Coupling of aggregation and immunogenicity in biotherapeutics: T- and B-cell immune epitopes may contain aggregation-prone regions.

abstract：PURPOSE:This study was conducted to investigate in vivo the impact of interferon-alpha (IFN)-alpha on P-glycoprotein (P-gp) activity in rats by studying how its administration modifies the bioavailability of digoxin, a fairly pure P-gp substrate. METHODS:Human recombinant IFN-alpha was given to rats (n = 5-7 per group...

journal_title：Pharmaceutical research

authors： Ben Reguiga M,Bonhomme-Faivre L,Orbach-Arbouys S,Farinotti R

更新日期：2005-11-01 00:00:00

abstract：PURPOSE:To investigate if gamma-Hydroxybutyrate (GHB) tolerance is mediated by alterations in GHB systemic pharmacokinetics, transport (blood brain barrier (BBB) and neuronal) or membrane fluidity. MATERIALS AND METHODS:GHB tolerance in rats was attained by repeated GHB administration (5.31 mmol/kg, s.c., QD for 5 day...

journal_title：Pharmaceutical research

authors： Bhattacharya I,Raybon JJ,Boje KM

更新日期：2006-09-01 00:00:00

abstract：:Gene delivery vectors based on adeno-associated virus (AAV) are highly promising due to several desirable features of this parent virus, including a lack of pathogenicity, efficient infection of dividing and non-dividing cells, and sustained maintenance of the viral genome. However, several problems should be addresse...

journal_title：Pharmaceutical research

authors： Kwon I,Schaffer DV

更新日期：2008-03-01 00:00:00

abstract：PURPOSE:To develop novel bioactive-chylomicrons to solve oral delivery obstacles of Berberine chloride and target the lymphatic system. METHODS:Berberine-loaded bioactive-chylomicrons were prepared and underwent full in vitro characterization. Intestinal permeability was appraised via both non-everted gut sac model an...

journal_title：Pharmaceutical research

authors： Elsheikh MA,Elnaggar YSR,Otify DY,Abdallah OY

更新日期：2018-01-05 00:00:00

abstract：:A method to provide near-constant sustained release of high molecular weight, water-soluble proteins from polyanhydride microspheres is described. The polyanhydrides used were poly(fatty acid dimer) (PFAD), poly(sebacic acid) (PSA), and their copolymers [P(FAD-SA)]. P(FAD-SA) microspheres containing proteins of differ...

journal_title：Pharmaceutical research

authors： Tabata Y,Gutta S,Langer R

更新日期：1993-04-01 00:00:00

abstract：PURPOSE:The specific interactions between three lectin-latex conjugates and different structures of rat intestinal mucosa have been studied ex vivo. METHODS:These systems were prepared by covalent coupling of different ligands, i.e., tomato lectin (TL), asparagus pea lectin (AL), mycoplasma gallisepticum lectin (ML), ...

journal_title：Pharmaceutical research

authors： Irache JM,Durrer C,Duchêne D,Ponchel G

更新日期：1996-11-01 00:00:00

abstract：:Nonstereospecific studies have indicated that the pharmacokinetics of propranolol (PR) are altered in inflammatory conditions such as arthritis. However, as the kinetics and dynamics of PR are stereoselective, we examined the effect of adjuvant arthritis (AA) on the disposition of the individual enantiomers. A novel n...

journal_title：Pharmaceutical research

authors： Piquette-Miller M,Jamali F

更新日期：1993-02-01 00:00:00

abstract：PURPOSE:Empirical formulae relate the mean size of primary droplets from jet and ultrasonic nebulizers to a fluid's physicochemical properties. Although the size selective "filtering" effects of baffling and evaporation may modify the secondary aerosol produced, this research sought to evaluate whether viscosity and su...

journal_title：Pharmaceutical research

authors： McCallion ON,Taylor KM,Thomas M,Taylor AJ

更新日期：1995-11-01 00:00:00

abstract：PURPOSES:To evaluate the effects of component contents in different colistin methanesulfonate (CMS) formulas on their clinical pharmacokinetics of the prodrug CMS and the formed colistin. METHODS:Two CMS formulas (CTTQ and Parkedale) were investigated in a single dose, randomized, open-label, crossover study conducted...

journal_title：Pharmaceutical research

authors： Fan YX,Chen YC,Li Y,Yu JC,Bian XC,Li X,Li WZ,Guo BN,Wu HL,Liu XF,Wang Y,Xu XY,Hu JL,Wang JJ,Wu XJ,Cao GY,Wu JF,Xue CJ,Feng J,Zhang YY,Zhang J

