Excretion of Berberine and Its Metabolites in Oral Administration in Rats. Issue 11 (4th September 2013)

• Record Type: Journal Article
• Authors: Ma, Jing‐Yi; Feng, Ru; Tan, Xiang‐Shan; Ma, Chao; Shou, Jia‐Wen; Fu, Jie; Huang, Min; He, Chi‐Yu; Chen, Shuo‐Nan; Zhao, Zhen‐Xiong; He, Wen‐Yi; Wang, Yan; Jiang, Jian‐Dong
• Is Part Of: Journal of pharmaceutical sciences. Volume 102:Issue 11(2013:Nov.)
• Page Start: 4181
• Page End: 4192
• Publication Date: 2013-09-04
• Subjects: Pharmacy -- Periodicals; 615.1
• DOI: 10.1002/jps.23718
• Languages: English
• ISSNs: 0022-3549

Abstract

<abstract abstract-type="main" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Berberine (BBR) has been confirmed to show extensive bioactivities for the treatments of diabetes and hypercholesterolemia in clinic. However, there are few pharmacokinetic studies to elucidate the excretions of BBR and its metabolites. Our research studied the excretions of BBR and its metabolites in rats after oral administration (200 mg/kg). Metabolites in bile, urine, and feces were detected by liquid chromatography coupled to ion trap time‐of‐flight mass spectrometry; meanwhile, a validated liquid chromatography coupled with tandem mass spectrometry method was developed for their quantifications. Sixteen metabolites, including 10 Phase I and six Phase II metabolites were identified and clarified after dosing <italic>in vivo</italic>. Total recovered rate of BBR was 22.83% (19.07% of prototype and 3.76% of its metabolites) with 9.2 × 10<sup>−6</sup>% in bile (24 h), 0.0939% in urine (48 h), and 22.74% in feces (48 h), respectively. 83% of BBR was excreted as thalifendine (M1) from bile, whereas thalifendine (M1) and berberrubine (M2) were the major metabolites occupying 78% of urine excretion. Most of BBR and its metabolites were found in feces containing 84% of prototype. In summary, we provided excretion profiles of BBR and its metabolites after oral administration in rats <italic>in vivo</italic>. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:4181–4192, 2013</p> </abstract>