当前位置： SCI文献检索 > ACTA PHARMACOLOGICA SINICA期刊下所有文献 > Pharmacokinetics of enantiomers of trans-tramadol and its active metabolite, trans-O-demethyltramadol, in human subjects.

Pharmacokinetics of enantiomers of trans-tramadol and its active metabolite, trans-O-demethyltramadol, in human subjects.

Abstract：

AIM:To study the stereoselectivity in pharmacokinetics of the enantiomers of trans-tramadol (trans-T) and its active metabolite, trans-O-demethyltramadol (M1) in human subjects. METHODS:Trans-T hydrochloride sustained-release tablets were taken orally by 12 healthy male volunteers. After a multiple dosage schedule, the serum concentrations of (+)-trans-T, (-)-trans-T, (+)-M1, and (-)-M1 were determined in serum by high performance capillary electrophoresis (HPCE). RESULTS:(+)-Trans-T, (-)-trans-T, (+)-M1 and (-)-M1 in human serum were separated by HPCE. The linear range was 2.5-320 microg/L for the enantiomers of trans-T, and 2.5-50 microg/L for the enantiomers of M1. For the enantiomers of trans-T and M1, the intra-day and inter-day RSD were less than 15 % and 20 %, and the relative recoveries were 94.3 %-106.2 % and 90.4 %-107.8 %, respectively; the limit of quantitation was 1.25 microg/L. The serum concentrations of the enantiomers of trans-T reached a steady state in 12 subjects on d 4 after the initial administration. The steady state serum concentrations of (+)-trans-T were higher than that of (-)-trans-T at every sampling points in the subjects. The differences were significant in the main pharmacokinetic parameters between (+)-trans-T and (-)-trans-T except Tmax. The serum concentrations of (-)-M1 were higher than that of (+)-M1 in most subjects and at most sampling time points. There were significant differences in Cmax and Cmin between the enantiomers of M1. CONCLUSION:The pharmacokinetics of trans-T and M1 was found to be stereoselective. (+)-Trans-T was shown to be absorbed completely, but eliminated more slowly. The pharmacokinetic stereoselectivity of M1 was different among human subjects.

journal_name

Acta Pharmacol Sin

journal_title

Acta pharmacologica Sinica

authors

Liu HC,Liu TJ,Yang YY,Hou YN

subject

Has Abstract

pub_date

2001-01-01 00:00:00

pages

91-6

issue

1

eissn

1671-4083

issn

1745-7254

journal_volume

22

pub_type

临床试验,杂志文章

相关文献

ACTA PHARMACOLOGICA SINICA文献大全
  • Cultured Mycelium Cordyceps sinensis allevi¬ates CCl4-induced liver inflammation and fibrosis in mice by activating hepatic natural killer cells.

    abstract：AIM:Recent evidence shows that cultured mycelium Cordyceps sinensis (CMCS) effectively protects against liver fibrosis in mice. Here, we investigated whether the anti-fibrotic action of CMCS was related to its regulation of the activity of hepatic natural killer (NK) cells in CCl4-treated mice. METHODS:C57BL/6 mice we...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2015.129

    authors： Peng Y,Huang K,Shen L,Tao YY,Liu CH

    更新日期：2016-02-01 00:00:00

  • Curcumin enhances vascular contractility via induction of myocardin in mouse smooth muscle cells.

    abstract：:A variety of cardiovascular diseases is accompanied by the loss of vascular contractility. This study sought to investigate the effects of curcumin, a natural polyphenolic compound present in turmeric, on mouse vascular contractility and the underlying mechanisms. After mice were administered curcumin (100 mg·kg-1·d-1...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2017.18

    authors： Sun SW,Tong WJ,Guo ZF,Tuo QH,Lei XY,Zhang CP,Liao DF,Chen JX

    更新日期：2017-10-01 00:00:00

  • Protective effect of polypeptide from Chlamys farreri on hairless mice damaged by ultraviolet A.

