Relationship between total body clearance of caffeine and urine flow rate in elderly men.

abstract：:Twenty-six healthy male volunteers received a single 10 mg dose of diazepam on two occasions in a crossover bioequivalence study comparing the reference product (Valium) and a generic formulation (NeoCalme). Concentrations of diazepam and its metabolite, desmethyldiazepam, were determined during 264h after each dose. ...

journal_title：Biopharmaceutics & drug disposition

authors： Locniskar A,Greenblatt DJ,Harmatz JS,Shader RI

更新日期：1989-11-01 00:00:00

abstract：:Based on the principle of superposition an expression has been established relating a drug concentration at steady-state to a concentration after a single dose. This relationship applies for drugs with linear pharmacokinetics given at equal dosage intervals and it is independent of the route of administration. The rel...

journal_title：Biopharmaceutics & drug disposition

authors： Love BL,Tsuei SE,Thomas J,Nation RL

更新日期：1982-07-01 00:00:00

abstract：:Remogliflozin etabonate (RE) is the prodrug of remogliflozin (R), an inhibitor of renal glucose transport designed to reduce blood glucose concentrations for the treatment of type 2 diabetes. This open-label, randomized, single-dose, four-way crossover study, (with one add-on arm) in eight healthy men evaluated the re...

journal_title：Biopharmaceutics & drug disposition

authors： O'Connor-Semmes RL,Sandefer EP,Hussey EK,Tao W,Doll WJ,Page RC,Dobbins R

更新日期：2013-03-01 00:00:00

abstract：:Pharmacokinetic compartment models were constructed to describe the absorption and metabolism of dopamine (DA) and DA prodrug, N-(N-acetyl-L-methionyl)0,0-bis-eth-oxycarbonyl) dopamine(1). Plasma concentrations of DA, DA-SO4, and DOPAC after oral administration of DA to dogs, were analysed using the pharmacokinetic mo...

journal_title：Biopharmaceutics & drug disposition

authors： Murata K,Noda K,Kohno K,Samejima M

更新日期：1990-03-01 00:00:00

abstract：:Regional pharmacokinetics is the study of the drug concentrations in specific regions of the body. It allows greater insight into the mechanisms of drug disposition than the study of systemic blood concentrations. Experimental methods in regional pharmacokinetics and their applications and limitations are reviewed. Po...

journal_title：Biopharmaceutics & drug disposition

authors： Upton RN,Runciman WB,Mather LE

更新日期：1990-12-01 00:00:00

abstract：:Rifampicin, a poorly soluble drug, has great importance in therapeutics as it is the main drug used to treat tuberculosis. The characterization of its permeability and the factors that influence it represent an important tool for predicting its bioavailability. Caco-2 cell monolayers were used as models of the intesti...

journal_title：Biopharmaceutics & drug disposition

authors： Gonçalves JE,Ballerini Fernandes M,Chiann C,Gai MN,De Souza J,Storpirtis S

更新日期：2012-09-01 00:00:00

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

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

更新日期：2003-04-01 00:00:00

abstract：:In the search for orally available drugs, the prediction of human pharmacokinetics (PK) is essential for successfully selecting compounds that will be clinically useful. This report describes the selection of TAK-272 (SCO-272), a novel orally active renin inhibitor, as a clinical candidate via the detailed investigati...

journal_title：Biopharmaceutics & drug disposition

authors： Ebihara T,Nishihara M,Takahashi J,Jinno F,Tagawa Y

更新日期：2018-03-01 00:00:00

abstract：:The 2-oxidation activity on the pyrimidine ring of RS-8359, a MAO-A inhibitor, is the major metabolic pathway catalysed by aldehyde oxidase. This study investigated the species differences in the 2-oxidation activity by using liver cytosolic fractions from rats, mice, guinea-pigs, rabbits, dogs, monkeys and humans. Th...

journal_title：Biopharmaceutics & drug disposition

authors： Itoh K,Yamamura M,Takasaki W,Sasaki T,Masubuchi A,Tanaka Y

更新日期：2006-04-01 00:00:00

abstract：:The tumour uptake as well as the anti-tumour activity of RS-1541 (palmitoyl rhizoxin), a potent antineoplastic agent, were investigated in mice bearing M5076 sarcoma. After intravenous administration, 14C-RS-1541 preferentially bound to the lipoproteins, to which 14C-rhizoxin did not bind. 14C-RS-1541 showed persistin...

