Elucidating the role of dose in the biopharmaceutics classification of drugs: the concepts of critical dose, effective in vivo solubility, and dose-dependent BCS.

abstract：PURPOSE:The objective of this study was to determine the pharmacokinetics and safety for NX1838 following injection into the vitreous humor of rhesus monkeys. METHODS:Plasma and vitreous humor pharmacokinetics were determined following a single bilateral 0.25, 0.50, 1.0, 1.5, or 2.0 mg/eye dose. In addition, the pharm...

journal_title：Pharmaceutical research

authors： Drolet DW,Nelson J,Tucker CE,Zack PM,Nixon K,Bolin R,Judkins MB,Farmer JA,Wolf JL,Gill SC,Bendele RA

更新日期：2000-12-01 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：PURPOSE:We compared cationic, polyamine-coated microparticles (MPs) and anionic, protein-coated MPs with respect to their phagocytosis and phagosomal fate in dendritic cells (DCs) and macrophages (Mphi). METHODS:Polystyrene MPs were surface modified by covalent coupling with fluorescein isothiocyanate-labeled polyamin...

journal_title：Pharmaceutical research

authors： Thiele L,Merkle HP,Walter E

更新日期：2003-02-01 00:00:00

abstract：PURPOSE:To study the structure and function of the intestinal H+/ peptide transporter PET1, we compared its amino acid sequence with those of related transporters belonging to the oligopeptide transporter family PTR, and with more distant transporter families. METHODS:We have developed a new approach to the sequence a...

journal_title：Pharmaceutical research

authors： Graul RC,Sadée W

更新日期：1997-04-01 00:00:00

abstract：PURPOSE:To develop resource-sparing in silico approaches that aim to reduce experimental effort and material required by developability assessments (DA) of monoclonal antibody (mAb) drug candidates. METHODS:A battery of standardized biophysical experiments was performed on high concentration formulations of 16 drug pr...

journal_title：Pharmaceutical research

authors： Tomar DS,Singh SK,Li L,Broulidakis MP,Kumar S

更新日期：2018-08-20 00:00:00

abstract：PURPOSE:A Selegiline Transdermal System (STS) is under development for indications which may not be optimally or safely treated with oral selegiline. Studies were conducted to evaluate the in vitro penetration and skin metabolism of selegiline in order to better understand the toxicological findings and the observed pl...

journal_title：Pharmaceutical research

authors： Rohatagi S,Barrett JS,McDonald LJ,Morris EM,Darnow J,DiSanto AR

更新日期：1997-01-01 00:00:00

abstract：PURPOSE:To study the role of unsaturated fatty acid ester substituents in the autoxidation of polysorbate 80 using quantitative kinetics. METHODS:Oxidation kinetics were monitored at 40 degrees C in aqueous solution by tracking head space oxygen consumption using a fiber optic oxygen sensor with phase shift fluorescen...

journal_title：Pharmaceutical research

authors： Yao J,Dokuru DK,Noestheden M,Park SS,Kerwin BA,Jona J,Ostovic D,Reid DL

更新日期：2009-10-01 00:00:00

abstract：PURPOSE:To investigate the mechanisms involved in transport of sulfasalazine in Caco-2 cells. METHODS:Permeability coefficients of sulfasalazine and its analogs across Caco-2 cell monolayers were measured as a function of direction of transport, energy and concentration dependence, and in the presence of inhibitors of...

journal_title：Pharmaceutical research

authors： Liang E,Proudfoot J,Yazdanian M

更新日期：2000-10-01 00:00:00

abstract：PURPOSE:The aim of the present study was to improve the dry powder inhalation behavior of steroid KSR-592 with lactose by altering the crystal shape and the particle size of the drug for use in a newly designed inhalation device, Jethaler. METHOD:The shape of the crystals was changed by polymorphic transformation of o...

journal_title：Pharmaceutical research

authors： Ikegami K,Kawashima Y,Takeuchi H,Yamamoto H,Isshiki N,Momose D,Ouchi K

更新日期：2002-10-01 00:00:00

abstract：:Prinomide tromethamine, a nonsteroidal antiinflammatory drug, was orally administered at doses of 250, 500, and 1000 mg every 12 hr for 28 days to healthy male volunteers. The pharmacokinetic behavior of prinomide and its primary plasma metabolite displayed nonlinear characteristics, while those of free prinomide and ...

journal_title：Pharmaceutical research

authors： Kochak GM,Pai S,Iannucci R,Honc F,Kachmar D,Perrino P,Egger H

更新日期：1993-01-01 00:00:00

abstract：PURPOSE:In this study we aimed to evaluate adaptive designs (ADs) by clinical trial simulation for a pharmacokinetic-pharmacodynamic model in oncology and to compare them with one-stage designs, i.e., when no adaptation is performed, using wrong prior parameters. METHODS:We evaluated two one-stage designs, ξ0 and ξ*, ...

journal_title：Pharmaceutical research

authors： Lestini G,Dumont C,Mentré F

更新日期：2015-10-01 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：PURPOSE:Evaluate the ability of (-)-6-aminocarbovir ((-)-6AC) to improve the CNS exposure to (-)-carbovir ((-)-CBV). METHODS:Activation of (-)-6AC in vitro was assessed by incubations of rat brain tissue homogenates. The in vivo brain exposure to (-)-CBV was then examined in rats after iv infusions of either (-)-CBV (...

