Stability and solubility of celecoxib-PVP amorphous dispersions: a molecular perspective.

abstract：PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...

journal_title：Pharmaceutical research

authors： Nicklasson F,Alderborn G

更新日期：2000-08-01 00:00:00

abstract：PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...

journal_title：Pharmaceutical research

authors： Tian R,Koyabu N,Takanaga H,Matsuo H,Ohtani H,Sawada Y

更新日期：2002-06-01 00:00:00

abstract：:The stability of a freeze-dried model protein, ribonuclease A (RNase), was investigated under accelerated storage conditions at 45 degrees C for time periods up to 60 days. Because RNase is a fairly stable molecule around pH 7, lyophilization was performed in phosphate buffers at pH 4.0 or 10.0 to accelerate degradati...

journal_title：Pharmaceutical research

authors： Townsend MW,Byron PR,DeLuca PP

更新日期：1990-10-01 00:00:00

abstract：:Nucleoside transporters play a critical role in the absorption, disposition, and targeting of therapeutically used nucleosides and nucleoside analogs. This review is focused on the Na(+)-dependent, concentrative nucleoside transporters which are found in a variety of cells including renal, intestinal and hepatic epith...

journal_title：Pharmaceutical research

authors： Wang J,Schaner ME,Thomassen S,Su SF,Piquette-Miller M,Giacomini KM

更新日期：1997-11-01 00:00:00

abstract：PURPOSE:A mechanism-based PK-PD model was developed to predict the time course of dopamine D(2) receptor occupancy (D(2)RO) in rat striatum following administration of olanzapine, an atypical antipsychotic drug. METHODS:A population approach was utilized to quantify both the pharmacokinetics and pharmacodynamics of ol...

journal_title：Pharmaceutical research

authors： Johnson M,Kozielska M,Pilla Reddy V,Vermeulen A,Li C,Grimwood S,de Greef R,Groothuis GM,Danhof M,Proost JH

更新日期：2011-10-01 00:00:00

abstract：:Semitelechelic poly[N-(2-hydroxypropyl)methacrylamide]s (ST-PHPMA) containing one amino end-group and differing in molecular weight were synthesized by radical polymerization in the presence of 2-aminoethanethiol (AET) as chain transfer agent. These polymers were covalently attached via amide bonds to the surface of n...

journal_title：Pharmaceutical research

authors： Kamei S,Kopecek J

更新日期：1995-05-01 00:00:00

abstract：PURPOSE:The aim of this study was to examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...

journal_title：Pharmaceutical research

authors： McNamara DP,Whitney KM,Goss SL

更新日期：2003-10-01 00:00:00

abstract：PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...

journal_title：Pharmaceutical research

authors： Kafedjiiski K,Föger F,Werle M,Bernkop-Schnürch A

更新日期：2005-09-01 00:00:00

abstract：PURPOSE:In pharmacokinetic (PK)/pharmacodynamic (PD) modelling and simulations (M&S), omitting dropouts can cause inaccuracies in parameter estimation and clinical trial simulations (CTS). This study examines the impact of different imputation methods for missing data on the interpretation of model results, as well as ...

journal_title：Pharmaceutical research

authors： Yuen E,Gueorguieva I,Aarons L

更新日期：2014-10-01 00:00:00

abstract：:Silk is a remarkable biopolymer with a long history of medical use. Silk fabrications have a robust track record for load-bearing applications, including surgical threads and meshes, which are clinically approved for use in humans. The progression of top-down and bottom-up engineering approaches using silk as the basi...

journal_title：Pharmaceutical research

authors： Tran SH,Wilson CG,Seib FP

更新日期：2018-11-05 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:Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4-10 fusion protein (IL4-10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic param...

journal_title：Pharmaceutical research

authors： Steen-Louws C,Boross P,Prado J,Meeldijk J,Langenhorst JB,Huitema ADR,den Hartog MT,Boon L,Lafeber FPJG,Hack CE,Eijkelkamp N,Popov-Celeketic J

更新日期：2019-12-26 00:00:00

abstract：PURPOSE:For selective inhibition of endothelial cell activation in chronic inflammation, we have developed a dexamethasone-anti-E-selectin immunoconjugate. The present study was performed to evaluate the cellular handling of this immunoconjugate by activated primary endothelial cells and to compare its drug delivery ca...

journal_title：Pharmaceutical research

authors： Kok RJ,Everts M,Asgeirsdóttir SA,Meijer DK,Molema G

更新日期：2002-11-01 00:00:00

abstract：PURPOSE:To develop and subsequently evaluate a novel phase inversion-based method used to formulate lipidic nanocapsules. METHODS:Mechanical properties of emulsions prepared by multiinversion phase processes were investigated using a drop tensiometer. Based on the results obtained, a formulation process was developed ...

journal_title：Pharmaceutical research

authors： Heurtault B,Saulnier P,Pech B,Proust JE,Benoit JP

更新日期：2002-06-01 00:00:00

abstract：:A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...

