Effects of excipients on protein conformation in lyophilized solids by hydrogen/deuterium exchange mass spectrometry.

abstract：PURPOSE:Gastroduodenal and intestinal permeability were compared after single doses of sustained release and regular release flurbiprofen in the rat to assess possible site-specific formulation-dependent toxicity. METHODS:Pharmacokinetics was assessed and gastrointestinal permeability was evaluated using sucrose and 5...

journal_title：Pharmaceutical research

authors： Davies NM,Jamali F

更新日期：1997-11-01 00:00:00

abstract：PURPOSE:The possibility of preparing nanoparticles in the supercooled thermotropic liquid crystalline state from cholesterol esters with saturated acyl chains as well as the incorporation of model drugs into the dispersions was investigated using cholesteryl myristate (CM) as a model cholesterol ester. METHODS:Nanopar...

journal_title：Pharmaceutical research

authors： Kuntsche J,Westesen K,Drechsler M,Koch MH,Bunjes H

更新日期：2004-10-01 00:00:00

abstract：PURPOSE:We recently showed that the perfusion of isolated rat livers with perfusates containing bovine serum albumin (BSA) would significantly stimulate the release of tumor necrosis factor (TNF)-alpha. Here, we hypothesize that BSA-induced increase in the release of TNF-alpha, and possibly other cytokines, would affec...

journal_title：Pharmaceutical research

authors： Vuppugalla R,Shah RB,Chimalakonda AP,Fisher CW,Mehvar R

更新日期：2003-01-01 00:00:00

abstract：PURPOSE:To evaluate the use of an in vitro intestinal permeability model to predict rat and human absorption as well as to evaluate the use of an internal standard to control for intra- and inter-rat variability. METHODS:In vivo peroral absorption and in vitro steady-state intestinal permeability coefficients were det...

journal_title：Pharmaceutical research

authors： Dowty ME,Dietsch CR

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:To study the influence of cytotoxicity of macromolecules, VEGF gene expression, and vascular permeability on the enhanced permeability and retention (EPR) effect. METHODS:Mice bearing xenografts of A2780 multidrug resistant human ovarian carcinoma were treated by free doxorubicin (DOX) and N-(2-hydroxypropyl)m...

journal_title：Pharmaceutical research

authors： Minko T,Kopeckova P,Pozharov V,Jensen KD,Kopecek J

更新日期：2000-05-01 00:00:00

abstract：PURPOSE:Reverse iontophoresis is an alternative to blood sampling for the monitoring of endogenous molecules. Here, the potential of the technique to measure urea and potassium levels non-invasively, and to track their concentrations during hemodialysis, has been examined. MATERIALS AND METHODS:In vitro experiments we...

journal_title：Pharmaceutical research

authors： Wascotte V,Delgado-Charro MB,Rozet E,Wallemacq P,Hubert P,Guy RH,Préat V

更新日期：2007-06-01 00:00:00

abstract：:Emulsions (o/w) were prepared from solid-state emulsions comprised of various matrix materials and oils and the resultant particle size properties determined. Results suggest that for those matrices that can form solid-state emulsions, the droplet size decreased as a function of time, as previously observed. The final...

journal_title：Pharmaceutical research

authors： Shively ML

更新日期：1993-08-01 00:00:00

abstract：PURPOSE:Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compou...

journal_title：Pharmaceutical research

authors： Chou SC,Kaur M,Thompson JA,Agarwal R,Agarwal C

更新日期：2010-04-01 00:00:00

abstract：PURPOSE:To evaluate the mechanism of renal transport of quinolone antibacterial drugs, we examined the interaction of levofloxacin with p-aminohippurate (PAH) transport systems and the transport of levofloxacin in renal epithelial cells. METHODS:Transport of [14C]PAH or [14C]levofloxacin was measured using OK cell mon...

journal_title：Pharmaceutical research

authors： Matsuo Y,Yano I,Habu Y,Katsura T,Hashimoto Y,Inui K

更新日期：2001-05-01 00:00:00

abstract：PURPOSE:To address the problem of precipitation of a poorly soluble drug during dissolution of highly soluble cocrystals by preparing granules intimately mixed with a water-soluble polymer. METHODS:Effectiveness of polymers as precipitation inhibitors during the dissolution of carbamazepine-nicotinamide (CBZ-NCT) cocr...

journal_title：Pharmaceutical research

authors： Yamashita H,Sun CC

更新日期：2019-04-23 00:00:00

abstract：PURPOSE:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...

