A pharmacokinetic study with the high-dose anticancer agent menadione in rabbits.

Abstract:

:The aim of this investigation was to assess the pharmacokinetic properties of high-dose menadione (VK3), as an anticancer agent, in plasma and red blood cells (RBCs) in rabbits. An extremely high dose of 75 mg menadiol sodium diphosphate (Synkayvite) was intravenously injected. HPLC analysis was applied to measure the major metabolite, menadione, VK3. The kinetic properties of VK3 in both plasma and red blood cells showed a short elimination half-life, high clearance, and large volume of distribution in plasma and RBCs. The mean elimination t1/2 values of menadione in plasma and in RBCs were 27.17 +/- 10.49 min and 35.22 +/- 11.82 min, respectively. The plasma clearance (CL/F) of VK3 was 0.822 +/- 0.254 L min-1. The systemic clearance in RBCs was 0.407 +/- 0.152 L min-1. The apparent volume of distribution (Vd/F) in plasma was 30.833 +/- 12.835 L and that in RBCs 20.488 +/- 9.401 L. The plasma AUC was 32.453 +/- 9.785 micrograms min mL-1 and that of RBCs 67.219 +/- 24.449 micrograms min mL-1. Menadiol was rapidly biotransformed to menadione in blood. The formation rate constant (kf) of menadione in plasma was 0.589 +/- 0.246 min-1, and that of RBCs 1.520 +/- 1.345 min-1. Through this study the estimated menadione dosage needed to maintain a plasma level of 1 microgram mL-1 for anticancer purposes was 19.7 mg kg-1 every hour.

journal_name

Biopharm Drug Dispos

authors

Hu OY,Wu CY,Chan WK,Wu FY,Whang-Peng J

doi

10.1002/(SICI)1099-081X(199608)17:6<493::AID-BDD97

subject

Has Abstract

pub_date

1996-08-01 00:00:00

pages

493-9

issue

6

eissn

0142-2782

issn

1099-081X

pii

10.1002/(SICI)1099-081X(199608)17:6<493::AID-BDD97

journal_volume

17

pub_type

杂志文章
  • Simultaneous modelling of mexiletine and hydroxy-methyl-mexiletine data after single- and multiple-dose administration of a sustained-release mexiletine formulation.

    abstract::The pharmacokinetics of mexiletine and its metabolite hydroxy-methyl-mexiletine have been investigated following single-dose and during multiple-dose administration of a sustained-release form of mexiletine to six post-myocardial infarct patients. Comparison of single-dose and washout pharmacokinetics, after short-ter...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510130702

    authors: Bruno R,Santoni Y,Iliadis A,Djiane P,Serradimigni A,Cano JP

    更新日期:1992-10-01 00:00:00

  • Use of affinity capillary electrophoresis for characterizing pharmaceutical colloidal vehicle systems thermodynamically.

    abstract::This review offers a detailed discussion of the interaction between pharmaceutical compounds and vehicles using the affinity capillary electrophoresis and the microemulsion electrokinetic chromatography. Partition coefficients of drugs were calculated between a micelle and an aqueous phases from the measurement of the...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章,评审

    doi:10.1002/bdd.287

    authors: Reinhard N,Mrestani Y

    更新日期:2001-10-01 00:00:00

  • Biopharmaceutics classification and intestinal absorption of chikusetsusaponin IVa.

    abstract::The objective of this study was to investigate the absorption behavior of chikusetsusaponin IVa (CHS-IVa) in the rat intestine using single-pass intestinal perfusion (SPIP) and to classify CHS-IVa into the biopharmaceutics classification system (BCS). The equilibrium solubility of CHS-IVa was determined by the shaker ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2200

    authors: Zhang W,Liu H,Liu C

    更新日期:2019-09-01 00:00:00

  • The relative bioavailability of two marketed controlled release diltiazem dosage forms at steady state in healthy volunteers.

    abstract::This study was conducted to determine the relative bioavailability of Dilacor XR capsules compared to Cardizem CD capsules at both low (180 mg d-1) and high (540 mg d-1) dose levels. Trough and serial plasma samples were obtained and pharmacokinetic parameters were calculated from the steady state concentration-time p...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/(SICI)1099-081X(199601)17:1<43::AID-BDD935

    authors: Lippert CL,Arumugham T,Bhargava VO,Eller M,Weir SJ

    更新日期:1996-01-01 00:00:00

  • Pharmacokinetic interaction of ketoconazole and itraconazole with ciprofloxacin.

    abstract::The effect of the concomitant administration of the antifungal drugs ketoconazole (KTC) and itraconazole (ITC) on the pharmacokinetics of ciprofloxacin (CIP) following short- and long-term administration in mice was investigated. Animals received either a dose of CIP (20 mg/kg, i.p.), CIP (20 mg/kg, i.p.) together wit...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.586

    authors: Abou-Auda HS,Mustafa AA,Al-Humayyd MS

    更新日期:2008-01-01 00:00:00

  • A pharmacokinetic evaluation of HIV protease inhibitors, cyclic ureas, in rats and dogs.

