Use of affinity capillary electrophoresis for characterizing pharmaceutical colloidal vehicle systems thermodynamically.

abstract：:We present a novel method for performing pharmacokinetic and metabolism studies on macromolecules that offers advantages over the existing techniques of radiolabeling, immunoassay or bioassays. Our strategy uses macromolecules with stable isotopes uniformly distributed throughout the structure. The stable isotope enri...

journal_title：Biopharmaceutics & drug disposition

authors： Osborn BL,Abramson FP

更新日期：1998-10-01 00:00:00

abstract：:Acyl glucuronidation is the major metabolic conjugation reaction of most carboxylic acid drugs in mammals. The physiological consequences of this biotransformation have been investigated incompletely but include effects on drug metabolism, protein binding, distribution and clearance that impact upon pharmacological an...

journal_title：Biopharmaceutics & drug disposition

authors： Regan SL,Maggs JL,Hammond TG,Lambert C,Williams DP,Park BK

更新日期：2010-10-01 00:00:00

abstract：:The pharmacokinetics of a new selective oestrogen receptor modulator levormeloxifene was investigated in mice, rats, cynomolgus monkeys and humans by compartmental pharmacokinetics. Levormeloxifene was administered as an oral solution in all studies. Allometric scaling was used to predict human pharmacokinetic paramet...

journal_title：Biopharmaceutics & drug disposition

authors： Østerberg O,Kiehr B,Erichsen L,Poulsen HE,Ingwersen SH

更新日期：2003-04-01 00:00:00

abstract：:The present study was conducted in order to examine the intranasal administration of verapamil and compare this route to oral and intravenous administration in a 3 way crossover protocol in five dogs. Unanesthetized, adult mongrel dogs were given verapamil intravenously (0.5 mg/kg), orally (2.5 mg/kg) and intranasally...

journal_title：Biopharmaceutics & drug disposition

authors： Arnold TH,Tackett RL,Vallner JJ

更新日期：1985-10-01 00:00:00

abstract：:The bioequivalence of three oral forms of nifedipine was assessed in a triple crossover study on 12 healthy volunteers. Single 10 mg dose was given and ten blood samples were drawn during the first 8 h after administration. Highly sensitive gas chromatographic method was used for the nifedipine assay. Pharmacokinetic ...

journal_title：Biopharmaceutics & drug disposition

authors： Kozjek F,Primozic S,Mrhar A,Karba R,Raemsch KD,Janezic A

更新日期：1987-01-01 00:00:00

abstract：:Comparative in vivo studies of aqueous solution, multiple w/o/w, and w/o emulsions showed that formulating 5-fluorouracil in emulsion systems significantly sustained the release of the drug from intramuscular injection sites in the rat. Intramuscular injection of the drug in both w/o and w/o/w emulsion systems produce...

journal_title：Biopharmaceutics & drug disposition

authors： Omotosho JA,Whateley TL,Florence AT

更新日期：1989-05-01 00:00:00

abstract：:Methotrexate (MTX) is an antifolate agent used in the treatment of numerous types of cancer, and eliminated by active tubular secretion via organic anion transporter 3 (OAT3). Gastric antisecretory drugs, such as proton pump inhibitors (PPIs) and histamine H2 receptor antagonists, are widely used among patients with c...

journal_title：Biopharmaceutics & drug disposition

authors： Narumi K,Sato Y,Kobayashi M,Furugen A,Kasashi K,Yamada T,Teshima T,Iseki K

更新日期：2017-12-01 00:00:00

abstract：:The pharmacokinetics of didanosine and ciprofloxacin were evaluated following the administration of multiple oral doses of each drug as a single agent or in combination. Didanosine was dosed as the Videx chewable/dispersible tablet, which contains the antacids dihydroxyaluminum sodium carbonate and magnesium hydroxide...

journal_title：Biopharmaceutics & drug disposition

authors： Knupp CA,Barbhaiya RH

更新日期：1997-01-01 00:00:00

abstract：:In order to determine the absolute bioavailability, both oral and intravenous administrations of a drug are often used. Recently a new method has been proposed to determine absolute bioavailability in the absence of intravenous dose. Following a single oral dose, this method requires oral and renal clearance data from...

journal_title：Biopharmaceutics & drug disposition

authors： Mahmood I

更新日期：1997-08-01 00:00:00

abstract：:EXP631, 4-(3-thienyl)-alpha, alpha,1-trimethyl-4-piperidine-methanol hemi-fumarate salt (I), is a centrally acting non-opioid analgesic compound with monoamine uptake blocking properties. EXP631 has analgesic effects in several animal models. It is intended to be used for the treatment of moderate to moderately severe...

