[Study on in vitro/in vivo correlation of extracts from Ligusticum chuanxiong after transdermal administration]

Zhongguo Zhong Yao Za Zhi. 2013 Feb;38(3):422-6.
[Article in Chinese]

Abstract

Objective: To study the transdermal permeation and in vivo pharmacokinetics of effective constituent ferulic acid from Ligusticum chuanxiong, in order to establish the in vitro/in vivo correlation in transdermal permeation.

Method: Franz diffusion cell was adopted in the in vitro transdermal permeation, with CD-1 nude rat abdominal skin as the permeation medium. Linear probes were implanted in CD-1 nude rats. With PBS as perfusate, microdialysis was employed to study the pharmacokinetics. Ferulic acid concentrations in the receptor solution and dialysate were assessed by high performance liquid chromatography (HPLC). The study on correlation between in vitro and in vivo data was conducted by deconvolution methods.

Result: The transdermal permeation rate of ferulic acid from Ligusticum chuanxiong was (0.094 4 +/- 0.049 4) microg x cm2 x min, with Cmax of ferulic acid being 808.91 microg x L(-1), and Tmax being 183 min after dermal administration. The in vitro/in vivo correlation was 93.61.

Conclusion: Ferulic acid in extracts from L. chuanxiong can quickly penetrate skins. By using the in vitro/in vivo correlation in transdermal permeation, simple in vitro transdermal permeation method can be adopted to study the changes in its pharmacokinetics.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Chromatography, High Pressure Liquid
  • Coumaric Acids / administration & dosage
  • Coumaric Acids / pharmacokinetics*
  • Drugs, Chinese Herbal / administration & dosage
  • Drugs, Chinese Herbal / pharmacokinetics*
  • In Vitro Techniques
  • Ligusticum
  • Metabolic Clearance Rate
  • Permeability
  • Rats
  • Rats, Nude
  • Skin / metabolism*
  • Skin Absorption*

Substances

  • Coumaric Acids
  • Drugs, Chinese Herbal
  • ferulic acid
  • chuangxiong extract