Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 102, Issue 11, Pages 4181-4192Publisher
WILEY
DOI: 10.1002/jps.23718
Keywords
excretion; mass spectrometry; metabolism; pharmacokinetics; analytical chemistry; berberine
Funding
- National Science and Technology Major Projects [2012ZX09301-002-001, 2012ZX09301-002006]
- National Natural Science Foundation of China [30873115, 81072611]
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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 (200mg/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 in vivo. Total recovered rate of BBR was 22.83% (19.07% of prototype and 3.76% of its metabolites) with 9.2x10(-6)% in bile (24h), 0.0939% in urine (48h), and 22.74% in feces (48h), 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 in vivo. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:4181-4192, 2013
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