    abstract::The pharmacokinetics of a series of novel cyclic, non-peptide inhibitors of HIV protease were studied in rats or dogs after intravenous and oral administration. Six symmetrically substituted cyclic urea compounds (XK234, XM311, XM320, XM321, XM323, and XM412), which effectively inhibited HIV virus replication, with IC...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510150702

    authors: Wong YN,Burcham DL,Saxton PL,Erickson-Viitanen S,Grubb MF,Quon CY,Huang SM

    更新日期:1994-10-01 00:00:00

  • Stable solid dispersion of lurasidone hydrochloride with augmented physicochemical properties for the treatment of schizophrenia and bipolar disorder.

    abstract::Crystalline solid dispersion of lurasidone hydrochloride (LH) was made with various polar and non-polar small molecules to overcome the poor aqueous solubility issue. LH-Glutathione (GSH) solid dispersion in 1:1 ratio was prepared by co-grinding method and characterized by using differential scanning calorimetry (DSC)...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2252

    authors: Pardhi VP,Flora S

    更新日期:2020-11-01 00:00:00

  • The effect of ciprofloxacin and clarithromycin on sildenafil oral bioavailability in human volunteers.

    abstract::Sildenafil is the first oral therapeutic agent for the management of male erectile dysfunction. Its oral bioavailability is only 40% due to extensive presystemic elimination, mainly by CYP3A4. This study examined the effect of coadministration of ciprofloxacin or clarithromycin, which inhibit CYP3A4, on the bioavailab...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.488

    authors: Hedaya MA,El-Afify DR,El-Maghraby GM

    更新日期:2006-03-01 00:00:00

  • Identification of rat faecal, urinary and biliary metabolites of thionorphine, a novel mixed agonist-antagonist analgesic, using liquid chromatography/electrospray ionization tandem mass spectrometry.

    abstract::The biotransformation of thionorphine (N-cyclopropylmethyl-7alpha-[(s)-1-hydroxy-1-methyl-3-(2thiophene)-propyl]-6,14-endo-ethano tetrahydrooripavine), a new analgesic, was in-vestigated in rats. The results of metabolite analysis by liquid chromatography/electrospray ionization tandem mass spectrometry with positive ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.360

    authors: Wei SX,Zhang ZQ,Wang XY,Guo JF

    更新日期:2004-04-01 00:00:00

  • Investigation of the effects of concomitant caffeine administration on the metabolic disposition of pyrazinamide in rats.

    abstract::The utility of pyrazinamide (PZA) in the short-course antituberculous treatment is well established. All available data support the idea that the PZA metabolite pyrazinoic acid (PA) is the active compound against M. tuberculosis. This situation warranted a deeper investigation of possible interactions with respect to ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.305

    authors: Mehmedagic A,Verite P,Menager S,Tharasse C,Chabenat C,Andre D,Lafont O

    更新日期:2002-07-01 00:00:00

  • In vitro reduction of rhein anthraquinone to rhein anthrone by rat cecal microflora and some intestinal bacterial strains.

    abstract::After in vitro incubation of cecal content from CVL or gnotobiotic rats with rhein anthraquinone (1 mg g-1) for 18 h at 37 degrees, the anthraquinone was converted to rhein anthrone for 23.5 (SD +/- 3.4) per cent and 19.4 (+/- 4.7) per cent, respectively. Liquid cultures of some strictly anaerobic fecal bacteria of ma...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510130403

    authors: de Witte P,Van Hoestenberghe A,Eyssen H

    更新日期:1992-05-01 00:00:00

  • Pharmacokinetics of D-propranolol following oral, intra-arterial and intraportal administration: contrasting effects of oral glucose pretreatment.

    abstract::Several research groups have reported that in man the oral administration of propranolol with food leads to a marked increase (about 50 per cent) in the area under the plasma concentration-time curve (AUCpo) of this well absorbed and highly metabolized drug. An acute change in hepatic metabolic enzyme activity has bee...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510140305

    authors: Chow HH,Lalka D

    更新日期:1993-04-01 00:00:00

  • Plasma lipoproteins as targeting carriers to tumour tissues after administration of a lipophilic agent to mice.

    abstract::We synthesized 14C-warfarin hexadecyl ether (14C-WHE) by addition of a palmityl moiety to the hydroxyl group at the 4-position of 14C-warfarin, a compound known to bind to serum albumin. 14C-WHE preferentially bound to the lipoproteins, low-density lipoprotein (LDL) and high-density lipoprotein (HDL), in mouse plasma ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510160204

    authors: Tokui T,Kuroiwa C,Muramatsu S,Tokui Y,Sasagawa K,Ikeda T,Komai T

    更新日期:1995-03-01 00:00:00

  • Intravenous administration of paclitaxel in Sprague-Dawley rats: what is a safe dose?

