Determination of scutellarin in rat plasma by high-performance liquid chromatography with ultraviolet detection

Zhong, Dafang; Yang, Binghua; Chen, Xiaoyan; Li, Ké; Xu, Jinghua

doi:10.1016/j.jchromb.2003.08.002

Cited by 34 publications

(25 citation statements)

References 22 publications

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“…The elution of scutellarin was achieved with an isocratic flow at a rate of 0.3 mL/min. Plasma samples collected were prepared before liquid chromatographic analysis (25). Drug extraction and protein precipitation of the samples were done by mixing 100 μL of plasma sample, 20 μL of internal standard working solution of baicalin (5 μg/mL), 1.0 mL of ethyl acetate, and 25 μL of 50% phosphoric acid, which was vortex mixed for 10 min followed by centrifugation at 3,000×g for 10 min.…”

Section: Plasma Samplesmentioning

confidence: 99%

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

et al. 2014

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Abstract. Breviscapine is used in the treatment of ischemic cerebrovascular diseases, but it has a low bioavailability in the brain due to its poor physicochemical properties and the activity of P-glycoprotein efflux pumps located at the blood-brain barrier. In the present study, breviscapine-loaded solid lipid nanoparticles (SLN) coated with polyethylene glycol (PEG) derivatives were formulated and evaluated for their ability to enhance brain bioavailability. The SLNs were either coated with polyethylene glycol (40) (PEG-40) stearate alone (Bre-GBSLN-PS) or a mixture of PEG-40 stearate and 1,2-distearoyl-snglycero-3-phosphoethanolamine-N-PEG2000 (DSPE-PEG 2000 ) (Bre-GBSLN-PS-DSPE) and were characterized both in vitro and in vivo. The mean particle size, polydispersity index, and entrapment efficiency for Bre-GBSLN-PS and Bre-GBSLN-PS-DSPE were 21.60±0.10 and 22.60±0.70 nm, 0.27±0.01 and 0.26 ±0.04, and 46.89±0.73% and 47.62±1.86%, respectively. The brain pharmacokinetic parameters revealed that the brain bioavailability of breviscapine from the Bre-GBSLN-PS and Bre-GBSLN-PS-DSPE was significantly enhanced (p<0.01) with the area under concentration-time curve (AUC) of 1.59±0.39 and 1.42±0.58 μg h/mL of breviscapine, respectively, in comparison to 0.11±0.02 μg h/mL from the commercial breviscapine injection. The ratios of the brain AUC for scutellarin in comparison with the plasma scutellarin AUC for commercial breviscapine injection, Bre-GBSLN-PS, and Bre-GBSLN-PS-DSPE were 0.66%, 2.82%, and 4.51%, respectively. These results showed that though both SLN formulations increased brain uptake of breviscapine, Bre-GBSLN-PS-DSPE which was coated with a binary combination of PEG-40 stearate and DSPE-PEG 2000 had a better brain bioavailability than Bre-GBSLN-PS. Thus, the coating of SLNs with the appropriate PEG derivative combination could improve brain bioavailability of breviscapine and can be a promising tool for brain drug delivery.

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Section: Plasma Samplesmentioning

confidence: 99%

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

et al. 2014

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“…In literature, it has been reported that the bioavailability of S-7-G was also low in rats (Zhong et al, 2003;Huang et al, 2005) and dogs (Ge et al, 2003). In a preliminary study, the plasma concentration of S-6-G was also found to be high in rats after an oral dose of S-7-G.…”

Section: Effectsmentioning

confidence: 99%

Absorption and Disposition of Scutellarin in Rats: A Pharmacokinetic Explanation for the High Exposure of Its Isomeric Metabolite

