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  • 1
    In: Journal of Bioequivalence & Bioavailability, 2013, Vol.04(07)
    ISSN: Journal of Bioequivalence & Bioavailability
    E-ISSN: 09750851
    Source: CrossRef
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  • 2
    Language: English
    In: Drugs in R & D, 2010, Vol.10(2), pp.83-90
    Description: Background: Tribendimidine is a new anthelmintic agent synthesized by Chinese scientists. It is a broad spectrum agent with high activity against parasites. However, its disposition and metabolism remain unknown. To investigate the metabolism, disposition, and metabolites of tribendimidine in healthy human volunteers. Twelve healthy Chinese volunteers were chosen after clinical assessment of health status and laboratory tests. They received single oral doses of tribendimidine 400mg enteric-coated tablets. Blood and urine samples were collected at scheduled timepoints. Samples were qualitatively and quantitatively analyzed by liquid chromatography-mass spectrometric (LC-MS) and high performance liquid chromatography (HPLC) methods, respectively. Tribendimidine was rapidly and completely broken down to -(1-dimethylamino ethylimino) aniline (dADT) and terephthalaldehyde (TPAL). Furthermore, dADT was partially transformed to acetylated dADT, and TPAL completely transformed to terephalic acid (TPAC). The main pharmacokinetic parameters (± SD) of dADT were as follows: elimination half life (t) 4.74 ± 1.80 h; elimination rate constant (K) 0.16 ± 0.06 h; apparent volume of distribution (Vd/F) 12.23 ± 8.69L • kg; apparent total clearance of the drug from plasma (CL/F) 1.63 ± 0.58L • h • kg; area under the plasma concentration-time curve (AUC) from time 0 to time 24 hours (AUC) 4.29 ± 1.88 μg • mL • h; AUC from time zero to infinity (AUC) 4.45 ± 1.81 μg • mL • h; maximum plasma drug concentration (C) 0.64 ± 0.27 μg • mL; and time to C (t) 4.20 ± 0.71 h. A total of 35.28% dADT and 28.50% TPAC were excreted through the urine within 24 hours after tribendimidine administration. These results reveal the disposition, metabolism, and main metabolites of tribendimidine in healthy Chinese volunteers.
    Keywords: Liquid Chromatography -- Usage ; Anthelmintics -- Structure ; Anthelmintics -- Usage ; Anthelmintics -- Health Aspects;
    ISSN: 1174-5886
    E-ISSN: 1179-6901
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  • 3
    Language: English
    In: Gene, 10 May 2012, Vol.499(1), pp.76-80
    Description: An effective DNA marker in authentication of the family Araliaceae was screened out of the five DNA regions ( , , ITS2, and ). In the present study, 1113 sequences of 276 species from 23 genera (Araliaceae) were collected from DNA sequencing and GenBank, in which 16 specimens were from 5 provinces in China and Japan. All of the sequences were assessed in the success rates of PCR amplifications, intra- and inter-specific divergence, DNA barcoding gaps and efficiency of identification. Compared with other markers, ITS2 showed superiority in species discrimination with an accurate identification of 85.23% and 97.29% at the species and genus levels, respectively, in plant samples from the 589 sequences derived from Araliaceae. Consequently, as one of the most popular phylogenetic markers, our study indicated that ITS2 was a powerful barcode for Araliaceae identification. ►ITS2 had a high authentication success rate of Araliaceae species. ►ITS2 provided a great efficiency of PCR amplification. ►ITS2 exhibited significantly high levels of inter-specific discriminatory ability. ►ITS2 was more suitable than other barcodes in Araliaceae species discrimination.
