Pharmacokinetic comparisons of puerarin, daidzin and the glucuronide metabolite of puerarin after administration of total flavonoid from Gegen alone and total flavonoid from Gegen combined with total saponin from Sanqi in rats under different physiological states

Liu, Xiaoming; Zhao, Yunli; Gao, Enze; Zhao, Xing; Liu, Zheng; Yu, Zhiguo

doi:10.1016/j.jchromb.2013.05.016

Cited by 9 publications

(7 citation statements)

References 19 publications

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“…Chinese herbal medicine contains a variety of effective active ingredients can effectively alleviate the symptoms of metabolic diseases, correct the disorder of glucose affect the efficacy of these drugs [17,18]. As for the Puerariae Lobatae Radix (PLR) extract, several studies have reported the pharmacokinetic behavior of its major components in human and health rats [19][20][21]. However, the comparative pharmacokinetic study of the main components in PLR extract in normal rats and rats with type 2 diabetes after oral administration of PLR extract is not available in the literature.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous determination of five isoflavones in rat plasma by LC‐MS/MS: Comparative pharmacokinetic characteristics of Puerariae lobatae radix in normal and type 2 diabetic rats

Zhang

Qiao

et al. 2019

J of Separation Science

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A rapid and sensitive liquid chromatography with tandem mass spectrometry method was developed and validated for simultaneous determination of puerarin, daidzin, daidzein, 3′‐hydroxy puerarin, and genistein in rat plasma after oral administration of Puerariae lobatae radix extract. The method of protein precipitation with acetonitrile was used for sample preparation. Chromatographic separation was achieved on a C18 column with the mobile phases of acetonitrile/water containing 0.1% formic acid. The analytes were detected by mass spectrometer with an electrospray ionization source operating in the negative ion mode. The linearity, precision, accuracy, dilution reliability, recovery, matrix effects, and stability of the method were within acceptable ranges. The developed method was successfully used to compare the pharmacokinetic characteristics of five analytes in normal and type 2 diabetics rats after oral administration of Puerariae lobatae radix extract. Several pharmacokinetic alterations were observed and this might be caused by the pathological state of type 2 diabetes.

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Section: Introductionmentioning

confidence: 99%

Simultaneous determination of five isoflavones in rat plasma by LC‐MS/MS: Comparative pharmacokinetic characteristics of Puerariae lobatae radix in normal and type 2 diabetic rats

Zhang

Qiao

et al. 2019

J of Separation Science

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“…In summary, M1 formation via first-pass metabolism had attenuated the oral bioavailability of CSA. Considering the importance of M1 in CSA bioavailability, the evident drug–drug interaction of M1 with other drugs interfering with UDP-glucuronosyltransferase activities requires much attention …”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetics of Cajaninstilbene Acid and Its Main Glucuronide Metabolite in Rats

Wang

Xue

Pan

et al. 2017

J. Agric. Food Chem.

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As a major active stilbene from the leaves of pigeon pea (Cajanus cajan), cajaninstilbene acid (CSA) exerts various pharmacological activities. The present study aimed to investigate the pharmacokinetics of CSA and one of its main metabolites (M1) to explore their fate in the body and provide a pharmacokinetic foundation for their in vivo biological activities and functional food or complementary medicine application. M1 was characterized as CSA-3-O-glucuronide using the multiple reaction monitoring-information-dependent acquisition-enhanced product ion technique. After oral and intravenous administration, plasma, urine, and bile were collected and analyzed to estimate pharmacokinetic properties of CSA and M1 and to explore the main excretion route. The oral bioavailability of CSA was estimated to be 44.36%. This study first reported that CSA is mainly metabolized to CSA-3-O-glucuronide via the first-pass effect to limit its oral bioavailability and excreted predominantly through the biliary route, while the enterohepatic circulation, extravascular distribution, and renal reabsorption characteristics of CSA might delay its elimination.

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“…The pharmacokinetic parameters after i.v. and oral administration at three doses (6.25, 12.5 and 25 mg/kg) were analyzed statistically using an independent sample t ‐test (Zhang et al ., ; Liu et al ., ). A difference was considered statistically significant when p was < 0.05.…”

Section: Methodsmentioning

confidence: 97%

Simultaneous determination of imperatorin and its metabolites in vitro and in vivo by a GC‐MS method: application to a bioavailability and protein binding ability study in rat plasma

Zhao

Peng

et al. 2013

Biomedical Chromatography

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In this study, a simple and sensitive gas chromatography-mass spectrometry method was developed for the study of bioavailability and protein binding and the metabolism of imperatorin in rat. The results showed that the pharmacokinetics of imperatorin after intravenous and oral administration in rats exhibited linear characteristics. The absolute bioavailability of imperatorin was calculated as ~3.85, ~33.51 and ~34.76% for 6.25, 12.5 and 25 mg/kg, respectively. The low bioavailability of imperatorin may be attributed to the poor absorption or extensive metabolism. The phase I metabolites of imperatorin formed in vitro by rat liver microsomes were studied, and two metabolites were isolated and identified as xanthotoxol and heraclenin. Following oral administration of imperatorin, one metabolite (heraclenin) was detected in rat plasma, and two potential metabolites (xanthotoxol and heraclenin) were detected in rat urine. However, none of potential metabolites was detected in rat feces and bile. The results showed that the metabolites of imperatorin were excreted by kidney, and heraclenin was associated with an active component. Demethylation and oxygenization were the main metabolic pathways. In vitro plasma protein binding of imperatorin was 90.1 and 92.6% for the spiked rat plasma concentrations of 1.0 and 50.0 µg/mL, respectively, indicating that imperatorin showed slow distribution into the intra- and extracellular space.

show abstract

Pharmacokinetic comparisons of puerarin, daidzin and the glucuronide metabolite of puerarin after administration of total flavonoid from Gegen alone and total flavonoid from Gegen combined with total saponin from Sanqi in rats under different physiological states

Cited by 9 publications

References 19 publications

Simultaneous determination of five isoflavones in rat plasma by LC‐MS/MS: Comparative pharmacokinetic characteristics of Puerariae lobatae radix in normal and type 2 diabetic rats

Simultaneous determination of five isoflavones in rat plasma by LC‐MS/MS: Comparative pharmacokinetic characteristics of Puerariae lobatae radix in normal and type 2 diabetic rats

Pharmacokinetics of Cajaninstilbene Acid and Its Main Glucuronide Metabolite in Rats

Simultaneous determination of imperatorin and its metabolites in vitro and in vivo by a GC‐MS method: application to a bioavailability and protein binding ability study in rat plasma

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