Characterizing the expression of CYP3A4 and efflux transporters (P-gp, MRP1, and MRP2) in CYP3A4-transfected Caco-2 cells after induction with sodium butyrate and the phorbol ester 12-O-tetradecanoylphorbol-13-acetate.

abstract：PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...

journal_title：Pharmaceutical research

authors： Costantino HR,Firouzabadian L,Hogeland K,Wu C,Beganski C,Carrasquillo KG,Córdova M,Griebenow K,Zale SE,Tracy MA

更新日期：2000-11-01 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: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 characterize the distribution of water among various components in a powder blend using solid-state NMR spectroscopy. METHODS:Water sorption behavior of theophylline anhydrate and excipients was determined by dynamic vapor sorption (DVS) and Karl Fischer Titration (KFT) after storing them in humidity chambe...

journal_title：Pharmaceutical research

authors： Mistry P,Chakravarty P,Lubach JW

更新日期：2016-10-01 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:To gain information on the chemical stability pattern and the kinetics of the degradation of recombinant hirudin variant HV1 (rHir), a thrombin-specific inhibitor protein of 65 amino acids, in aqueous solution as a function of pH. METHODS:Stability of rHir was monitored at 50 degrees C in the framework of a cl...

journal_title：Pharmaceutical research

authors： Gietz U,Alder R,Langguth P,Arvinte T,Merkle HP

更新日期：1998-09-01 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：PURPOSE:To develop an enzymatically-controlled pulsatile drug release system based on an impermeable capsule body, which contains the drug and is closed by an erodible pectin/pectinase-plug. METHODS:The plug was prepared by direct compression of pectin and pectinase in different ratios. In addition to the disintegrati...

journal_title：Pharmaceutical research

authors： Krögel I,Bodmeier R

更新日期：1999-09-01 00:00:00

abstract：PURPOSE:4-Phenylbutyrate (4-PBA) is expected to be a potential therapeutic for several neurodegenerative diseases. These activities require 4-PBA transport into the brain across the blood-brain barrier (BBB). The objective of the present study was to characterize the brain transport mechanism of 4-PBA through the BBB. ...

journal_title：Pharmaceutical research

authors： Lee NY,Kang YS

更新日期：2016-07-01 00:00:00

abstract：PURPOSE:The aim was to investigate the influence of polymer content and molecular weight on the morphology and heat- and moisture-induced transformations, as indicators of stability, of spray-dried composite particles of amorphous lactose and poly(vinylpyrrolidone) (PVP). METHODS:Amorphous lactose and composite partic...

journal_title：Pharmaceutical research

authors： Berggren J,Alderborn G

更新日期：2003-07-01 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:We prepared injectable microspheres for controlled release of TAK-029, a water-soluble GPIIb/IIIa antagonist and discussed the characteristics of controlled release from microspheres. METHODS:Copoly(dl-lactic/glycolic)acid (PLGA) microspheres were used for controlled release of TAK-029 [4-(4-amidinobenzoylglyc...

journal_title：Pharmaceutical research

authors： Takada S,Kurokawa T,Miyazaki K,Iwasa S,Ogawa Y

更新日期：1997-09-01 00:00:00

abstract：:Indomethacin microspheres based on a combination of ethylcellulose and polyethyleneglycol were prepared using the solvent evaporation process. Release profiles of ensemble and individual microspheres were measured. Both were found to follow first-order kinetics, in contrast to what was expected. This was attributed to...

journal_title：Pharmaceutical research

authors： Benita S,Babay D,Hoffman A,Donbrow M

更新日期：1988-03-01 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:In principle, maximum transepidermal fluxes of solutes should be similar for different vehicles, except when the solute or vehicle modifies the skin. Here we estimated maximum flux, stratum corneum solubility, diffusivity and permeability coefficient for a range of similarly sized phenolic compounds with varyin...

journal_title：Pharmaceutical research

authors： Zhang Q,Li P,Liu D,Roberts MS

更新日期：2013-01-01 00:00:00

abstract：PURPOSE:To test the hypothesis that modification of release pattern of nonsteroidal anti-inflammatory drugs (NSAIDs) formulations shifts gastrointestinal (GI) toxicity of the drugs from the upper GI region to the distal intestine. METHODS:We assessed tiaprofenic acid (TA)-induced upper and lower increased GI permeabil...

journal_title：Pharmaceutical research

authors： Vakily M,Khorasheh F,Jamali F

更新日期：1999-01-01 00:00:00

abstract：:The glass transition temperature of an amorphous pharmaceutical solid is a critical physical property which can dramatically influence its chemical stability, physical stability, and viscoelastic properties. Water frequently acts as a potent plasticizer for such materials, and since many amorphous solids spontaneously...

journal_title：Pharmaceutical research

authors： Hancock BC,Zografi G

更新日期：1994-04-01 00:00:00

abstract：PURPOSE:Because interleukin-10 (IL-10) seems a promising new antifibrotic drug, we investigated the pharmacokinetic and biodistribution profile of this potent therapeutic cytokine in rats with extensive liver fibrosis (BDL-3). IL-10 receptor expression was also determined in relation to these aspects. METHODS:To study...

