Preparation and Evaluation of Antidiabetic Agents of Berberine Organic Acid Salts for Enhancing the Bioavailability

  • Molecules. 2018 Dec 28;24(1):103. doi: 10.3390/molecules24010103.
Hong-Xin Cui  1  2 ,  Ya-Nan Hu  3 ,  Jing-Wan Li  4 ,  Ke Yuan  5 ,  Ying Guo  6
Affiliations
  • 1. College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China [email protected] (H.-X.C.). [email protected].
  • 2. Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & Chinese Medicine Development of Henan Province, Zhengzhou 450046, China. [email protected].
  • 3. College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China [email protected] (H.-X.C.). [email protected].
  • 4. Forestry and biotechnology College, Zhejiang Agriculture and Forestry University, Lin'an 311300, China. [email protected].
  • 5. Jiyang College of Zhejiang Agriculture and Forestry University, Zhu'ji 311800, China. [email protected].
  • 6. Zhejiang Chinese Medical University, Zhejiang, Hangzhou, 310053, China. [email protected].
PMID: 30597911 DOI: 10.3390/molecules24010103
Abstract

Berberine has many pharmacological effects, such as antidiabetic, antimicrobial, anti-inflammatory, and antioxidant, but the question remains on how its low oral bioavailability has greatly limited its clinical application. As a safer hypoglycemic agent, we must evaluate the bioavailability of berberine organic acid salts (BOAs) to ensure that the bioavailability of berberine is not negatively affected. It has been proven that the bioavailability of BOAs is higher than that of BH (berberine hydrochloride); especially BF (berberine fumarate) and BS (berberine succinate), which are improved by 1.278-fold and 1.313-fold, respectively. After 1 h of oral administration, berberine mainly acted on the stomach of mice, it also influenced the liver, kidney, lungs, and intestines after 4 h. The accumulation of BF in the lung is more evident than BH. Our analysis shows that these results are closely related to the regulation of organic acids and berberine in the intestinal tract, they also indicate the influence of intestinal flora on berberine metabolism.

Keywords
berberine organic acid salts; in-vivo imaging; intestinal flora; pharmacokinetics; type 2 diabetes.
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