Low oral bioavailability and pharmacokinetics of senkyunolide a, a major bioactive component in Rhizoma Chuanxiong, in the rat.

Abstract:

:The pharmacokinetics of senkyunolide A, one of the major bioactive ingredients in the traditional Chinese medicinal herb Rhizoma Chuanxiong, which is commonly used for the treatment of cardiovascular diseases, was studied in rats. After intravenous (IV) administration, senkyunolide A was extensively distributed (Vd/F: 6.74 +/- 0.73 L/kg) and rapidly eliminated from the plasma (CL/F: 7.20 +/- 0.48 L/h per kilogram and t1/2: 0.65 +/- 0.06 hr). Hepatic metabolism was suggested as the major route of senkyunolide A elimination as indicated by the results of in vitro S9 fraction study. After intraperitoneal (IP) administration, senkyunolide A exhibited dose-independent pharmacokinetics. The absorption after IP administration was rapid (Tmax: 0.04 +/- 0.01 hours), and the bioavailability was 75%. After oral administration, senkyunolide A was also absorbed rapidly (Tmax: 0.21 +/- 0.08 hours); however, its oral bioavailability was low (approximately 8%). The contributing factors were determined to be instability in the gastrointestinal tract (accounting for 67% of the loss) and hepatic first-pass metabolism (accounting for another 25%). Pharmacokinetics of senkyunolide A were unaltered when Chuanxiong extract was administered, which suggests that components in the extract have insignificant effects on senkyunolide A pharmacokinetics.

journal_name

Ther Drug Monit

authors

Yan R,Lin G,Ko NL,Tam YK

doi

10.1097/FTD.0b013e31802c5862

subject

Has Abstract

pub_date

2007-02-01 00:00:00

pages

49-56

issue

1

eissn

0163-4356

issn

1536-3694

pii

00007691-200702000-00008

journal_volume

29

pub_type

杂志文章
  • Spironolactone as a source of interference in commercial digoxin immunoassays.

    abstract::Eight commercial digoxin immunoassay methods were tested in 17 subjects taking spironolactone (but not digoxin) to evaluate cross-reactivity from parent drug and/or metabolites. Four of these methods showed significant (up to 1.9 nmol/L) and variable "apparent digoxin" concentrations, despite the absence of digoxin in...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-198706000-00014

    authors: Morris RG,Lagnado PY,Lehmann DR,Frewin DB,Glistak ML,Burnet RB

    更新日期:1987-06-01 00:00:00

  • Distribution of amitriptyline and nortriptyline in blood: role of alpha-1-glycoprotein.

    abstract::To interpret blood levels of tricyclic antidepressants, we studied the distributions of amitriptyline and nortriptyline in human blood and explored their control by plasma factors. Each compound (300 ng/ml) was added to whole adult blood and to cord blood with decreased alpha-1-glycoprotein (AGP). Drugs (250 ng/ml) we...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-199308000-00002

    authors: Amitai Y,Kennedy EJ,DeSandre P,Frischer H

    更新日期:1993-08-01 00:00:00

  • Plasma cannabinoid concentrations during dronabinol pharmacotherapy for cannabis dependence.

    abstract:BACKGROUND:Recently, high-dose oral synthetic delta-9-tetrahydrocannabinol (THC) was shown to alleviate cannabis withdrawal symptoms. The present data describe cannabinoid pharmacokinetics in chronic, daily cannabis smokers who received high-dose oral THC pharmacotherapy and later a smoked cannabis challenge. METHODS:...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0b013e3182a5c446

    authors: Milman G,Bergamaschi MM,Lee D,Mendu DR,Barnes AJ,Vandrey R,Huestis MA

    更新日期:2014-04-01 00:00:00

  • Determination of thiopurine methyltransferase activity in human erythrocytes by high-performance liquid chromatography: comparison with the radiochemical method.

