The absorption characterization effects and mechanism of Radix Angelicae dahuricae extracts on baicalin in Radix Scutellariae using in vivo and in vitro absorption models

J Ethnopharmacol. 2012 Jan 6;139(1):52-7. doi: 10.1016/j.jep.2011.10.001. Epub 2011 Oct 15.

Abstract

Ethnopharmacological relevance: Angelicae Dahurica(Hoffm.)Benth.&Hook.f.ex Franch.&Sav combined with Scutellaria baicalensis Georgi. has been widely used as herb-pairs in traditional Chinese medicine (TCM) to treat migraine headache and cataract, but the underlying compatibility mechanism of the two herbs remains unknown.

Aim of study: In the present work, we investigated the additive or synergistic effects of absorption behavior of Radix Angelicae dahuricae extracts on baicalin, and the absorption-enhancing mechanism of Radix Angelicae dahuricae extracts on baicalin.

Materials and methods: Total coumarins (Cou) and volatile oil (VO), as the two main components of Radix Angelicae dahuricae, were extracted by supercritical fluid extraction (SFE) further treated with liquid-liquid separation method. The absorption behavior was investigated by applying the everted gut sac technique and in situ single-pass intestinal perfusion method.

Results and conclusions: The results showed that both the Cou and the VO could improve the intestinal absorption of baicalin in vivo, and had synergistic action the enhanced absorption of baicalin. Since verapamil did not affect the P(app) and K(a) of baicalin significantly, we concluded that the absorption of Baicalin could not be an active transportation in dependent of P-glycoprotein-Mediated efflux systems. Based on intestinal absorption of drug studying was one of the efficacious methods to clarify the compatibility of principles of herb-pairs. The everted gut sac technique and in situ single-pass intestinal perfusion technique model were the effective methods to study the absorption of drug, the application of the animal model to investigating the absorption of herb-drug interactions or other relevant research purposes is envisioned.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Angelica*
  • Animals
  • Coumarins / pharmacology*
  • Drugs, Chinese Herbal / pharmacology*
  • Female
  • Flavonoids / blood
  • Flavonoids / metabolism
  • Flavonoids / pharmacokinetics*
  • Herb-Drug Interactions
  • In Vitro Techniques
  • Intestinal Absorption / drug effects
  • Intestinal Mucosa / metabolism
  • Male
  • Oils, Volatile / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Scutellaria baicalensis*

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Coumarins
  • Drugs, Chinese Herbal
  • Flavonoids
  • Oils, Volatile
  • baicalin