Pharmacokinetics and pharmacodynamics of mivacurium stereoisomers in beagle dogs using twitch height and train-of-four response.

abstract：:The lipophilic weak base amodiaquine is an antimalarial drug that has been in use for over 40 years. Little is known of amodiaquine's mechanism of transport across membranes. Transport experiments of amodiaquine in Caco-2 cells showed a low recovery of 30% and rapid disappearance from the apical chamber. Compounds str...

journal_title：Biopharmaceutics & drug disposition

authors： Hayeshi R,Masimirembwa C,Mukanganyama S,Ungell AL

更新日期：2008-09-01 00:00:00

abstract：:The hypothesis that higher molecular weight (MW) quaternary ammoniums (QAs) form lipophilic ion-pair complexes with bile salts in the liver, and are subsequently excreted into bile via a canalicular transporter, P-gp, was re-examined in the present study for its validity. The biliary excretion of tributylmethyl ammoni...

journal_title：Biopharmaceutics & drug disposition

authors： Choi MK,Song IS,Kim DD,Chung SJ,Shim CK

更新日期：2007-12-01 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：: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：:A major component of physiologically based pharmacokinetic (PBPK) models is the prediction of the rate and extent of absorption of orally dosed drugs for which knowledge of effective passive intestinal permeability (Peff ) is essential. Single-pass intestinal perfusion (SPIP) studies are used to establish effective pe...

journal_title：Biopharmaceutics & drug disposition

authors： Pade D,Jamei M,Rostami-Hodjegan A,Turner DB

更新日期：2017-03-01 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：:Sulforaphane (SFN) is an isothiocyanate that is present in widely consumed vegetables. Previous studies have shown that SFN is effective in preventing carcinogenesis induced by carcinogens in rodents. Recently it was found that SFN could also suppress the growth of intestinal polyps in the ApcMin/+ mouse. In the prese...

journal_title：Biopharmaceutics & drug disposition

authors： Khor TO,Hu R,Shen G,Jeong WS,Hebbar V,Chen C,Xu C,Nair S,Reddy B,Chada K,Kong AN

更新日期：2006-12-01 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：: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：: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：: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：PURPOSE:Amifostine is a prodrug in which selectivity is largely determined by the preferential formation and uptake of its cytoprotective metabolite, WR-1065, in normal tissues as a result of differences in membrane-bound alkaline phosphatase activity. It was hypothesized that amifostine may be a good candidate for reg...

journal_title：Biopharmaceutics & drug disposition

authors： Levi M,DeRemer SJ,Dou C,Ensminger WD,Smith DE

更新日期：2004-01-01 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：:'Casodex' (bicalutamide) is an orally active, non-steroidal, pure antiandrogen; it is a racemate with antiandrogenic activity residing predominantly in the (R)-enantiomer. Healthy male volunteers (n = 15) were administered single oral doses of bicalutamide (50 mg) after food and after fasting as part of a three-treatm...

journal_title：Biopharmaceutics & drug disposition

authors： Cockshott ID,Oliver SD,Young JJ,Cooper KJ,DC Jones

更新日期：1997-08-01 00:00:00

abstract：:The objective was to develop a population pharmacokinetic-pharmacodynamic model of caffeine's psychomotor effects in healthy, non-habitual users of caffeine. Twenty Chinese males each received a single dose of 250 mg of caffeine orally. Plasma concentrations of caffeine were determined at various times within 24 h aft...

journal_title：Biopharmaceutics & drug disposition

authors： Seng KY,Teo WL,Fun CY,Law YL,Lim CL

更新日期：2010-07-01 00:00:00

abstract：:Studies were designed to allow an in vivo estimation of the hepatic extraction ratio and to test the hypothesis that the pharmacokinetic parameters of (-)-CBV are significantly different during anesthesia. (-)-CBV was administered as an i.v. bolus followed by i.v. infusion into either the portal (n = 3) or the jugular...

journal_title：Biopharmaceutics & drug disposition

authors： Soria I,Zimmerman CL

更新日期：1995-05-01 00:00:00

abstract：:The pharmacokinetics and pharmacodynamics of furosemide were compared after an oral administration or a direct administration of Lasix into the duodenum in humans (40 mg). Furosemide was absorbed quickly after a direct administration of Lasix into the duodenum; the peak plasma concentration of furosemide was reached w...

