The effects of berberine on the pharmacokinetics of cyclosporin A in healthy volunteers.

  • Xin H
  • Wu X
  • Li Q
 et al. 
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The effects of berberine (BBR) on the pharmacokinetics of ciclosporin A (CsA) were examined in healthy volunteers. Six healthy male volunteers were orally treated with 0.3 g BBR, twice daily for 10 days. Pharmacokinetic investigations on CsA at 6 mg/kg were done both before and at the end of the BBR treatment period. Another six healthy male volunteers were involved in the pharmacokinetic study with 3 mg CsA/kg, in which the subjects orally received the second single dose of 3 mg CsA/kg, followed by a single oral dose of 0.3 g BBR. The blood CsA concentrations were determined by fluorescence polarization immunoassay. In the pharmacokinetic study with 6 mg CsA/kg, BBR caused no significant changes in the pharmacokinetic parameters of CsA. However, in the trial with 3 mg CsA/kg, the average percentage increase in area under the blood concentration-time curve of CsA was 19.2% (P < 0.05) and the mean C12 increased to 123 microg/l from 104 microg/l (P < 0.05), without altering elimination half-life (t(1/2)), maximum blood drug concentration (Cmax), time to Cmax (tmax), apparent oral clearance (CL/F). The present results suggest that BBR can increase the oral bioavailability of CsA at the dosage of 3 mg/kg. The BBR-mediated increase in CsA bioavailability may be partly attributed to a decrease in liver and/or intestinal metabolism through the inhibition of CYP3A4 in the liver and/or gut wall. The BBR-induced increase in emptying time of stomach and small intestine might be another reason for the increase in CsA bioavailability. However, the speculation should be proved by further investigation.

Author-supplied keywords

  • Adult
  • Berberine
  • Berberine: pharmacology
  • Biological Availability
  • Cyclosporine
  • Cyclosporine: pharmacokinetics
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme System
  • Cytochrome P-450 Enzyme System: antagonists & inhi
  • Cytochrome P-450 Enzyme System: metabolism
  • Drug Interactions
  • Enzyme Inhibitors
  • Enzyme Inhibitors: pharmacology
  • Gastric Emptying
  • Gastric Emptying: drug effects
  • Humans
  • Intestine, Small
  • Intestine, Small: enzymology
  • Liver
  • Liver: enzymology
  • Male

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  • H-W Xin

  • X-C Wu

  • Q Li

  • a-R Yu

  • M-Y Zhong

  • Y-Y Liu

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