S-(4-Nitrobenzyl)-6-thioinosine (NBMPR) is Not a Selective Inhibitor of Equilibrative Nucleoside Transporters but Also Blocks Efflux Activity of Breast Cancer Resistance Protein.

abstract：PURPOSE:To evaluate the potential for the acidic intestinal unstirred water layer (UWL) to induce drug supersaturation and enhance drug absorption from intestinal mixed micelles, via the promotion of fatty acid absorption. METHODS:Using a single-pass rat jejunal perfusion model, the absorptive-flux of cinnarizine and ...

journal_title：Pharmaceutical research

authors： Yeap YY,Trevaskis NL,Porter CJ

更新日期：2013-12-01 00:00:00

abstract：PURPOSE:To create poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), where a drug-encapsulating NP core is covered with polyethylene glycol (PEG) in a normal condition but exposes a cell-interactive TAT-modified surface in an environment rich in matrix metalloproteinases (MMPs). METHODS:PLGA NPs were modified w...

journal_title：Pharmaceutical research

authors： Gullotti E,Park J,Yeo Y

更新日期：2013-08-01 00:00:00

abstract：PURPOSE:We have already demonstrated that the HMG-CoA reductase inhibitor, pravastatin is actively taken up by isolated rat hepatocytes via a multispecific anion transporter (Yamazaki et al., Am. J. Physiol. 264, G36-44, (1993)). We further attempted the quantitative evaluation of this uptake in different experimental ...

journal_title：Pharmaceutical research

authors： Ishigami M,Tokui T,Komai T,Tsukahara K,Yamazaki M,Sugiyama Y

更新日期：1995-11-01 00:00:00

abstract：PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The mor...

journal_title：Pharmaceutical research

authors： Lee WR,Shen SC,Sun CK,Aljuffali IA,Suen SY,Lin YK,Wang JJ,Fang JY

更新日期：2015-05-01 00:00:00

abstract：PURPOSE:To study the impact of different process conditions and formulation compositions on metastable mannitol forms in protein formulations during lyophilization. METHODS:Mannitol was studied with and without other formulation components. A cryostage was used to mimic the different processing steps during lyophiliza...

journal_title：Pharmaceutical research

authors： Cao W,Xie Y,Krishnan S,Lin H,Ricci M

更新日期：2013-01-01 00:00:00

abstract：:A new method of analysis for the antihypertensive drug, hydralazine, is introduced. The assay involves the addition of p-nitrobenzaldehyde to blood samples containing hydralazine, to form a stable Schiff's base, hydralazine p-nitrobenzaldehyde hydrazone. The derivative is extracted from the blood into hexane and the s...

journal_title：Pharmaceutical research

authors： Semple HA,Tam YK,Tin S,Coutts RT

更新日期：1988-06-01 00:00:00

abstract：PURPOSE:To investigate the destruction of clinically-relevant bacteria within biofilms via the sustained release of the antibiotic tetracycline from zein-based electrospun polymeric fibrous matrices and to demonstrate the compatibility of such wound dressing matrices with human skin cells. METHODS:Zein/PCL triple laye...

journal_title：Pharmaceutical research

authors： Alhusein N,Blagbrough IS,Beeton ML,Bolhuis A,De Bank PA

更新日期：2016-01-01 00:00:00

abstract：PURPOSE:Since glomerular filtration rate (GFR) is responsible for the elimination of a large number of water-soluble drugs, the aim of this study was to develop a semi-physiological function for GFR maturation from neonates to adults. METHODS:In the pharmacokinetic analysis (NONMEM VI) based on data of gentamicin, tob...

journal_title：Pharmaceutical research

authors： De Cock RF,Allegaert K,Brussee JM,Sherwin CM,Mulla H,de Hoog M,van den Anker JN,Danhof M,Knibbe CA

更新日期：2014-10-01 00:00:00

abstract：PURPOSE:There is evidence that cholesterol affects the ATPase and transport functions of P-glycoprotein (P-gp). To study the influence of cholesterol on P-gp in a well defined lipid environment, we reconstituted P-gp in egg phosphatidylcholine (PhC) and PhC/cholesterol proteoliposomes with negligible residual amounts o...

journal_title：Pharmaceutical research

authors： Bucher K,Belli S,Wunderli-Allenspach H,Krämer SD

更新日期：2007-11-01 00:00:00

abstract：PURPOSE:To evaluate different dissolution testing methods and subsequently develop a simple to perform but reproducible and discriminating dissolution technique for inhalative powders. METHODS:From a dry powder a fraction of aerosolized particles with an aerodynamic particle size below 5 μm was collected on regenerate...

journal_title：Pharmaceutical research

authors： May S,Jensen B,Wolkenhauer M,Schneider M,Lehr CM

更新日期：2012-08-01 00:00:00

abstract：PURPOSE:A theoretical study was performed to generate a pharmacophore model for chemically diverse structures that specifically interact with the diltiazem binding site of L-type calcium channels. METHODS:Via molecular mechanics and quantum chemical methods solvation energies, logP values, conformational and electroni...

journal_title：Pharmaceutical research

authors： Schleifer KJ,Tot E

更新日期：1999-10-01 00:00:00

abstract：:The fluxes of nitroglycerine (NG) through human abdominal epidermis from different individuals were measured in vitro at 32°C. The mean NG flux for the entire group was 16.9 µg/cm(2) × hr, with a standard deviation of 47.7%. There are no significant differences in the means and the variances of NG fluxes between males...

