Absorption and enterohepatic circulation of baicalin in rats

Xing, Jie; Chen, Xiaoyan; Zhong, Dafang

doi:10.1016/j.lfs.2005.04.072

Cited by 185 publications

(121 citation statements)

References 12 publications

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“…This cycle is known as enterohepatic recirculation and may result in a longer exposure of the body to the polyphenol. Evidence for such enterohepatic recirculation has been obtained for the flavonoid baicalein 7-O-glucuronide with a rat model [87], but whether a similar process occurs in humans for some flavonoids is not known.…”

Section: Absorption Metabolism and Distribution Of Polyphenolsmentioning

confidence: 99%

Improving the oral bioavailability of beneficial polyphenols through designed synergies

2009

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Section: Absorption Metabolism and Distribution Of Polyphenolsmentioning

confidence: 99%

Improving the oral bioavailability of beneficial polyphenols through designed synergies

2009

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“…6 Though BA has been widely used in a number of therapeutic areas because of its antioxidant, anti-inflammatory, antibacterial, and anticancer effects, [6][7][8] its poor solubility (the maximum solubility is reported to be 91 µg/mL in water at 20°C) and low oral bioavailability (the absolute bioavailability was 2.2% after oral administration of BA in rats) severely limit its clinical application. 6,9,10 In order to overcome the shortcoming of BA, the development of novel dosages and formulations of BA has attracted an increasing attention in the pharmaceutical field in recent years. These have included microspheres, 11 microcapsules, 12 nanoemulsions, 13 inclusion complexes, 14,15 solid lipid nanoparticles, 16 BA-polyvinylpyrrolidone coprecipitate, and a BA-phospholipid complex.…”

Section: Introductionmentioning

confidence: 99%

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Wei

Guo

Zheng

et al. 2014

IJN

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Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi , a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-loaded liposome (BA-LP) to enhance oral bioavailability. BA-LP, composed of BA, Tween ® 80, Phospholipon ® 90H, and citric acid at weight ratio of 96/50/96/50, respectively, was prepared by the effervescent dispersion technique and characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and the in vitro release. Pharmacokinetics and biodistribution studies were carried out in rats after oral administration of BA-LP and a carboxymethyl cellulose suspension containing BA (BA-CMC) as a control. BA-LP exhibited a spherical shape by transmission electron microscopy observation. BA-LP had a mean particle size of 373±15.5 nm, zeta potential of −20.1±0.22 mV, and encapsulation efficiency of 82.7%±0.59%. The BA-LP showed a sustained-release behavior, and the in vitro drug-release kinetic model fit well with the Weibull distribution equation: lnln (1/(1−Q)) =0.609 lnt −1.230 ( r =0.995). The oral bioavailability and the peak concentration of the BA-LP was threefold and 2.82-fold that of BA-CMC, respectively. The in vivo distribution results indicated that drug concentrations were significantly increased in the liver, kidney, and lung in the case of BA-LP, which were 5.59-fold, 2.33-fold, and 1.25-fold higher than those of BA-CMC, respectively. In conclusion, the study suggested that BA-LP might be a potential oral drug delivery system to improve bioavailability of BA.

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“…The plasma concentrations declined rapidly for up to 3 h, and then slightly increased; the second peak appeared at 6-12 h; this could be due to enterohepatic circulation. 19 The peaks found in the MRM channel for baicalin, wogonin, and wogonoside are supposed to be their isobaric forms, generated through the metabolism of Scutellariae flavonoids (Figure 2). The mean arterial plasma concentration-time profiles of the 4 major flavonoids after oral administration of HPO12 at doses of 200 mg/kg in rats are shown in Figure 4, and some relevant pharmacokinetic parameters are listed in Table 3.…”

Section: 15mentioning

confidence: 99%

“…The first peak occurred at 15-30 min, and the second at 6-12 h after administration, and then plasma concentrations fluctuated up to the last measured time. This could be due to enterohepatic circulation 19 and subsequent continuous absorption of the flavonoids.…”

Section: 15mentioning

confidence: 99%

Simultaneous Determination of Baicalein, Baicalin, Wogonin, and Wogonoside in Rat Plasma by LC-MS/MS for Studying the Pharmacokinetics of the Standardized Extract of Scutellariae Radix

Chung¹,

Lim²,

Kim³

et al. 2012

Bulletin of the Korean Chemical Society

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A new composition of standardized Scutellariae Radix extract (HPO12) was developed for treatment of Alzheimer's disease. For the preclinical pharmacokinetic study of HPO12, a rapid, sensitive, and selective LC-MS/MS method was developed and validated for the simultaneous determination of 4 bioactive compounds, baicalein, baicalin, wogonin, and wogonoside. After extraction with ethylacetate, chromatographic analysis was performed on a Thermo C 18 column (150 mm × 2.1 mm, 3 μm) with a mobile phase consisting of 0.1% formic acid (A) and 0.1% formic acid in 95% acetonitrile (B) by using gradient elution at a flow rate of 250 μL/min. Analytes introduced to a mass spectrometer were monitored by multiple reaction monitoring (MRM) in positive ion mode. Using 25 μL of plasma sample, the method was validated over the following concentration ranges: 25-5000 ng/mL for baicalein, 20-40000 ng/mL for baicalin, 1-1000 ng/mL for wogonin, and 5-10000 ng/mL for wogonoside. The intra-and inter-day precision and accuracy of the quality control samples at the 4 concentrations showed ≤ 13.7% relative standard deviation (RSD) and 86.6-105.5% accuracy. The method was successfully applied to determine the concentrations of baicalein, baicalin, wogonin, and wogonoside in rat plasma after intraperitoneal and oral administrations of HPO12.

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Absorption and enterohepatic circulation of baicalin in rats

Cited by 185 publications

References 12 publications

Improving the oral bioavailability of beneficial polyphenols through designed synergies

Improving the oral bioavailability of beneficial polyphenols through designed synergies

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Simultaneous Determination of Baicalein, Baicalin, Wogonin, and Wogonoside in Rat Plasma by LC-MS/MS for Studying the Pharmacokinetics of the Standardized Extract of Scutellariae Radix

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