journal_title：Biopharmaceutics & drug disposition

authors： Wong YN,Burcham DL,Huang SM,Quon CY

更新日期：1993-08-01 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：: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：:In this comparative bioavailability study two sustained release capsule formulations of propranolol, one a clinical trial formulation and the other the U.K. sales formulation ('Inderal' LA), were compared with a conventional 'Inderal' tablet. Twelve healthy adult male volunteers received, on cross-over basis, on three...

journal_title：Biopharmaceutics & drug disposition

authors： McAinsh J,Baber NS,Holmes BF,Young J,Ellis SH

更新日期：1981-01-01 00:00:00

abstract：:A novel 5-aminolevulinic acid (ALA)-containing microparticulate system was produced recently, based on incorporation of ALA into particles prepared from a suppository base that maintains drug stability during storage and melts at skin temperature to release its drug payload. The novel particulate system was applied to...

journal_title：Biopharmaceutics & drug disposition

authors： Donnelly RF,McCarron PA,Al-Kassas R,Juzeniene A,Juzenas P,Iani V,Woolfson AD,Moan J

更新日期：2009-03-01 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

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：: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：: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：:An evaluation of the literature indicated that certain aspects of the disposition kinetics of iothalamate, important to the accurate determination of glomerular filtration rate in dogs and humans, remain to be resolved. The simultaneous clearances of iothalamate and inulin in 5 dogs were determined at three steady-sta...

journal_title：Biopharmaceutics & drug disposition

authors： Prueksaritanont T,Lui CY,Lee MG,Chiou WL

更新日期：1986-07-01 00:00:00

abstract：:The bioavailability of an improved formulation of enteric-coated phenylbutazone with faster dissolution, more consistent in vitro rate of drug release and improved stability was compared in 8 normal subjects at doses of 100 and 200 mg with commercially available Butacote. Phenylbutazone was more rapidly absorbed from ...

journal_title：Biopharmaceutics & drug disposition

authors： John VA,Goldsborough S,Morrison PJ,Rogers HJ,Spector RG,Bradbrook ID

更新日期：1982-01-01 00:00:00

abstract：:Human organic anion transporter 3 (hOAT3) is localized at the basolateral membrane of renal proximal tubule cells and facilitates the renal secretion of numerous clinical drugs, including anti-HIV therapeutics, anti-tumor drugs, antibiotics, antihypertension drugs and anti-inflammatories. The present study explored th...

journal_title：Biopharmaceutics & drug disposition

authors： Wang H,You G

更新日期：2017-11-01 00:00:00

abstract：:Pharmacokinetic studies of riluzole show a large inter-individual variability of the drug's clearance and serum concentrations. Optimizing the individual dosage of riluzole may have the potential to improve the effect of riluzole treatment on survival of patients with amyotrophic lateral sclerosis (ALS). Limited data ...

journal_title：Biopharmaceutics & drug disposition

authors： van Kan HJ,van den Berg LH,Groeneveld GJ,van der Straaten RJ,van Vught PW,Lie-A-Huen L,Guchelaar HJ

更新日期：2008-04-01 00:00:00

abstract：:Telaprevir, a chronic hepatitis C virus (HCV) protease inhibitor, is known to be a cytochrome P450 (CYP) 3A4/5 substrate and inhibitor. In the present study, the in vitro inhibitory effect of telaprevir on the metabolism of tacrolimus in human liver microsomes was investigated using 13-O-demethyltacrolimus (M-I) as a ...

journal_title：Biopharmaceutics & drug disposition

authors： Oda K,Yamano K

更新日期：2014-12-01 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 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：:The pharmacokinetics of the cardioselective beta-adrenoreceptor blocking agent atenolol have been determined following intravenous and oral dosing to the dog. After intravenous administration at 200 mg the blood levels of parent drug were found to decay tri-exponentially with a final elimination phase half-life of abo...

journal_title：Biopharmaceutics & drug disposition

authors： McAinsh J,Holmes BF

更新日期：1983-07-01 00:00:00

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 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：:The biotransformation of thionorphine (N-cyclopropylmethyl-7alpha-[(s)-1-hydroxy-1-methyl-3-(2thiophene)-propyl]-6,14-endo-ethano tetrahydrooripavine), a new analgesic, was in-vestigated in rats. The results of metabolite analysis by liquid chromatography/electrospray ionization tandem mass spectrometry with positive ...

journal_title：Biopharmaceutics & drug disposition

authors： Wei SX,Zhang ZQ,Wang XY,Guo JF

更新日期：2004-04-01 00:00:00

abstract：:Pharmacokinetic compartment models were constructed to describe the absorption and metabolism of dopamine (DA) and DA prodrug, N-(N-acetyl-L-methionyl)0,0-bis-eth-oxycarbonyl) dopamine(1). Plasma concentrations of DA, DA-SO4, and DOPAC after oral administration of DA to dogs, were analysed using the pharmacokinetic mo...

journal_title：Biopharmaceutics & drug disposition

authors： Murata K,Noda K,Kohno K,Samejima M

更新日期：1990-03-01 00:00:00