journal_title：Pharmaceutical research

authors： Wolff M,Cordes G,Luckow V

更新日期：1985-01-01 00:00:00

abstract：PURPOSE:To study the reaction of artelinic acid with chemical model systems of cytochrome P-450 as a means of obtaining authentic samples of the putative metabolites necessary for identification of the mammalian metabolites of artelinic acid. METHODS:Artelinic acid was reacted with different organic complexes of iron(...

journal_title：Pharmaceutical research

authors： Idowu OR,Lin AJ,Grace JM,Peggins JO

更新日期：1997-10-01 00:00:00

abstract：PURPOSE:To investigate the effect of tyrphostin 8 (T-8), a GTPase inhibitor, on transferrin receptor (TfR)-mediated transcytosis of insulin-transferrin (In-Tf) conjugate in cultured enterocyte-like Caco-2 cells and on gastrointestinal (GI) absorption of In-Tf in streptozotocin (STZ)-induced diabetic rats. METHODS:Caco...

journal_title：Pharmaceutical research

authors： Xia CQ,Shen WC

更新日期：2001-02-01 00:00:00

abstract：PURPOSE:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...

journal_title：Pharmaceutical research

authors： Kaul G,Amiji M

更新日期：2002-07-01 00:00:00

abstract：PURPOSE:The purpose of this investigation was to determine the influence on the antimicrobial activity of cetylpyridinium chloride of the various components of the formulation of each of six candy based lozenges. METHODS:In vivo activity was investigated using six volunteers by determining the reduction in colony form...

journal_title：Pharmaceutical research

authors： Richards RM,Xing JZ,Weir LF

更新日期：1996-04-01 00:00:00

abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...

journal_title：Pharmaceutical research

authors： Fenart L,Buée-Scherrer V,Descamps L,Duhem C,Poullain MG,Cecchelli R,Dehouck MP

更新日期：1998-07-01 00:00:00

abstract：PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...

journal_title：Pharmaceutical research

authors： Joiris E,Di Martino P,Berneron C,Guyot-Hermann AM,Guyot JC

更新日期：1998-07-01 00:00:00

abstract：PURPOSE:The objective of this study is to evaluate the feasibility of using coated microneedles to deliver vaccines into the oral cavity to induce systemic and mucosal immune responses. METHOD:Microneedles were coated with sulforhodamine, ovalbumin and two HIV antigens. Coated microneedles were inserted into the inner...

journal_title：Pharmaceutical research

authors： Ma Y,Tao W,Krebs SJ,Sutton WF,Haigwood NL,Gill HS

更新日期：2014-09-01 00:00:00

abstract：:Microbial metabolism studies of the semisynthetic antimalarial anhydrodihydroartemisinin (1), have shown that it is metabolized by a number of microorganisms. Large scale fermentation with Streptomyces lavendulae L-105 and Rhizopogon species (ATCC 36060) have resulted in the isolation of four microbial metabolites. Th...

journal_title：Pharmaceutical research

authors： Khalifa SI,Baker JK,Rogers RD,el-Feraly FS,Hufford CD

更新日期：1994-07-01 00:00:00

abstract：PURPOSE:The aim of the study is to suppress the progress of estrogen-dependent breast cancer by inhibiting the membrane transporter, which mediates the internalization of estrone-3-sulfate as estrogen precursor in the cancer cells. METHODS:The uptake of estrone-3-sulfate by estrogen-dependent breast cancer MCF-7 cells...

journal_title：Pharmaceutical research

authors： Nozawa T,Suzuki M,Yabuuchi H,Irokawa M,Tsuji A,Tamai I

更新日期：2005-10-01 00:00:00

abstract：:A new enteric-coated formulation of sodium ursodeoxycholate was prepared and administered to man. The barrier film disintegrates and releases the drug only at pH > or = 5.5. The sodium salt of glycoursodeoxycholate was also prepared and encapsulated like ursodeoxycholate. Serum levels of ursodeoxycholate and glycourso...

journal_title：Pharmaceutical research

authors： Roda A,Roda E,Marchi E,Simoni P,Cerrè C,Pistillo A,Polimeni C

更新日期：1994-05-01 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：: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：:The interdependent relationship between pharmacology and toxicology is fundamental to the concepts of efficacy and safety of both drugs and xenobiotics. The traditional concept of establishing efficacious and tolerated doses to define a 'therapeutic window' appears simplistic in the context of an exponentially increas...

journal_title：Pharmaceutical research

authors： Sayes CM,Staats H,Hickey AJ

更新日期：2014-09-01 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:Studies were conducted to evaluate whether the use of an in vitro model of the blood-brain barrier (BBB) resulted in more accurate predictions of the in vivo transport of compounds compared to the use of a human intestinal cell line (Caco-2). METHODS:The in vitro BBB model employs bovine brain capillary endoth...

journal_title：Pharmaceutical research

authors： Lundquist S,Renftel M,Brillault J,Fenart L,Cecchelli R,Dehouck MP

更新日期：2002-07-01 00:00:00