journal_title：Pharmaceutical research

authors： Ogata S,Ito S,Masuda T,Ohtsuki S

更新日期：2019-07-31 00:00:00

abstract：:To evaluate the effects of a neutron activation radiolabeling technique on an enteric-coated multiparticulate formulation of erythromycin, test quantities were produced under industrial pilot scale conditions. The pellets contained the stable isotope erbium oxide (Er-170), which was later converted by neutron activati...

journal_title：Pharmaceutical research

authors： Parr AF,Digenis GA,Sandefer EP,Ghebre-Sellassie I,Iyer U,Nesbitt RU,Scheinthal BM

更新日期：1990-03-01 00:00:00

abstract：:The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...

journal_title：Pharmaceutical research

authors： Colthorpe P,Farr SJ,Smith IJ,Wyatt D,Taylor G

更新日期：1995-03-01 00:00:00

abstract：PURPOSE:The encapsulation of pancreatic β-cells in biocompatible matrix has generated great interest in diabetes treatment. Our work has shown improved microcapsules when incorporating the bile acid ursodeoxycholic acid (UDCA), in terms of morphology and cell viability although cell survival remained low. Thus, the stu...

journal_title：Pharmaceutical research

authors： Mooranian A,Negrulj R,Al-Salami H

更新日期：2016-05-01 00:00:00

abstract：PURPOSE:Following extracellular drug clearance, we analyzed the rate of doxorubicin efflux from the nucleus of three human leukemic cells (K562, Molt4 and CCRF-CEM) and related it to their differential sensitivity to this drug, after a short drug pulse. RESULTS:For many pulse-chase regimes, K562 cell viability was lea...

journal_title：Pharmaceutical research

authors： Chen VY,Posada MM,Zhao L,Rosania GR

更新日期：2007-11-01 00:00:00

abstract：:We report the chemical and enzymatic hydrolysis of two hydrophobic prodrugs of ganciclovir (3 = dipropionate ester; 4 = diadamantoate ester). Both prodrugs undergo hydrolysis showing a pH dependence of kobs = kH+aH+ + ko + kHO-aHO- and a pH of maximum stability near pH 5. Only 4 exhibited a shelf life (t90) greater th...

journal_title：Pharmaceutical research

authors： Powell MF,Magill A,Chu N,Hama K,Mau CI,Foster L,Bergstrom R

更新日期：1991-11-01 00:00:00

abstract：PURPOSE:An in vitro dynamic pharmacokinetic (PK) cell culture system was developed to more precisely simulate physiologic nanoparticle/drug exposure. METHODS:A dynamic PK cell culture system was developed to more closely reflect physiologic nanoparticle/drug concentrations that are changing with time. Macrophages were...

journal_title：Pharmaceutical research

authors： Kutscher HL,Morse GD,Prasad PN,Reynolds JL

更新日期：2019-02-01 00:00:00

abstract：PURPOSE:Since the adoption of highly active antiretroviral therapy, HIV disease progression has slowed across the world; however, patients are often required to take multiple medications daily of poorly bioavailable drugs via the oral route, leading to gastrointestinal irritation. Recently, long acting antiretroviral i...

journal_title：Pharmaceutical research

authors： Collier MA,Gallovic MD,Bachelder EM,Sykes CD,Kashuba A,Ainslie KM

更新日期：2016-08-01 00:00:00

abstract：PURPOSE:Previously, we have shown that complexes of plasmid DNA with the biodegradable polymer poly(2-dimethylamino ethylamino)phosphazene (p(DMAEA)-ppz) mediated tumor selective gene expression after intravenous administration in mice. In this study, we investigated the effect of p(DMAEA)-ppz molecular weight on both ...

journal_title：Pharmaceutical research

authors： de Wolf HK,de Raad M,Snel C,van Steenbergen MJ,Fens MH,Storm G,Hennink WE

更新日期：2007-08-01 00:00:00

abstract：:An empirical mass-transfer model for enteric-coating dissolution that uses in vivo dissolution data to characterize the pH-dependent solubility properties of the polymer film and a mass-transfer coefficient determined from in vivo dissolution or disintegration studies is developed. Once the in vivo mass-transfer coeff...

journal_title：Pharmaceutical research

authors： Ebel JP,Jay M,Beihn RM

更新日期：1993-02-01 00:00:00

abstract：PURPOSE:Comparison of the dissociation kinetics of rapid-acting insulins lispro, aspart, glulisine and human insulin under physiologically relevant conditions. METHODS:Dissociation kinetics after dilution were monitored directly in terms of the average molecular mass using combined static and dynamic light scattering....

