Comparative pharmacokinetics of a marker compound, baicalin in KOB extract after oral administration to normal and allergic-induced rats

Drug Deliv. 2014 Sep;21(6):453-8. doi: 10.3109/10717544.2013.876561. Epub 2014 Jan 22.

Abstract

KOB extracts are a polyherbal medicine had been prescribed for the treatment of hyperhydrosis and allergic diseases such as allergic asthma and rhinitis in oriental clinics. Therefore, the pharmacokinetic studies of the KOB extract administered orally to normal rats and rhinitis-induced rats to understand the correlation of the efficacy and plasma concentration of KOB in patients of allergic rhinitis in future were performed. The study was conducted according to administration for pure baicalin in normal rats, baicalin in KOB extract in normal rats and rhinitis-induced rats. Baicalin in rat plasma was analyzed and validated by HPLC analysis. The interday precision based on the standard deviation of replicates of quality control samples ranged from 3.6% to 7.9% with accuracy ranging from 92.9% to 101.2% for baicalin. Based on validated analysis, pharmacokinetic study was carried out. Pure baicalin in normal rats and baicalin in KOB extract in normal rats showed bimodal curves due to direct absorption and glucuronidation. The Tmax, Cmax and AUC of pure baicalin in normal rats or baicalin in KOB extract in normal rats were 12 h, 0.68 µg/ml and 9.85 µg h/ml, respectively, or 12 h, 0.46 µg/ml and 6.36 µg h/ml, respectively. The analytical method showed excellent sensitivity, precision and accuracy, being successfully employed in a pharmacokinetic study of polyherbal medicine, KOB extract. Allergic-induced condition did not affect the pharmacokinetics of KOB extracts, suggesting KOB extracts did not require dosage adjustment in subjects with allergic-induced diseases.

Keywords: Allergic-induced rat; KOB extract; baicalin; pharmacokinetic; polyherbal.

Publication types

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

MeSH terms

  • Administration, Oral
  • Animals
  • Area Under Curve
  • Chromatography, High Pressure Liquid / methods
  • Flavonoids / administration & dosage*
  • Flavonoids / blood
  • Flavonoids / pharmacokinetics*
  • Intestinal Absorption / physiology
  • Male
  • Plant Extracts / administration & dosage*
  • Plant Extracts / blood
  • Plant Extracts / pharmacokinetics*
  • Plant Preparations / administration & dosage*
  • Plant Preparations / blood
  • Plant Preparations / pharmacokinetics*
  • Rats
  • Rats, Sprague-Dawley
  • Rhinitis / blood
  • Rhinitis / drug therapy*

Substances

  • Flavonoids
  • Plant Extracts
  • Plant Preparations
  • baicalin