Safety, tolerability and pharmacokinetics of 2-pyridylacetic acid, a major metabolite of betahistine, in a phase 1 dose escalation study in subjects with ADHD.

abstract：:The objective of this study was to investigate the absorption behavior of chikusetsusaponin IVa (CHS-IVa) in the rat intestine using single-pass intestinal perfusion (SPIP) and to classify CHS-IVa into the biopharmaceutics classification system (BCS). The equilibrium solubility of CHS-IVa was determined by the shaker ...

journal_title：Biopharmaceutics & drug disposition

authors： Zhang W,Liu H,Liu C

更新日期：2019-09-01 00:00:00

abstract：:Vitamin K antagonists (VKAs) remain the oral anticoagulant of choice in venous thromboembolic disease. These drugs are characterized by a large inter-individual variability requiring frequent dose tailoring. Genetic polymorphisms for cytochrome CYP2C9 and VKORC1 explain some of the variability, especially in warfarin ...

journal_title：Biopharmaceutics & drug disposition

authors： Espana B,Couturier S,Prouillac C

更新日期：2017-01-01 00:00:00

abstract：:The pharmacokinetics and the dose proportionality of a new anticonvulsant compound, HEPP (D,L-3-hydroxy-3-ethyl-3-phenylpropionamide) was studied in healthy male volunteers as part of the pharmacological evaluation for new drugs. Study was performed administering doses of 250, 375, 500 and 625 mg of HEPP to six male v...

journal_title：Biopharmaceutics & drug disposition

authors： González-Esquivel DF,Rubio-Donnadieu F,Carvajal-Sandoval G,Jung HC

更新日期：1998-12-01 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：:An equation based on the absorption potential concept was developed. This enabled us to establish an approach for the quantitative prediction of the fraction of dose absorbed. Classification of drugs into three broad categories, according to their absorption potential values in relation to the fraction of dose absorbe...

journal_title：Biopharmaceutics & drug disposition

authors： Macheras PE,Symillides MY

更新日期：1989-01-01 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：PURPOSE:The sonodynamically induced anti-tumor effect of chlorin-e6 (Ce6) was studied in mice bearing hepatoma-22 solid tumors. METHODS:In order to determine the optimum timing of ultrasound exposure after administration of Ce6, the Ce6 concentrations in plasma, skin, muscle and tumor were estimated by measuring the f...

journal_title：Biopharmaceutics & drug disposition

authors： Shi H,Liu Q,Qin X,Wang P,Wang X

更新日期：2011-09-01 00:00:00

abstract：:The purpose of this mechanistic drug interaction study was to investigate the effects of ketoconazole on the pharmacokinetics of safinamide. Ketoconazole was applied as a potent prototypic inhibitor of cytochrome CYP3A4, to determine the role of CYP3A4 in the metabolic clearance of safinamide. In an open-label, random...

journal_title：Biopharmaceutics & drug disposition

authors： Krösser S,Marquet A,Gallemann D,Wolna P,Fauchoux N,Hermann R,Johne A

更新日期：2012-12-01 00:00:00

abstract：:Macelignan is a natural phenolic compound that possesses many types of health benefits such as antiinflammation. This study aimed to characterize the metabolism of macelignan via the glucuronidation pathway and to identify the main UGT enzymes involved in macelignan glucuronidation. The rates of glucuronidation were d...

journal_title：Biopharmaceutics & drug disposition

authors： Liu H,Wu Z,Ma Z,Wu B

更新日期：2014-12-01 00:00:00

abstract：:This open-label, two-way crossover study was undertaken to determine whether the enteric formulation of didanosine influences the pharmacokinetics of itraconazole or fluconazole, two agents frequently used to treat fungal infections that occur with HIV infection, and whose bioavailability may be influenced by changes ...