journal_title：Biopharmaceutics & drug disposition

authors： Lee WI,Yoon WH,Shin WG,Song IS,Lee MG

更新日期：1997-12-01 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：:The study examined the effect of doxorubicin (DOX) on the hepatic expression of CYP2C and its activity for metabolizing tolbutamide (TB), a specific CYP2C substrate, in rats and whether the pharmacokinetics of tolbutamide were altered by doxorubicin exposure. The expression level of hepatic CYP2C11 was depressed 1 day...

journal_title：Biopharmaceutics & drug disposition

authors： Fukuno S,Nagai K,Yamamoto K,Tanimura T,Nabe T,Konishi H

更新日期：2019-07-01 00:00:00

abstract：:A pharmacokinetic study of sachets containing nalidixic acid (0.66 g) associated with sodium citrate (3.75 g)--NSC--was carried out in 10 healthy volunteers in order to determine the influence of the urine alcalinization due to sodium citrate on the elimination of nalidixic acid (NA) and its 7-hydroxy (HNA) and 7-carb...

journal_title：Biopharmaceutics & drug disposition

authors： Ferry N,Cuisinaud G,Sassard J,Pozet N,Zech PY

更新日期：1984-07-01 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：:A chiral gas chromatographic assay previously developed for quantitative analysis of ethosuximide and its major metabolites in rat urine has been adapted for the analysis of the drug in plasma. Ethosuximide, both as a racemic mixture and as the individual enantiomers, was administered to conscious rats by the intraven...

journal_title：Biopharmaceutics & drug disposition

authors： Mifsud J,Collier PS,Millership JS

更新日期：2001-03-01 00:00:00

abstract：:Oral doses of amygdalin and intraperitoneal (i.p.) doses of potassium cyanide (KCN) in the near-lethal range were administered to CD2F1 female mice. Blood cyanide levels were then measured as a function of time. The maximum cyanide level after amygdalin administration was reached at about 11/2 to 2 h and was within th...

journal_title：Biopharmaceutics & drug disposition

authors： Hill HZ,Backer R,Hill GJ 2nd

更新日期：1980-04-01 00:00:00

abstract：PURPOSE:The chromone derivative MBL-II-141, specifically designed to inhibit ABCG2, was previously demonstrated to combine strong inhibition potency, low toxicity and good efficiency in reversing resistance to irinotecan in a xenografted mouse model. Here, the pharmacokinetic interactions in mice between irinotecan, it...

journal_title：Biopharmaceutics & drug disposition

authors： Hénin E,Honorat M,Guitton J,Di Pietro A,Payen L,Tod M

更新日期：2017-07-01 00:00:00

abstract：:In a double-blind, placebo-controlled, single-dose ascending pharmacokinetics and tolerance study, we evaluated the bispyridinium oxime HI-6 dichloride monohydrate (62.5, 125, 250, and 500 mg), administered intramuscularly with atropine sulphate, 2 mg, in 24 healthy male volunteers. The plasma HI-6 peak concentration ...

journal_title：Biopharmaceutics & drug disposition

authors： Clement JG,Bailey DG,Madill HD,Tran LT,Spence JD

更新日期：1995-07-01 00:00:00

abstract：:The bioavailability of the thiazide diuretic bemetizide from a tablet containing 25 mg of this drug and 50 mg of the chemically unrelated diuretic triamterene was lower than, and significantly different (p less than 0.01) from that from a tablet containing 25 mg bemetizide alone. The mean peak plasma level of bemetizi...

journal_title：Biopharmaceutics & drug disposition

authors： Brodie RR,Chasseaud LF,Darragh A,Taylor T,Walmsley LM

更新日期：1982-10-01 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：: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：: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：:Flow microcalorimetry was used to estimate primary binding constants for drug-albumin interactions. Measurements of heat of reaction at two temperatures illustrated the danger of extrapolation for pharmacokinetic purposes of measurements made at temperatures other than 37 degrees. The method could be used to predict c...

journal_title：Biopharmaceutics & drug disposition

authors： Hardee GH,Fleitman JS,Otagiri M,Perrin JH

更新日期：1984-10-01 00:00:00