Enantioselective pharmacokinetics in animals of pazinaclone, a new isoindoline anxiolytic, and its active metabolite.

abstract：:Stobadin dihydrochloride was administered p.o. to rats at a dose of 1 mg kg-1 once daily for 25 consecutive days. The peak and trough concentrations of the sum of stobadin metabolites, determined from Days 6-16 of treatment, demonstrated a steady-state. The mean daily excretion of 3H-radioactivity during this period w...

journal_title：Biopharmaceutics & drug disposition

authors： Kállay Z,Soltés L,Trnovec T

更新日期：1991-04-01 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：:Previously we demonstrated that a hydrophilic HMG-CoA reductase inhibitor, pravastatin, was actively taken up by the liver via the 'multispecific anion transporter' using isolated rat hepatocytes (M. Yamazaki, H. Suzuki, M. Hanano, T. Tokui, T. Komai, and Y. Sugiyama, Am. J. Physiol., 264, G36-G44 (1993)). Such a carr...

journal_title：Biopharmaceutics & drug disposition

authors： Yamazaki M,Tokui T,Ishigami M,Sugiyama Y

更新日期：1996-12-01 00:00:00

abstract：:Zopiclone is a new sedative showing a rapid onset of hypnotic effect and a relatively short duration of action. The goal of this study was to assess the kinetic parameters of zopiclone and its interaction with trimipramine when administered concomitantly. Ten normal subjects each received doses of zopiclone (7.5 mg), ...

journal_title：Biopharmaceutics & drug disposition

authors： Caille G,du Souich P,Spenard J,Lacasse Y,Vezina M

更新日期：1984-04-01 00:00:00

abstract：:The pharmacokinetic regularity of the murine monoclonal antibody ior EGF/r3 across mammals was studied using allometry. The allometric relationship between the volume of distribution and body weight (W) across mammalian species was characterized by the power equation V(d)=218.8 W(0.84) (r=0.92), and that for clearance...

journal_title：Biopharmaceutics & drug disposition

authors： Ducongé J,Fernández-Sánchez E,Alvarez D

更新日期：2004-05-01 00:00:00

abstract：:Acute viral infection has long been recognized to down-regulate cytochrome P-450 enzymes and subsequently to result in changes in the pharmacological and toxicological responses to xenobiotics. In our previous research, chronic retrovirus infection induced by inoculating a susceptible strain of mice with LP-BM5 murine...

journal_title：Biopharmaceutics & drug disposition

authors： Chow HH,Tang Y,Li P,Brookshier G,Liang B,Watson R

更新日期：1998-01-01 00:00:00

abstract：:Dihydroergotoxine is a mixture of semi-synthetic ergot alkaloids mainly used for age-related cognitive impairment. In this study, dihydroergotoxine (30 microM) was added to incubates of rat and bovine liver microsomes, and the resulting major metabolites were identified as hydroxy-dihydroergocornine, hydroxy-dihydroer...

journal_title：Biopharmaceutics & drug disposition

authors： Bicalho B,Giolo JM,Lilla S,De Nucci G

更新日期：2008-01-01 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：:It was reported that gastric motility was delayed and gastric acid secretion was reduced in vagotomized dogs which mimics a low gastric acidity in humans. A delay in gastric motility causes long residence of amlodipine in the stomach. More unionized fractions of amlodipine could exist in less acidic conditions of gast...

journal_title：Biopharmaceutics & drug disposition

authors： Kwak HH,Kim JO,Chung HK,Choi SM,Kim JH,Kwon JW,Yoo M,Lee JH,Lee MG

更新日期：2006-04-01 00:00:00

abstract：:The inhibition of rat hepatic mitochondrial aldehyde dehydrogenase (ALDH) isozymes was studied in apparent steady-state conditions after repeated intra-peritoneal cyanamide administration. The low-Km mitochondrial ALDH isozyme was more susceptible to cyanamide-induced inhibition (DI50 = 0.104 mg kg-1) than the high-Km...

journal_title：Biopharmaceutics & drug disposition

authors： Pruñonosa Piera J,Obach R,Sagristá ML,Bozal J

更新日期：1993-07-01 00:00:00

abstract：:A semisolid self-emulsifying system (SES) of itraconazole consisting of oleic acid, polysorbate 80 and coajuvant (citric acid) was prepared by a hot-melt technique and then compared with hydroxypropylmethylcellulose (HPMC) solid dispersion (SD) coated onto inert sugar spheres as a reference formulation for in vitro an...

journal_title：Biopharmaceutics & drug disposition

authors： Park MJ,Ren S,Lee BJ

更新日期：2007-05-01 00:00:00

abstract：:The bioavailability of orally administered therapies are often significantly limited in the human intestine by the metabolic activities of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp). Predicting whether candidate compounds induce CYP3A4 and P-gp is a crucial stage in the drug development process, as drug-dr...

journal_title：Biopharmaceutics & drug disposition

authors： Inami K,Sasaki T,Kumagai T,Nagata K

更新日期：2015-04-01 00:00:00

abstract：:Telaprevir, a chronic hepatitis C virus (HCV) protease inhibitor, is known to be a cytochrome P450 (CYP) 3A4/5 substrate and inhibitor. In the present study, the in vitro inhibitory effect of telaprevir on the metabolism of tacrolimus in human liver microsomes was investigated using 13-O-demethyltacrolimus (M-I) as a ...