journal_title：Pharmaceutical research

authors： Gast K,Schüler A,Wolff M,Thalhammer A,Berchtold H,Nagel N,Lenherr G,Hauck G,Seckler R

更新日期：2017-11-01 00:00:00

abstract：PURPOSE:The purpose of this work was to study the influence of cell differentiation on the mRNA expression of transporters and channels in Caco-2 cells and to assess Caco-2 cells as a model for carrier-mediated drug transport in the intestines. METHOD:Gene mRNA expression was measured using a custom-designed microarra...

journal_title：Pharmaceutical research

authors： Anderle P,Rakhmanova V,Woodford K,Zerangue N,Sadée W

更新日期：2003-01-01 00:00:00

abstract：PURPOSE:Using human lung cancer cells, we evaluated the involvement of plasminogen activator inhibitor-1 (PAI-1) in the anti-invasive action of cannabidiol, a non-psychoactive cannabinoid. METHODS:Invasion was quantified by a modified Boyden chamber assay. PAI-1 protein in cell culture media and PAI-1 mRNA were determ...

journal_title：Pharmaceutical research

authors： Ramer R,Rohde A,Merkord J,Rohde H,Hinz B

更新日期：2010-10-01 00:00:00

abstract：:Lidocaine was administered to healthy volunteers at different sites in the rectum. Unchanged drug and monoethylglycinexylidide (MEGX) concentrations were measured in plasma with a newly developed gas chromatographic method. Lidocaine was given rectally by means of an osmotic system (Osmet(®)) which delivered 25 mg/h a...

journal_title：Pharmaceutical research

authors： de Leede LG,de Boer AG,Feijen CD,Breimer DD

更新日期：1984-05-01 00:00:00

abstract：PURPOSE:Several phenomena in tablets indicate that an inhomogeneous pore distribution is formed during the compaction process. Examples are lamination and the capping of corners. In order to gain an understanding of the relation between structure and compact properties, analyzing the structure in a location dependent m...

journal_title：Pharmaceutical research

authors： Wu YS,Frijlink HW,van Vliet LJ,Stokroos I,van der Voort Maarschalk K

更新日期：2005-08-01 00:00:00

abstract：PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...

journal_title：Pharmaceutical research

authors： Ulery BD,Phanse Y,Sinha A,Wannemuehler MJ,Narasimhan B,Bellaire BH

更新日期：2009-03-01 00:00:00

abstract：OBJECTIVE:The objective of this work was to determine plasma protein adsorption and macrophage phagocytosis of biodegradable polyanhydride, polylactic acid and polylactic-co-glycolic acid microspheres prepared by both spray-drying and solvent evaporation techniques. METHODS:Microspheres were characterized by scanning ...

journal_title：Pharmaceutical research

authors： Lacasse FX,Filion MC,Phillips NC,Escher E,McMullen JN,Hildgen P

更新日期：1998-02-01 00:00:00

abstract：PURPOSE:To analyze the effects of chemical enhancers and iontophoresis on the buccal transmucosal delivery of lidocaine and nicotine. METHODS:Porcine oral mucosal samples were pretreated with chemical enhancers before conducting 8-hr Franz diffusion-cell experiments. In studies addressing the influence of iontophoresi...

journal_title：Pharmaceutical research

authors： Wei R,Simon L,Hu L,Michniak-Kohn B

更新日期：2012-04-01 00:00:00

abstract：PURPOSE:To identify the molecules responsible for amyloid beta-peptide (1-40) (Abeta(1-40)) uptake by the liver, which play a major role in the systemic clearance of Abeta(1-40). METHODS:The liver uptake index method was used to examine the mechanisms of Abeta(1-40) uptake by the liver in vivo. RESULTS:[125I]Abeta(1-...

journal_title：Pharmaceutical research

authors： Tamaki C,Ohtsuki S,Iwatsubo T,Hashimoto T,Yamada K,Yabuki C,Terasaki T

更新日期：2006-07-01 00:00:00

abstract：PURPOSE:In the present work, we developed water-in-oil (w/o) nanoemulsions for the intravesical administration of cisplatin. METHODS:The nanoemulsions were made up of soybean oil as the oil phase and Span 80, Tween 80, or Brij 98 as the emulsifier system. alpha-Terpineol and oleic acid were incorporated as permeation ...

journal_title：Pharmaceutical research

authors： Hwang TL,Fang CL,Chen CH,Fang JY

更新日期：2009-10-01 00:00:00