Improved prediction of in vivo peroral absorption from in vitro intestinal permeability using an internal standard to control for intra- and inter-rat variability.

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:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...

journal_title：Pharmaceutical research

authors： Kaul G,Amiji M

更新日期：2002-07-01 00:00:00

abstract：:To clarify the mechanism by which basic drugs accumulate in the lung, the binding selectivity of drugs to different subcellular structures of the perfused rat lung was examined. Imipramine, quinine, and metoclopramide were used as examples of basic drugs. The accumulation of basic drugs was highest in the mitochondria...

journal_title：Pharmaceutical research

authors： Yoshida H,Okumura K,Hori R

更新日期：1987-02-01 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：PURPOSE:Studies were conducted to evaluate whether the use of an in vitro model of the blood-brain barrier (BBB) resulted in more accurate predictions of the in vivo transport of compounds compared to the use of a human intestinal cell line (Caco-2). METHODS:The in vitro BBB model employs bovine brain capillary endoth...

journal_title：Pharmaceutical research

authors： Lundquist S,Renftel M,Brillault J,Fenart L,Cecchelli R,Dehouck MP

更新日期：2002-07-01 00:00:00

abstract：PURPOSE:To develop and subsequently evaluate a novel phase inversion-based method used to formulate lipidic nanocapsules. METHODS:Mechanical properties of emulsions prepared by multiinversion phase processes were investigated using a drop tensiometer. Based on the results obtained, a formulation process was developed ...

journal_title：Pharmaceutical research

authors： Heurtault B,Saulnier P,Pech B,Proust JE,Benoit JP

更新日期：2002-06-01 00:00:00

abstract：PURPOSE:The purpose of the present study is to explore whether a poly-L-arginine (poly-L-Arg)-induced increase in tight junctions (TJ) permeability of fluorescein isothiocyanate-labeled dextran (MW 4.4 kDa, FD-4) is associated with the Ca2+-dependent signaling and occurs following the phosphorylation/dephosphorylation ...

journal_title：Pharmaceutical research

authors： Ohtake K,Maeno T,Ueda H,Ogihara M,Natsume H,Morimoto Y

更新日期：2003-11-01 00:00:00

abstract：PURPOSE:Knowledge about the uptake mechanism and subsequent intracellular routing of non-viral gene delivery systems is important for the development of more efficient carriers. In this study we compared two established cationic polymers pDMAEMA and PEI with regard to their transfection efficiency and mechanism of cell...

journal_title：Pharmaceutical research

authors： van der Aa MA,Huth US,Häfele SY,Schubert R,Oosting RS,Mastrobattista E,Hennink WE,Peschka-Süss R,Koning GA,Crommelin DJ

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:Models to predict membrane-water partition coefficients (Kp) as a function of drug structure, membrane composition, and solution properties would be useful. This study explores the partitioning of dexamethasone (Dex) and its ionizable 21-phosphate (Dex-P) in liposomes varying in acyl chain length, physical stat...

journal_title：Pharmaceutical research

authors： Modi S,Anderson BD

更新日期：2013-12-01 00:00:00

abstract：:Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from cap...

journal_title：Pharmaceutical research

authors： Van den Mooter G,Samyn C,Kinget R

更新日期：1995-02-01 00:00:00

abstract：PURPOSE AND METHODS:Data from 358 pharmacist-patient encounters in 12 community pharmacies were used to investigate the association of prescription status, patient age, patient gender, and patient question asking with the content of pharmacist-patient communication. RESULTS:There was an association between prescriptio...

journal_title：Pharmaceutical research

authors： Schommer JC,Wiederholt JB

更新日期：1997-02-01 00:00:00

abstract：:Physicochemical effects caused by intestinal fluids on drugs in the gastrointestinal (GI) tract can be a contributing factor in food induced changes in bioavailability. To identify physicochemical properties of gemfibrozil that may be altered by endogenous and dietary lipids, in vitro studies were conducted in model s...

