Bioavailability Study of Berberine and the Enhancing Effects of TPGS on Intestinal Absorption in Rats
Bioavailability Study of Berberine and the Enhancing Effects of TPGS on Intestinal Absorption in Rats
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DOI：
10.1208/s12249-011-9632-z
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发表时间：
2011-06-01
影响因子：
3.3
通讯作者：
Tang, Xing
中科院分区：
文献类型：
--
作者：
Chen, Wei;Miao, Yu-Qiang;Tang, Xing
氯化小檗碱（BBR）是从草药中提取的天然异喹啉类生物碱。据报道，BBR的肠道吸收非常低。本研究研究了BBR的绝对生物利用度，并研究了d- α -生育酚聚乙二醇1000琥珀酸酯（TPGS）对大鼠肠道吸收的促进作用。静脉注射组经股静脉给药，剂量为1.0 mg kg(-1)； BBR对照组（对照组）和BBR- tpgs组（试验组）分别以100 mg kg（-1）灌胃给药。结果表明，BBR的绝对生物利用度极低，为0.68%，TPGS可显著提高BBR的肠道吸收。2.5%浓度的TPGS可使BBR的峰浓度（C (max)）和曲线下面积（AUC(0-36)）分别提高2.9倍和1.9倍。TPGS促进吸收的能力可能是由于其能够影响p -糖蛋白的生物活性，从而减少吸收的BBR排泄到肠腔。本研究表明，BBR在大鼠体内的绝对生物利用度为0.68%，TPGS是一种良好的吸收促进剂，能显著促进BBR的肠道吸收。
Berberine chloride (BBR) is a natural isoquinoline alkaloid extracted from medicinal herbs. It has been reported that the intestinal absorption of BBR is very low. In this study, the absolute bioavailability of BBR was studied, and the enhancing effects of d-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) on intestinal absorption were investigated in rats. BBR injection was administrated via the femoral vein at a dose of 1.0 mg kg(-1) in intravenous group, and BBR oral formulations were administrated by oral gavage at a dose of 100 mg kg(-1) in BBR control (control) group and BBR-TPGS (test) group, respectively. The result showed that BBR had a very low absolute bioavailability of 0.68%, and TPGS could enhance intestinal absorption of BBR significantly. TPGS at a concentration of 2.5% could improve peak concentration (C (max)) and area under the curve (AUC(0-36)) of BBR by 2.9 and 1.9 times, respectively. The absorption enhancing ability of TPGS may be due to its ability to affect the biological activity of P-glycoprotein and thereby reduce the excretion of absorbed BBR into the intestinal lumen. This study indicated that absolute bioavailability of BBR was 0.68% in rats, and TPGS was a good absorption enhancer capable of enhancing intestinal absorption of BBR significantly.