Pharmacokinetic comparisons of rutaecarpine and evodiamine after oral administration of Wu-Chu-Yu extracts with different purities to rats

J Ethnopharmacol. 2012 Jan 31;139(2):395-400. doi: 10.1016/j.jep.2011.11.023. Epub 2011 Nov 22.

Abstract

Ethnopharmacological relevance: Wu-Chu-Yu is a well-known herbal drug used for hypertension. Rutaecarpine and evodiamine are main bioactive components of the medicine.

Materials and methods: A sensitive and specific HPLC method was developed to analyze rutaecarpine (Rut) and evodiamine (Evo) in rat whole blood. The pharmacokinetics of Rut and Evo after oral administration of Wu-Chu-Yu extracts with different purities to rats was compared to evaluate the effect of purity of Wu-Chu-Yu extracts on the absorption of Rut and Evo. Male Sprague-Dawley rats were given Wu-Chu-Yu extracts with different purities (high, medium and low) approximately the same doses of equivalent to Rut (40 mg/kg) and Evo (31 mg/kg). The contents of Rut and Evo were 45 and 35%, 28 and 21%, 9 and 7% in high, medium and low purity extracts, respectively. At different time points (0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3 and 4h) after administration, the concentrations of Rut and Evo in rat whole blood were determined by HPLC, and main pharmacokinetic parameters were calculated.

Results: The results indicated that the absorption of Rut and Evo in Wu-Chu-Yu extracts was improved when compared with the pure Rut and Evo and there were significant differences among different groups.

Conclusions: The bioavailability of Rut and Evo was increased along with the increasing of purity (16%-80%) in Wu-Chu-Yu extracts.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Alkaloids / administration & dosage
  • Alkaloids / blood
  • Alkaloids / chemistry
  • Alkaloids / pharmacokinetics*
  • Animals
  • Biological Availability
  • Calibration
  • Chromatography, High Pressure Liquid / standards
  • Drug Stability
  • Drugs, Chinese Herbal / administration & dosage
  • Drugs, Chinese Herbal / chemistry
  • Drugs, Chinese Herbal / pharmacokinetics*
  • Evodia / chemistry
  • Indole Alkaloids / administration & dosage
  • Indole Alkaloids / analysis
  • Indole Alkaloids / blood
  • Indole Alkaloids / pharmacokinetics*
  • Intestinal Absorption
  • Male
  • Plant Extracts / administration & dosage
  • Plant Extracts / blood
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacokinetics*
  • Quinazolines / administration & dosage
  • Quinazolines / analysis
  • Quinazolines / blood
  • Quinazolines / pharmacokinetics*
  • Quinolines / administration & dosage
  • Quinolines / blood
  • Quinolines / chemistry
  • Quinolines / pharmacokinetics*
  • Rats
  • Rats, Sprague-Dawley
  • Reference Standards

Substances

  • Alkaloids
  • Drugs, Chinese Herbal
  • Gosyuyu
  • Indole Alkaloids
  • Plant Extracts
  • Quinazolines
  • Quinolines
  • rutecarpine
  • evodiamine