A sensitive LC–MS/MS method for simultaneous determination of six flavonoids in rat plasma: Application to a pharmacokinetic study of total flavonoids from mulberry leaves

He, Jun; Feng, Yi; Ouyang, Hongwei; Yu, Bin; Chang, Yan‐xu; Pan, Guixiang; Dong, Gai-ying; Wang, Tao; Gao, Xiumei

doi:10.1016/j.jpba.2013.06.019

Cited by 83 publications

(47 citation statements)

References 27 publications

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“…The gut microbiota has also been thought to hydrolyze glucosides (Bokkenheuser et al, 1987). It was reported that rutin was not absorbed until it was hydrolyzed by gut microbiota, and the absorption peak of its metabolites occurred at 7 hours (He et al, 2013). However, we found that, after oral administration, CG and its metabolites were rapidly absorbed, with an absorption peak at 45 minutes (Fig.…”

Section: Discussionmentioning

confidence: 68%

SGLT-1 Transport and Deglycosylation inside Intestinal Cells Are Key Steps in the Absorption and Disposition of Calycosin-7-O- -D-Glucoside in Rats

Shi

Zheng

et al. 2015

Drug Metabolism and Disposition

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Hydrolysis by lactase-phloridzin hydrolase (LPH) is the first and critical step in the absorption of isoflavonoid glucosides. However, the absorption characteristics of calycosin-7-O-b-D-glucoside (CG) slightly differ from other isoflavonoid glucosides. In this study, we used the rat intestinal perfusion model and performed pharmacokinetic studies and in vitro experiments to determine the factors influencing CG absorption and disposition. After oral administration of isoflavonoid glucosides, LPH was found to play minimal or no role on the hydrolysis of CG, in contrast to that of daidzin. CG was mainly transported into the small intestinal cells by sodium-dependent glucose transporter 1 (SGLT-1) as intact. This pathway could be the main mechanism underlying the high permeability of CG in the small intestine. CG was likely to be hydrolyzed in enterocytes to its aglycone calycosin by broad-specific b-glucuronides (BSbG) and glucocerebrosidase or rapidly metabolized. Calycosin was also rapidly and extensively metabolized to 39-glucuronide in the enterocytes and liver, and the glucuronidation rates of calycosin and CG were much higher in the former. The metabolites were also transported into lumen by breast cancer resistance protein and multidrug resistance-associated protein 2. In conclusion, the enterocytes could be an important site for CG absorption, deglycosylation, and metabolism in rats. This study could contribute to the theoretical foundation and mechanism of absorption and disposition of flavonoid compounds.

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Section: Discussionmentioning

confidence: 68%

SGLT-1 Transport and Deglycosylation inside Intestinal Cells Are Key Steps in the Absorption and Disposition of Calycosin-7-O- -D-Glucoside in Rats

Shi

Zheng

et al. 2015

Drug Metabolism and Disposition

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“…To our knowledge, no published data are available related to the in vivo effects of NADES as administration tools for bioactive constituents. These eutectics, prepared using different starting materials, can be divided into five groups, the first is based on urea (1-4), the second on polyalcohols and sugars (5-6), the third on organic acid and sugars (7)(8)(9), the fourth on organic acid and amino acid (10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27), and the fifth group was prepared using choline chloride, sugars and amino acid (28)(29)(30). Our results show the ability of various NADES to dissolve rutin.…”

Section: Rutin Solubility In the Different Prepared Nadesmentioning

confidence: 99%

“…Considering the solubility properties nine NADES (2,3,4,10,11,17,28,29,30) were able to solubilize half of the rutin compared to the best solvent (ethanol). On the other hand, eutectic 11 and 28 (proline/glutamic acid 2:1 and proline/choline chloride 1:2 respectively) resulted to be the most promising NADES presenting rutin solubilization higher than ethanol and methanol.…”

Section: Pharmacokinetics In Mice Of Proline-glutamic Acid Rutin Eutementioning

confidence: 99%

“…In a methodological paper describing an HPLC-MS/MS method for rutin quantification in rat plasma, preliminary pharmacokinetic data were published showing the maximum concentration (1659 ng/mL) 5 min after 2.5 mg/kg sublingual vein administration of rutin [28]. He et al reported that the three flavonoid glycosides (rutin, astragalin and isoquercitin) were rapidly absorbed and eliminated from rat plasma after oral administration of total flavonoids from mulberry leaves [30].…”