    abstract::The current article describes a new assay to measure thiopurine methyltransferase (TPMT) activity from red blood cells. This method is based on the measurement of the reaction product 6-methylmercaptopurine (6-MMP) by high-performance liquid chromatography (HPLC). 6-MMP is extracted by ethyl acetate with recoveries of...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-200110000-00007

    authors: Menor C,Fueyo JA,Escribano O,Cara C,Fernández-Moreno MD,Román ID,Guijarro LG

    更新日期:2001-10-01 00:00:00

  • Subtherapeutic Linezolid Concentration in a Patient With Bullous Pemphigoid Complicated by Methicillin-Resistant Staphylococcus aureus Infection: A Case Study.

    abstract::We presented a case of subtherapeutic linezolid concentration in a patient with bullous pemphigoid characterized by large area skin anabrosis complicated by methicillin-resistant Staphylococcus aureus infections. ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0000000000000758

    authors: Chen C,Zhang M,Chen H,Fang J

    更新日期:2020-08-01 00:00:00

  • 6-mercaptopurine plasma levels in children with acute lymphoblastic leukemia: relation to relapse risk and myelotoxicity.

    abstract::Plasma levels of 6-mercaptopurine were determined in 22 consecutive children with acute lymphoblastic leukemia on oral remission maintenance therapy during the time period of August 1984 to January 1988. Each child received the drug once daily for up to 3 years and was studied repeatedly (1-12 times). An HPLC method w...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-198911000-00001

    authors: Hayder S,Lafolie P,Björk O,Peterson C

    更新日期:1989-11-01 00:00:00

  • A simple fluorescence high-performance liquid chromatographic assay for dihydroquinidine in serum.

    abstract::A simple and rapid reversed-phase C-18 high-performance liquid chromatography (HPLC) assay without a prior extraction step for dihydroquinidine (HQD) in serum is described. The method is selective and useful for monitoring HQD and its presumed metabolites, quinidine (QD), N-oxide QD, 3-hydroxy QD (3-OHQD), and 10-11-d...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-198412000-00017

    authors: Camsonne R,Moulin MA,Albessard F,Perault M

    更新日期:1984-01-01 00:00:00

  • Determination of cefsulodin in biological fluids by high-pressure liquid chromatography.

    abstract::Cefsulodin is a third-generation cephalosporin with a unique specificity for Pseudomonas aeruginosa. To study the pharmacokinetics of this agent in children, a rapid and sensitive high-performance liquid chromatographic micromethod was developed for plasma and urine. Protein was precipitated from plasma with one volum...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-198403000-00015

    authors: Ackers IM,Myers CM,Blumer JL

    更新日期:1984-01-01 00:00:00

  • Clinical use of a simultaneous HPLC assay for indinavir, saquinavir, ritonavir and nelfinavir in children and adults.

    abstract::PROTEASE INHIBITOR TDM: This study examines the importance of therapeutic drug monitoring (TDM) of protease inhibitors (PI) in adults and children infected with the human immunodeficiency virus (HIV). Pediatric patients were included because information in this population is limited. A high performance liquid chromato...

    journal_title:Therapeutic drug monitoring

    pub_type: 更正并重新发布的文章,杂志文章

    doi:10.1097/00007691-200312000-00002

    authors: Walson PD,Cox S,Utkin I,Gerber N,Crim L,Brady M,Koranyi K

    更新日期:2003-12-01 00:00:00

  • Serial free and plasma valproic acid and phenytoin monitoring and drug interactions.

    abstract::In 12 institutionalized epilepsy patients who had been treated 19 months (SD +/- 5) with valproic acid, 27.0 mg/kg (SD +/- 11.9), phenytoin, 6.33 mg/kg (SD +/- 1.36), and co-anticonvulsants, the mean percentage of daily free valproic acid was 11.72 (SD +/- 2.10) and of phenytoin 20.39 (SD +/- 3.32). By serial within-d...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-198103000-00013

    authors: Haidukewych D,Rodin EA

    更新日期:1981-01-01 00:00:00

  • Rapid protein determinations on ultrafiltrates prepared for free phenytoin quantification.

