In vitro lipolysis and intestinal transport of β-arteether-loaded lipid-based drug delivery systems.

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：PURPOSE:Carboxylesterases are important in the detoxification of drugs, pesticides and other xenobiotics. This study was to evaluate a series of substrates and inhibitors for characterizing these enzymes. METHODS:A series of novel aliphatic esters and thioesters were used in spectral assays to monitor human, murine an...

journal_title：Pharmaceutical research

authors： Huang TL,Shiotsuki T,Uematsu T,Borhan B,Li QX,Hammock BD

更新日期：1996-10-01 00:00:00

abstract：PURPOSE:To produce and characterize a nonviral ultrasound-controlled release system of plasmid DNA (pDNA) encapsulated in gas-filled poly(D,L-lactide-co-glycolide) microparticles (PLGA-MPs). METHODS:Different cationic polymers were used to form pDNA/polymer complexes to enhance the stability of pDNA during micropartic...

journal_title：Pharmaceutical research

authors： Seemann S,Hauff P,Schultze-Mosgau M,Lehmann C,Reszka R

更新日期：2002-03-01 00:00:00

abstract：PURPOSE:Previous studies by other investigators have shown an enhancement of mitomycin C (MMC) activity at acidic extracellular pH (pHe) in monolayer cultures of human cells. The goal of the present study was to determine if the efficacy of intravesical MMC therapy in patients treated for superficial bladder cancer can...

journal_title：Pharmaceutical research

authors： Yen WC,Schmittgen T,Au JL

更新日期：1996-12-01 00:00:00

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 investigate the feasibility of using the Aerosol Solvent Extraction System (ASES) to produce fine powders of recombinant human deoxyribonuclease (rhDNase), lysozyme-lactose and rhDNase-lactose powders from aqueous based solutions. METHODS:The ASES technique using high pressure carbon dioxide modified with e...

journal_title：Pharmaceutical research

authors： Bustami RT,Chan HK,Sweeney T,Dehghani F,Foster NR

更新日期：2003-12-01 00:00:00

abstract：PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...

journal_title：Pharmaceutical research

authors： Shukla RS,Qin B,Wan YJ,Cheng K

更新日期：2011-12-01 00:00:00

abstract：PURPOSE:The aim was to evaluate fluorescent molecular rotors (DCVJ and CCVJ), which are mainly sensitive to viscosity, for the characterization of polysorbate-containing IgG formulations and compare them to the polarity-sensitive dyes ANS, Bis-ANS and Nile Red. METHODS:IgG formulations with polysorbate 20 or 80 were s...

journal_title：Pharmaceutical research

authors： Hawe A,Filipe V,Jiskoot W

更新日期：2010-02-01 00:00:00

abstract：PURPOSE:The major goal of this study was to compare the relative utility of the Hanson Microette and the Van Kel apparatus, two fully automated devices, as in vitro release tests (IVRT) for semisolids. We attempted to develop methodology that can be used to discriminate formulation changes, and to evaluate the precisio...

journal_title：Pharmaceutical research

authors： Rapedius M,Blanchard J

更新日期：2001-10-01 00:00:00

abstract：PURPOSE:This study investigated the penetration of lidocaine around and through a sutured incision following the application of iontophoretic and passive patches in the CD Hairless rat. MATERIALS AND METHODS:Concentrations in localized areas (suture, dermis, subcutaneous, and vascular) were determined using microdialy...

journal_title：Pharmaceutical research

authors： Holovics HJ,Anderson CR,Levine BS,Hui HW,Lunte CE

更新日期：2008-08-01 00:00:00

abstract：PURPOSE:To evaluate the effect of the size of low molecular weight hyaluronan (LMW-HA) oligomers on the targeting ability of the HA-containing copolymers to the CD44-overexpressing cells for delivering Paclitaxel (PTX) to ovarian cancer. METHODS:LMW-HA oligosaccharides of 4, 6, 8, 10, 12 and 14 sugar residues were att...

journal_title：Pharmaceutical research

authors： Journo-Gershfeld G,Kapp D,Shamay Y,Kopeček J,David A

更新日期：2012-04-01 00:00:00

abstract：PURPOSE:The purpose of the current study is to evaluate the solubility advantage offered by celecoxib (CEL) amorphous systems and to characterize and correlate the physical and thermodynamic properties of CEL and its amorphous molecular dispersions containing poly(vinylpyrrolidone) (PVP). METHODS:The measurement of cr...

journal_title：Pharmaceutical research

authors： Gupta P,Kakumanu VK,Bansal AK

更新日期：2004-10-01 00:00:00

abstract：:Physiologically-based pharmacokinetic (PBPK) models explicitly incorporate tissue-specific blood flows, partition coefficients, and metabolic processes. Since PBPK models are derived using physiologic parameters and interactions of the compound with tissue components, these models are considered to be "bottom up" as o...

journal_title：Pharmaceutical research

authors： Korzekwa K,Nagar S

更新日期：2017-03-01 00:00:00

abstract：PURPOSE:The study was performed for clarifying the mechanism of interaction between indoxyl sulfate (IS), a typical uremic toxin bound to site II, and site I-ligands when bound to human serum albumin (HSA). The effect of the N to B transition on the interactions was also examined. METHODS:Quantitative investigation of...