    abstract::Few studies describe the administration of Taxol to rats; however, rats are typically used to study the toxicity of new drugs or novel formulations. A dose finding study was conducted to determine a safe dose of Taxol following intravenous administration in rats. Male Sprague-Dawley rats received a bolus of paclitaxel...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.503

    authors: Shord SS,Camp JR

    更新日期:2006-05-01 00:00:00

  • Pharmacokinetics of budesonide and formoterol administered via a series of single-drug and combination inhalers: four open-label, randomized, crossover studies in healthy adults.

    abstract:OBJECTIVE:To investigate the pharmacokinetics of budesonide and formoterol administered concomitantly in healthy adults. METHODS:Three single-dose, open-label crossover studies (n=28 each) were conducted (Study I: budesonide pMDI, formoterol DPI, budesonide pMDI+formoterol DPI; Study II: budesonide/formoterol pMDI, bu...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章,随机对照试验

    doi:10.1002/bdd.622

    authors: Eklund A,Tronde A,Johannes-Hellberg I,Gillen M,Borgström L

    更新日期:2008-10-01 00:00:00

  • Pharmacokinetics of fluvoxamine maleate after increasing single oral doses in healthy subjects.

    abstract::The pharmacokinetics of fluvoxamine after single oral administration of 25, 50, and 100 mg fluvoxamine maleate was studied in a three-way cross-over study in 12 healthy male subjects. Fluvoxamine was administered orally in a solution. For dose-proportionality, AUC, and Cmax-dose relationships were evaluated by linear ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/bdd.2510140403

    authors: De Vries MH,Van Harten J,Van Bemmel P,Raghoebar M

    更新日期:1993-05-01 00:00:00

  • Biotransformation and urinary excretion of 4-substituted amphetamines in pregnant mice.

    abstract::The urinary elimination of 4-hydroxyamphetamine (PHA) and a series of homologous 4-alkoxy-substituted amphetamines and their metabolites was examined after single and multiple oral administration to pregnant and non-pregnant mice. The metabolic profile and extent of biotransformation in a series of alkoxy analogues we...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510140807

    authors: Foster BC,Litster DL,Buttar HS,Dawson B,Zamecnik J

    更新日期:1993-11-01 00:00:00

  • Absorption and disposition of a new low-dose combination formulation of hydrochlorothiazide and triamterene.

    abstract::Two studies are reported that assess the bioequivalence of a new half-strength drug combination containing 25 mg hydrochlorothiazide and 37.5 mg triamterene compared to a full-strength formulation containing 50 mg hydrochlorothiazide and 75 mg triamterene. The first study (I) compared the absorption and disposition of...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/bdd.2510110308

    authors: Williams RL,Lin ET,Liang-Gee W,Blume CD,Benet LZ

    更新日期:1990-04-01 00:00:00

  • Pharmacokinetics and allometric scaling of levormeloxifene, a selective oestrogen receptor modulator.

    abstract::The pharmacokinetics of a new selective oestrogen receptor modulator levormeloxifene was investigated in mice, rats, cynomolgus monkeys and humans by compartmental pharmacokinetics. Levormeloxifene was administered as an oral solution in all studies. Allometric scaling was used to predict human pharmacokinetic paramet...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.344

    authors: Østerberg O,Kiehr B,Erichsen L,Poulsen HE,Ingwersen SH

    更新日期:2003-04-01 00:00:00

  • Pharmacodynamics of acute intranasal administration of verapamil: comparison with i.v. and oral administration.

    abstract::The present study was conducted in order to examine the intranasal administration of verapamil and compare this route to oral and intravenous administration in a 3 way crossover protocol in five dogs. Unanesthetized, adult mongrel dogs were given verapamil intravenously (0.5 mg/kg), orally (2.5 mg/kg) and intranasally...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510060411

    authors: Arnold TH,Tackett RL,Vallner JJ

    更新日期:1985-10-01 00:00:00

  • Immunodynamics of methylprednisolone induced T-cell trafficking and deactivation using whole blood lymphocyte proliferation techniques in the rat.

    abstract::Glucocorticoids have diverse effects on various components of the immune system and assessment of such activities in vivo often involves complex techniques and numerous animals. We developed a whole blood technique for determining proliferation rate of lymphocytes in minute amounts of rat blood (5 microL as opposed to...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(199907)20:5<255::aid-bdd18

    authors: Fasanmade AA,Jusko WJ

    更新日期:1999-07-01 00:00:00

  • Use of a limited physiologic model to explain target organ toxicity of bupivacaine as a function of route of administration.

