Inhibition of rat hepatic mitochondrial aldehyde dehydrogenase isozymes by repeated cyanamide administration: pharmacokinetic-pharmacodynamic relationships.

abstract：:Aim. To study the pharmacokinetics of dihydroartemisinin (DHA) in Artekin (compound dihydroartemisinin) tablets in Chinese healthy volunteers. Methods. Eighteen healthy volunteers (9 males, 9 females) received Artekin tablets for oral administration. The plasma samples of DHA were analysed by liquid-liquid extraction ...

journal_title：Biopharmaceutics & drug disposition

authors： Hong X,Liu CH,Huang XT,Huang TL,Ye SM,Ou WP,Wang NS,Mi SQ

更新日期：2008-05-01 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：: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：: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：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：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 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：: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：:The pharmacokinetics of an intravenous injection of disopyramide was studied in five normal subjects and six patients with varying degrees of renal impairment. The elimination rate constant (beta) was related to the endogenous creatinine clearance (Clcr). However, a decrease in beta was not observed until the Clcr was...

journal_title：Biopharmaceutics & drug disposition

authors： Shen DD,Cunningham JL,Shudo I,Azarnoff DL

更新日期：1980-01-01 00:00:00

abstract：:SYL-927, a novel and selective S1P1 agonist, is transferred to its active phosphate for the regulation of lymphocyte recirculation. This in vitro metabolism study is to elucidate the P450-mediated oxidation pathway of SYL-927 in human liver microsomes (HLMs). The results demonstrated that the ω-1 hydroxylated metaboli...

journal_title：Biopharmaceutics & drug disposition

authors： Yang S,Hu J,Li Y,Zhao Z

更新日期：2018-11-01 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：: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：: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：:The objective of this study was to assess the effect of dietary fibers on the transport of losartan, an angiotensin II type 1 receptor blocker, in small intestinal cells. Using Caco-2 cells in vitro, losartan uptake and transport were evaluated in the presence of various fibers (cellulose, chitosan, sodium alginate an...

journal_title：Biopharmaceutics & drug disposition

authors： Iwazaki A,Takahashi N,Miyake R,Hiroshima Y,Abe M,Yasui A,Imai K

更新日期：2016-05-01 00:00:00

abstract：:In the search for orally available drugs, the prediction of human pharmacokinetics (PK) is essential for successfully selecting compounds that will be clinically useful. This report describes the selection of TAK-272 (SCO-272), a novel orally active renin inhibitor, as a clinical candidate via the detailed investigati...

journal_title：Biopharmaceutics & drug disposition

authors： Ebihara T,Nishihara M,Takahashi J,Jinno F,Tagawa Y

更新日期：2018-03-01 00:00:00

abstract：:In a multiple dose cross-over experiment in 12 healthy male adults the bioavailability and sustained release characteristics of new once daily BY912 400 mg theophylline capsules (= B, Byk Gulden Research Laboratories, FRG) were studied using Theo-24 capsules (= T, Searle & Co., USA) as reference. Both products were gi...

journal_title：Biopharmaceutics & drug disposition

authors： Jonkman JH,Steinijans VW,Beier W,van der Boon WJ,Crasmeijer G

更新日期：1989-03-01 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 present study aimed to examine the potential pharmacokinetic drug interaction between valsartan and gemfibrozil. Compared with the control given valsartan (10 mg/kg) alone, the concurrent use of gemfibrozil (10 mg/kg) significantly (p < 0.05) increased the oral exposure of valsartan in rats. In the presence of gem...

journal_title：Biopharmaceutics & drug disposition

authors： Yang SJ,Kim BJ,Mo L,Han HK

更新日期：2016-07-01 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：: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 plasma protein binding of celecoxib was determined for animals and humans using in vitro and ex vivo methods. Eight, healthy, human volunteers (three male, five female, 20-39 years) received celecoxib (600 mg) BID for 7 days, blood samples were collected and concentrations of bound and unbound celecoxib determined...

journal_title：Biopharmaceutics & drug disposition

authors： Paulson SK,Kaprak TA,Gresk CJ,Fast DM,Baratta MT,Burton EG,Breau AP,Karim A

更新日期：1999-09-01 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：: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：:The following results were obtained recently from our laboratories; in rats with 72-h water deprivation (rats with dehydration), the hepatic cytochrome P450 2E1 (CYP2E1) was three-fold induced with an increase in the mRNA. Rehydration of 48-h water-deprived rats for the next 24 h with free access of food (rats with re...

journal_title：Biopharmaceutics & drug disposition

authors： Kim YC,Kim YG,Kim EJ,Cho MK,Kim SG,Lee MG

更新日期：2003-03-01 00:00:00

abstract：:Mivacurium, a non-depolarizing neuromuscular blocking agent, consists of three isomers; trans-trans (57%), cis-trans (36%) and cis-cis (7%). The purpose of this study was to characterize the pharmacokinetics and pharmacodynamics of mivacurium after various inputs. Four beagle dogs weighing between 7.95 and 9.89 kg wer...

journal_title：Biopharmaceutics & drug disposition

authors： Lugo SI,Liang Z,Eddington ND

更新日期：1998-11-01 00:00:00

abstract：:Although nifedipine has been characterized in terms of its general vasodilatory effects, this dihydropyridine must still be regarded as investigational with regard to available pharmacokinetic and pharmacodynamic data. Although limited studies are available, it is clear that the pharmacokinetic and pharmacodynamic dat...

journal_title：Biopharmaceutics & drug disposition

authors： Hamann SR,Piascik MT,McAllister RG Jr

更新日期：1986-01-01 00:00:00

abstract：:The pharmacokinetic behavior of glycyrrhizin in four patients with acute hepatitis (hepatitis group) and six patients with liver cirrhosis (cirrhosis group) receiving chronically an IV administration of a 120 mg dose once a day or once every other day of glycyrrhizin was investigated. The plasma concentration of glycy...

journal_title：Biopharmaceutics & drug disposition

authors： Yamamura Y,Tanaka N,Santa T,Kotaki H,Aikawa T,Uchino K,Osuga T,Sawada Y,Iga T

更新日期：1995-01-01 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：:We synthesized 14C-warfarin hexadecyl ether (14C-WHE) by addition of a palmityl moiety to the hydroxyl group at the 4-position of 14C-warfarin, a compound known to bind to serum albumin. 14C-WHE preferentially bound to the lipoproteins, low-density lipoprotein (LDL) and high-density lipoprotein (HDL), in mouse plasma ...

journal_title：Biopharmaceutics & drug disposition

authors： Tokui T,Kuroiwa C,Muramatsu S,Tokui Y,Sasagawa K,Ikeda T,Komai T

更新日期：1995-03-01 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