    Keywords: Araliaceae ; DNA Barcoding ; Its2 ; Engineering ; Biology ; Anatomy & Physiology
    ISSN: 0378-1119
    E-ISSN: 1879-0038
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  • 4
    In: Biomedical Chromatography, March 2014, Vol.28(3), pp.348-353
    Description: Glucuronidation plays critical role in the elimination of bergenin; however the metabolic mechanism of UDP‐glucuronosyltransferases (UGTs) in the process remains to be investigated. In this study, the kinetics of bergenin glucuronidation by pooled human liver microsomes (HLMs) and 12 recombinat UGT isozymes were investigated. The glucuronidation of bergenin can be shown in HLMs with a value of 231.62 ± 14.08 µ and a value of 2.17 ± 0.21 nmol/min/(mg protein). Among the 12 human UGTs investigated, UGT1A1 was identified as the major isoform catalyzing the glucuronidation of bergenin [ value of 200.37 ± 26.73 µ and value of 1.88 ± 0.26 nmol/min/(mg protein)]. The bergenin glucuronosyltransferase activities in HLMs and UGT1A1 were inhibited by phenylbutazone, estradiol and bilirubin. The results demonstrate that bergenin glucuronidation in HLMs is specifically catalyzed by UGT1A1. Copyright © 2013 John Wiley & Sons, Ltd.
    Keywords: Bergenin ; Udp‐Glucuronosyltransferases ; Human Liver Microsomes ; Ugt1a1 ; In Vitro
    ISSN: 0269-3879
    E-ISSN: 1099-0801
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  • 5
    Language: English
    In: International journal of clinical pharmacology and therapeutics, August 2018, Vol.56(8), pp.387-392
    Description: Tetramethylpyrazine, isolated from Ligusticum wallichii Franch., is widely used for the treatment of cerebrovascular and cardiovascular diseases in China. To assess and compare the pharmacokinetic characteristics and bioequivalence of two tetramethylpyrazine phosphate (TMPP) tablets in healthy Chinese male subjects. 20 healthy male subjects were randomly divided into two groups according to a two-period crossover design test. A single oral dose of 200 mg test or reference tablets was given with a 7-day washout period under fasting conditions. Blood samples were taken at scheduled time points, and the concentration of TMPP was measured by LC-MS. Drug And Statistical Software-Version 2.0 was used to calculate the pharmacokinetic parameters and assess bioequivalence of the two formulations. 20 subjects were enrolled in the study, and none dropped out. The main pharmacokinetic parameters of test and reference formulations were as follows: T1/2 was (1.79 ± 0.82) hours and (1.64 ± 0.52) hours, tmax was (0.76 ± 0.37) hours and (0.94 ± 0.44) hours, Cmax was (961.14 ± 309.64) ng/mL and (1,059.09 ± 350.69) ng/mL, AUC0-12h was (1,744.69 ± 643.49) ng×h/mL and (1,726.32 ± 494.11) ng×h/mL, AUC0-∞ was (1,756.95 ± 643.63) ng×h/mL and (1,740.16 ± 504.89) ng×h/mL, respectively. The relative bioavailability of TMPP tablets was 102.4 ± 26.0%, and no serious adverse events were reported. This single-dose study in healthy Chinese male fasted subjects showed that the TMPP test and reference tablets were bioequivalent.
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    Keywords: Plant Extracts -- Pharmacokinetics ; Pyrazines -- Pharmacokinetics
    ISSN: 0946-1965
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  • 6
    Language: English
    In: Biomedical Chromatography, Oct, 2012, Vol.26(10), p.1176(7)
    Description: Byline: Dujuan Zhang, Yanni Teng, Keguang Chen, Sha Liu, Chunmin Wei, Benjie Wang, Guiyan Yuan, Rui Zhang, Xiaoyan Liu, Ruichen Guo ABSTRACT A sensitive and selective liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) was developed and validated for the determination of salbutamol in human plasma and urine, and successfully applied to the pharmacokinetic study of salbutamol in Chinese healthy volunteers after inhalation of salbutamol sulfate aerosol. Salbutamol and the internal standard (IS) acetaminophen in plasma and urine were extracted with ethyl acetate, separated on a C.sub.18 reversed-phase column, eluted with mobile phase of acetonitrile-ammonium acetate (5m m; 30:70, v/v), ionized by positive ion pneumatically assisted electrospray and detected in the multi-reaction monitoring mode using precursoraproduct ions of m/z 240.2a148.1 for salbutamol and 152a110 for the IS. The lower limits of quantitation of salbutamol in human plasma and urine by this method were 0.02 and 1ng/mL, respectively. The specificity, matrix effect, recovery, sensitivity, linearity, accuracy, precision and several stabilities were validated for salbutamol in human plasma and urine. In conclusion, the validation results showed that this method is robust, specific and sensitive, and can successfully fulfill the requirement of clinical pharmacokinetic study of salbutamol in healthy Chinese volunteers. Copyright A[c] 2011 John Wiley & Sons, Ltd. Correspondence: Ruichen Guo, Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, 107 West Wenhua Road Jinan 250012, People's Republic of China. E-mail: grc7636@126.com
