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

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 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：:Data from sustained-release and enteric-coated oral formulations, and the suppository formulation of diclofenac sodium are fitted simultaneously using NONMEM and the general linear model, ADVAN 5. Absorption and disposition parameters, serum levels, and absorption profiles were determined. The in vivo absorption profi...

journal_title：Biopharmaceutics & drug disposition

authors： Idkaidek NM,Amidon GL,Smith DE,Najib NM,Hassan MM

更新日期：1998-04-01 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：: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：:A method for calculating the mean residence times of metabolites in the body, systemic circulation, and peripheral tissue is described. The calculations require the AUC, AUMC, and derivatives of the plasma concentration versus time curves of the metabolite and its precursor. The method is applicable to metabolites wit...

journal_title：Biopharmaceutics & drug disposition

authors： Cheng HY

更新日期：1991-07-01 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：: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 antimalarial drug, halofantrine, is chiral and is administered clinically as the racemate. In order to define the pharmacokinetic properties of halofantrine enantiomers in the rat, male Sprague-Dawley rats (264-311 g) were given halofantrine HCl orally (n = 5; 14 mg/kg) or intravenously (i.v.) (n = 5; 2 mg/kg). Pl...

journal_title：Biopharmaceutics & drug disposition

authors： Brocks DR,Toni JW

更新日期：1999-04-01 00:00:00

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

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

更新日期：1996-01-01 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

abstract：:Cardizem SR and Bi-Tildiem were both approved in their respective countries on the basis of clinical trials demonstrating efficacy and safety in the treatment of angina pectoris. In this cross-over randomized study, we assessed whether these two sustained-release formulations of diltiazem have equivalent pharmacokinet...

journal_title：Biopharmaceutics & drug disposition

authors： Guimont S,Landriault H,Klischer K,Grace M,Lambert C,Caillé G,Gossard D,Russell A,Raymond M,Hutchings E

更新日期：1993-12-01 00:00:00

abstract：AIM:The aim of this study was to build and verify a preliminary physiologically based pharmacokinetic (PBPK) model of Chinese pregnant women. The model was used to predict maternal pharmacokinetics (PK) of 6 predominantly renally cleared drugs. METHOD:Based on SimCYP Caucasian pregnancy population dataset, the prelimi...

journal_title：Biopharmaceutics & drug disposition

authors： Song L,Yu Z,Xu Y,Li X,Liu X,Liu D,Zhou T

更新日期：2020-06-01 00:00:00

abstract：:The plasma levels and tissue penetration of pefloxacin were studied after prophylactic administration to patients undergoing elective biliary surgery. Pefloxacin was administered as a single dose of 800 mg given intravenously as an infusion 1 h before surgery. Over a period of two years, cultures of bile and stone wer...

journal_title：Biopharmaceutics & drug disposition

authors： Gascón AR,Campo E,Olea E,Hernández RM,Calvo B,Errasti J,Pedraz JL

更新日期：2002-10-01 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：: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 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：:Utilization of nitric oxide (NO) synthase (NOS) inhibitors to probe the role of NO in various central nervous system processes requires use of an inhibitor selective for neuronal NOS, and is facilitated by knowledge of the pharmacokinetics of the inhibitor. The present project was undertaken to elucidate the dispositi...

journal_title：Biopharmaceutics & drug disposition

authors： Bush MA,Pollack GM

更新日期：2000-09-01 00:00:00

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

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

更新日期：2008-10-01 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：: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：:The objective of this study was to assess the effect of food on the pharmacokinetics of nefazodone (NEF). A group of 24 healthy adult male volunteers received a single 200 mg dose of NEF under fasting conditions as well as 5 min after a high-fat breakfast. There was a 1 week washout between treatments. Serial blood sa...

journal_title：Biopharmaceutics & drug disposition

authors： Dockens RC,Greene DS,Barbhaiya RH

更新日期：1996-03-01 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：:The inhibition potencies of aripiprazole and its active metabolite, dehydroaripiprazole, on the activities of human multidrug resistance protein 1 (MDR1/ABCB1; P-glycoprotein), breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated protein 4 (MRP4/ABCC4), that are drug efflux transporters ex...

journal_title：Biopharmaceutics & drug disposition

authors： Nagasaka Y,Oda K,Iwatsubo T,Kawamura A,Usui T

更新日期：2012-09-01 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：: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

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

更新日期：2008-01-01 00:00:00

abstract：:Biliary clearance (Clb) of sotalol (STL) enantiomers was assessed in anaesthetized Sprague-Dawley rats (419 +/- 9 g, mean +/- SEM, n = 4) following administration of a 10 mg kg-1 i.v. dose of the racemate. Clb for S- and R-STL (0.0675 +/- 0.0090 and 0.0662 +/- 0.0089 mL min-1 kg-1, respectively) represented approximat...

journal_title：Biopharmaceutics & drug disposition

authors： Carr RA,Pasutto FM,Foster RT

更新日期：1996-11-01 00:00:00

abstract：:The effects of age on hepatic microsomal enzyme induction were studied in male CD-1 mice. Six week old and 1 year old animals were treated with either phenobarbital (80 mg kg-1) or saline once daily for 3d. Twenty-four hours after the last treatment, animals were sacrificed and livers were harvested. Hepatic microsoma...

journal_title：Biopharmaceutics & drug disposition

authors： Charpentier KP,von Moltke LL,Poku JW,Harmatz JS,Shader RI,Greenblatt DJ

更新日期：1997-03-01 00:00:00

abstract：:Ritalin, an immediate release form of racemic methylphenidate hydrochloride, has been available in the USA since 1955 and is used for the treatment of ADHD. The objective of this study was to evaluate the pharmacokinetics of modified-release methylphenidate (highest single dose), Ritalin LA, when administered under fa...

journal_title：Biopharmaceutics & drug disposition

authors： Lee L,Kepple J,Wang Y,Freestone S,Bakhtiar R,Wang Y,Hossain M

更新日期：2003-09-01 00:00:00

abstract：:A relative bioavailability study of conventional tablet of propranolol hydrochloride was conducted in a group of 18 healthy volunteers employing the innovator's product as the reference tablet formation. Based on plasma levels of propranolol for the 24 h following administration of 2 x 40 mg oral propranolol hydrochlo...

journal_title：Biopharmaceutics & drug disposition

authors： Roscoe R,Cooper J,Wilson TW,Joshi NN,Midha KK

更新日期：1982-04-01 00:00:00