    abstract：AIM:To study the protective effect of the polypeptide isolated from Chlamys farreri (PCF) on hairless mice skin damaged by ultraviolet A. METHODS:Enzymes and malondialdehyde (MDA) were determined by biochemical methods; the expressions of Bcl-2 protein and NOS protein were examined by immunohistochemical technique. Th...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：

    authors： Wang CB,Yao RY,Liu ZT,Zhong WZ,Liu XP,Wang YJ

    更新日期：2002-09-01 00:00:00

  • Cardiovascular actions of Radix Stephaniae Tetrandrae: a comparison with its main component, tetrandrine.

    abstract：:A comparison of the cardiovascular actions of the extract of Radix Stephaniae Tetrandrae (RST), the root of a Chinese hero Stephania tetrandra S Moore, in rats with those of tetrandrine (Tet), the best known active component of RST was reviewed. The RST extract inhibits Ca2+ influx into the myocyte and reduces protein...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章,评审

    doi：

    authors： Wong TM,Wu S,Yu XC,Li HY

    更新日期：2000-12-01 00:00:00

  • Population pharmacokinetics of lamotrigine in Chinese children with epilepsy.

    abstract：AIM:To establish a population pharmacokinetics (PPK) model for lamotrigine (LTG) in Chinese children with epilepsy in order to formulate an individualized dosage guideline. METHODS:LTG steady-state plasma concentration data from therapeutic drug monitoring (TDM) were collected retrospectively from 284 patients, with a...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2012.118

    authors： He DK,Wang L,Qin J,Zhang S,Lu W,Li L,Zhang JM,Bao WQ,Song XQ,Liu HT

    更新日期：2012-11-01 00:00:00

  • Effects of formoterol-budesonide on airway remodeling in patients with moderate asthma.

    abstract：AIM:To evaluate the effect of inhaled formoterol-budesonide on airway remodeling in adult patients with moderate asthma. METHODS:Thirty asthmatic patients and thirty control subjects were enrolled. Asthmatic subjects used inhaled Symbicort 4.5/160 μg twice daily for one year. The effect of formoterol-budesonide on air...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2010.170

    authors： Wang K,Liu CT,Wu YH,Feng YL,Bai HL,Ma ES,Wen FQ

    更新日期：2011-01-01 00:00:00

  • Composite glycidyl methacrylated dextran (Dex-GMA)/gelatin nanoparticles for localized protein delivery.

    abstract：AIM:Localized delivery of growth factors has significant potential as a future therapeutic strategy in tissue engineering and regenerative medicine. A nanoparticle vehicle was created and evaluated in this study with the intent to deliver growth factors for periodontal regeneration. METHODS:Novel composite nanoparticl...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2009.15

    authors： Chen FM,Ma ZW,Dong GY,Wu ZF

    更新日期：2009-04-01 00:00:00

  • Anti-PD-L1 mediating tumor-targeted codelivery of liposomal irinotecan/JQ1 for chemo-immunotherapy.

    abstract：:Immune checkpoint blockade therapy has become a first-line treatment in various cancers. But there are only a small percent of colorectal patients responding to PD-1/PD-L1 blockage immunotherapy. How to increase their treatment efficacy is an urgent and clinically unmet need. It is acknowledged that immunogenic cell d...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/s41401-020-00570-8

    authors： He ZD,Zhang M,Wang YH,He Y,Wang HR,Chen BF,Tu B,Zhu SQ,Huang YZ

    更新日期：2020-12-11 00:00:00

  • Growth inhibitory effects and molecular mechanisms of crotoxin treatment in esophageal Eca-109 cells and transplanted tumors in nude mice.

    abstract：AIM:To investigate the antitumor actions of the Crotalus durissus neurotoxin (crotoxin) on human esophageal carcinoma (Eca-109) cells in vitro and transplanted esophageal Eca-109 tumors in nude mice. METHODS:The growth-inhibitory effect was analyzed in Eca-109 cells using MTT assay. Cell morphology changes in nuclei w...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2012.156

    authors： He JK,Wu XS,Wang Y,Han R,Qin ZH,Xie Y

    更新日期：2013-02-01 00:00:00

  • Retinol induces morphological alterations and proliferative focus formation through free radical-mediated activation of multiple signaling pathways.

