AAPS PharmSciTech

, Volume 11, Issue 1, pp 372–382 | Cite as

Enhancement of Sodium Caprate on Intestine Absorption and Antidiabetic Action of Berberine

Research Article


Berberine, a plant alkaloid used in traditional Chinese medicine, has a wide spectrum of pharmacological actions, but the poor bioavailability limits its clinical use. The present aim was to observe the effects of sodium caprate on the intestinal absorption and antidiabetic action of berberine. The in situ, in vitro, and in vivo models were used to observe the effect of sodium caprate on the intestinal absorption of berberine. Intestinal mucosa morphology was measured to evaluate the toxic effect of sodium caprate. Diabetic model was used to evaluate antidiabetic effect of berberine coadministrated with sodium caprate. The results showed that the absorption of berberine in the small intestine was poor and that sodium caprate could significantly improve the poor absorption of berberine in the small intestine. Sodium caprate stimulated mucosal-to-serosal transport of berberine; the enhancement ratios were 2.08, 1.49, and 3.49 in the duodenum, jejunum, and ileum, respectively. After coadministration, the area under the plasma concentration–time curve of berberine was increased 28% than that in the absence of sodium caprate. Furthermore, both berberine and coadministration with sodium caprate orally could significantly decrease fasting blood glucose and improve glucose tolerance in diabetic rats (P < 0.05). The hypoglycemic effect of coadministration group was remarkably stronger, and the areas under the glucose curves was decreased 22.5%, compared with berberine treatment group (P < 0.05). Morphologic analysis indicated that sodium caprate was not significantly injurious to the intestinal mucosa. The study demonstrates that sodium caprate could significantly promote the absorption of berberine in intestine and enhance its antidiabetic effect without any serious mucosal damage.

Key words

berberine intestinal absorption enhancer sodium caprate type 2 diabetes 



Thanks to Pharmaceutical Sciences Department of Jilin University for the help of HPLC and LC–MS technique. The subject supported by administration of traditional Chinese medicine of Jilin province (2004-076) and National Natural Science Foundation of China (30572218).


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Copyright information

© American Association of Pharmaceutical Scientists 2010

Authors and Affiliations

  1. 1.Department of Pharmacology, Norman Bethune Medical CollegeJilin UniversityChangchunChina
  2. 2.Department of Cadre WardFirst Affiliated Hospital of Jilin UniversityChangchunChina

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