journal_title：Pharmaceutical research

authors： Sakai T,Yamasaki K,Sako T,Kragh-Hansen U,Suenaga A,Otagiri M

更新日期：2001-04-01 00:00:00

abstract：PURPOSE:TXA9, a novel cardiac glycoside, has a potent anti-proliferative effect against A549 human lung cancer cells, however, possesses a poor water-solubility and a rapid metabolic rate in vivo which limited the further development of TXA9. To overcome the shortcomings of TXA9, four polymer prodrugs of TXA9 were desi...

journal_title：Pharmaceutical research

authors： Li Y,Ye C,Cai C,Zhao M,Han N,Liu Z,Zhai J,Yin J

更新日期：2020-03-12 00:00:00

abstract：PURPOSE:The purpose of the present study was to investigate the transport of organic monocarboxylic acids mediated by the anion exchanger AE2, which has been already reported to be present at several tissue cell membranes, including intestinal brush border membrane in rabbit. METHODS:Membrane transport of organic mono...

journal_title：Pharmaceutical research

authors： Yabuuchi H,Tamai I,Sai Y,Tsuji A

更新日期：1998-03-01 00:00:00

abstract：PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...

journal_title：Pharmaceutical research

authors： Mano Y,Usui T,Kamimura H

更新日期：2006-07-01 00:00:00

abstract：PURPOSE:The purpose of this study was to clarify the localization and function of the ATP-binding cassette transporter G2 (ABCG2; BCRP/MXR/ABCP) in retinal capillary endothelial cells, which form the inner blood-retinal barrier, as an efflux transport system. METHODS:The expression was determined by reverse transcript...

journal_title：Pharmaceutical research

authors： Asashima T,Hori S,Ohtsuki S,Tachikawa M,Watanabe M,Mukai C,Kitagaki S,Miyakoshi N,Terasaki T

更新日期：2006-06-01 00:00:00

abstract：PURPOSE:To develop a new bionic system from an existing drug dissolution/absorption simulating system (DDASS) to simultaneously predict the release and absorption of enteric-coated formulations. METHODS:In accordance with the pH-dependent characteristics of enteric-coated formulations, the modified DDASS was designed ...

journal_title：Pharmaceutical research

authors： Liu W,He X,Li Z,Gao X,Ma Y,Xun M,Liu C

更新日期：2013-02-01 00:00:00

abstract：PURPOSE:The aim of this work was to develop a quantitative, flow cytometric method for tracking the endolysosomal escape of a fluorescently labelled saporin toxin. METHODS:Flow cytometric measurements of fluorescent pulse width and height were used to track the endocytic uptake into Daudi cells of a fluorescently labe...

journal_title：Pharmaceutical research

authors： Wensley HJ,Johnston DA,Smith WS,Holmes SE,Flavell SU,Flavell DJ

更新日期：2019-12-23 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:Previously, we have shown that complexes of plasmid DNA with the biodegradable polymer poly(2-dimethylamino ethylamino)phosphazene (p(DMAEA)-ppz) mediated tumor selective gene expression after intravenous administration in mice. In this study, we investigated the effect of p(DMAEA)-ppz molecular weight on both ...

journal_title：Pharmaceutical research

authors： de Wolf HK,de Raad M,Snel C,van Steenbergen MJ,Fens MH,Storm G,Hennink WE

更新日期：2007-08-01 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：: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:To determine of the pharmacokinetic profile of methotrexate (MTX) in blood and extracellular fluid (ECF) of VX2 tumor and muscle in rabbits. METHODS:Microdialysis probes were inserted into VX2 tumor and in muscle tissue. Following intravenous administration of MTX (30 mg/kg), serial collection of arterial bloo...

journal_title：Pharmaceutical research

authors： Dukic S,Kaltenbach ML,Gourdier B,Marty H,Vistelle R

更新日期：1998-01-01 00:00:00

abstract：PURPOSE:To develop a semi-physiological-based model describing simultaneously the time course of immature and mature B-lymphocytes after topotecan (TPT) administration to tumor-bearing rats. METHODS:Twenty-four tumor-bearing BDIX male rats received a single 6 mg/kg intra-peritoneal dose of TPT or saline. Mature and im...

journal_title：Pharmaceutical research

authors： Vélez de Mendizábal N,Martínez-Forero I,Garrido MJ,Bandrés E,García-Foncillas J,Segura C,Trocóniz IF

更新日期：2010-03-01 00:00:00

abstract：PURPOSE:We examined the subcellular distribution of the basic drugs, chlorpromazine (CPZ), imipramine (IMP) and biperiden (BP), in rat liver, and evaluated the contribution of lysosome (Lys) to their intracellular distribution in comparison with that of mitochondria (Mit). METHODS:In an in vivo distribution, the conce...

journal_title：Pharmaceutical research

authors： Ishizaki J,Yokogawa K,Hirano M,Nakashima E,Sai Y,Ohkuma S,Ohshima T,Ichimura F

更新日期：1996-06-01 00:00:00

abstract：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...

journal_title：Pharmaceutical research

authors： Bergen JM,Park IK,Horner PJ,Pun SH

更新日期：2008-05-01 00:00:00

abstract：PURPOSE:To investigate the potential of chitosan nanoparticles as a system for improving the systemic absorption of insulin following nasal instillation. METHODS:Insulin-loaded chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate anions. They were characterized for their size a...

journal_title：Pharmaceutical research

authors： Fernández-Urrusuno R,Calvo P,Remuñán-López C,Vila-Jato JL,Alonso MJ

更新日期：1999-10-01 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