Drug disposition in three dimensions: an update on stereoselectivity in pharmacokinetics.

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：:The pharmacokinetics of didanosine and ciprofloxacin were evaluated following the administration of multiple oral doses of each drug as a single agent or in combination. Didanosine was dosed as the Videx chewable/dispersible tablet, which contains the antacids dihydroxyaluminum sodium carbonate and magnesium hydroxide...

journal_title：Biopharmaceutics & drug disposition

authors： Knupp CA,Barbhaiya RH

更新日期：1997-01-01 00:00:00

abstract：:The steady-state pharmacokinetics of an ultralong sustained release formulation of theophylline (Unilong) twice daily (bid) in elderly hospitalized patients suffering from chronic obstructive pulmonary disease (COPD) have been studied in order to establish guidelines for monitoring. The study was carried out in 37 pat...

journal_title：Biopharmaceutics & drug disposition

authors： Armijo JA,Sánchez BM,Peralta FG,González-Ruiz M,Cuadrado A,Verdejo A,Cos MA,Arjona R

更新日期：2003-05-01 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 study sought to investigate the effect of genetic variants of OCT1 (OCT1-P283L and -P341L) and OCT2 (OCT2-T199I, -T201M and -A270S), which were identified in a Korean population, on the transport of lamivudine in vitro and to compare the substrate dependent effects of OCT1 and OCT2 variants with 1-methyl-4-phenylp...

journal_title：Biopharmaceutics & drug disposition

authors： Choi MK,Song IS

更新日期：2012-04-01 00:00:00

abstract：:A new sustained release dosage form of valproic acid (VPA) was developed. The new sustained release dosage form was administered (twice, with and without food) to five dogs in comparison to a standard tablet (Depakine, Labaz) and an i.v. preparation of the drug. Drug level monitoring in the plasma was performed by a G...

journal_title：Biopharmaceutics & drug disposition

authors： Bialer M,Friedman M,Dubrovsky J

更新日期：1984-01-01 00:00:00

abstract：:The effects of gender on the pharmacokinetics of verapamil and its active metabolite, norverapamil, following single oral dose (80 mg, Isoptin) to 12 healthy male (mean age: 25.75+/-2.42 years, mean body weight: 70.59+/-9.94 kg) and 12 healthy female subjects (mean age: 24.08+/-2.84 years, mean body weight: 56.67+/-5....

journal_title：Biopharmaceutics & drug disposition

authors： Dadashzadeh S,Javadian B,Sadeghian S

更新日期：2006-10-01 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：: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：:The present study aimed to investigate the effect of atorvastatin on the intravenous and oral pharmacokinetics of verapamil in rats. The pharmacokinetic parameters of verapamil were measured after an oral (9 mg/kg) or intravenous (3 mg/kg) administration of verapamil to rats in the presence and absence of atorvastatin...

journal_title：Biopharmaceutics & drug disposition

authors： Choi DH,Chang KS,Hong SP,Choi JS,Han HK

更新日期：2008-01-01 00:00:00

abstract：:The mechanism of intestinal transport of valacyclovir (VACV), the L-valyl ester prodrug of acyclovir, was investigated in rats using an in situ intestinal perfusion technique. VACV demonstrates an oral bioavailability that is three to five time greater than acyclovir, concentration dependent, and saturable in humans. ...

journal_title：Biopharmaceutics & drug disposition

authors： Sinko PJ,Balimane PV

更新日期：1998-05-01 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 comparative bioavailability and steady state fluctuations resulting from the administration of Tegretol 200 mg commercial tablets and carbamazepine OROS controlled delivery tablets were investigated in 22 adult and 12 pediatric epileptic patients. Tegretol commercial tablets were dosed according to previously esta...