更新日期：2021-01-26 00:00:00

abstract：:Primaquine, an 8-aminoquinoline antimalarial, is shown to undergo unexpectedly rapid aromatic proton exchange with the medium. At a pH less than 4, the exchange of C-5 is so fast as to be unmeasurable by proton nmr methods. At a pH of 6-6.5 the half-time for exchange is 4 to 5 minutes. This unexpectedly high rate of e...

journal_title：Pharmaceutical research

authors： McChesney JD,Sarangan S

更新日期：1984-07-01 00:00:00

abstract：PURPOSE:The objective of this work is to understand the sequence specificity of HAV peptides and to improve their selectivity in regulating E-cadherin-E-cadherin interactions in the intercellular junctions. METHODS:Peptide 1 was modified using an alanine scanning method to give peptides 2-6. The ability of these pepti...

journal_title：Pharmaceutical research

authors： Makagiansar IT,Avery M,Hu Y,Audus KL,Siahaan TJ

更新日期：2001-04-01 00:00:00

abstract：:The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulation...

journal_title：Pharmaceutical research

authors： Sylte I,Dahl SG

更新日期：1991-04-01 00:00:00

abstract：PURPOSE:For selective inhibition of endothelial cell activation in chronic inflammation, we have developed a dexamethasone-anti-E-selectin immunoconjugate. The present study was performed to evaluate the cellular handling of this immunoconjugate by activated primary endothelial cells and to compare its drug delivery ca...

journal_title：Pharmaceutical research

authors： Kok RJ,Everts M,Asgeirsdóttir SA,Meijer DK,Molema G

更新日期：2002-11-01 00:00:00

abstract：PURPOSE:To assess the efficacy of lipid-protein-sugar particles (LPSPs) in providing prolonged duration local anesthesia by percutaneous injection. METHODS:Bupivacaine-containing LPSPs were characterized and optimized in vitro. Male Sprague-Dawley rats were given sciatic nerve blocks with bupivacaine-containing LPSPs....

journal_title：Pharmaceutical research

authors： Kohane DS,Lipp M,Kinney RC,Lotan N,Langer R

更新日期：2000-10-01 00:00:00

abstract：PURPOSE:[corrected] The purpose of this study was to design novel gastroretentive dosage forms (GRDFs) based on unfolding multilayer polymeric films, to investigate the mechanism of their gastroretentivity in dogs, and to assess the effect of compounding a narrow absorption window drug in a GRDF on the drug's absorptio...

journal_title：Pharmaceutical research

authors： Klausner EA,Lavy E,Stepensky D,Friedman M,Hoffman A

更新日期：2002-10-01 00:00:00

abstract：:The bioavailability of dipyridamole, a poorly soluble weak base, was evaluated in 11 healthy, older subjects (> or = 65 years), 6 with a low fasting gastric pH (control) and 5 with a fasting gastric pH > 5 (achlorhydric), in a randomized, crossover design. Subjects received 50 mg dipyridamole as a single oral dose bot...

journal_title：Pharmaceutical research

authors： Russell TL,Berardi RR,Barnett JL,O'Sullivan TL,Wagner JG,Dressman JB

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:One of the drawbacks of polycationic and cationic liposomal gene transfer is its sensitivity to serum. Gene therapy requires the transfectant-DNA complex to be resistant to serum as well as blood. Since Ca2+ has proved to be an efficient cofactor of polycationic gene transfer, we decided to investigate its effe...

journal_title：Pharmaceutical research

authors： Haberland A,Knaus T,Zaitsev SV,Buchberger B,Lun A,Haller H,Böttger M

更新日期：2000-02-01 00:00:00

abstract：PURPOSE:Polyethylenimine (PEI) is a highly effective gene delivery vector, but because it is an off-the shelf material, its properties may not be optimal. To investigate the effects of the protonation properties of the polymer, we generated PEI derivatives by acetylating varying fractions of the primary and secondary a...

journal_title：Pharmaceutical research

authors： Forrest ML,Meister GE,Koerber JT,Pack DW

更新日期：2004-02-01 00:00:00

abstract：PURPOSE:To demonstrate a very effective and easy way of stabilization of amorphous indomethacin (IMC) by preparing binary mixtures with octaacetylmaltose (acMAL). In order to understand the origin of increased stability of amorphous system inter- and intramolecular interactions between IMC and acMAL were studied. METH...