    abstract：AIM:Toxicity of retinol (vitamin A) has been previously associated with apoptosis and/or cell malignant transformation. Thus, we investigated the pathways involved in the induction of proliferation, deformation and proliferative focus formation by retinol in cultured Sertoli cells of rats. METHODS:Sertoli cells were i...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2011.202

    authors： Gelain DP,Pasquali MA,Caregnato FF,Castro MA,Moreira JC

    更新日期：2012-04-01 00:00:00

  • The transcription factor PBX3 promotes tumor cell growth through transcriptional suppression of the tumor suppressor p53.

    abstract：:Pre-B-cell leukemia transcription factor 3 (PBX3) is a member of the PBX family and contains a highly conserved homologous domain. PBX3 is involved in the progression of gastric cancer, colorectal cancer, and prostate cancer; however, the detailed mechanism by which it promotes tumor growth remains to be elucidated. H...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/s41401-020-00599-9

    authors： Li WF,Herkilini A,Tang Y,Huang P,Song GB,Miyagishi M,Kasim V,Wu SR

    更新日期：2021-02-01 00:00:00

  • Double-mismatched siRNAs enhance selective gene silencing of a mutant ALS-causing allele.

    abstract：AIM:Our previous study demonstrated an siRNA-mediated, allele-specific silencing of mutant genes that cause amyotrophic lateral sclerosis. To improve siRNA design for better therapeutic use of RNA interference, we systematically tested the base-pairing mismatch strategy in the design of asymmetric siRNA. METHODS:A nat...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1111/j.1745-7254.2008.00740.x

    authors： Geng CM,Ding HL

    更新日期：2008-02-01 00:00:00

  • Chromosome 1q21 amplification and oncogenes in hepatocellular carcinoma.

    abstract：:Hepatocellular carcinoma (HCC) is among the most lethal of human malignancies. During human multistep hepatocarcinogenesis, genomic gain represents an important mechanism in the activation of proto-oncogenes. In many circumstances, activated oncogenes hold clinical implications both as prognostic markers and targets f...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章,评审

    doi：10.1038/aps.2010.94

    authors： Chen L,Chan TH,Guan XY

    更新日期：2010-09-01 00:00:00

  • Caveolin-1 is important for nitric oxide-mediated angiogenesis in fibrin gels with human umbilical vein endothelial cells.

    abstract：AIM:The role of caveolin-1 (Cav-1) in angiogenesis remains poorly understood. The endothelial nitric oxide (NO) synthase (eNOS), a caveolin-interacting protein, was demonstrated to play a predominant role in vascular endothelial growth factor (VEGF) -induced angiogenesis. The purpose of our study was to examine the rol...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1111/j.1745-7254.2006.00462.x

    authors： Pan YM,Yao YZ,Zhu ZH,Sun XT,Qiu YD,Ding YT

    更新日期：2006-12-01 00:00:00

  • IL-12p40 is not required for islet allograft rejection.

    abstract：AIM:To investigate whether IL-12p40 plays a crucial role in regulating islet allograft rejection in a streptozotocin (STZ)-induced diabetes mouse model. METHODS:C57BL/6 and IL-12p40 gene knockout mice were selected as recipient mice, to which the diabetes was induced with a treatment of STZ (150-200 mg/kg) by a single...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1111/j.1745-7254.2006.00341.x

    authors： Bi EG,Shi W,Zou J,Hao ZH,Li ZH,Cai D,Zhang HQ,Sun B

    更新日期：2006-08-01 00:00:00

  • Activation of CaMKIIδA promotes Ca2+ leak from the sarcoplasmic reticulum in cardiomyocytes of chronic heart failure rats.

    abstract：:Activation of the Ca2+/calmodulin-dependent protein kinase II isoform δA (CaMKIIδA) disturbs intracellular Ca2+ homeostasis in cardiomyocytes during chronic heart failure (CHF). We hypothesized that upregulation of CaMKIIδA in cardiomyocytes might enhance Ca2+ leak from the sarcoplasmic reticulum (SR) via activation o...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2018.20

    authors： Gui L,Guo X,Zhang Z,Xu H,Ji YW,Wang RJ,Zhu JH,Chen QH

    更新日期：2018-10-01 00:00:00

  • Improvement of mechanical heart function by trimetazidine in db/db mice.

