Lysosomal trapping of amodiaquine: impact on transport across intestinal epithelia models.

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 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：:Loxoprofen (LX) is a prodrug-type non-steroidal anti-inflammatory drug which is used not only as an oral drug but also as a transdermal formulation. As a pharmacologically active metabolite, the trans-alcohol form of LX (trans-OH form) is generated after oral administration to humans. The objectives of this study were...

journal_title：Biopharmaceutics & drug disposition

authors： Sawamura R,Sakurai H,Wada N,Nishiya Y,Honda T,Kazui M,Kurihara A,Shinagawa A,Izumi T

更新日期：2015-09-01 00:00:00

abstract：:In this study, a quantitative threshold was determined for the high/low extent of urinary excretion (UE) of compounds in humans, using a straightforward but robust statistical method known as receiver operating characteristic curve (ROC) analysis, and also 18 potential physicochemical determinants of UE were evaluated...

journal_title：Biopharmaceutics & drug disposition

authors： Dave RA,Morris ME

更新日期：2016-07-01 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：:The pharmacokinetics and tolerability of a new putative non-benzodiazepine type anxiolytic compound deramciclane was studied in two consecutive studies. An open dose-escalation design was used to study doses from 0.2 to 50 mg in 18 healthy male volunteers. In the second study doses from 50 to 150 mg were investigated ...

journal_title：Biopharmaceutics & drug disposition

authors： Kanerva H,Kilkku O,Heinonen E,Helminen A,Rouru J,Tarpila S,Scheinin M,Huupponen R,Klebovich I,Drabant S,Urtti A

更新日期：1999-10-01 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：:The purpose of this study was to formulate a drug-in-adhesive (DIA) transdermal patch containing letrozole, a third generation aromatase inhibitor for the treatment of breast cancer, using pressure-sensitive-adhesives (PSAs) and to evaluate the percutaneous penetration and pharmacokinetics of letrozole after transderm...

journal_title：Biopharmaceutics & drug disposition

authors： Li L,Fang L,Xu X,Liu Y,Sun Y,He Z

更新日期：2010-03-01 00:00:00

abstract：:Methotrexate (MTX) is an anchor drug used to treat rheumatoid arthritis (RA), but responsiveness is variable in effectiveness and toxicity. Methotrexate and its polyglutamate conjugates (MTXPG(n)) in red blood cells (RBC) have been associated with patient response. In the current study, 13 collagen-induced arthritic (...

journal_title：Biopharmaceutics & drug disposition

authors： Liu DY,Lon HK,Wang YL,DuBois DC,Almon RR,Jusko WJ

更新日期：2013-05-01 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：: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：:The usefulness of a limited sampling method (LSM) to determine the bioequivalence of highly variable drugs with long half-lives was investigated. The LSM uses multiple linear regression of observed drug plasma concentrations versus area under the curve (AUC) or C(max) (peak plasma concentration) to obtain a best set o...

journal_title：Biopharmaceutics & drug disposition

authors： Jackson AJ

更新日期：2001-07-01 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：:Glucocorticoids have diverse effects on various components of the immune system and assessment of such activities in vivo often involves complex techniques and numerous animals. We developed a whole blood technique for determining proliferation rate of lymphocytes in minute amounts of rat blood (5 microL as opposed to...

journal_title：Biopharmaceutics & drug disposition

authors： Fasanmade AA,Jusko WJ

更新日期：1999-07-01 00:00:00

abstract：:Remogliflozin etabonate (RE) is the prodrug of remogliflozin (R), an inhibitor of renal glucose transport designed to reduce blood glucose concentrations for the treatment of type 2 diabetes. This open-label, randomized, single-dose, four-way crossover study, (with one add-on arm) in eight healthy men evaluated the re...

journal_title：Biopharmaceutics & drug disposition

authors： O'Connor-Semmes RL,Sandefer EP,Hussey EK,Tao W,Doll WJ,Page RC,Dobbins R

更新日期：2013-03-01 00:00:00

abstract：:Several research groups have reported that in man the oral administration of propranolol with food leads to a marked increase (about 50 per cent) in the area under the plasma concentration-time curve (AUCpo) of this well absorbed and highly metabolized drug. An acute change in hepatic metabolic enzyme activity has bee...

journal_title：Biopharmaceutics & drug disposition

authors： Chow HH,Lalka D

更新日期：1993-04-01 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：: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 intestinal lymphatic absorption of cyclosporin A (CyA) following oral administration of 6.5 +/- 0.6 and 25.2 +/- 1.4 mg kg-1 doses of the drug dissolved in an olive oil solution was studied using a thoracic duct-cannulated rat model. Cumulative lymph samples were collected for up to 114 h post-dosing and assayed b...

journal_title：Biopharmaceutics & drug disposition

authors： Ueda CT,Lemaire M,Gsell G,Nussbaumer K

更新日期：1983-04-01 00:00:00

abstract：:Four normal volunteers each received two intravenous doses of PA. The mean low dose was 3.30 mg kg-1 (infused over 20 minutes) while the mean high dose was 12.5 mg kg-1 (infused over 60 minutes). Blood samples were collected for 12 hours and urine was collected for 48 hours after each dose. PA concentrations were dete...

journal_title：Biopharmaceutics & drug disposition

authors： Coyle JD,Boudoulas H,Mackichan JJ,Lima JJ

更新日期：1985-04-01 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：: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：:The pharmacokinetics and pharmacodynamics of furosemide were investigated after intravenous (i.v.), 1 mg/100 g body weight, and oral administration, 2 mg per 100 g body weight, to spontaneously hypertensive rats (SHRs) and deoxycorticosterone acetate-salt-induced hypertensive rats (DOCA-salt rats). After i.v. administ...

journal_title：Biopharmaceutics & drug disposition

authors： Jang SH,Lee MG,Kim ND

更新日期：1994-04-01 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：:Crystalline solid dispersion of lurasidone hydrochloride (LH) was made with various polar and non-polar small molecules to overcome the poor aqueous solubility issue. LH-Glutathione (GSH) solid dispersion in 1:1 ratio was prepared by co-grinding method and characterized by using differential scanning calorimetry (DSC)...

journal_title：Biopharmaceutics & drug disposition

authors： Pardhi VP,Flora S

更新日期：2020-11-01 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：: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：:This review offers a detailed discussion of the interaction between pharmaceutical compounds and vehicles using the affinity capillary electrophoresis and the microemulsion electrokinetic chromatography. Partition coefficients of drugs were calculated between a micelle and an aqueous phases from the measurement of the...

journal_title：Biopharmaceutics & drug disposition

authors： Reinhard N,Mrestani Y

更新日期：2001-10-01 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：: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