journal_title：Biopharmaceutics & drug disposition

authors： Thakker KM,Mangat S,Garnett WR,Levy RH,Kochak GM

更新日期：1992-11-01 00:00:00

abstract：:Reducing the maximum plasma concentration whilst maintaining the exposure was shown to ameliorate adverse events following the oral administration of 6-hydroxybuspirone. This observation, along with a desire to provide for once daily dosing of this compound, provided the basis for the development of an extended releas...

journal_title：Biopharmaceutics & drug disposition

authors： Nicholson SJ,Timmins P,Dockens RC,Connor A,Croop R,Ferrie P,Zeng J,Dennis AB,Wilding I

更新日期：2012-12-01 00:00:00

abstract：:Ciclesonide, a new corticosteroid for allergic rhinitis, is administered as an inactive parent compound that is converted by esterases to the pharmacologically active metabolite, desisobutyryl-ciclesonide (des-CIC). This study investigated the in vitro activation of ciclesonide in nasal mucosa of multiple animal speci...

journal_title：Biopharmaceutics & drug disposition

authors： Sato H,Nave R,Nonaka T,Mochizuki T,Takahama S,Kondo S

更新日期：2007-03-01 00:00:00

abstract：:The following results were obtained recently from our laboratories; in rats with 72-h water deprivation (rats with dehydration), the hepatic cytochrome P450 2E1 (CYP2E1) was three-fold induced with an increase in the mRNA. Rehydration of 48-h water-deprived rats for the next 24 h with free access of food (rats with re...

journal_title：Biopharmaceutics & drug disposition

authors： Kim YC,Kim YG,Kim EJ,Cho MK,Kim SG,Lee MG

更新日期：2003-03-01 00:00:00

abstract：:The citrus flavonoid hesperetin (4'-methoxy-3',5,7-trihydroxyflavanone) is the aglycone of hesperidin, the major flavonoid present in sweet oranges. Hesperetin 7-O-glucuronide (H7G) and hesperetin 3'-O-glucuronide (H3'G) are the two most abundant metabolites of hesperetin in vivo. In this study, their interaction with...

journal_title：Biopharmaceutics & drug disposition

authors： Brand W,Oosterhuis B,Krajcsi P,Barron D,Dionisi F,van Bladeren PJ,Rietjens IM,Williamson G

更新日期：2011-12-01 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 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：:An evaluation of the literature indicated that certain aspects of the disposition kinetics of iothalamate, important to the accurate determination of glomerular filtration rate in dogs and humans, remain to be resolved. The simultaneous clearances of iothalamate and inulin in 5 dogs were determined at three steady-sta...

journal_title：Biopharmaceutics & drug disposition

authors： Prueksaritanont T,Lui CY,Lee MG,Chiou WL

更新日期：1986-07-01 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：: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 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：: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：:Understanding the performance of a drug product in vivo plays a key role in the development of meaningful in vitro drug release methodology. In case of functional chewing gums, the mode and the mechanism of release and the site of application differ significantly from other conventional solid oral dosage forms and req...

journal_title：Biopharmaceutics & drug disposition

authors： Gajendran J,Kraemer J,Langguth P

更新日期：2012-10-01 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：: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：: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：:p-hydroxymethamphetamine (OHMAP) is one of the major metabolites of the widely abused drug methamphetamine (MAP). The demethylation of OHMAP to p-hydroxyamphetamine (OHAP) has been shown in vitro but has never been reported in vivo. The disposition kinetics as well as the metabolism of OHMAP was investigated employing...

journal_title：Biopharmaceutics & drug disposition

authors： Hutchaleelaha A,Mayersohn M

更新日期：1997-07-01 00:00:00

abstract：:The total body clearance (CL), renal clearance (CLR), and nonrenal clearance (CLNR) of caffeine from plasma were determined following the intravenous administration of caffeine (4 mg kg-1) to ten healthy men (aged 66-86 years) on three separate occasions. Positive correlations were observed between CL and urine flow r...

journal_title：Biopharmaceutics & drug disposition

authors： Trang JM,Blanchard J,Conrad KA,Harrison GG

更新日期：1985-01-01 00:00:00