Abstract

Simple and rapid high-performance liquid chromatography methods were developed for the determination of berberine (BB) in various rat tissues so as to evaluate a P-gp inhibitor, glycyrrhetinic acid (GA), on BB's oral bioavailability. Acetonitrile was used to extract BB from tissues and showed different extraction recoveries in diverse tissues. The intra- and interday precision and accuracy were less than 10%. Long-term stability, pre (post) -preparative stability, and freeze-thaw stability were evaluated, and the results showed it could meet the need of this study. The proposed methods were subsequently applied to investigate the possible drug-drug interaction of GA and BB in vivo from the aspect of tissue distribution. The results showed that no significant difference was found between the group of low dose and high dose at the same time point. The tissue distributions show a saturated model, i.e., the content of BB in tissue tends to be constant while its dose is more than 200 mg/kg. Besides, the contents of BB ranged from high to low according to the order of the liver, kidney, and spleen. The BB content in the liver is especially high as compared to other tissues.

Highlights

  • Berberine (BB) is an isoquinoline alkaloid, which is the main ingredient of some traditional Chinese medicines (TCMs), such as Phellodendri Cortex, Coptidis Rhizoma, and Radix Berberidis [1, 2]

  • Berberine bought form Aladdin Chemistry Co., Ltd. (HPLC purity 97%); glycyrrhetinic acid was obtained from AR, Fluka Chemical Corp., product of Spain; methanol and acetonitrile (HPLC grade) were obtained from Amethyst Chemicals (China); and sodium carboxymethyl cellulose was obtained from Aladdin Chemistry Co., Ltd

  • Selectivity of high-performance liquid chromatograph (HPLC) Analysis. e selectivity of HPLC analysis was evaluated by comparing chromatograms of blank tissue samples prior to drug administration, blank tissue spiked with Berberine Glycyrrhetinic acid (GA) (BB) standard solution, and samples after drug administration

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Summary

Introduction

Berberine (BB) is an isoquinoline alkaloid, which is the main ingredient of some traditional Chinese medicines (TCMs), such as Phellodendri Cortex, Coptidis Rhizoma, and Radix Berberidis [1, 2]. Glycyrrhizic acid (GL), a triterpenoid, is one of the characteristic ingredients of licorice which is the most commonly used TCM in prescription. Clinical trials have clearly shown that GA has a good effect on all types of dermatitis [13] and purulent scar disease [14]. As to BB, antibacterial [15], antitumor [16, 17], antioxidant [17, 18], anti-inflammatory [19], and cholesterol-lowering [20,21,22] effects have been documented. BB has been proved its potential in future clinic application for hyperlipidemia [21], diabetes [24], and cardiovascular [23] and neuroprotective diseases [25]

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