    abstract::Ultrafiltration techniques for the separation of bound and free ligand are dependent on minimal amounts of protein-bound drug leakage through the membrane devices. A dye-impregnated test strip protein assay (Chemstrip-9) provides a rapid, visual assessment of membrane protein leakage. The test strips are sensitive to ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-198507030-00014

    authors: Turley CP,Milligan T

    更新日期:1985-01-01 00:00:00

  • Associations between ABCB1, CYP2A6, CYP2B6, CYP2D6, and CYP3A5 alleles in relation to efavirenz and nevirapine pharmacokinetics in HIV-infected individuals.

    abstract:BACKGROUND:Human immunodeficiency virus (HIV)-infected individuals show large interindividual variation in response to antiretroviral therapy. Efavirenz (EFV) and nevirapine (NVP) are nonnucleoside reverse transcriptase inhibitors, which are prescribed in combination with other antiretroviral therapy in so-called highl...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0b013e31824868f3

    authors: Heil SG,van der Ende ME,Schenk PW,van der Heiden I,Lindemans J,Burger D,van Schaik RH

    更新日期:2012-04-01 00:00:00

  • Binding parameters of valproic acid to serum protein in healthy adults at steady state.

    abstract::Two hundred milligrams of valproic acid (VPA) was administered orally to seven healthy adults at 9:00 and 21:00 h for 5 consecutive days, including the morning dose on day 6. On the sixth day, blood samples were drawn at 0, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 3, and 6 h after the morning dose. Binding of VPA to serum prote...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-199202000-00009

    authors: Kodama Y,Koike Y,Kimoto H,Yasunaga F,Takeyama M,Teraoka I,Fujii I

    更新日期:1992-02-01 00:00:00

  • Quetiapine serum concentrations in psychiatric patients: the influence of comedication.

    abstract::Steady-state serum concentrations of quetiapine were recorded in 62 psychiatric patients under routine conditions. Doses were administered twice daily, and serum quetiapine levels were measured in the morning about 12 hours after the last dose. Eight patients were in monotherapy, whereas the rest received various addi...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章

    doi:10.1097/00007691-200410000-00005

    authors: Hasselstrøm J,Linnet K

    更新日期:2004-10-01 00:00:00

  • Effects of the CYP2D6*10 allele on the steady-state plasma concentrations of aripiprazole and its active metabolite, dehydroaripiprazole, in Japanese patients with schizophrenia.

    abstract::The CYP2D6*10(*10) allele that causes decreased CYP2D6 activity is present in Asians with a high frequency of approximately 50%. We studied the effects of the *10 allele on the steady-state plasma concentrations of aripiprazole and its active metabolite, dehydroaripiprazole. The subjects were 63 Japanese patients with...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0b013e3182031021

    authors: Suzuki T,Mihara K,Nakamura A,Nagai G,Kagawa S,Nemoto K,Ohta I,Arakaki H,Uno T,Kondo T

    更新日期:2011-02-01 00:00:00

  • Should 6-thioguanine nucleotides be monitored in heart transplant recipients given azathioprine?

    abstract::The commonly used immunosuppressive regimen after orthotopic heart transplantation consists of cyclosporine (CsA), azathioprine (AZA), and steroids. Although AZA therapy is generally regarded as unproblematic, its use can be associated with severe side effects, particularly myelosuppression. Since AZA is a prodrug, wh...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章

    doi:10.1097/00007691-199606000-00002

    authors: Schütz E,Gummert J,Mohr FW,Armstrong VW,Oellerich M

    更新日期:1996-06-01 00:00:00

  • Polymorphisms in CYP3A5, CYP3A4, and ABCB1 are not associated with cyclosporine pharmacokinetics nor with cyclosporine clinical end points after renal transplantation.

    abstract:BACKGROUND:The association of CYP3A5, CYP3A4, and ABCB1 single nucleotide polymorphisms (SNPs) with cyclosporine (CsA) pharmacokinetics is controversial. The authors studied the influence of these SNPs on CsA pharmacokinetics as well as on the incidence of biopsy-proven acute rejection (BPAR) and renal function after k...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,多中心研究,随机对照试验

    doi:10.1097/FTD.0b013e31820feb8e

    authors: Bouamar R,Hesselink DA,van Schaik RH,Weimar W,Macphee IA,de Fijter JW,van Gelder T

