The influence of cytotoxicity of macromolecules and of VEGF gene modulated vascular permeability on the enhanced permeability and retention effect in resistant solid tumors.

abstract：:Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...

journal_title：Pharmaceutical research

authors： Yata N,Toyoda T,Murakami T,Nishiura A,Higashi Y

更新日期：1990-10-01 00:00:00

abstract：PURPOSE:To identify the mechanism behind the unexpected bio-performance of two amorphous solid dispersions: BMS-A/PVP-VA and BMS-A/HPMC-AS. METHODS:Solubility of crystalline BMS-A in PVP-VA and HPMC-AS was measured by DSC. Drug-polymer interaction parameters were obtained by Flory-Huggins model fitting. Drug dissoluti...

journal_title：Pharmaceutical research

authors： Qian F,Wang J,Hartley R,Tao J,Haddadin R,Mathias N,Hussain M

更新日期：2012-10-01 00:00:00

abstract：PURPOSE:This study demonstrates the nasal administration (NA) of nanoemulsions complexed with the plasmid encoding for IDUA protein (pIDUA) as an attempt to reach the brain aiming at MPS I gene therapy. METHODS:Formulations composed of DOPE, DOTAP, MCT (NE), and DSPE-PEG (NE-PEG) were prepared by high-pressure homogen...

journal_title：Pharmaceutical research

authors： Schuh RS,Bidone J,Poletto E,Pinheiro CV,Pasqualim G,de Carvalho TG,Farinon M,da Silva Diel D,Xavier RM,Baldo G,Matte U,Teixeira HF

更新日期：2018-09-26 00:00:00

abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

journal_title：Pharmaceutical research

authors： Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:Within-subject dependency of observations has a strong impact on the evaluation of population pharmacokinetic (PK) and/or pharmacodynamic (PD) models. To our knowledge, none of the current model evaluation tools correctly address this issue. We present a new method with a global test and easy diagnostic plot wh...

journal_title：Pharmaceutical research

authors： Laffont CM,Concordet D

更新日期：2011-08-01 00:00:00

abstract：PURPOSE:To study epidermal and polyethylene membrane penetration and retention of the sunscreen benzophenone-3 (BP) from a range of single solvent vehicles and evaluate solvent effects on permeability parameters. METHODS:The solubility of BP was measured in a number of solvents. Penetration of BP across human epidermi...

journal_title：Pharmaceutical research

authors： Jiang R,Benson HA,Cross SE,Roberts MS

更新日期：1998-12-01 00:00:00

abstract：PURPOSE:In this work a novel pH-responsive nanoscale polymer network was investigated for potential applications in nanomedicine. These consisted of a polybasic core surface stabilized with poly(ethylene glycol) grafts. The ability to control swelling properties via changes in core hydrophobicity and crosslinking feed ...

journal_title：Pharmaceutical research

authors： Fisher OZ,Kim T,Dietz SR,Peppas NA

更新日期：2009-01-01 00:00:00

abstract：PURPOSE:The work aims at investigating the correlation of water sorption potential with different measures of molecular mobility in an annealed amorphous model compound (trehalose). METHODS:Amorphous trehalose, prepared by freeze-drying, was annealed at 100°C (17°C < T (g)) for up to 120 h. Global mo...

journal_title：Pharmaceutical research

authors： Bhardwaj SP,Suryanarayanan R

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:The stability of lipid emulsions (LE) containing various cosurfactants (oleic acid, cholesterol, Tween 80, or HCO-60) was evaluated using the maximum total interaction energy, Vtmax and the energy barrier for coalescence, W. METHODS:The Vtmax and W were calculated from the zeta potential and the rate of increa...

journal_title：Pharmaceutical research

authors： Yamaguchi T,Nishizaki K,Itai S,Hayashi H,Ohshima H

更新日期：1995-09-01 00:00:00

abstract：PURPOSE:In vitro in vivo correlation (IVIVC) is a biopharmaceutical tool recommended for use in formulation development. When validated, IVIVC can be used to set dissolution limits and, based on the dissolution limits, as a surrogate for an in vivo study. The purpose of this paper is to study the various methods used t...

journal_title：Pharmaceutical research

authors： Roudier B,Davit BM,Beyssac E,Cardot JM

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:Manufacturing processes for polypeptide/protein drugs are designed to ensure robust quality, efficacy and safety. Process differences introduced by follow-on manufacturers may result in changes in quality and clinical outcomes. This study investigated the impact of production methods on the stability and impuri...

journal_title：Pharmaceutical research

authors： Staby A,Steensgaard DB,Haselmann KF,Marino JS,Bartholdy C,Videbæk N,Schelde O,Bosch-Traberg H,Spang LT,Asgreen DJ

更新日期：2020-06-08 00:00:00

abstract：PURPOSE:Radial basis function artificial neural networks and theoretical descriptors were used to develop a quantitative structure-pharmacokinetic relationship for structurally diverse drug compounds. METHODS:Human bioavailability values were taken from the literature and descriptors were generated from the drug struc...

journal_title：Pharmaceutical research

authors： Turner JV,Maddalena DJ,Agatonovic-Kustrin S

更新日期：2004-01-01 00:00:00

abstract：PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...

