Comparative pharmacokinetics of three alkaloids in normal and acute hepatitis rats after oral administration of Yanhuanglian total alkaloids extract

Biomed Chromatogr. 2018 Nov;32(11):e4329. doi: 10.1002/bmc.4329. Epub 2018 Aug 7.

Abstract

Acute hepatitis is a severe inflammatory disease with high mortality rates. Dehydrocavidine (DC), berberine (BB) and palmatine (PT), the bioactive components of Yanhuanglian total alkaloids extract (YTAE), may play important roles in its protective effect against acute hepatitis. The present study was designed to compare the pharmacokinetic properties of DC, BB and PT after oral administration of YTAE in normal and acute hepatitis rats. The plasma pharmacokinetic profiles of three major bioactive alkaloids from YTAE were analyzed using an LC-MS/MS method. It was found that the pharmacokinetic parameters of DC, BB and PT represented a statistically significant difference (p ˂ 0.05) between the normal rats and the acute hepatitis rats after administration of YTAE. The results indicated that the Cmax , T1/2β and AUC of DC, BB and PT in acute hepatitis rats were significantly increased, whereas the CL and Vd values were remarkably decreased (p ˂ 0.05) over those of the normal rats. The results suggested that the pharmacokinetic behavior of the active constituents from YTAE could be changed when it was used in acute hepatitis animals, which provide a meaningful basis for developing a clinical dosage regimen in the treatment of acute hepatitis by YTAE.

Keywords: Yanhuanglian total alkaloids extract; acute hepatitis; berberine; dehydrocavidine; palmatine; pharmacokinetics.

MeSH terms

  • Acute Disease
  • Administration, Oral
  • Alkaloids / administration & dosage
  • Alkaloids / blood
  • Alkaloids / pharmacokinetics*
  • Animals
  • Drugs, Chinese Herbal / administration & dosage
  • Drugs, Chinese Herbal / pharmacokinetics*
  • Hepatitis / metabolism*
  • Linear Models
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Reproducibility of Results
  • Sensitivity and Specificity

Substances

  • Alkaloids
  • Drugs, Chinese Herbal