The effects of berberine on the pharmacokinetics of ciclosporin A in healthy volunteers
Abstract
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.
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A separate study in healthy volunteers confirmed the direction of the cyclosporine interaction.
“A separate study in healthy volunteers confirmed the direction of the interaction [117].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [117]
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- Authors
- Xin, H.-W., Wu, X.-C., Li, Q., Yu, A.-R., & Zhong, M.-Y.
- Affiliations
- Wuhan General Hospital of Guangzhou (CN)
- ORCID
- Yu, A.-R.
- Venue
- Methods and Findings in Experimental and Clinical Pharmacology
- Publisher
- Portico
- Published
- 2006
- Volume
- 28
- Issue
- 1
- Pages
- 25
- ISSN
- 0379-0355 (ISSN-L)
- 2013-0155
- OpenAlex
- W2049586555
- Cited by
- 63
- References
- 0
- Citations by year
- 2026: 1 · 2025: 2 · 2024: 3 · 2023: 2 · 2022: 3 · 2021: 5 · 2020: 4 · 2019: 2 · 2018: 3 · 2016: 7 · 2015: 3 · 2014: 5 · 2013: 4 · 2012: 9
- FWCI
- 1.66
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Methods and Findings in Experimental and Clinical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- berberine, cyclosporine, pharmacokinetics, drug-drug interactions, oral bioavailability, CYP3A4 inhibition, hepatic metabolism, intestinal metabolism, healthy volunteers
- MeSH terms
- Adult, Berberine, Biological Availability, Cytochrome P-450 Enzyme System, Drug Interactions, Enzyme Inhibitors, Gastric Emptying, Humans, Intestine, Small, Liver, Male, Cyclosporine, Cytochrome P-450 CYP3A, Cytochrome P-450 Enzyme Inhibitors
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