Section: Introductionmentioning

confidence: 99%

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Natural Deep Eutectic Solvents (NADES) as a Tool for Bioavailability Improvement: Pharmacokinetics of Rutin Dissolved in Proline/Glycine after Oral Administration in Rats: Possible Application in Nutraceuticals

et al. 2016

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There is a need for innovation in plant-derived pharmaceuticals, food supplements and nutraceutical products regarding the use of more eco-sustainable solvents for their extraction. Furthermore, the poor oral bioavailability of several phytochemicals with health promoting effects stimulates the research in the field of pharmaceutical formulations. Natural Deep Eutectic Solvents (NADES) are formed by natural compounds, and can be considered as future solvents being especially useful for the preparation of nutraceuticals and food-grade extracts. In this paper various NADES were prepared using sugars, aminoacids and organic acids. Rutin (quercetin-3-O-α-L-rhamnopyranosyl-(1→6))-β-D-glucopyranose) was used as a model compound to study NADES. Moreover, the effect of various eutectic mixtures on rutin's water solubility was studied. Proline/glutamic acid (2:1) and proline/choline chloride (1:1) mixtures have a solubility comparable to ethanol. The proline/glutamic acid (2:1) eutectic containing rutin was used in a pharmacokinetic study in Balb/c mice while bioavailability was compared to oral dosing of water suspension. Plasmatic levels of rutin were measured by HPLC-MS/MS showing increased levels and longer period of rutin permanence in plasma of NADES treated animals. This paper reports the possible use of non-toxic NADES for pharmaceutical and nutraceutical preparations.

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“…The system (ALS 1290 series; USA) consist of binary pump, vacuum degasser and auto-sampler system connected electro spray ionization (ESI) source). Samples obtained from Franz diffusion cell were injected, using acetonitrile and 0.1% formic acid in water (50:50, v/v) pumped at a constant flow of 0.3 ml/min (Duan et al, 2011;He et al, 2013). The standard graphs for the pure components (Quercetin, Kaempferol and Isorhamnetine) were made within the range of 2.5 -15mg/ml for each component.…”

Section: Release Kinetics: Lc-ms Methodsmentioning

confidence: 99%

Development, characterization and cytotoxicity evaluation of Gingko biloba extract (EGB761) loaded microemulsion for intra-nasal application

Singh¹,

Singh²,

Rachana³

2017

J App Pharm Sci

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Background: Ginkgo biloba is therapeutically important fossil species with extended benefits against CNS disorders as; it contains various potential constituents which are known for their specific actions. In spite of this fact its medicinal usage are limited due to the limited absorption, rapid elimination, vigorous biotransformation and low bioavailability of its therapeutic components. Objective: The present study is an attempt to develop a microemulsion system of standardized extract of Ginkgo biloba (EGB761) for intranasal application. Material and methods: It is developed by water titration method using Isopropyl Myristate (oil), Tween 80 (surfactant) and Ethanol (co surfactant). Results: EGB761 loaded microemulsions were developed and characterized. The optimized formulation showed particle size of 259.8 ± 6.3 nm, PDI score of 0.186 ± 0.092 and zeta potential as -9.87 ± 2.23 mv. Also, TEM images showed size range from 84 -260 nm with smooth and spherical morphology. In vitro phyto-constituents release through isolated nasal mucosa showed release pattern of zero order kinetics with sustained release (up to 16 hours). Moreover, cytotoxicity evaluation (RPMI2650 cell lines) didn't show cytotoxicity for both GBME (99.3 % ± 2.28 % and 98.17 % ± 1.86%) and plain EGB761 extract (95.3 % ± 2.1 and 91.7 % ± 1.07) with different time periods (3 and 12 hours). Conclusion: Therefore, it has been concluded from the results that, EGB761 based microemulsion (GBME) is developed with particle size range between 84 -260 nm, having zero order release kinetics. GBME is found to be safe on RPMI2650 cell line and can be further, investigated in in vivo system.

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A sensitive LC–MS/MS method for simultaneous determination of six flavonoids in rat plasma: Application to a pharmacokinetic study of total flavonoids from mulberry leaves

Cited by 83 publications

References 27 publications

SGLT-1 Transport and Deglycosylation inside Intestinal Cells Are Key Steps in the Absorption and Disposition of Calycosin-7-O- -D-Glucoside in Rats

SGLT-1 Transport and Deglycosylation inside Intestinal Cells Are Key Steps in the Absorption and Disposition of Calycosin-7-O- -D-Glucoside in Rats

Natural Deep Eutectic Solvents (NADES) as a Tool for Bioavailability Improvement: Pharmacokinetics of Rutin Dissolved in Proline/Glycine after Oral Administration in Rats: Possible Application in Nutraceuticals

Development, characterization and cytotoxicity evaluation of Gingko biloba extract (EGB761) loaded microemulsion for intra-nasal application

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