journal_title：Pharmaceutical research

authors： Schmidt ST,Neustrup MA,Harloff-Helleberg S,Korsholm KS,Rades T,Andersen P,Christensen D,Foged C

更新日期：2017-08-01 00:00:00

abstract：PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...

journal_title：Pharmaceutical research

authors： Fernandez S,Chevrier S,Ritter N,Mahler B,Demarne F,Carrière F,Jannin V

更新日期：2009-08-01 00:00:00

abstract：:The effect of γ-cyclodextrin and its four derivatives on the solubility of progesterone in phosphate buffer pH 7.4 was investigated. γ-Cyclodextrin forms a complex precipitating from solution at low cyclodextrin concentrations. No precipitation of complexes was observed with the γ-cyclodextrin derivatives. This change...

journal_title：Pharmaceutical research

authors： Müller BW,Brauns U

更新日期：1985-11-01 00:00:00

abstract：PURPOSE:The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited b...

journal_title：Pharmaceutical research

authors： Fournier E,Dufresne MH,Smith DC,Ranger M,Leroux JC

更新日期：2004-06-01 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:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

journal_title：Pharmaceutical research

authors： Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

更新日期：1997-08-01 00:00:00

abstract：PURPOSE:The addition of high amounts of calcium remains a pharmaceutical concern due to its precipitation with phosphate in total parenteral nutrient (TPN) admixtures, compromising also the stability of the lipid emulsion. MATERIALS AND METHODS:Calcium-phosphate solubility was compared when using binary PN solutions v...

journal_title：Pharmaceutical research

authors： Chaieb D S,Chaumeil JC,Jebnoun S,Khrouf N,Hedhili A,Sfar S

更新日期：2008-11-01 00:00:00

abstract：:Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...

journal_title：Pharmaceutical research

authors： Tang C,Prueksaritanont T

更新日期：2010-09-01 00:00:00

abstract：PURPOSE:The purpose of this human intestinal perfusion study was to investigate the transport and metabolism of R/S-verapamil in the human jejunum (in vivo). METHODS:A regional single-pass perfusion of the jejunum was performed using a Loc-I-Gut perfusion tube in 12 healthy volunteers. Each perfusion lasted for 200 mi...

journal_title：Pharmaceutical research

authors： Sandström R,Karlsson A,Knutson L,Lennernäs H

更新日期：1998-06-01 00:00:00

abstract：:Chimeric L6 is a mouse-human monoclonal antibody specific for tumor cell-associated antigens. The factors affecting the physical and chemical stability of chimeric L6 were assessed at elevated temperatures (30-60 degrees C) and by multiple freezing and thawing. Three routes of degradation were observed: chemical degra...

journal_title：Pharmaceutical research

authors： Paborji M,Pochopin NL,Coppola WP,Bogardus JB

更新日期：1994-05-01 00:00:00

abstract：PURPOSE:This study seeks to develop fiber membranes for local sustained delivery of 25-hydroxyvitamin D3 to induce the expression and secretion of LL-37 at or near the surgical site, which provides a novel therapeutic approach to minimize the risk of infections. METHODS:25-hydroxyvitamin D3 loaded poly(L-lactide) (PLA...

journal_title：Pharmaceutical research

authors： Jiang J,Chen G,Shuler FD,Wang CH,Xie J

更新日期：2015-09-01 00:00:00

abstract：PURPOSE:To determine whether a Protected Graft Copolymer (PGC) containing fatty acid can be used as a stabilizing excipient for GLP-1 and whether PGC/GLP-1 given once a week can be an effective treatment for diabetes. METHODS:To create a PGC excipient, polylysine was grafted with methoxypolyethyleneglycol and fatty ac...

journal_title：Pharmaceutical research

authors： Castillo GM,Reichstetter S,Bolotin EM

更新日期：2012-01-01 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：:Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to th...

journal_title：Pharmaceutical research

authors： Quadros E,Landzert NM,LeRoy S,Gasparini F,Worosila G

更新日期：1994-02-01 00:00:00

abstract：PURPOSE:Anticancer chemotherapy usually involves the administration of several anticancer drugs that differ in their action mechanisms. Here, we aimed to test whether the combination of omacetaxine mepesuccinate (OMT) and doxorubicin (DOX) could show synergism, and whether the liposomal co-delivery of these two drugs c...

journal_title：Pharmaceutical research

authors： Shim G,Lee S,Choi J,Lee S,Kim CW,Oh YK

更新日期：2014-08-01 00:00:00

abstract：PURPOSE:The effect of the molecular weight of dextran on the molecular mobility and protein stability of freeze-dried serum gamma-globulin (BGG) formulations was studied. The stabilizing effect of higher molecular weight dextran is discussed in relation to the molecular mobility of the formulations. METHODS:The molecu...

journal_title：Pharmaceutical research

authors： Yoshioka S,Aso Y,Kojima S

更新日期：1997-06-01 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:We describe the AERX aerosol delivery system, a new, bolus inhalation device that is actuated at preprogrammed values of inspiratory flow rate and inhaled volume. We report on its in vitro characterization using a particular set of conditions used in pharmacokinetic and scintigraphic studies. METHODS:Multiple ...

journal_title：Pharmaceutical research

authors： Schuster J,Rubsamen R,Lloyd P,Lloyd J

更新日期：1997-03-01 00:00:00