    更新日期:2011-04-01 00:00:00

  • Effects of heparin sodium on gentamicin assay measured by fluorescence polarization immunoassay method.

    abstract::The effect of heparin sodium on the assay of gentamicin using the fluorescence polarization immunoassay system was investigated with varying heparin and gentamicin concentrations. Heparin had no significant effect on gentamicin concentrations as measured by this system. ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-198409000-00011

    authors: Jackson DS,Bertino JS Jr

    更新日期:1984-01-01 00:00:00

  • Evaluation of the practicability of limited sampling strategies for the estimation of mycophenolic acid exposure in Chinese adult renal recipients.

    abstract::The immunosuppressive potential of mycophenolic acid (MPA) correlates well with MPA exposure [area under the concentration-time curve (AUC)]. Monitoring MPA AUC is important and helpful for maintaining the efficacy of mycophenolate mofetil while minimizing its side effects, but full MPA AUC monitoring is laborious, co...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0b013e3181559f8a

    authors: Zicheng Y,Xianghui W,Peijun Z,Da X,Weixia Z,Hongzhuan C

    更新日期:2007-10-01 00:00:00

  • Cancer Chemotherapy: The Case for Therapeutic Drug Monitoring.

    abstract::The selection of an appropriate therapy and dosing regimen is a significant challenge in the treatment of cancer. Although there are recommended standardized chemotherapy protocols for some types of cancer, protocol changes that usually only occur after large clinical trials demonstrate improvements and individual pat...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0000000000000701

    authors: Knezevic CE,Clarke W

    更新日期:2020-02-01 00:00:00

  • Excretion of the principal urinary metabolites of phenytoin and absolute oral bioavailability determined by use of a stable isotope in patients with epilepsy.

    abstract:BACKGROUND:The anticonvulsant properties of phenytoin (PHT) were discovered in 1938. Since then, it has been one of the most widely used antiepileptic drugs. It is slowly absorbed, extensively plasma protein-bound, exhibits a nonlinear, concentration-dependent pharmacokinetic profile, and has a narrow therapeutic range...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0b013e3182081089

    authors: Aliwarga T,Cloyd JC,Goel V,Brundage RC,Marino SE,Leppik IE,Remmel RP

    更新日期:2011-02-01 00:00:00

  • Comparison of cyclosporine blood levels measured by radioimmunoassay and TDx assay using monoclonal antibodies.

    abstract::Whole blood steady-state trough concentrations of cyclosporine were measured by radioimmunoassay (RIA) and TDx assays employing monoclonal antibodies in 82 samples from 39 renal transplant patients. Intra- and interassay coefficients of variation for the new TDx technique averaged 3.2 and 5.4%, respectively. In the co...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-199109000-00012

    authors: Klotz U

    更新日期:1991-09-01 00:00:00

  • Acute antidepressant response and plasma levels of bupropion and metabolites in a pediatric-aged sample: an exploratory study.

    abstract::Studies examining associations between antidepressant response and plasma levels of bupropion and its metabolites have yielded contradictory findings. There have been no such studies in youth. This study explored such associations in 8 boys and 8 girls, age 11 to 17 years, all prescribed bupropion sustained release (S...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章

    doi:10.1097/01.ftd.0000197093.92559.7a

    authors: Daviss WB,Perel JM,Brent DA,Axelson DA,Rudolph GR,Gilchrist R,Nuss S,Birmaher B

    更新日期:2006-04-01 00:00:00

  • Population Pharmacokinetic Analysis of Meropenem in Critically Ill Patients With Acute Kidney Injury Treated With Continuous Hemodiafiltration.

    abstract:BACKGROUND:The aim of this study was to conduct a population pharmacokinetic (PK) analysis of meropenem and to explore the optimal dosing strategy for meropenem in critically ill patients with acute kidney injury receiving treatment with continuous hemodiafiltration (CHDF). METHODS:Blood samples were obtained on days ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0000000000000741

    authors: Niibe Y,Suzuki T,Yamazaki S,Suzuki T,Takahashi N,Hattori N,Nakada TA,Oda S,Ishii I