    abstract：AIM:To investigate the influence of trimetazidine, which is known to be an antioxidant and modulator of metabolism, on cardiac function and the development of diabetic cardiomyopathy in db/db mouse. METHODS:Trimetazidine was administered to db/db mice for eight weeks. Cardiac function was measured by inserting a Milla...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2010.31

    authors： Li YJ,Wang PH,Chen C,Zou MH,Wang DW

    更新日期：2010-05-01 00:00:00

  • Induction of collateral artery growth and improvement of post-infarct heart function by hepatocyte growth factor gene transfer.

    abstract：AIM:To study the effect of adenovirus5-mediated human hepatocyte growth factor (Ad(5)-HGF) transfer on post-infarct heart failure in a swine model. METHODS:Twelve young Suzhong swine were randomly divided into 2 groups: the Ad(5)-HGF group (n=6) and the null-Ad(5) group (n=6). Four weeks after left anterior descending...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1111/j.1745-7254.2006.00306.x

    authors： Wang W,Yang ZJ,Ma DC,Wang LS,Xu SL,Zhang YR,Cao KJ,Zhang FM,Ma WZ

    更新日期：2006-05-01 00:00:00

  • Signaling pathway mediated by kappa-opioid receptor is impaired in cardiac hypertrophy.

    abstract：AIM:The responses of the intracellular calcium ([Ca2+]i) and the intracellular pH (pHi) to kappa-opioid receptor stimulation were determined in the single right ventricular myocytes isolated from the hearts of chronically hypoxic rats which exhibited right ventricular hypertrophy (RVH). METHODS:With the spectrofluorom...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：

    authors： Pei JM,Wang YM,Zhu YL,Chen M,Wong TM

    更新日期：2001-10-01 00:00:00

  • Resveratrol alleviates diabetic cardiomyopathy in rats by improving mitochondrial function through PGC-1α deacetylation.

    abstract：:Recent evidence shows that resveratrol (RSV) may ameliorate high-glucose-induced cardiac oxidative stress, mitochondrial dysfunction and myocardial fibrosis in diabetes. However, the mechanisms by which RSV regulates mitochondrial function in diabetic cardiomyopathy have not been fully elucidated. Mitochondrial dysfun...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2017.50

    authors： Fang WJ,Wang CJ,He Y,Zhou YL,Peng XD,Liu SK

    更新日期：2018-01-01 00:00:00

  • Synergistic protection of allopregnanolone and phenobarbital against maximal electroshock seizures in mice.

    abstract：AIM:To examine the interactions of allopregnanolone and phenobarbital for the protection against seizures. METHODS:The protective activity of allopregnanolone and/or phenobarbital against seizures was studied in the C57 mice, using the maximal electroshock seizure (MES) test. The modulations by allopregnanolone and/or...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：

    authors： Lu YQ,Yu R

    更新日期：2001-04-01 00:00:00

  • Microbial transformation of naproxen by Cunninghamella species.

    abstract：AIM:The metabolites of naproxen produced by Cunninghamella species were isolated and identified, and further to compare the similarities between microbial transformation and mammalian metabolism. METHODS:Naproxen was transformed by three strains of Cunninghammella species (Cunninghamella blakeslesna AS 3.153, Cunningh...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：

    authors： Zhong DF,Sun L,Liu L,Huang HH

    更新日期：2003-05-01 00:00:00

  • Tubeimoside-1, a triterpenoid saponin, induces cytoprotective autophagy in human breast cancer cells in vitro via Akt-mediated pathway.

    abstract：:Autophagy, a form of cellular self-digestion by lysosome, is associated with various disease processes including cancers, and modulating autophagy has shown promise in the treatment of various malignancies. A number of natural products display strong antitumor activity, yet their mechanisms of action remain unclear. T...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/s41401-018-0165-9

    authors： Jiang SL,Guan YD,Chen XS,Ge P,Wang XL,Lao YZ,Xiao SS,Zhang Y,Yang JM,Xu XJ,Cao DS,Cheng Y

    更新日期：2019-07-01 00:00:00

  • Cellular mechanism for spontaneous calcium oscillations in astrocytes.