journal_title：Pharmaceutical research

authors： Rachmawati H,Beljaars L,Reker-Smit C,Van Loenen-Weemaes AM,Hagens WI,Meijer DK,Poelstra K

更新日期：2004-11-01 00:00:00

abstract：PURPOSE:The gastric mucoadhesive property of tetracycline-sucralfate acidic complex (CO) was evaluated by using a novel method in vitro to compare with the in vivo test. The mucoadhesive mechanism of the acidic complex was also studied. METHODS:The gastric mucosa removed from a rat was placed covering the end of a plu...

journal_title：Pharmaceutical research

authors： Higo S,Ori K,Takeuchi H,Yamamoto H,Hino T,Kawashima Y

更新日期：2004-03-01 00:00:00

abstract：PURPOSE:A thermodynamic analysis of the binding to rat cortex adenosine A1 receptor of N6-substituted (full agonists) and N6-substituted-deoxyribose (partial agonists) adenosine derivatives was performed. The intrinsic activity of the compounds was evaluated by measurements of the inhibition of forskolin stimulated 3',...

journal_title：Pharmaceutical research

authors： Dalpiaz A,Scatturin A,Pavan B,Varani K,IJzerman AP,Andrea Borea P

更新日期：1999-07-01 00:00:00

abstract：PURPOSE:This study examines methylprednisolone (MPL) effects on the dynamics of hepatic low-density lipoprotein receptor (LDLR) mRNA and plasma lipids associated with increased risks for atherosclerosis. MATERIALS AND METHODS:Normal male Wistar rats were given 50 mg/kg MPL intramuscularly (IM) and sacrificed at variou...

journal_title：Pharmaceutical research

authors： Hazra A,Pyszczynski NA,DuBois DC,Almon RR,Jusko WJ

更新日期：2008-04-01 00:00:00

abstract：PURPOSE:To characterize the uptake mechanism of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor, in syncytiotrophoblast cells using the TR-TBT 18d-1 cell line previously established by our group. MATERIALS AND METHODS:The effects of several transporter inhibitors on the initial and steady-state apical u...

journal_title：Pharmaceutical research

authors： Sai Y,Nishimura T,Shimpo S,Chishu T,Sato K,Kose N,Terasaki T,Mukai C,Kitagaki S,Miyakoshi N,Kang YS,Nakashima E

更新日期：2008-07-01 00:00:00

abstract：PURPOSE:The purpose of the present study was to explore the involvement of indoxyl sulfate (IS) in nephrotoxicity and central nervous system (CNS) toxicity in cisplatin (CDDP)-treated rats. MATERIALS AND METHODS:Renal function was evaluated by serum creatinine and BUN levels. The IS levels in the serum, brain and kidn...

journal_title：Pharmaceutical research

authors： Iwata K,Watanabe H,Morisaki T,Matsuzaki T,Ohmura T,Hamada A,Saito H

更新日期：2007-04-01 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：:The interaction of dicumarol and phenothiazine neuroleptics binding to alpha 1-acid glycoprotein (AGP) was investigated by circular dichroism (CD) and equilibrium dialysis. The induced CD spectra of the dicumarol-AGP complex were affected differently by the different substituents of the phenothiazine molecule. The sig...

journal_title：Pharmaceutical research

authors： Miyoshi T,Yamamichi R,Maruyama T,Otagiri M

更新日期：1992-07-01 00:00:00

abstract：:The pentahydrate (alpha form) of cefazolin sodium (CEZ) exhibited sharp X-ray diffraction peaks, while the dehydrated alpha form showed weak but distinct diffraction peaks. As expected the amorphous form exhibited a diffuse and halo diffraction pattern. The X-ray procedure to estimate the degree of crystallinity of CE...

journal_title：Pharmaceutical research

authors： Kamat MS,Osawa T,DeAngelis RJ,Koyama Y,DeLuca PP

更新日期：1988-07-01 00:00:00

abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

journal_title：Pharmaceutical research

authors： Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

更新日期：2004-07-01 00:00:00

abstract：:This review describes the design and current development of leukotriene biosynthesis inhibitors as potential antiinflammatory agents. Knowledge of the enzymatic mechanism of 5-lipoxygenase led to specific inhibitors of this enzyme which catalyzes a key step in the leukotriene pathway. Competitive inhibitors include ir...

journal_title：Pharmaceutical research

authors： Cashman JR

更新日期：1985-11-01 00:00:00

abstract：PURPOSE:An asymmetric membrane (AM) tablet was developed for a soluble model compound to study the in vitro drug release mechanisms in challenge conditions, including osmotic gradients, concentration gradients, and under potential coating failure modes. Porous, semipermable membrane integrity may be compromised by a hi...

journal_title：Pharmaceutical research

authors： Am Ende MT,Miller LA

更新日期：2007-02-01 00:00:00

abstract：PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...

journal_title：Pharmaceutical research

authors： Trichard L,Delgado-Charro MB,Guy RH,Fattal E,Bochot A

更新日期：2008-02-01 00:00:00