journal_title：Biopharmaceutics & drug disposition

authors： Tokui T,Kuroiwa C,Tokui Y,Sasagawa K,Kawai K,Kobayashi T,Ikeda T,Komai T

更新日期：1994-03-01 00:00:00

abstract：:Fexofenadine hydrochloride is a non-sedating antihistamine that is used in the treatment of symptoms associated with seasonal allergic rhinitis and chronic idiopathic urticaria. A pooled analysis of pharmacokinetic data from children 6 months to 12 years of age and adults was conducted to identify the dose(s) in child...

journal_title：Biopharmaceutics & drug disposition

authors： Krishna R,Krishnaswami S,Kittner B,Sankoh AJ,Jensen BK

更新日期：2004-12-01 00:00:00

abstract：:The pharmacokinetics of an intravenous injection of disopyramide was studied in five normal subjects and six patients with varying degrees of renal impairment. The elimination rate constant (beta) was related to the endogenous creatinine clearance (Clcr). However, a decrease in beta was not observed until the Clcr was...

journal_title：Biopharmaceutics & drug disposition

authors： Shen DD,Cunningham JL,Shudo I,Azarnoff DL

更新日期：1980-01-01 00:00:00

abstract：:The pharmacokinetic behavior of glycyrrhizin in four patients with acute hepatitis (hepatitis group) and six patients with liver cirrhosis (cirrhosis group) receiving chronically an IV administration of a 120 mg dose once a day or once every other day of glycyrrhizin was investigated. The plasma concentration of glycy...

journal_title：Biopharmaceutics & drug disposition

authors： Yamamura Y,Tanaka N,Santa T,Kotaki H,Aikawa T,Uchino K,Osuga T,Sawada Y,Iga T

更新日期：1995-01-01 00:00:00

abstract：:Six healthy lactating women ranging in age from 28 to 35 years were selected to participate in the study. The women had been nursing their infants from 3 1/2 weeks up to 17 weeks. On the morning of the study each participant received 100 mg dose of caffeine. The oral dose of caffeine was taken with a glass of water on...

journal_title：Biopharmaceutics & drug disposition

authors： Stavchansky S,Combs A,Sagraves R,Delgado M,Joshi A

更新日期：1988-05-01 00:00:00

abstract：:The effects of differences in the rate and composition of intravenous fluid replacement for urine loss on the pharmacokinetics and pharmacodynamics of azosemide were evaluated using rabbit as the animal model. Each rabbit received a 4h constant intravenous infusion of 1 mg kg-1 azosemide with 0% replacement (treatment...

journal_title：Biopharmaceutics & drug disposition

authors： Park KJ,Yoon WH,Shin WG,Lee MG

更新日期：1997-10-01 00:00:00

abstract：:Sulfotransferase (SULT) 1A1 and SULT1A3 play important roles in the presystemic inactivation of beta(2) agonists in the liver and intestine, respectively. The study aimed to investigate the inhibitory effects of grapefruit juice, orange juice, green tea, black tea and oolong tea and their constituents on the activitie...

journal_title：Biopharmaceutics & drug disposition

authors： Nishimuta H,Ohtani H,Tsujimoto M,Ogura K,Hiratsuka A,Sawada Y

更新日期：2007-12-01 00:00:00

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

authors： Arnold TH,Tackett RL,Vallner JJ

更新日期：1985-10-01 00:00:00

abstract：:MDL 26479 is a new drug undergoing clinical evaluation for the treatment of depression and for memory loss associated with Alzheimer's disease. As part of a dose tolerance trial, the single- (SD) and multiple-dose (MD) pharmacokinetics of MDL 26479 were evaluated in healthy male volunteers. SDs ranging from 2 to 465 m...

journal_title：Biopharmaceutics & drug disposition

authors： Robbins DK,Hutcheson SJ,Miller TD,Green VI,Bhargava VO,Weir SJ

更新日期：1997-05-01 00:00:00

abstract：AIMS:To study the dose-ranging population pharmacokinetics of controlled release verapamil in healthy subjects and patients with angina or hypertension. To characterize the pharmacodynamics of controlled-release verapamil in patients with hypertension. METHODS:Dose-ranging studies were conducted in healthy volunteers ...

