Pharmacokinetics and Pharmacological Activities of Berberine in Diabetes Mellitus Treatment
Open accessAbstract
Traditional Chinese medicine (TCM) has good clinical application prospects in diabetes treatment. In addition, TCM is less toxic and/or has fewer side effects and provides various therapeutic effects. Berberine (BBR) is isolated as the main component in many TCM kinds (e.g., Rhizoma Coptidis and Berberidis Cortex). Furthermore, BBR can reduce blood sugar and blood fat, alleviate inflammation, and improve the state of patients. Based on the recent study results of BBR in diabetes treatment, the BBR pharmacokinetics and mechanism on diabetes are mainly studied, and the specific molecular mechanism of related experimental BBR is systematically summarized and analyzed. Clinical studies have proved that BBR has a good therapeutic effect on diabetes, suggesting that BBR may be a promising drug candidate for diabetes. More detailed BBR mechanisms and pathways of BBR need to be studied further in depth, which will help understand the BBR pharmacology in diabetes treatment.
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A usual oral dose of 400-500 mg gives peak plasma concentrations of a few nanograms per milliliter, roughly 1-10 nM.
“A usual oral dose of 400–500 mg gives peak plasma concentrations of a few nanograms per milliliter, which for a molecule of about 336 Da is roughly 1–10 nM [49,56].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [56]
Section 2.2 (Distribution; page unavailable) says berberine has low plasma content after oral administration, supporting the general point. Neither that section nor Section 2.1 (Absorption; page unavailable) gives a 400–500 mg dose, a peak concentration in ng/mL, or a value in nM; searches for those terms found no such passage. (LLM, conf=0.82)
Experimental — accuracy not yet measuredPeak plasma concentration of berberine after usual doses is on the order of nanograms per milliliter, frequently below the in vitro activity threshold.
“The peak plasma concentration after usual doses is on the order of nanograms per milliliter, frequently below the activity threshold observed in vitro [49,56]”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [56]
Section 2.2 (Distribution; page unavailable) says berberine has low plasma content after oral administration, and Section 2.1 (Absorption; page unavailable) describes poor oral bioavailability. Neither section gives a peak concentration in ng/mL after usual doses or compares plasma concentrations with an in vitro activity threshold. (LLM, conf=0.84)
Experimental — accuracy not yet measured
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- Authors
- Han, Y., Xiang, Y., Shi, Y., Tang, X., Pan, L., Gao, J., Bi, R., & Lai, X.
- Affiliations
- Chengdu University of Traditional Chinese Medicine (CN)
- Corresponding author
- Lai, Xianrong
- Venue
- Evidence-Based Complementary and Alternative Medicine
- Publisher
- Wiley
- Published
- 2021-08-21
- Volume
- 2021
- Pages
- 1-15
- ISSN
- 1741-427X (ISSN-L)
- 1741-4288
- PMC
- PMC8405293
- OpenAlex
- W3194644078
- Cited by
- 51
- References
- 131
- Citations by year
- 2026: 10 · 2025: 11 · 2024: 11 · 2023: 9 · 2022: 8 · 2021: 2
- FWCI
- 0.95
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Locations
- Evidence-based Complementary and Alternative Medicine (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- National Natural Science Foundation of China (81774007, 81473427, 81173360, 81560806, 2017YFC1703904, 16ZA0120)
- National Key R&D Projects (81774007, 81473427, 81173360, 81560806, 2017YFC1703904, 16ZA0120)
- Education Department of Sichuan Province (81774007, 81473427, 81173360, 81560806, 2017YFC1703904, 16ZA0120)
- Topics
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Keywords
- berberine, diabetes mellitus, pharmacokinetics, traditional Chinese medicine, Coptidis Rhizoma, blood glucose reduction, lipid metabolism, anti-inflammatory activity, molecular mechanisms, drug candidates
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