    abstract：AIM:To determine the Ca2+ source and cellular mechanisms of spontaneous Ca2+ oscillations in hippocampal astrocytes. METHODS:The cultured cells were loaded with Fluo-4 AM, the indicator of intracellular Ca2+, and the dynamic Ca2+ transients were visualized with confocal laser-scanning microscopy. RESULTS:The spontane...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1111/j.1745-7254.2006.00397.x

    authors： Wang TF,Zhou C,Tang AH,Wang SQ,Chai Z

    更新日期：2006-07-01 00:00:00

  • Pharmacokinetic difference between S-(+)- and R-(-)-etodolac in rats.

    abstract：AIM:To study whether etodolac enantiomers have pharmacokinetic difference after oral administration. METHODS:Fourteen rats, divided into two groups randomly, were orally given S-(+)- or R-(-)-etodolac at a single dose of 20 mg/kg, respectively. Blood samples were collected before and at 5, 10, 20, 30 min and 1, 3, 6, ...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：

    authors： Shi JM,Lai SG,Xu CJ,Duan GL,Li D

    更新日期：2004-08-01 00:00:00

  • Hypertonic and isotonic potassium solutions have different effects on vessel contractility resulting in differences in optimal resting tension in rat aorta.

    abstract：AIM:To compare high K(+ )-induced contraction and optimal resting tension measured by two commonly used techniques of hypertonic and isotonic K(+ ) in aortas with and without adventitial fat from various age rats. METHODS:Three age groups of rats (15, 25, and 62 weeks) were used to prepare thoracic aortic rings in whi...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1111/j.1745-7254.2007.00548.x

    authors： Guan YF,Chen RH,Wang P,Qin Y,Su DF,Miao CY

    更新日期：2007-05-01 00:00:00

  • Effects of brain histamine on memory deficit induced by nucleus basalis-lesion in rats.

    abstract：AIM:To investigate whether or not brain histamine was involved in memory deficits induced by lesions of nucleus basalis magnocellularis (NBM) in rats. METHODS:Passive avoidance response was used to measure memory process in rats, and NBM was bilaterally lesioned by injection of ibotenic acid (6 microg/site). RESULTS:...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：

    authors： Chen Z,Shen YJ

    更新日期：2002-01-01 00:00:00

  • Human T-cell lymphotropic virus type 1 and its oncogenesis.

    abstract：:Human T-cell lymphotropic virus type 1 (HTLV-1) is the etiologic agent of adult T-cell leukemia/lymphoma (ATL), a rapidly progressing clonal malignancy of CD4+ T lymphocytes. Exploring the host-HTLV-1 interactions and the molecular mechanisms underlying HTLV-1-mediated tumorigenesis is critical for developing efficien...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章,评审

    doi：10.1038/aps.2017.17

    authors： Zhang LL,Wei JY,Wang L,Huang SL,Chen JL

    更新日期：2017-08-01 00:00:00

  • Myosin light chain kinase is responsible for high proliferative ability of breast cancer cells via anti-apoptosis involving p38 pathway.

    abstract：AIM:To investigate whether myosin light chain kinase (MLCK) contributed to the high proliferative ability of breast cancer cells. METHODS:Soft agar colony formation on the MCF-7 and LM-MCF-7 cell lines was determined. The cell cycles of MCF-7 and LM-MCF-7 were detected using flow cytometry analysis. Western blot analy...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2010.56

    authors： Cui WJ,Liu Y,Zhou XL,Wang FZ,Zhang XD,Ye LH

    更新日期：2010-06-01 00:00:00

  • The combination of baicalin and baicalein enhances apoptosis via the ERK/p38 MAPK pathway in human breast cancer cells.

    abstract：AIM:To examine whether the cell growth inhibitory effect of the combination of baicalin and baicalein is related to apoptosis. Moreover, to determine whether the expression of some apoptosis-related proteins is regulated by the ERK/p38 MAPK pathway. METHODS:Cell viability was measured using a 3-(4,5-dimethylthiazol-2-...

    journal_title：Acta pharmacologica Sinica

    pub_type： 杂志文章

    doi：10.1038/aps.2009.166

    authors： Zhou QM,Wang S,Zhang H,Lu YY,Wang XF,Motoo Y,Su SB

    更新日期：2009-12-01 00:00:00