Human jejunal permeability of cyclosporin A: influence of surfactants on P-glycoprotein efflux in Caco-2 cells.

abstract：:A quantitative analysis of the dependence of dissolution rate on the relative surface area occupied by two non-interacting drug mixtures from co-compressed slabs is described. The results from the experimental dissolution rates of each component from naproxen/phenytoin co-compressed slabs under laminar flow conditions...

journal_title：Pharmaceutical research

authors： Neervannan S,Southard MZ,Stella VJ

更新日期：1994-10-01 00:00:00

abstract：PURPOSE:Vancomycin (VCM) concentration is often out of therapeutic range (10-20 μg/ml) in patients receiving continuous renal replacement therapy (CRRT). The purposes of this study were to develop a practical VCM population pharmacokinetic (PPK) model and to evaluate the potential of Bayesian prediction-based therapeut...

journal_title：Pharmaceutical research

authors： Oda K,Jono H,Kamohara H,Nishi K,Tanoue N,Saito H

更新日期：2020-05-28 00:00:00

abstract：PURPOSE:To determine the different conformations of the acyloxyalkoxy-linked cyclic prodrug 1 of the model hexapeptide 2 in solution and to investigate the relationship between these solution conformations and the cellular permeability characteristics of this prodrug. METHODS:Two-dimensional Homonuclear Hartmann-Hahn ...

journal_title：Pharmaceutical research

authors： Gangwar S,Jois SD,Siahaan TJ,Vander Velde DG,Stella VJ,Borchardt RT

更新日期：1996-11-01 00:00:00

abstract：:Gene delivery systems are designed to control the location of administered therapeutic genes within a patient's body. Successful in vivo gene transfer may require (i) the condensation of plasmid and its protection from nuclease degradation, (ii) cellular interaction and internalization of condensed plasmid, (iii) esca...

journal_title：Pharmaceutical research

authors： Mahato RI,Rolland A,Tomlinson E

更新日期：1997-07-01 00:00:00

abstract：PURPOSE:To evaluate and classify the hydrolases of the primate lung. METHODS:Homologous series of aromatic, aliphatic, and choline ester substrates were assayed with the pH-stat method to obtain the Michaelis-Menten kinetic constants, Vmax and K(m), for the enzymes in pulmonary alveolar tissue with esterase activity. ...

journal_title：Pharmaceutical research

authors： Leng HM,Syce JA

更新日期：1997-02-01 00:00:00

abstract：:A new magnetic microsphere carrier has been formulated that may localize drugs by both biochemical and physical means. The microspheres, prepared from the polysaccharide chitosan, are designed to bind to anionic glycosaminoglycan receptors on the surface of capillary endothelial cells. The microspheres were formulated...

journal_title：Pharmaceutical research

authors： Gallo JM,Hassan EE

更新日期：1988-05-01 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:To develop a new intradermal antigen delivery system by coating microneedle arrays with lipid bilayer-coated, antigen-loaded mesoporous silica nanoparticles (LB-MSN-OVA). METHODS:Synthesis of MSNs with 10-nm pores was performed and the nanoparticles were loaded with the model antigen ovalbumin (OVA), and coate...

journal_title：Pharmaceutical research

authors： Tu J,Du G,Reza Nejadnik M,Mönkäre J,van der Maaden K,Bomans PHH,Sommerdijk NAJM,Slütter B,Jiskoot W,Bouwstra JA,Kros A

更新日期：2017-08-01 00:00:00

abstract：PURPOSE:Paclitaxel is active and widely used to treat multiple types of solid tumors. The commercially available paclitaxel formulation uses Cremophor/ethanol (C/E) as the solubilizers. Other formulations including nanoparticles have been introduced. This study evaluated the effects of nanoparticle formulation of pacli...