journal_title：Pharmaceutical research

authors： Langguth P,Spahn H,Mutschler E

更新日期：1986-02-01 00:00:00

abstract：:Enoximone and piroximone are cardiotonic agents for use in patients with congestive heart failure. Electroanalytical studies revealed that the dihydroimidazolone functionality was oxidizable and that this property can be analytically useful. The compounds undergo a two-electron, irreversible oxidation in neutral to ac...

journal_title：Pharmaceutical research

authors： Housmyer CL,Lewis RL Jr

更新日期：1991-07-01 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:To identify and quantify, in vitro and in vivo (in humans), the charge-carrying species during transdermal iontophoresis of lidocaine hydrochloride as a function of the concentration of drug relative to that of sodium chloride in the anodal solution. METHODS:In vitro experiments in standard diffusion cells qua...

journal_title：Pharmaceutical research

authors： Marro D,Kalia YN,Delgado-Charro MB,Guy RH

更新日期：2001-12-01 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：:Leucine enkephalin (YGGFL) undergoes rapid degradation in sheep nasal mucosa to yield GGFL which is further degraded to FL. The activity of the nasal mucosal homogenate against YGGFL and GGFL (t1/2 12 and 7 min) was significantly greater than that observed with a nasal wash fluid (t1/2 40 and 13 min). The effect of cy...

journal_title：Pharmaceutical research

authors： Irwin WJ,Dwivedi AK,Holbrook PA,Dey MJ

更新日期：1994-12-01 00:00:00

abstract：:This study utilized different statistical techniques to evaluate the reliability (internal consistency) and the discriminant validity of the most widely used measures of organizational commitment and intention to quit (the employing organization). Data were obtained from a national mail survey of members of the Americ...

journal_title：Pharmaceutical research

authors： Kong SX,Wertheimer AI,Serradell J,McGhan WF

更新日期：1994-01-01 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:A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063 (trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-[(2-methoxy)pyrimidin-4-yl] imidazole), a potent and selective p38 MAP kinase inhibitor. METHODS:SB-239063 was administered both i.v. and p.o. in the rat, dog, cynomol...

journal_title：Pharmaceutical research

authors： Ward KW,Proksch JW,Azzarano LM,Salyers KL,McSurdy-Freed JE,Molnar TM,Levy MA,Smith BR

更新日期：2001-09-01 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：:Equations for the steady-state volumes of distribution (Vss) and the mean residence times in the body (MRT) are derived for a drug and its metabolite subject to reversible metabolism and separately infused intravenously at a constant rate to steady state of both compounds. The Vss and MRT parameters are functions of t...

journal_title：Pharmaceutical research

authors： Cheng H,Jusko WJ

更新日期：1990-06-01 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:Near-infrared reflectance spectroscopy (NIRS) was used to evaluate and quantify the effect of compression force on the NIR spectra of tablets. METHODS:Flat, white tablets with no orientation (scoring, etc.) were manufactured on a Stokes Rotary Tablet Press. NIRS was used to predict tablet hardness on the follo...

journal_title：Pharmaceutical research

authors： Morisseau KM,Rhodes CT

更新日期：1997-01-01 00:00:00

abstract：PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...

journal_title：Pharmaceutical research

authors： Cheruvallath VK,Riley CM,Narayanan SR,Lindenbaum S,Perrin JH

更新日期：1996-01-01 00:00:00

abstract：PURPOSE:A polysaccharide-flavonoid conjugate was developend and proposed for the treatment of pancreatic ductal adenocarcinoma (PDAC). METHODS:The conjugate was synthesized by free radical grafting reaction between catechin and dextran. The chemical characterization of the conjugate was obtained by UV-Vis, 1H-NMR, FT-...

journal_title：Pharmaceutical research

authors： Vittorio O,Cirillo G,Iemma F,Di Turi G,Jacchetti E,Curcio M,Barbuti S,Funel N,Parisi OI,Puoci F,Picci N

更新日期：2012-09-01 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:The purpose of this study is to show how disaccharides differ in their ability to protect lyophilized β-galactosidase from enzymatic activity loss and secondary structure changes during storage. METHODS:β-galactosidase was lyophilized with trehalose, sucrose, cellobiose or melibiose at 2:1, 20:1 and 40:1 excip...

journal_title：Pharmaceutical research

authors： Heljo VP,Jouppila K,Hatanpää T,Juppo AM

更新日期：2011-03-01 00:00:00

abstract：PURPOSE:A patient was denoted to be generic brittle (GB) if they had a negative opinion about generics (e.g. prior history of a switch problem) or took the innovator brand of their most problematic anti-epileptic drug (AED) when generic was available. The aim of this hypothesis-generating study was to assess possible g...

journal_title：Pharmaceutical research

authors： Das S,Guo D,Jiang X,Jiang W,Shu Y,Ting TY,Polli JE

更新日期：2020-02-26 00:00:00

abstract：PURPOSE:This study aimed to characterize the transepithelial transport of miltefosine (HePC), the first orally effective drug against visceral leishmaniasis, across the intestinal barrier to further understand its oral absorption mechanism. MATERIALS AND METHODS:Caco-2 cell monolayers were used as an in vitro model of...

journal_title：Pharmaceutical research

authors： Ménez C,Buyse M,Dugave C,Farinotti R,Barratt G

更新日期：2007-03-01 00:00:00