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  1. Article ; Online: Effect of apatinib on the pharmacokinetics of tramadol and O-desmethyltramadol in rats.

    Bao, Su-Su / Tang, Peng-Fei / Gao, Nan-Yong / Xiao, Zhong-Xiang / Qian, Jian-Chang / Zheng, Long / Hu, Guo-Xin / Xu, Huan-Hai

    PeerJ

    2023  Volume 11, Page(s) e16051

    Abstract: Since the combination of anticancer drugs and opioids is very common, apatinib and tramadol are likely to be used in combination clinically. This study evaluated the effects of apatinib on the pharmacokinetics of tramadol and its main metabolite O- ... ...

    Abstract Since the combination of anticancer drugs and opioids is very common, apatinib and tramadol are likely to be used in combination clinically. This study evaluated the effects of apatinib on the pharmacokinetics of tramadol and its main metabolite O-desmethyltramadol in Sprague-Dawley (SD) rats and the inhibitory effects of apatinib on tramadol in rat liver microsomes (RLMs), human liver microsomes (HLMs) and recombinant human CYP2D6.1. The samples were determined by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). The
    MeSH term(s) Humans ; Rats ; Animals ; Tramadol/pharmacology ; Chromatography, Liquid ; Cytochrome P-450 CYP2D6 ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry ; Microsomes, Liver
    Chemical Substances O-demethyltramadol (2WA8F50C3F) ; Tramadol (39J1LGJ30J) ; apatinib (5S371K6132) ; Cytochrome P-450 CYP2D6 (EC 1.14.14.1)
    Language English
    Publishing date 2023-09-11
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2703241-3
    ISSN 2167-8359 ; 2167-8359
    ISSN (online) 2167-8359
    ISSN 2167-8359
    DOI 10.7717/peerj.16051
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Development and Validation of a UHPLC-MS/MS Method for Quantitation of Almonertinib in Rat Plasma: Application to an

    Tang, Peng-Fei / Bao, Su-Su / Gao, Nan-Yong / Shao, Chuan-Feng / Xie, Wei-Fei / Wu, Xue-Meng / Zhao, Le-Ping / Xiao, Zhong-Xiang

    Frontiers in pharmacology

    2022  Volume 13, Page(s) 960311

    Abstract: Almonertinib was approved for the first-line treatment of advanced NSCLC patients with EGFR-TKI-sensitive genetic mutations by National Medical Products Administration (NMPA) in 2021.The purpose of this study was to establish and validate a fast, ... ...

    Abstract Almonertinib was approved for the first-line treatment of advanced NSCLC patients with EGFR-TKI-sensitive genetic mutations by National Medical Products Administration (NMPA) in 2021.The purpose of this study was to establish and validate a fast, accurate, stable and facile ultra-performance liquid chromatography-tandem mass spectrometry method for the quantification of almonertinib in rat plasma, it was employed to explore the effect of Paxlovid on the pharmacokinetics of almonertinib in rats. Zanubrutinib was used as an internal standard (IS), and the plasma samples were prepared by the protein precipitation method using acetonitrile. Chromatographic separation was carried out on a Shimadzu LC-20AT ultra-performance liquid chromatography system using a Shim-pack velox C18 (2.1× 50 mm, 2.7 μM) column. The mobile phase consisted of methanol and 0.1% formic acid-water. Mass spectrum analysis was executed using Shimadzu 8040 Triple quadrupole mass spectrometry. The precursor and product ions of the analyte and internal standard were detected in multiple reaction monitoring (MRM) mode. The typical fragment ions were
    Language English
    Publishing date 2022-07-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2022.960311
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Effect of flavonoids and CYP3A4 variants on midostaurin metabolism.

    Xu, Ren-Ai / Li, Qing-Qing / Gao, Nan-Yong / Wang, Jing / Li, Xin-Yue / Ye, Feng / Ni, Jin-Huan / Hu, Guo-Xin / Qian, Jian-Chang

    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association

    2023  Volume 174, Page(s) 113669

    Abstract: The objective of this study was to determine the effect of flavonoids on midostaurin disposition considering co-administration and metabolic enzyme gene polymorphism. Enzymatic incubation assays were performed in vitro, while in vivo experiments were ... ...