journal_title：Pharmaceutical research

authors： Yeh TK,Lu Z,Wientjes MG,Au JL

更新日期：2005-06-01 00:00:00

abstract：PURPOSE:We aimed to assess the fate of β-arteether lipid-based drug delivery systems (AE-LBDDS) in terms of resistance to lipolysis and permeation across intestinal cells. METHODS:AE-LBDDS contained Tween 80 or Cremophor EL as surfactants, ethanol, Maisine 35-1 and vegetable oil. The solubilization behavior of AE was ...

journal_title：Pharmaceutical research

authors： Memvanga PB,Eloy P,Gaigneaux EM,Préat V

更新日期：2013-10-01 00:00:00

abstract：:Growing tumors develop additional new blood vessels to meet the demand for adequate nutrients and oxygen, a process called angiogenesis. Cancer is a highly complex disease promoted by excess angiogenesis; interfering with this process poses for an attractive approach for controlling tumor growth. This hypothesis led t...

journal_title：Pharmaceutical research

authors： Sudhakar A,Boosani CS

更新日期：2008-12-01 00:00:00

abstract：PURPOSE:An integrated ionic mobility-pore model for epidermal iontophoresis is developed from theoretical considerations using both the free volume and pore restriction forms of the model for a range of solute radii (rj) approaching the pore radii (rp) as well as approximation of the pore restriction form for rj/rp < 0...

journal_title：Pharmaceutical research

authors： Roberts MS,Lai PM,Anissimov YG

更新日期：1998-10-01 00:00:00

abstract：PURPOSE:This study aims to conduct an impact investigation in the hydrophobic-hydrophilic balance as an important factor for dissolution improvement of a hydrophilic carrier-based solid dispersion system. METHODS:Polymeric carriers with different hydrophobic to hydrophilic ratios were used to prepare several electrosp...

journal_title：Pharmaceutical research

authors： Teoh XY,Yeoh Y,Yoong LK,Chan SY

更新日期：2020-01-07 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：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

abstract：PURPOSE:To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6 substrate, metoprolol, between microsomes prepared from human intestinal mucosa and from human livers. METHODS:Microsomes were prepared from a panel of 31 human...

journal_title：Pharmaceutical research

authors： Madani S,Paine MF,Lewis L,Thummel KE,Shen DD

更新日期：1999-08-01 00:00:00

abstract：:Monte Carlo simulation technique used to evaluate the effect of the arrangement of concentrations on the efficiency of estimation of population pharmacokinetic parameters in the preclinical setting is described. Although the simulations were restricted to the one compartment model with intravenous bolus input, they pr...

journal_title：Pharmaceutical research

authors： Ette EI,Howie CA,Kelman AW,Whiting B

更新日期：1995-05-01 00:00:00

abstract：PURPOSE:Non-small cell lung cancer is the leading cause of cancer related deaths globally. Considering the side effects and diminishing chemosensitivity to chemotherapy, novel treatment approaches are sought. Hence, we aim to develop a liposomal co-delivery system of pDNA expressing shRNA against PFKFB3 (pshPFKFB3) and...

journal_title：Pharmaceutical research

authors： Chowdhury N,Vhora I,Patel K,Doddapaneni R,Mondal A,Singh M

更新日期：2017-11-01 00:00:00

abstract：:To achieve time-controlled or site-specific drug delivery in the gastrointestinal tract, a sigmoidal release system (SRS) was developed, which achieved a prolonged lag time, followed by rapid release. The theophylline beads with a thick Eudragit RS film coating showed very low drug release in water, whereas the releas...

journal_title：Pharmaceutical research

authors： Narisawa S,Nagata M,Danyoshi C,Yoshino H,Murata K,Hirakawa Y,Noda K

更新日期：1994-01-01 00:00:00

abstract：:The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution. The effective human dose of once-a-month injectable microspheres of leuprolide was estimated to be about 3.2 to 8.1 mg analogue/month using these param...

