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  • Li, Rong  (5)
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  • 1
    Language: English
    In: Journal of Chromatography B, 2011, Vol.879(20), pp.1741-1747
    Description: Norcantharidin (NCTD), the demethylated analogue of cantharidin, inhibits the proliferation of a variety of human tumor cell lines, and appears to cause the least nephrotoxic and inflammatory side effects. Although NCTD has been used to treat human cancers in China for years, there is no report regarding its metabolism up to now. This is the first report to separate and identify the main metabolites of NCTD in vivo by GC–MS using TMS derivatives. Two hydrolyzed products and five phase I or phase II metabolites were found in rat by the chromatogram comparisons of the blank with incurred biological samples. Multiple stages of fragmentation patterns were used to confirm the metabolites characterizations. The established GC–MS method can also be applied to identifying unknown metabolites of the drugs containing hydroxyl or carbonyl groups in molecular structure.
    Keywords: Norcantharidin ; Metabolites ; Gc–MS ; Derivate ; Metabolism ; Anatomy & Physiology
    ISSN: 1570-0232
    E-ISSN: 1873-376X
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  • 2
    In: Biomedical Chromatography, November 2013, Vol.27(11), pp.1398-1405
    Description: Bergenin is the major component of and with many biological activities. Although bergenin has been used to treat human diseases in China for man years, there is no report regarding its metabolism. This is the first report to separate and identify the metabolites of bergenin . In the study, HPLC/Q‐TOF‐MS/MS was used to investigate the metabolites of bergenin by analyzing the rat body fluid and feces samples. Three metabolites of bergenin were finally identified by the TIC chromatograms, and the structures were also confirmed by their MS spectra. Copyright © 2013 John Wiley & Sons, Ltd.
    Keywords: Bergenin ; In Vivo ; Metabolites ; Hplc/Q‐Tof‐Ms/Ms
    ISSN: 0269-3879
    E-ISSN: 1099-0801
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  • 3
    In: Clinical Pharmacology in Drug Development, March 2018, Vol.7(3), pp.256-262
    Description: This study was designed to investigate the pharmacokinetics of an innovative film‐coated warfarin sodium tablet and to compare it with the marketed sugar‐coated warfarin sodium tablet in humans. A single‐dose, open‐label, randomized, two‐way crossover study was performed in 24 healthy Chinese male volunteers. They were administered 2.5 mg of innovative film‐coated warfarin sodium tablets or the marketed sugar‐coated warfarin sodium tablets. Blood samples were collected at different time points after dosing for investigation of the pharmacokinetics of warfarin in human plasma. A sensitive liquid chromatography mass spectrometry method was established to determine warfarin in plasma. Drug and Statistics 2.1.1 was applied to calculate the pharmacokinetics parameters. The main pharmacokinetic parameters for film‐coated and sugar‐coated warfarin were the following: t, 103.5 ± 18.8 and 105.8 ± 21.3 hours; T, 0.7 ± 0.5 and 1.3 ± 0.8 hours; C, 347.8 ± 74.8 and 322.9 ± 75.7 ng/mL; AUC, 16,024.2 ± 3713.9 and 15,586.6 ± 3477.0 ng·mL·h; AUC, 17,335.7 ± 4089.1 and 16,912.0 ± 3911.2 ng·mL·h, respectively. The human pharmacokinetics of film‐coated and sugar‐coated warfarin were slightly different. The oral absorption and bioavailability of innovative film‐coated warfarin were slightly higher than those of the sugar‐coated warfarin. This study is vital to clinical usage of warfarin not only because of the pharmacokinetic parameters of the 2 pharmaceutical dosage forms of warfarin but also to obtain data on the prevalence of CYP2C9 and VKORC1 genes and their influence on the concentration of warfarin.
    Keywords: Warfarin ; Pharmacokinetics ; Bioequivalence ; Gene Polymorphism ; Hplc‐Ms
    ISSN: 2160-763X
    E-ISSN: 2160-7648
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  • 4
    Language: English
    In: Bioscience trends, 12 September 2017, Vol.11(4), pp.475-482
    Description: Cyclosporin A (CyA) is an immunosuppressive agent widely used in clinical therapy. In the therapeutic process, the blood concentration of CyA should be monitored to avoid or prevent rejection and toxicity. The objectives of this study were to compare the correlation of liquid chromatography-tandem mass spectrometry (LC-MS/MS) and enzyme-multiplied immunoassay technique (EMIT) for the determination of the CyA concentration in human blood and to provide evidence for the rational usage of EMIT in clinical practice. Blood samples collected from 132 patients undergoing a liver or kidney transplant or patients with aplastic anemia at Qilu Hospital of Shandong University were tested using the two methods. The calibration curve was linear from 25-500 ng·mL for LC-MS/MS and from 50-450 ng·mL for EMIT. The inter- and intra-day RSDs were less than 15%. The CyA blood concentration according to EMIT was 3.5 ng·mL more than that according to LC-MS/MS. The 95% confidence interval was -10.0~16.9 ng·mL. The CyA blood concentration according to the two methods did not differ significantly (p 〉 0.05). LC-MS/MS and EMIT were suitable methods for determining the CyA blood concentration. The two methods were closely correlated (r = 0.969), but the CyA blood concentration according to EMIT was slightly higher than that according to LC-MS/MS. The clinical significance of this finding needs to be further evaluated.
    Keywords: Cyclosporin A ; LC-MS/MS ; Comparison ; Enzyme-Multiplied Immunoassay Technique ; Therapeutic Drug Monitoring ; Asian Continental Ancestry Group ; Enzyme Multiplied Immunoassay Technique ; Chromatography, Liquid -- Methods ; Cyclosporine -- Blood ; Tandem Mass Spectrometry -- Methods
    ISSN: 18817815
    E-ISSN: 1881-7823
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  • 5
    Language: English
    In: Current Pharmaceutical Analysis, 2018, Vol.14(6), p.541-546
    Description: Background and Objectives: To establish a simple and reproducible High Performance Liquid Chromatography (HPLC) method for the determination of mizoribine in human plasma using glipizide as Internal Standard (IS). Methods: The mizoribine in plasma was precipitated with 10% perchloric acid and separated on a Phenomenex Luna NH2 (250 mm × 4.6 mm, 5 µm) column with a mobile phase consisted of acetonitrile and 0.3% glacial acetic acid aqueous solution (48:52, V/V) at a flow rate of 1.0 mL/min. The detection wavelength was 280 nm and the column temperature was room temperature. Results: The assay exhibited a linear range of 0.05-10.0 µg/mL (r = 0.9992) and the lower limit of quantification was 0.05 µg/mL. The specificity, linearity, accuracy, precision and stability were in accordance to China Food and Drug Administration (CFDA) guidelines. Conclusion: Therefore, the method was successfully applied in the routine therapeutic mizoribine monitoring in Chinese kidney transplant patients after an oral administration of 100 mg (2 Bredinin® 50 mg tablets) or 150 mg (3 Bredinin® 50 mg tablets) mizoribine.
    Keywords: Mizoribine Hplc Therapeutic Drug Monitoring Clinical Application Validation.
    ISSN: 1573-4129
    E-ISSN: 1875-676X
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