journal_title：Biopharmaceutics & drug disposition

authors： Oda K,Yamano K

更新日期：2014-12-01 00:00:00

abstract：:The influence of caffeine (60 mg) was studied on the pharmacokinetic characteristics of acetaminophen (500 mg single dose) in ten healthy male human volunteers in a complete cross-over design. A high-performance liquid chromatography (HPLC) method was used to analyse serum drug concentrations. Caffeine caused a highly...

journal_title：Biopharmaceutics & drug disposition

authors： Iqbal N,Ahmad B,Janbaz KH,Gilani AU,Niazi SK

更新日期：1995-08-01 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：: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：:Beta-adrenoceptor blocking drugs are widely used as effective antihypertensive and antianginal agents. We have determined the effect of beta-blockade in the rat to ascertain whether there are differences between metoprolol (MET) and acebutolol (AC) with respect to regional blood flow (RBF). Both AC and MET were admini...

journal_title：Biopharmaceutics & drug disposition

authors： Mostafavi S,Lewanczuk R,Foster R

更新日期：2000-05-01 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：:Multidrug resistance (MDR) is common in patients and has been linked to transforming growth factor-β1 (TGF-β1) and overexpression of drug efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), although the molecular mechanisms remain largely unknown. This study aimed to investigate the ...

journal_title：Biopharmaceutics & drug disposition

authors： Kong J,Qiu Y,Li Y,Zhang H,Wang W

更新日期：2019-02-01 00:00:00

abstract：:Equilibrative nucleoside transporters (ENTs) 1 and 2 reportedly accept fluorouracil as a substrate. Here, we evaluated ENT1/2 expression at the messenger RNA (mRNA), protein, and functional levels in a panel of four triple-negative breast cancer (TNBC) cell lines, BT-549, Hs578T, MDA-MB-231, and MDA-MB-435, and we exa...

journal_title：Biopharmaceutics & drug disposition

authors： Noguchi S,Takagi A,Tanaka T,Takahashi Y,Pan X,Kibayashi Y,Mizokami R,Nishimura T,Tomi M

更新日期：2021-01-10 00:00:00

abstract：:This study assessed steady-state azimilide pharmacokinetics and pharmacodynamics in 119 healthy male and female volunteers. Parallel groups of 18-40-year-old subjects received doses of 35, 100, 150 or 200 mg day(-1) for up to 14 days, with 1, 2 or 3 days of loading. Another group of > 55-year-old subjects received 100...

journal_title：Biopharmaceutics & drug disposition

authors： Corey A,Al-Khalidi H,Brezovic C,Marcello S,Parekh N,Taylor K,Karam R

更新日期：1999-03-01 00:00:00

abstract：:The effect of water deprivation on the physiologic, biochemical, and disposition parameters of erythromycin was investigated in rabbits. The packed cell volume, plasma glucose, and total lipid concentration increased significantly in dehydration. The pharmacokinetic parameters of erythromycin after intravenous adminis...

journal_title：Biopharmaceutics & drug disposition

authors： Ahmad M,Niazi SK,Ahmad T,Muzaffar NA,Nawaz M

更新日期：1992-03-01 00:00:00

abstract：:The bioavailability of an improved formulation of enteric-coated phenylbutazone with faster dissolution, more consistent in vitro rate of drug release and improved stability was compared in 8 normal subjects at doses of 100 and 200 mg with commercially available Butacote. Phenylbutazone was more rapidly absorbed from ...

journal_title：Biopharmaceutics & drug disposition

authors： John VA,Goldsborough S,Morrison PJ,Rogers HJ,Spector RG,Bradbrook ID

更新日期：1982-01-01 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 bioequivalence of three oral forms of nifedipine was assessed in a triple crossover study on 12 healthy volunteers. Single 10 mg dose was given and ten blood samples were drawn during the first 8 h after administration. Highly sensitive gas chromatographic method was used for the nifedipine assay. Pharmacokinetic ...

journal_title：Biopharmaceutics & drug disposition

authors： Kozjek F,Primozic S,Mrhar A,Karba R,Raemsch KD,Janezic A

更新日期：1987-01-01 00:00:00

abstract：:Radix Scutellariae (RS) and Coptis Chinensis (CC) are the most popular components in traditional Chinese medicine prescriptions. Flavonoids are the main effective ingredients in RS and berberine is the main effective ingredient in CC. The aim of this study was to determine the influence of CC on the pharmacokinetics o...

journal_title：Biopharmaceutics & drug disposition

authors： Shi R,Zhou H,Liu Z,Ma Y,Wang T,Liu Y,Wang C

更新日期：2009-10-01 00:00:00

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

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

更新日期：2009-10-01 00:00:00

abstract：:The pharmacokinetics and pharmacodynamics of torasemide were evaluated after intravenous administration of the same total dose of torasemide at a dose of 1mg/kg to rabbits with different infusion times, 1 min (treatment I), 30 min (treatment II) and 2 h (treatment III). The loss of water and electrolytes in urine indu...

journal_title：Biopharmaceutics & drug disposition

authors： Kim YC,Lee MG,Ko SH,Kim SH

更新日期：2004-07-01 00:00:00

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

authors： Dave RA,Morris ME

更新日期：2016-07-01 00:00:00

abstract：:Pharmacokinetics in rabbits following intravenous administration and in vitro protein binding were studied for two new salts of erythromycin (erythromycin maltobionate and erythromycin fumarate). Serum erythromycin levels following intravenous injection were described by two compartment model kinetics, and values for ...

journal_title：Biopharmaceutics & drug disposition

authors： Basu SK,Manna PK,Goswami BB

更新日期：1992-08-01 00:00:00