constants of skin permeation of aconitine and mesaconitine were determined by high-performance liquid chromatography (HPLC).

Results

Under the condition that the concentrations of azone and propylene glycol were both 4%, the cumulative doses of skin permeation (Q) of mesaconitine and aconitine in the extracts of Radix Aconitum kusnezoffii (600 mg/ml) for 24 hours were 165.819 and 487.747 μg/cm 2 respectively, and their rate constants of skin permeation were 18.391 and 78.805 μg·cm –2·h –1 respectively. 

Conclusion

The aconitine and mesaconitine in the extracts of Radix Aconitum kusnezoffii can penetrate well through the skin of rats. Propylene glycol and azone can promote this penetration effects. The formula of skin permeation of mesaconitine and aconitine is in accordance with Higuchi equation and there is a linear relationship between Q and t1/2.

Key words: Plant extracts, Chinese, Radix Aconitum kusnezoffii, Mesaconitine, Aconitine, Percutaneous absorption, High-performance liquid chromatography

CLC Number: 

  • R943.4

Figure 1

Chromatogram of standard samples of aconitine and mesaconitineA: Peak of mesaconitine; B: Peak of aconitine."

Tab 1

Results of sample recovery"

Sample Sample concentration
(μg/ml)		 Sample added
(μg)		 Concentration of standard
sample added (μg/ml)		 Concentration tested
(?x±s, μg/ml)		 Recovery
(%)		 RSD
(%)
Mesaconitine 39.470 1 414.4 41.44 79.453 6±1.543 8 98.20 1.94
Aconitine 6.898 4 164.0 16.40 22.896 4±0.563 2 98.27 2.46

Figure 2

Chromatogram of high-dose extracts of Radix Aconitum kusnezoffii at the 18th hourA: Peak of mesaconitine; B: Peak of aconitine."

Tab 2

Contents of aconitine in extracts of Radix Aconitum kusnezoffii after permeation through the skin of rat (ヌ±S, μg/10 μl)"

Group n 1st hour 3rd hour 6th hour 12th hour 18th hour 24th hour
High-dose extracts 5 0.371±0.201 0.430±0.221* 0.415±0.158 0.427±0.177* 0.409±0.263* 0.398±0.180*
Medium-dose extracts 5 0.221±0.075 0.344±0.185 0.318±0.129 0.370±0.164 0.345±0.160 0.255±0.114
Low-dose extracts 5 0.228±0.070 0.367±0.134 0.345±0.076 0.345±0.155 0.282±0.107 0.275±0.099

Tab 3

Contents of mesaconitine in extracts of Radix Aconitum kusnezoffii after permeation through the skin of rat (ヌ±S,μg/10 μl)"

Group n 1st hour 3rd hour 6th hour 12th hour 18th hour 24th hour
High-dose extracts 5 0.611±0.263 0.746±0.340 0.764±0.336 1.055±0.494* 0.962±0.548* 1.443±0.547*
Medium-dose extracts 5 0.682±0.298 0.826±0.312 0.629±0.224 0.634±0.207 0.803±0.417 0.829±0.289
Low-dose extracts 5 0.454±0.158 0.791±0.251 0.799±0.220 0.716±0.410 0.646±0.189 0.798±0.357

Tab 4

Cumulative dose of skin permeation of aconitine in extracts of Radix Aconitum kusnezoffii (μg/cm2)"

Group n 1 h 3 h 6 h 12 h 18 h 24 h
High-dose extracts 5 88.843 115.894 126.921 144.082 154.329 165.819
Medium-dose extracts 5 53.027 90.089 95.668 119.010 125.623 115.980
Low-dose extracts 5 54.682 95.839 103.045 114.925 111.521 119.678

Tab 5

Cumulative dose of skin permeation of mesaconitine in extract of Radix Aconitum Kusnezoffii (μg/cm2)"

Group n 1 h 3 h 6 h 12 h 18 h 24 h
High-dose extracts 5 146.401 199.654 229.695 325.658 339.438 487.747
Medium-dose extracts 5 163.373 221.425 202.377 225.158 287.288 321.079
Low-dose extracts 5 108.812 205.216 234.230 241.582 249.288 307.884

Tab 6

Higuchi equation and rate constants of skin permeation of aconitine in extract of Radix Aconitum kusnezoffii"

Group Higuchi equation J (μg·cm–2·h–1) r
High-dose extracts Q=18.391X+78.127 18.391 0.984
Medium-dose extracts Q=15.963X+52.577 15.963 0.893
Low-dose extracts Q=13.563X+59.749 13.563 0.857

Tab 7

Higuchi equation and rate constants of skin permeation of mesaconitine in extract of Radix Aconitum kusnezoffii"

Group Higuchi equation J (μg·cm–2·h–1) r
High-dose extracts Q=78.805X+54.477 78.805 0.965
Medium-dose extracts Q=35.733X+130.850 35.733 0.931
Low-dose extracts Q=39.705X+106.764 39.705 0.905
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