journal_title：Pharmaceutical research

authors： Luner PE,Babu SR,Radebaugh GW

更新日期：1994-12-01 00:00:00

abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...

journal_title：Pharmaceutical research

authors： Park K,Kim YS,Lee GY,Nam JO,Lee SK,Park RW,Kim SY,Kim IS,Byun Y

更新日期：2007-01-01 00:00:00

abstract：PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...

journal_title：Pharmaceutical research

authors： Tian R,Koyabu N,Takanaga H,Matsuo H,Ohtani H,Sawada Y

更新日期：2002-06-01 00:00:00

abstract：:Previous work from this laboratory showed site-dependent variations in the apparent permeability of insulin as measured using the everted rat gut sac technique, with the greatest permeability in the distal jejunum and the lowest in the duodenum (5). To quantify better the rate and extent of insulin absorption from the...

journal_title：Pharmaceutical research

authors： Schilling RJ,Mitra AK

更新日期：1992-08-01 00:00:00

abstract：PURPOSE:The cause of antibody positive pure red cell aplasia associated with the subcutaneous administration of EPREX to patients with chronic kidney failure has been determined to be due to the leaching of weakly adjuvant compounds from the uncoated rubber stoppers that were formerly used in prefilled syringes. Other ...

journal_title：Pharmaceutical research

authors： Villalobos AP,Gunturi SR,Heavner GA

更新日期：2005-07-01 00:00:00

abstract：PURPOSE:The lack of effective delivery vehicles impedes in vivo applications of siRNA. The trimethyl chitosan-cysteine (TC) nanoparticles (NPs) were developed for in vivo delivery of tumor necrosis factor α (TNF-α) siRNA via oral gavage and intraperitoneal injection. METHODS:The nanoparticles formulated from TC conjug...

journal_title：Pharmaceutical research

authors： He C,Yin L,Tang C,Yin C

更新日期：2013-10-01 00:00:00

abstract：PURPOSE:We present a smart intradermal interface suitable for skin-attached drug delivery devices. Our solution enables injections or infusions that are less invasive compared to subcutaneous injections and are leakage-free at the location of penetration. METHODS:The intradermal interface is based on a 31-gauge cannul...

journal_title：Pharmaceutical research

authors： Vosseler M,Jugl M,Zengerle R

更新日期：2011-03-01 00:00:00

abstract：PURPOSE:To study the influence of crystallizing and non-crystallizing cosolutes on the crystallization behavior of trehalose in frozen solutions and to monitor the phase behavior of trehalose dihydrate and mannitol hemihydrate during drying. METHODS:Trehalose (a lyoprotectant) and mannitol (a bulking agent) are widely...

journal_title：Pharmaceutical research

authors： Sundaramurthi P,Suryanarayanan R

更新日期：2010-11-01 00:00:00

abstract：PURPOSE:Overexpression of the serine protease urokinase (uPA) is recognised as an important biomarker of metastatic disease and a druggable anticancer target. Plasminogen activator inhibitor type-2 (PAI-2/SerpinB2) is a specific uPA inhibitor with proven potential for use in targeted therapy. However, PAI-2 is rapidly ...

journal_title：Pharmaceutical research

authors： Vine KL,Lobov S,Indira Chandran V,Harris NL,Ranson M

更新日期：2015-03-01 00:00:00

abstract：PURPOSE:To co-crystallise mannitol and lactose with a view to obtaining crystals with more favourable morphological features than either lactose or mannitol alone, suitable for use as carriers in formulations for dry powder inhalers (DPIs) using simultaneous engineering of lactose-mannitol mixtures. METHODS:Mannitol a...