    Keywords: Mass Spectrometry ; Antiasthmatic Agents ; Albuterol ; Esters ; Liquid Chromatography
    ISSN: 0269-3879
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  • 7
    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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  • 8
    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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  • 9
    Language: English
    In: Journal of Ethnopharmacology, 07 May 2012, Vol.141(1), pp.242-249
    Description: Medicinal vines listed in Chinese pharmacopoeia possess important medicinal efficacy in traditional Chinese medicines. The ITS2 region, which has several characteristics that make it a valuable DNA barcode, was studied to discriminate the stems of medicinal vines to confirm their identities and ensure their safe application in pharmaceuticals by using complementary discrimination methods. Complementary discrimination methods were performed on two datasets, including 393 samples of 170 species from 22 genera 13 families, which belonged to medicinal vines and their adulterants. Based on the primary ITS2 sequences, three main discrimination methods (phylogenetic tree, the nearest distance, and BLAST 1) were adopted to identify species. Moreover, we applied both two-dimensional (2-D) and three-dimensional (3-D) structures of ITS2 to differentiate species. ITS2 performed well, with over 95.0% of species and 100% of genera being correctly differentiated for the two datasets. All results showed that the ITS2 region unveiled a remarkable ability to identify closely related species within different families and genera. Our findings supported that the ITS2 region was an efficient marker for authentication of medicinal vines.
    Keywords: DNA Barcoding ; Medicinal Vines ; Its2 ; 3-D Structure ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0378-8741
    E-ISSN: 1872-7573
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  • 10
    Language: English
    In: Bioscience trends, 2018, Vol.12(2), pp.201-207
    Description: An economical, rapid, and sensitive method of gas chromatography-mass spectrometry (GC-MS) was developed and validated to determine the presence of six pesticides (dichlorvos, acetochlor, atrazine, chlorpyrifos, α-endosulfan, and β-endosulfan) in human plasma. The pesticides were extracted with acetonitrile and concentrated using anhydrous sodium sulfate. Then, the target compounds were analyzed and quantified with GC-MS using borneol as an internal standard. Separation was performed on a HP-5MS capillary column (30 m × 0.25 mm × 0.25 µm) with temperature programming. Detection was accomplished under electro-spray ionization (ESI) in selected ion monitoring (SIM) mode. Under optimized conditions, satisfactory linear ranges of 0.05-10 μg/mL were obtained for all of the analyzed pesticides. The linear correlation coefficients were greater than 0.99. The average recovery was between 86.8 and 106.5%. The inter- and intra-day precision ranged from 1.7-14.5% and 4.2-13.8%, respectively. Dichlorvos was unstable in plasma both at room temperature and when frozen. The other five pesticides were stable after storage at - 20°C for 17 days and two freeze-thaw cycles. Thirty-five plasma samples from 15 patients with acute self-poisoning were analyzed using this method. Dichlorvos was found in 13 plasma samples with a mean concentration of 0.289 μg/mL, and atrazine was found in 6 with a mean concentration of 0.261 μg/mL. Acetochlor was found in one plasma sample (0.153 μg/mL). This method is simple, reliable and cost-effective. It takes little time and does not waste solvents, and it can be used to routinely detect six pesticides in patients with acute poisoning.
    Keywords: Gas Chromatography-Mass Spectrometry ; Determination ; Pesticides ; Plasma ; Gas Chromatography-Mass Spectrometry -- Methods ; Pesticides -- Blood ; Poisoning -- Blood
    ISSN: 18817815
    E-ISSN: 1881-7823
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