    Abstract The objective of this study was to determine the effect of flavonoids on midostaurin disposition considering co-administration and metabolic enzyme gene polymorphism. Enzymatic incubation assays were performed in vitro, while in vivo experiments were conducted in Sprague-Dawley rats. The analytes were determined via UPLC-MS/MS. We found that myricetin was the most potent among the investigated 10 flavonoids in suppressing the metabolism of midostaurin, with an IC
    MeSH term(s) Rats ; Humans ; Animals ; Cytochrome P-450 CYP3A/metabolism ; Rats, Sprague-Dawley ; Chromatography, Liquid ; Tandem Mass Spectrometry ; Flavonoids/pharmacology
    Chemical Substances midostaurin (ID912S5VON) ; Cytochrome P-450 CYP3A (EC 1.14.14.1) ; Flavonoids ; CYP3A4 protein, human (EC 1.14.14.55)
    Language English
    Publishing date 2023-02-17
    Publishing country England
    Document type Journal Article
    ZDB-ID 782617-5
    ISSN 1873-6351 ; 0278-6915
    ISSN (online) 1873-6351
    ISSN 0278-6915
    DOI 10.1016/j.fct.2023.113669
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Inhibitory effect of resveratrol on the pharmacokinetics of ticagrelor in vivo and in vitro.

    Wang, Peng / Hu, Xiao-Xia / Li, Ying-Hui / Gao, Nan-Yong / Chen, Guo-Quan / Chen, Jia-le

    Canadian journal of physiology and pharmacology

    2021  Volume 99, Issue 8, Page(s) 821–826

    Abstract: This study was to evaluate the effect of resveratrol on the pharmacokinetics of ticagrelor in rats and the metabolism of ticagrelor in human cytochrome P450 (CYP) 3A4 (CYP3A4) and liver microsomes. Eighteen Sprague-Dawley rats were randomly divided into ... ...

    Abstract This study was to evaluate the effect of resveratrol on the pharmacokinetics of ticagrelor in rats and the metabolism of ticagrelor in human cytochrome P450 (CYP) 3A4 (CYP3A4) and liver microsomes. Eighteen Sprague-Dawley rats were randomly divided into three groups: group A (control group), group B (50 mg/kg resveratrol), and group C (150 mg/kg resveratrol). After 30 min administration of resveratrol, a single dose of ticagrelor (18 mg/kg) was administered orally. The in vitro experiment was performed to examine the influence of resveratrol on ticagrelor metabolism in CYP3A4*1, human, and rat liver microsomes. Serial biological samples were assayed by validated ultra high-performance liquid chromatography - tandem mass spectrometer methods. For the in vivo study, the area under the concentration-time curve and mean peak plasma concentrations of ticagrelor in group B and C appeared to be significantly higher than the control group, while volume of distribution in terminal phase and apparent clearance of ticagrelor in group B and C were significantly decreased. For the in vitro study, resveratrol exhibited an inhibitory effect on CYP3A4*1, human and rat liver microsomes. The half-maximal inhibitory concentration values of resveratrol were 56.75 μM, 69.07 μM, and 14.22 μM, respectively. Our results indicated that resveratrol had an inhibitory effect on the metabolism of ticagrelor in vitro and in vivo. Further research should focus on the clinical combination of resveratrol with ticagrelor, and ticagrelor plasma concentration should be monitored to avoid the occurrence of adverse reaction.
    MeSH term(s) Animals ; Microsomes, Liver ; Rats ; Ticagrelor
    Chemical Substances Ticagrelor (GLH0314RVC)
    Language English
    Publishing date 2021-01-05
    Publishing country Canada
    Document type Journal Article
    ZDB-ID 127527-6
    ISSN 1205-7541 ; 0008-4212
    ISSN (online) 1205-7541
    ISSN 0008-4212
    DOI 10.1139/cjpp-2020-0512
    Database MEDical Literature Analysis and Retrieval System OnLINE

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