journal_title：Pharmaceutical research

authors： Wen YD,Remmel RP,Pham PT,Vince R,Zimmerman CL

更新日期：1995-06-01 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:Simvastatin (SIM), a HMG-CoA reductase inhibitor widely prescribed for hypercholesterolemia, has been reported to ameliorate inflammation and promote osteogenesis. Its clinical applications on these potential secondary indications, however, have been hampered by its lack of osteotropicity and poor water solubil...

journal_title：Pharmaceutical research

authors： Wang X,Jia Z,Almoshari Y,Lele SM,Reinhardt RA,Wang D

更新日期：2018-06-25 00:00:00

abstract：PURPOSE:This paper aims to investigate the immunoinhibitory properties of a lymph nodes-targeting suppressive oligonucleotide (ODN) for the potential treatment of autoimmune diseases or chronic inflammation. METHODS:Synthetic suppressive ODN engineered with an albumin-binding diacyl lipid at the 5'-terminal (lipo-ODN)...

journal_title：Pharmaceutical research

authors： Yu C,An M,Jones E,Liu H

更新日期：2018-02-08 00:00:00

abstract：:The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...

journal_title：Pharmaceutical research

authors： Stebler T,Guentert TW

更新日期：1992-10-01 00:00:00

abstract：PURPOSE:E-selectin is a cell adhesion molecule that is specifically expressed in the inflammatory vascular endothelium in response to cytokines such as IL-1 beta and TNF-alpha, and interacts with specific ligands containing sialyl Lewis X (Neu5Ac alpha 2-3Gal beta 1-4(Fuc alpha 1-3)GlcNAc-, SLex). In order to investiga...

journal_title：Pharmaceutical research

authors： Horie K,Sakagami M,Kuramochi K,Hanasaki K,Hamana H,Ito T

更新日期：1999-02-01 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：: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:To study Cereport (RMP-7, bradykinin B2 agonist) effects on human brain microvascular endothelial cell (HBMEC) monolayer permeability. METHODS:HBMEC grown on transwell membranes were exposed to Cereport. The monolayer permeability was determined with [14C]-inulin (MW. 5,200) and [3H]-dextran (MW. 70,000). RES...

journal_title：Pharmaceutical research

authors： Mackic JB,Stins M,Jovanovic S,Kim KS,Bartus RT,Zlokovic BV

更新日期：1999-09-01 00:00:00

abstract：PURPOSE:This study examined the rheological and textural characteristics (hardness, compressibilty, adhesiveness and cohesiveness) of bioadhesive oral gels containing the antimicrobial agent chlorhexidine. METHODS:Textural analysis was performed using a Stable Micro Systems texture analyser (model TA-XT 2) in texture ...

journal_title：Pharmaceutical research

authors： Jones DS,Woolfson AD,Brown AF

更新日期：1997-04-01 00:00:00

abstract：:Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...

journal_title：Pharmaceutical research

authors： Rathore AS,Garcia-Aponte OF,Golabgir A,Vallejo-Diaz BM,Herwig C

更新日期：2017-02-01 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：:The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or...

journal_title：Pharmaceutical research

authors： Bodmeier R,Paeratakul O

更新日期：1994-06-01 00:00:00

abstract：PURPOSE:The relationship between rat intestinal permeability (Papp) of a range of hydrophilic probe molecules and probe geometry was examined. METHODS:Molecules studies included mannitol, the polyethylene glycols (PEGs) 400, 900, and 4000, the dextran conjugated dye Texas Red (MW 3000) and the polysaccharide inulin (M...

journal_title：Pharmaceutical research

authors： Lane ME,O'Driscoll CM,Corrigan OI

更新日期：1996-10-01 00:00:00

abstract：:Celiac disease (CD) is an immune-mediated enteropathy triggered by the ingestion of gluten-containing grains that affects ~1% of the white ethnic population. In the last decades, a rise in prevalence of CD has been observed that cannot be fully explained by improved diagnostics. Genetic predisposition greatly influenc...

journal_title：Pharmaceutical research

authors： Matoori S,Fuhrmann G,Leroux JC

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:Interferon beta is commonly used as therapeutic in the first line of therapy for multiple sclerosis. However, depending on the product, it induces an antibody response in up to 60% of patients. This study evaluated the impact of therapy related factors like dose, route of administration and administration frequ...

journal_title：Pharmaceutical research

authors： Kijanka G,Jiskoot W,Schellekens H,Brinks V

更新日期：2013-06-01 00:00:00

abstract：PURPOSE:Magnetic resonance imaging (MRI) is widely used for diagnostic imaging in preclinical studies and in clinical settings. Considering the intrinsic low sensitivity and poor specificity of standard MRI contrast agents, the enhanced delivery of MRI tracers into tumors is an important challenge to be addressed. This...

journal_title：Pharmaceutical research

authors： Kato Y,Zhu W,Backer MV,Neoh CC,Hapuarachchige S,Sarkar SK,Backer JM,Artemov D

更新日期：2015-11-01 00:00:00

abstract：PURPOSE:To characterize temporal exposure and elimination of 5 gold/dendrimer composite nanodevices (CNDs) (5 nm positive, negative, and neutral, 11 nm negative, 22 nm positive) in mice using a physiologically based mathematical model. METHODS:400 ug of CNDs is injected intravenously to mice bearing melanoma cell line...

journal_title：Pharmaceutical research

authors： Mager DE,Mody V,Xu C,Forrest A,Lesniak WG,Nigavekar SS,Kariapper MT,Minc L,Khan MK,Balogh LP

更新日期：2012-09-01 00:00:00