journal_title：Pharmaceutical research

authors： Kaminska E,Adrjanowicz K,Zakowiecki D,Milanowski B,Tarnacka M,Hawelek L,Dulski M,Pilch J,Smolka W,Kaczmarczyk-Sedlak I,Kaminski K

更新日期：2014-10-01 00:00:00

abstract：:Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...

journal_title：Pharmaceutical research

authors： Rapaka RS,Porreca F

更新日期：1991-01-01 00:00:00

abstract：:The fluxes of nitroglycerine (NG) through human abdominal epidermis from different individuals were measured in vitro at 32°C. The mean NG flux for the entire group was 16.9 µg/cm(2) × hr, with a standard deviation of 47.7%. There are no significant differences in the means and the variances of NG fluxes between males...

journal_title：Pharmaceutical research

authors： Langguth P,Spahn H,Mutschler E

更新日期：1986-02-01 00:00:00

abstract：PURPOSE:The gadopentetic acid (Gd-DTPA)-loaded chitosan nanoparticles (Gd-nanoCPs) were prepared for gadolinium neutron-capture therapy (Gd-NCT) and characterized and evaluated as a device for intratumoral (i.t.) injection. METHODS:Gd-nanoCPs were prepared by a novel emulsion-droplet coalescence technique. The effects...

journal_title：Pharmaceutical research

authors： Tokumitsu H,Ichikawa H,Fukumori Y

更新日期：1999-12-01 00:00:00

abstract：PURPOSE:The aim of the study is to suppress the progress of estrogen-dependent breast cancer by inhibiting the membrane transporter, which mediates the internalization of estrone-3-sulfate as estrogen precursor in the cancer cells. METHODS:The uptake of estrone-3-sulfate by estrogen-dependent breast cancer MCF-7 cells...

journal_title：Pharmaceutical research

authors： Nozawa T,Suzuki M,Yabuuchi H,Irokawa M,Tsuji A,Tamai I

更新日期：2005-10-01 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：:Human monocytes/macrophages (MO/MAC) were isolated from peripheral blood and cultivated on hydrophobic Teflon membranes. This culture system is suitable for HIV infection of MO/MAC in vitro. After transfer into 24-well plates the mature macrophages (infected or uninfected) were used for measurements of phagocytosis. T...

journal_title：Pharmaceutical research

authors： Schäfer V,von Briesen H,Andreesen R,Steffan AM,Royer C,Tröster S,Kreuter J,Rübsamen-Waigmann H

更新日期：1992-04-01 00:00:00

abstract：:Various carboxylic acid esters of the N-hydroxymethyl derivative of N-benzyloxycarbonylglycine benzylamide, used as a peptide-like model, were prepared and their decomposition kinetics studied in aqueous solution and in human plasma solutions. These N-acyloxymethylamide derivatives were found to undergo a facile decom...

journal_title：Pharmaceutical research

authors： Bundgaard H,Rasmussen GJ

更新日期：1991-10-01 00:00:00

abstract：PURPOSE:Monocarboxylate transporter (MCT) inhibition represents a potential treatment strategy for γ-hydroxybutyric acid (GHB) overdose by blocking its renal reabsorption in the kidney. This study further evaluated the effects of a novel, highly potent MCT inhibitor, AR-C155858, on GHB toxicokinetics/toxicodynamics (TK...

journal_title：Pharmaceutical research

authors： Vijay N,Morse BL,Morris ME

更新日期：2015-06-01 00:00:00

abstract：PURPOSE:Changes in drug absorption and first-pass metabolism have been reported throughout the pediatric age range. Our aim is to characterize both intestinal and hepatic CYP3A-mediated metabolism of midazolam in children in order to predict first-pass and systemic metabolism of CYP3A substrates. METHODS:Pharmacokinet...

journal_title：Pharmaceutical research

authors： Brussee JM,Yu H,Krekels EHJ,Palić S,Brill MJE,Barrett JS,Rostami-Hodjegan A,de Wildt SN,Knibbe CAJ

更新日期：2018-07-30 00:00:00

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:To advance fundamental biological and translational research with the bacterium Neisseria gonorrhoeae through the prediction of novel small molecule growth inhibitors via naïve Bayesian modeling methodology. METHODS:Inspection and curation of data from the publicly available ChEMBL web site for small molecule ...

journal_title：Pharmaceutical research

authors： Pereira JC,Daher SS,Zorn KM,Sherwood M,Russo R,Perryman AL,Wang X,Freundlich MJ,Ekins S,Freundlich JS

更新日期：2020-07-13 00:00:00