journal_title：Biopharmaceutics & drug disposition

authors： Damle B,Hess H,Kaul S,Knupp C

更新日期：2002-03-01 00:00:00

abstract：:The utility of pyrazinamide (PZA) in the short-course antituberculous treatment is well established. All available data support the idea that the PZA metabolite pyrazinoic acid (PA) is the active compound against M. tuberculosis. This situation warranted a deeper investigation of possible interactions with respect to ...

journal_title：Biopharmaceutics & drug disposition

authors： Mehmedagic A,Verite P,Menager S,Tharasse C,Chabenat C,Andre D,Lafont O

更新日期：2002-07-01 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 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：: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：: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 determination of therapeutic levels of glyceryl trinitrate (GTN), isosorbide dinitrate (ISDN), pentaerythritol tetranitrate (PETN), and their metabolites in human plasma was conducted using the TEA Analyzer interfaced to a high-performance liquid chromatograph (HPLC-TEA). Chromatographic separation of these compou...

journal_title：Biopharmaceutics & drug disposition

authors： Yu WC,Goff EU

更新日期：1983-10-01 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：:The oral pharmacokinetics (concentration-time profile) of four proprietary compounds in humans were predicted using the C(vss)-MRT method. The first step was to demonstrate superposition of intravenous (i.v.) pharmacokinetic profiles of preclinical species following mathematical transformation of their respective conc...

journal_title：Biopharmaceutics & drug disposition

authors： Fura A,Vyas V,Humphreys W,Chimalokonda A,Rodrigues D

更新日期：2008-11-01 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：: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：: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

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：: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：:Antiretroviral therapy has been the mainstay of treatment for neonates born to HIV infected mothers. Neonates born prematurely to HIV positive mothers are underdeveloped not only in anatomical terms but also in their physiological systems. Zidovudine, the first antiretroviral drug in clinical therapy for the treatment...

journal_title：Biopharmaceutics & drug disposition

authors： Wei L,Mansoor N,Khan RA,Czejka M,Ahmad T,Ahmed M,Ali M,Yang DH

更新日期：2019-11-01 00:00:00

abstract：:The pharmacokinetics of 3-(decyldimethylsilyl)-N-[2-(4-methylphenyl)-1-phenylethyl]propanamide (DMPP), an inhibitor of acyl-CoA:cholesterol acyltransferase, have been studied in the dog and the rat using 14C and 3H dual-labelled drug. In both species, gastrointestinal absorption of DMPP was slow and incomplete, amount...

journal_title：Biopharmaceutics & drug disposition

authors： Tse FL,Jaffe JM

更新日期：1987-09-01 00:00:00

abstract：:The aim of this investigation was to assess the pharmacokinetic properties of high-dose menadione (VK3), as an anticancer agent, in plasma and red blood cells (RBCs) in rabbits. An extremely high dose of 75 mg menadiol sodium diphosphate (Synkayvite) was intravenously injected. HPLC analysis was applied to measure the...

journal_title：Biopharmaceutics & drug disposition

authors： Hu OY,Wu CY,Chan WK,Wu FY,Whang-Peng J

更新日期：1996-08-01 00:00:00

abstract：:Photodynamic therapy (PDT) using the photosensitizer BPD-Verteporfin (liposomal benzoporphyrin derivative-monoacid ring A) has been shown in previous studies to be effective in the amelioration of inflammatory arthritis in both the MRL-lpr mouse and the New Zealand White (NZW) rabbit models, and could potentially offe...

journal_title：Biopharmaceutics & drug disposition

authors： Chowdhary RK,Ratkay LG,Canaan AJ,Waterfield JD,Richter AM,Levy JG

更新日期：1998-09-01 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：:The pharmacokinetics of verapamil, a calcium channel blocker, were studied in male Sprague-Dawley rats following i.v. administration at a dose of 1 mg kg-1. Both arterial and venous blood were collected and the plasma drug concentrations were determined by reversed-phase high-performance liquid chromatography. Verapam...

journal_title：Biopharmaceutics & drug disposition

authors： Manitpisitkul P,Chiou WL

更新日期：1993-10-01 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