Acyl glucuronides: the good, the bad and the ugly.

abstract：:The first day test dose versus steady-state relationship for predicting drug doses was evaluated for the situation where metabolites are produced. An organ clearance model incorporated into a digital computer program simulated drug and metabolite disposition. When the terminal elimination rate for metabolite was simil...

journal_title：Biopharmaceutics & drug disposition

authors： Devane CL,Jusko WJ

更新日期：1983-01-01 00:00:00

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

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

abstract：:The intestinal absorptive characteristics and the efflux mechanisms of candesartan (CDS), a novel angiotensin II type 1 receptor blocker, were investigated. The Caco-2 cells were used as models of the intestinal mucosa to assess uptake and transport of CDS. The determination of CDS was performed by HPLC-Flu. In the Ca...

journal_title：Biopharmaceutics & drug disposition

authors： Zhou L,Chen X,Gu Y,Liang J

更新日期：2009-07-01 00:00:00

abstract：:Gastrointestinal distress resulting from drug intake is often remedied by administering the drug with antacids. However, antacids have been shown to modify the absorption and excretion of many drugs. This study was designed to delineate the effects of aluminium and magnesium hydroxide antacid suspension (Maalox) on th...

journal_title：Biopharmaceutics & drug disposition

authors： Caillé G,du Souich P,Vézina M,Pollock SR,Stalker DJ

更新日期：1989-11-01 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：: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 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 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：: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：: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

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

更新日期：1992-10-01 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：: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：: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：: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

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

更新日期：1992-05-01 00:00:00

abstract：:The absorption characteristics of ethiofos were studied using the rat in situ intestine circulating perfusion technique. Slow absorption kinetics were observed for ethiofos with varying rates of absorption and metabolism/degradation in situ as a function of buffer and absorption enhancers. In most cases less than 10 p...

journal_title：Biopharmaceutics & drug disposition

authors： Geary RS,Swynnerton NF,Timmons SF,Mangold DJ

更新日期：1991-05-01 00:00:00

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

authors： Eddington ND,Adekoya F,Kharidia J

更新日期：1998-07-01 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 relative lung and systemic bioavailability of sodium cromoglycate following inhalation by different methods have been determined using a urinary excretion pharmacokinetic method. On three separate randomised study days, 7 days apart, subjects inhaled (i) 4x5 mg from an Intal metered dose inhaler (MDI), (ii) 4x5 mg...

journal_title：Biopharmaceutics & drug disposition

authors： Aswania O,Chrystyn H

更新日期：2002-05-01 00:00:00

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

authors： Denson DD,Thompson GA,Coyle DE

更新日期：1986-03-01 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：:EMA401, (the S-enantiomer of 5-(benzyloxy)-2-(2,2-diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid), also known as Olodanrigan, is an orally active selective angiotensin II type 2 receptor (AT2 R) antagonist that is in Phase IIb clinical development as a novel analgesic for the relief of chro...

journal_title：Biopharmaceutics & drug disposition

authors： Murgasova R,Carreras ET,Suetterlin-Hachmann M,da Silva Torrao LR,Kittelmann M,Alexandra V,Fredenhagen A

更新日期：2020-04-01 00:00:00

abstract：:The definitions of mean residence time of drug molecules in the body (MRT) from the literature are reviewed. A formal definition of MRT, based on excretion of drug molecules and amount of drug, a parameter which is independent of constancy of both clearance and volume of distribution, is introduced and compared to oth...

journal_title：Biopharmaceutics & drug disposition

authors： Kasuya Y,Hirayama H,Kubota N,Pang KS

更新日期：1987-05-01 00:00:00

abstract：:Infliximab (IFX) is used as a therapeutic agent for ulcerative colitis (UC) and Crohn's disease (CD). Although the dosage regimen has been established through clinical trial experience, it has yet to be assessed with a pharmacokinetic and pharmacodynamic model. The present study analysed sequential changes of clinical...

journal_title：Biopharmaceutics & drug disposition

authors： Kimura K,Yoshida A,Katagiri F,Takayanagi R,Yamada Y

更新日期：2019-07-01 00:00:00

abstract：:The effect of the combination of a new anticonvulsant drug HEPP and carbamazepine (CBZ) on the pharmacokinetics of HEPP and CBZ was investigated using rabbits as an animal model. The study was performed in 18 male New Zealand white rabbits which were randomly divided into three groups, according to a balanced incomple...

journal_title：Biopharmaceutics & drug disposition

authors： García AL,Medina RL,Pérez MR,Jung CH

更新日期：2003-07-01 00:00:00

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

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

abstract：:Twenty-four healthy volunteers, aged 21-59 years, received single 30 mg oral doses of the benzodiazepine hypnotic temazepam. Levels of intact temazepam were determined in multiple plasma samples drawn during 48 h after dosage. Intact temazepam, its direct glucuronide conjugate, and the conjugate of its demethylated (o...

journal_title：Biopharmaceutics & drug disposition

authors： Locniskar A,Greenblatt DJ

更新日期：1990-08-01 00:00:00

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

authors： Shord SS,Camp JR

更新日期：2006-05-01 00:00:00

abstract：:The pharmacokinetics of a non-narcotic analgesic, DA-5018, were compared after single intravenous (i.v.), subcutaneous (s.c.), and oral administrations, and after multiple (seven consecutive days) s.c. administration to rats. After i.v. administration of DA-5018, 1, 2, and 5 mg kg-1, the pharmacokinetic parameters of ...

journal_title：Biopharmaceutics & drug disposition

authors： Lee JJ,Shim HJ,Kim SH,Lee SD,Kim WB,Yang J,Lee MG

更新日期：1998-03-01 00:00:00

abstract：:This study aims to characterize the pharmacodynamic properties of denosumab, a RANK ligand inhibitor, and ibandronate, a bisphosphonate, using an integrated bone homeostasis model in postmenopausal women. Mean temporal profiles of denosumab, serum and urine N-telopeptide (sNTX, uNTX), lumbar spine bone mineral density...

journal_title：Biopharmaceutics & drug disposition

authors： Marathe DD,Marathe A,Mager DE

更新日期：2011-11-01 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