Bioavailability study of berberine and the enhancing effects of TPGS on intestinal absorption in rats
Open accessAbstract
Berberine chloride (BBR) is a natural isoquinoline alkaloid extracted from medicinal herbs. It has been reported that the intestinal absorption of BBR is very low. In this study, the absolute bioavailability of BBR was studied, and the enhancing effects of D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on intestinal absorption were investigated in rats. BBR injection was administrated via the femoral vein at a dose of 1.0 mg kg(-1) in intravenous group, and BBR oral formulations were administrated by oral gavage at a dose of 100 mg kg(-1) in BBR control (control) group and BBR-TPGS (test) group, respectively. The result showed that BBR had a very low absolute bioavailability of 0.68%, and TPGS could enhance intestinal absorption of BBR significantly. TPGS at a concentration of 2.5% could improve peak concentration (C(max)) and area under the curve (AUC(0-36)) of BBR by 2.9 and 1.9 times, respectively. The absorption enhancing ability of TPGS may be due to its ability to affect the biological activity of P-glycoprotein and thereby reduce the excretion of absorbed BBR into the intestinal lumen. This study indicated that absolute bioavailability of BBR was 0.68% in rats, and TPGS was a good absorption enhancer capable of enhancing intestinal absorption of BBR significantly.
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Clinical literature dedicated to berberine interactions remains fragmented, dispersed across isolated pharmacokinetic studies, case reports, and broad pharmacological reviews.
“Nonetheless, the clinical literature dedicated to berberine interactions remains fragmented, dispersed across isolated pharmacokinetic studies, case reports, and broad pharmacological reviews in which interactions are treated only marginally [2,41].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [41]
The Animal Studies results and Pharmacokinetics Analysis identify this as a berberine pharmacokinetic study in rats, so it can serve as an example of an individual study. The paper does not assess whether clinical literature on berberine interactions is fragmented or dispersed across case reports and reviews; its rat study is not itself clinical evidence. Page numbers are unavailable in our copy. (LLM, conf=0.77)
Experimental — accuracy not yet measuredFormulations designed to raise absorption, whether TPGS-based, dihydroberberine or other enhanced-bioavailability preparations, change systemic exposure deliberately, so an effect size measured with one product cannot be carried over to another even when the labeled dose matches.
“Formulations designed to raise absorption, whether TPGS-based, dihydroberberine or other enhanced-bioavailability preparations, change systemic exposure deliberately, so an effect size measured with one product cannot be carried over to another even when the labeled dose matches.”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [41]
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“The taxonomy of mechanisms, across four axes, together with the exposure modifier and the risk-stratification framework proposed here, provides a reproducible reasoning tool, intended to turn a fragmented field into a coherent safety practice [41,67].”
Influential
- Authors
- Chen, W., Miao, Y.-Q., Fan, D.-J., Yang, S.-S., Lin, X., Meng, L.-K., & Tang, X.
- Affiliations
- Shenyang Pharmaceutical University (CN)
- Corresponding author
- Tang, Xing
- Venue
- AAPS PharmSciTech
- Published
- 2011-06
- Volume
- 12
- Issue
- 2
- Pages
- 705-711
- ISSN
- 1530-9932 (ISSN-L)
- PMC
- PMC3134654
- OpenAlex
- W2038231515
- Cited by
- 363
- References
- 27
- Citations by year
- 2026: 33 · 2025: 39 · 2024: 30 · 2023: 30 · 2022: 46 · 2021: 49 · 2020: 26 · 2019: 21 · 2018: 16 · 2017: 17 · 2016: 13 · 2015: 16 · 2014: 9 · 2013: 7 · 2012: 10
- FWCI
- 5.29
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- www.springer.com/tdm (tdm)
- Locations
- AAPS PharmSciTech (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Department of Science and Technology of Liaoning Province (2009ZX09301–012)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Keywords
- berberine, TPGS, absolute bioavailability, intestinal absorption, absorption enhancers, P-glycoprotein, isoquinoline alkaloids, oral bioavailability, rats
- MeSH terms
- Administration, Oral, Animals, Berberine, Biological Availability, Drug Carriers, Drug Synergism, Intestinal Absorption, Male, Polyethylene Glycols, Random Allocation, Vitamin E, Rats, Wistar, Rats
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