    abstract::A physiologic model to describe bupivacaine uptake by and elimination from brain and heart was developed. Preliminary validation of the model was accomplished by comparing concentration data predicted by the model with those determined in rabbits. The model was modified to examine similarities and differences followin...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510070204

    authors: Denson DD,Thompson GA,Coyle DE

    更新日期:1986-03-01 00:00:00

  • Metabolism and disposition of EXP631--a novel antidepressant analgesic.

    abstract::EXP631, 4-(3-thienyl)-alpha, alpha,1-trimethyl-4-piperidine-methanol hemi-fumarate salt (I), is a centrally acting non-opioid analgesic compound with monoamine uptake blocking properties. EXP631 has analgesic effects in several animal models. It is intended to be used for the treatment of moderate to moderately severe...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510140608

    authors: Wong YN,Burcham DL,Huang SM,Quon CY

    更新日期:1993-08-01 00:00:00

  • A quantitative threshold for high/low extent of urinary excretion of compounds in humans.

    abstract::In this study, a quantitative threshold was determined for the high/low extent of urinary excretion (UE) of compounds in humans, using a straightforward but robust statistical method known as receiver operating characteristic curve (ROC) analysis, and also 18 potential physicochemical determinants of UE were evaluated...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2013

    authors: Dave RA,Morris ME

    更新日期:2016-07-01 00:00:00

  • Atazanavir increases the plasma concentrations of 1200 mg raltegravir dose.

    abstract::Raltegravir is a human immunodeficiency virus (HIV)-1 integrase strand transfer inhibitor currently marketed at a dose of 400 mg twice-daily (b.i.d.). Raltegravir 1200 mg once-daily (q.d.) (investigational q.d. formulation of 2 × 600 mg tablets; q.d. RAL) was found to be generally well tolerated and non-inferior to th...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章,随机对照试验

    doi:10.1002/bdd.2043

    authors: Krishna R,East L,Larson P,Valiathan C,Deschamps K,Luk JA,Bethel-Brown C,Manthos H,Brejda J,Gartner M

    更新日期:2016-12-01 00:00:00

  • SGK1/Nedd4-2 signaling pathway regulates the activity of human organic anion transporters 3.

    abstract::Human organic anion transporter 3 (hOAT3) is localized at the basolateral membrane of renal proximal tubule cells and facilitates the renal secretion of numerous clinical drugs, including anti-HIV therapeutics, anti-tumor drugs, antibiotics, antihypertension drugs and anti-inflammatories. The present study explored th...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2085

    authors: Wang H,You G

    更新日期:2017-11-01 00:00:00

  • Stability of cucurbitacin E in human plasma: chemical hydrolysis and role of plasma esterases.

    abstract::It was shown previously that the anticancerous cytotoxic oxygenated triterpenes, cucurbitacin E (Cuc E) and its deacetylated form, cucurbitacin I (Cuc I), interacted differently with human serum albumin. In this study, the biochemical stability of Cuc E was investigated in vitro by reverse-phase high performance liqui...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.673

    authors: Saade M,Magdalou J,Ouaini N,Greige-Gerges H

    更新日期:2009-10-01 00:00:00

  • Prednisone and prednisolone interconversion in the rabbit utilizing unbound concentrations.

    abstract::Prednisolone (POH) and prednisone (PO) were both administered via seven different intravenous infusions (three POH and four PO) in each of six rabbits to obtain steady state. Bolus doses of POH and PO were also administered to four of the rabbits. Plasma samples of POH and PO were analyzed by normal phase HPLC. Unboun...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510120608

    authors: Hammarlund-Udenaes M,Benet LZ

    更新日期:1991-08-01 00:00:00

  • The influence of moderate and chronic exercise training on the pharmacokinetics of procainamide and N-acetylprocainamide.

    abstract::The effect of moderate and prolonged exercise on the disposition and metabolism of drugs has not been extensively examined. The present study examined the effect of exercise training on the pharmacokinetics of procainamide and its active metabolite, N-acetylprocainamide. Male Sprague Dawley rats were randomly assigned...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(199807)19:5<291::aid-bdd10

    authors: Eddington ND,Adekoya F,Kharidia J

    更新日期:1998-07-01 00:00:00

  • Pharmacokinetics and pharmacodynamics of furosemide after direct administration into the stomach or duodenum.

    abstract::The pharmacokinetics and pharmacodynamics of furosemide were compared after an oral administration or a direct administration of Lasix into the duodenum in humans (40 mg). Furosemide was absorbed quickly after a direct administration of Lasix into the duodenum; the peak plasma concentration of furosemide was reached w...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/(sici)1099-081x(199712)18:9<753::aid-bdd63

    authors: Lee WI,Yoon WH,Shin WG,Song IS,Lee MG

    更新日期:1997-12-01 00:00:00