journal_title：Biopharmaceutics & drug disposition

authors： Gupta S,Modi NB,Sathyan G,Ho Pl PL,Aarons L

更新日期：2002-01-01 00:00:00

abstract：:Comparative in vivo studies of aqueous solution, multiple w/o/w, and w/o emulsions showed that formulating 5-fluorouracil in emulsion systems significantly sustained the release of the drug from intramuscular injection sites in the rat. Intramuscular injection of the drug in both w/o and w/o/w emulsion systems produce...

journal_title：Biopharmaceutics & drug disposition

authors： Omotosho JA,Whateley TL,Florence AT

更新日期：1989-05-01 00:00:00

abstract：:The oral pharmacokinetics (concentration-time profile) of four proprietary compounds in humans were predicted using the C(vss)-MRT method. The first step was to demonstrate superposition of intravenous (i.v.) pharmacokinetic profiles of preclinical species following mathematical transformation of their respective conc...

journal_title：Biopharmaceutics & drug disposition

authors： Fura A,Vyas V,Humphreys W,Chimalokonda A,Rodrigues D

更新日期：2008-11-01 00:00:00

abstract：:BMS-378806 is a prototype of novel HIV attachment inhibitors that block the gp120 and CD4 interaction, the first step of HIV-1 entry into cells. The present work investigated the pharmacokinetics of BMS-378806 in rats, dogs and monkeys and assessed its in vitro permeability and metabolism. BMS-378806 exhibited species...

journal_title：Biopharmaceutics & drug disposition

authors： Yang Z,Zadjura L,D'Arienzo C,Marino A,Santone K,Klunk L,Greene D,Lin PF,Colonno R,Wang T,Meanwell N,Hansel S

更新日期：2005-12-01 00:00:00

abstract：:The systemic availability of a solid dispersion (coevaporate) of clofazimine (CLF) in poly(vinyl methyl ether maleic anhydride) copolymer (PVM/MA) was tested in the pig. Single 100 mg oral doses of the coevaporate and the commercial product, Lamprene (Ciba-Geigy) were administered on separate occasions (separated by a...

journal_title：Biopharmaceutics & drug disposition

authors： Krishnan TR,Abraham I

更新日期：1994-05-01 00:00:00

abstract：:The pharmacokinetics and the dose proportionality of a new anticonvulsant compound, HEPP (D,L-3-hydroxy-3-ethyl-3-phenylpropionamide) was studied in healthy male volunteers as part of the pharmacological evaluation for new drugs. Study was performed administering doses of 250, 375, 500 and 625 mg of HEPP to six male v...

journal_title：Biopharmaceutics & drug disposition

authors： González-Esquivel DF,Rubio-Donnadieu F,Carvajal-Sandoval G,Jung HC

更新日期：1998-12-01 00:00:00

abstract：:We present a novel method for performing pharmacokinetic and metabolism studies on macromolecules that offers advantages over the existing techniques of radiolabeling, immunoassay or bioassays. Our strategy uses macromolecules with stable isotopes uniformly distributed throughout the structure. The stable isotope enri...

journal_title：Biopharmaceutics & drug disposition

authors： Osborn BL,Abramson FP

更新日期：1998-10-01 00:00:00

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

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

更新日期：2004-04-01 00:00:00

abstract：:Circadian variations in disposition have been observed for a variety of agents, including anticonvulsants. Valproic acid (VPA), an anticonvulsant used to control generalized and partial seizures, has exhibited diurnal oscillations in steady-state concentrations during long-term administration to humans and non-human p...

journal_title：Biopharmaceutics & drug disposition

authors： Arens TL,Pollack GM

更新日期：2001-09-01 00:00:00

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

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

更新日期：1993-05-01 00:00:00

abstract：:Many marketed drugs are chiral and are administered as the racemate, a 50:50 combination of two enantiomers. Pharmacodynamic and pharmacokinetic differences between enantiomers are well documented. Because of enantioselectivity in pharmacokinetics, results of in vitro pharmacodynamic studies involving enantiomers may ...

journal_title：Biopharmaceutics & drug disposition

authors： Brocks DR

更新日期：2006-11-01 00:00:00

abstract：:Methotrexate (MTX) is an anchor drug used to treat rheumatoid arthritis (RA), but responsiveness is variable in effectiveness and toxicity. Methotrexate and its polyglutamate conjugates (MTXPG(n)) in red blood cells (RBC) have been associated with patient response. In the current study, 13 collagen-induced arthritic (...

journal_title：Biopharmaceutics & drug disposition

authors： Liu DY,Lon HK,Wang YL,DuBois DC,Almon RR,Jusko WJ

更新日期：2013-05-01 00:00:00