Gao

Chen²,

Zhong³

2011

Drug Metab Dispos

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ABSTRACT:Scutellarin or scutellarein-7-O-glucuronide (S-7-G) is a flavonoid used in the treatment of cardiovascular diseases. After oral administration to humans, S-7-G can hardly be detected, whereas its isomeric metabolite [scutellarein-6-O-glucuronide (S-6-G)] dominates in plasma. A preliminary study in rats also revealed a low bioavailability of S-7-G, as well as a high plasma concentration of S-6-G. Therefore, the present study tried to explore the possible causes of the unusual pharmacokinetics of scutellarin in humans through investigating the absorption and disposition of S-7-G in rats. After oral administration to rats, S-7-G was largely hydrolyzed in the intestinal tract and was absorbed as aglycone. While passing through the intestinal wall, aglycone was extensively glucuronidated into S-7-G and S-6-G (approximately 20:1), which subsequently entered the mesenteric blood (approximately 15:1). However, because S-7-G exhibited more rapid uptake in hepatocytes, was glucuronidated at a 2.7-fold higher rate in the liver, and was excreted in greater amounts through bile and urine than S-6-G, the S-7-G/S-6-G ratio eventually declined to approximately 1.5:1 in the systemic circulation. Findings revealed that S-7-G cannot be absorbed directly; S-7-G and S-6-G in the body were mostly generated from aglycone in the intestinal wall; a larger amount of S-7-G than S-6-G entered the mesenteric blood at the absorption stage, but the gap between them shrank quickly mainly because of the higher hepatic first-pass elimination of S-7-G. These findings in rats are of great value as reference for further study to accurately interpret the pharmacokinetics of S-7-G in humans.

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“…In order to evaluate scientifically the pharmacokinetics and bioequivalence of scutellarin formulations, it is essential to develop a sensitive and reliable analytical assay to determine the concentration of scutellarin in human plasma. Some HPLC methods have been described for the detection of scutellarin in animals given a high oral dosage of scutellarin or injected intravenously (Zhong et al, 2003;Ge et al, 2003;Hao et al, 2005;Huang et al, 2006) and the lower limits of quantification of these assays were mostly above 20 ng/mL. However, the concentration of archetypal scutellarin in human plasma was found to be very low (C max = 5 ng/mL) after oral administration of a clinical dosage (80 mg).…”

Section: Introductionmentioning

confidence: 99%

Retracted: Determination of scutellarin isomer, a predominant metabolite of scutellarin, in human plasma by HPLC/tandem mass spectrometry and its application to a pharmacokinetic study in Chinese healthy volunteers

Xia¹,

Xiong²,

Wang³

2007

Biomedical Chromatography

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A liquid chromatography/tandem mass spectrometric (LC-MS/MS) method was developed to determine scutellarin isomer, a predominant metabolite of scutellarin, in human plasma for the pharmacokinetic study of scutellarin in Chinese healthy volunteers. Samples were acidified with formic acid and extracted with ethyl acetate. Chromatographic separation was achieved on a C 18 column with the mobile phase of water (containing 0.5% formic acid) and methanol (33:67, v/v). The analytes were detected using an electrospray positive ionization mass spectrometry in the selected reaction monitoring (SRM) mode. The calibration curve was linear over the range of 0.5-200.0 ng/mL and the lower limit of quantification was 0.5 ng/mL. The average extraction recoveries were 81.1 ± 7.5, 84.5 ± 6.9 and 83.4 ± 5.8% at concentrations of 2.0, 20.0 and 100.0 ng/mL, respectively. The intra-and inter-day precisions at three different concentrations were all less than 7.3% and accuracies were within the range 98.9-106.7%. The method described was precise, accurate and successfully applied to evaluate the pharmacokinetics and bioequivalence of scutellarin in 20 Chinese healthy volunteers. The results showed that the main pharmacokinetic parameters between scutellarin guttate pills and tablets had no statistically significant difference and the two formulations were bioequivalent.

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Determination of scutellarin in rat plasma by high-performance liquid chromatography with ultraviolet detection

Cited by 34 publications

References 22 publications

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

Absorption and Disposition of Scutellarin in Rats: A Pharmacokinetic Explanation for the High Exposure of Its Isomeric Metabolite

Retracted: Determination of scutellarin isomer, a predominant metabolite of scutellarin, in human plasma by HPLC/tandem mass spectrometry and its application to a pharmacokinetic study in Chinese healthy volunteers

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