کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2484803 | 1114337 | 2013 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Excretion of Berberine and Its Metabolites in Oral Administration in Rats
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
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 (200Â mg/kg). Metabolites in bile, urine, and feces were detected by liquid chromatography coupled to ion trap timeâofâflight 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 9.2Â ÃÂ 10â6% in bile (24Â h), 0.0939% in urine (48Â h), and 22.74% in feces (48Â 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 in vivo.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 11, November 2013, Pages 4181-4192
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 11, November 2013, Pages 4181-4192
نویسندگان
JingâYi Ma, Ru Feng, XiangâShan Tan, Chao Ma, JiaâWen Shou, Jie Fu, Min Huang, ChiâYu He, ShuoâNan Chen, ZhenâXiong Zhao, WenâYi He, Yan Wang, JianâDong Jiang,