journal_title：Pharmaceutical research

authors： Okada H,Inoue Y,Heya T,Ueno H,Ogawa Y,Toguchi H

更新日期：1991-06-01 00:00:00

abstract：:Biotherapeutics, including recombinant or plasma-derived human proteins and antibody-based molecules, have emerged as an important class of pharmaceuticals. Aggregation and immunogenicity are among the major bottlenecks during discovery and development of biotherapeutics. Computational tools that can predict aggregati...

journal_title：Pharmaceutical research

authors： Kumar S,Singh SK,Wang X,Rup B,Gill D

更新日期：2011-05-01 00:00:00

abstract：PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...

journal_title：Pharmaceutical research

authors： Houdaihed L,Evans JC,Allen C

更新日期：2020-01-21 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：:The pharmacokinetics of cefixime, a new orally active cephalosporin, was studied after an intravenous dose of 50 mg/kg to four beagle dogs. Cefixime was shown to exhibit concentration dependent serum protein binding and saturable tubular reabsorption. The drug was excreted mainly in the urine, the net result of glomer...

journal_title：Pharmaceutical research

authors： Tonelli AP,Bialer M,Look ZM,Carson S,Yacobi A

更新日期：1986-06-01 00:00:00

abstract：:Nasal sprays containing different concentrations of the somatostatin analogue octreotide and sodium tauro-24,25-dihydrofusidate (STDHF) as an absorption promoter were evaluated in two consecutive pharmacokinetic studies in healthy volunteers to characterize their bioavailability and local tolerability. The concentrati...

journal_title：Pharmaceutical research

authors： Kissel T,Drewe J,Bantle S,Rummelt A,Beglinger C

更新日期：1992-01-01 00:00:00

abstract：PURPOSE:The main goal of this research was to assess the mechanical properties of APIs' polymorphic forms at the single-crystal level (piroxicam, famotidine, nifedipine, olanzapine) in order to predict their bulk deformational attributes, which are critical for some pharmaceutical technology processes. METHODS:The mec...

journal_title：Pharmaceutical research

authors： Egart M,Janković B,Lah N,Ilić I,Srčič S

更新日期：2015-02-01 00:00:00

abstract：PURPOSE:This study uses high drug content solid dispersions for dose window extension beyond current demonstrations using fused deposition modelling (FDM) to; i) accommodate pharmaceutically relevant doses of drugs of varying potencies at acceptable dosage form sizes and ii) enable enhanced dose flexibility via modular...

journal_title：Pharmaceutical research

authors： Govender R,Abrahmsén-Alami S,Folestad S,Larsson A

更新日期：2019-12-17 00:00:00

abstract：PURPOSE:Interleukin-10 (IL-10) is an anti-inflammatory molecule that has achieved interest as a therapeutic for neuropathic pain. In this work, the potential of plasmid DNA-encoding IL-10 (pDNA-IL-10) slowly released from biodegradable microparticles to provide long-term pain relief in an animal model of neuropathic pa...

journal_title：Pharmaceutical research

authors： Soderquist RG,Sloane EM,Loram LC,Harrison JA,Dengler EC,Johnson SM,Amer LD,Young CS,Lewis MT,Poole S,Frank MG,Watkins LR,Milligan ED,Mahoney MJ

更新日期：2010-05-01 00:00:00

abstract：:A new technique has been developed to calculate rapidly the solid-state room-temperature degradation rate of drugs and drug candidates. The technique utilizes measurements of the initial rate of heat output at several elevated temperatures by isothermal calorimetry and the degradation rate of the compound determined a...

journal_title：Pharmaceutical research

authors： Koenigbauer MJ,Brooks SH,Rullo G,Couch RA

更新日期：1992-07-01 00:00:00

abstract：PURPOSE:Previous literature has suggested the absence of an effective barrier between the nasal mucosa and the brain for compounds administered via the nasal route. These experiments were conducted to elucidate the role of the blood-brain barrier efflux transporter P-glycoprotein (P-gp) in attenuating delivery of P-gp ...

journal_title：Pharmaceutical research

authors： Graff CL,Pollack GM

更新日期：2003-08-01 00:00:00