    更新日期:2020-08-01 00:00:00

  • Saliva as a valid alternative to serum in monitoring intravenous caffeine treatment for apnea of prematurity.

    abstract::Caffeine is a potentially useful alternative to theophylline for the treatment and prevention of apnea of prematurity because of its lower toxicity and longer terminal half-life. Monitoring of salivary caffeine concentrations is less invasive than blood sampling, especially in very sick premature neonates. Caffeine ci...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00007691-199606000-00012

    authors: Lee TC,Charles BG,Steer PA,Flenady VJ

    更新日期:1996-06-01 00:00:00

  • Impact of Laboratory Practices on Interlaboratory Variability in Therapeutic Drug Monitoring of Immunosuppressive Drugs.

    abstract::The immunosuppressants cyclosporine, tacrolimus, sirolimus, everolimus, and probably also mycophenolic acid require therapeutic drug monitoring (TDM)-guided dosing to ensure that blood concentrations are kept within the target range in transplant patients. Reliable, accurate, and precise test methods are therefore ess...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0000000000000205

    authors: Christians U,Vinks AA,Langman LJ,Clarke W,Wallemacq P,van Gelder T,Renjen V,Marquet P,Meyer EJ

    更新日期:2015-12-01 00:00:00

  • Assessment of VerifyNow P2Y12 assay accuracy in evaluating clopidogrel-induced platelet inhibition.

    abstract::The emergence of point-of-care assays enabling bedside testing such as the VerifyNow P2Y12 system might prove useful in clinical settings. The aim of this study was to evaluate the ability of the VerifyNow P2Y12 assay to estimate the inhibition of platelet aggregation provided by clopidogrel in the absence of baseline...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,随机对照试验

    doi:10.1097/FTD.0b013e3181757c59

    authors: Lordkipanidzé M,Pharand C,Nguyen TA,Schampaert E,Diodati JG

    更新日期:2008-06-01 00:00:00

  • Creatinine clearance as predictor of tobramycin elimination in adult patients with cystic fibrosis.

    abstract::Assessment of renal function and relating this parameter to amino-glycoside clearance is important for an appropriate individualization of dosage regimens in patients with impaired renal function. However, it has been suggested that in cystic fibrosis (CF), creatinine clearance (CrCl) is not a good predictor of tobram...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/00007691-199610000-00007

    authors: Town DJ,Vinks AA,Jacobs F,Heijerman HG,Bakker W

    更新日期:1996-10-01 00:00:00

  • A Dried Blood Spot Analysis for Solithromycin in Adolescents, Children, and Infants: A Short Communication.

    abstract:BACKGROUND:Solithromycin is a fourth-generation macrolide antibiotic with potential efficacy in pediatric community-acquired bacterial pneumonia. Pharmacokinetic (PK) studies of solithromycin in pediatric subjects are limited, therefore application of minimally invasive drug sampling techniques, such as dried blood spo...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章

    doi:10.1097/FTD.0000000000000670

    authors: Beechinor RJ,Cohen-Wolkowiez M,Jasion T,Hornik CP,Lang JE,Hernandez R,Gonzalez D

    更新日期:2019-12-01 00:00:00

  • No pharmacokinetic but pharmacodynamic interactions between cisapride and bromperidol or haloperidol.

    abstract::Pharmacokinetic and pharmacodynamic interactions between the gastrokinetic drug cisapride and the antipsychotic drugs bromperidol and haloperidol were studied in 29 schizophrenic inpatients. Fourteen patients were taking bromperidol (12-24 mg/d), and 15 were taking haloperidol (12-36 mg/d). Cisapride 10 mg/d was coadm...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章

    doi:10.1097/00007691-199906000-00007

    authors: Mihara K,Otani K,Yasui N,Ishida M,Kondo T,Suzuki A,Furukori H,Nagashima U,Kaneko S,Inoue Y

    更新日期:1999-06-01 00:00:00