journal_title：Pharmaceutical research

authors： Kaialy W,Larhrib H,Martin GP,Nokhodchi A

更新日期：2012-08-01 00:00:00

abstract：PURPOSE:To investigate the effect of tyrphostin 8 (T-8), a GTPase inhibitor, on transferrin receptor (TfR)-mediated transcytosis of insulin-transferrin (In-Tf) conjugate in cultured enterocyte-like Caco-2 cells and on gastrointestinal (GI) absorption of In-Tf in streptozotocin (STZ)-induced diabetic rats. METHODS:Caco...

journal_title：Pharmaceutical research

authors： Xia CQ,Shen WC

更新日期：2001-02-01 00:00:00

abstract：PURPOSE:The purpose of this study was to evaluate an effect of the proteolytic enzyme papain on permeation of low molecular weight heparin (LMWH) in vitro and in vivo. MATERIALS AND METHODS:In vitro permeation studies were performed using rat small intestine as permeation barrier. In order to determine the ratio of pa...

journal_title：Pharmaceutical research

authors： Grabovac V,Schmitz T,Föger F,Bernkop-Schnürch A

更新日期：2007-05-01 00:00:00

abstract：:A new high-performance liquid chromatographic (HPLC) assay suitable for pharmacokinetic studies of enantiomers of fenoprofen (FEN) was developed. Following the addition of internal standard (IS; racemic ketoprofen), the plasma or urine constituents are extracted into a mixture of isooctane:isopropanol (95:5), back ext...

journal_title：Pharmaceutical research

authors： Mehvar R,Jamali F

更新日期：1988-01-01 00:00:00

abstract：PURPOSE:A double-mutant E224A/E262A full-length botulinum neurotoxin (BoNT) Type A with structural similarity to native BoNT/A but lacking the endopeptidase activity provides an ideal surrogate for testing pharmacokinetics and immunochemical characteristics of BoNT. METHODS:We determined lethality (LD50) of deactivate...

journal_title：Pharmaceutical research

authors： Ravichandran E,Janardhanan P,Patel K,Riding S,Cai S,Singh BR

更新日期：2016-03-01 00:00:00

abstract：PURPOSE:Due to protease inhibitor (PI) efflux transport by P-glycoprotein (P-gp), insufficient PI concentrations result in low ongoing HIV replication in the so-called virus sanctuaries (brain and testes). The aim of the present study was to evaluate indinavir-loaded nanocapsules (Ind-LNC) including Solutol HS15, an ex...

journal_title：Pharmaceutical research

authors： Pereira de Oliveira M,Garcion E,Venisse N,Benoit JP,Couet W,Olivier JC

更新日期：2005-11-01 00:00:00

abstract：PURPOSE:Mannosylation of vaccines is a promising strategy to selectively target vaccine antigens to the mannose receptor expressed on dendritic cells (DCs). The purpose of this study was to investigate the effect of mannan (MN) chemically conjugated to poly(D, L-lactide-co-glycolic acid) (PLGA) nanoparticles (NPs) on a...

journal_title：Pharmaceutical research

authors： Hamdy S,Haddadi A,Shayeganpour A,Samuel J,Lavasanifar A

更新日期：2011-09-01 00:00:00

abstract：PURPOSE:To investigate the underlying cause for the observed differences in self-associating and viscoelastic behavior between two monoclonal antibodies, MAb1, and MAb2. METHODS:Several mutants were designed by swapping charged residues in MAb1 with those present in MAb2 at their respective positions and vice versa. R...

journal_title：Pharmaceutical research

authors： Yadav S,Sreedhara A,Kanai S,Liu J,Lien S,Lowman H,Kalonia DS,Shire SJ

更新日期：2011-07-01 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：:High molecular weight drugs in general, and peptides in particular, are usually delivered by parenteral route because they are poorly absorbed or degraded in the gastrointestinal tract. To optimize therapy, it is desirable to search for nonparenteral routes of administration and to deliver the drug in a controlled-rel...

journal_title：Pharmaceutical research

authors： Golomb G,Avramoff A,Hoffman A

更新日期：1993-06-01 00:00:00