Reversal of signs of induced cotton effects of dicumarol-alpha 1-acid glycoprotein systems by phenothiazine neuroleptics through ternary complexation.

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：BACKGROUND:Little is known about the affinity and stability of 99mTc-labeled 2-methoxyisobutylisonitrile (99mTc-MIBI) and tetrofosmin (99mTc-TF) for imaging of multiple drug resistance transporters in cancer. We examined the affinity of 99mTc-labeled compounds for these transporters and their stability. METHODS:99mTc-...

journal_title：Pharmaceutical research

authors： Kobayashi M,Tsujiuchi T,Okui Y,Mizutani A,Nishi K,Nakanishi T,Nishii R,Fukuchi K,Tamai I,Kawai K

更新日期：2018-11-29 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：:Apigenin, a naturally occurring plant flavone, abundantly present in common fruits and vegetables, is recognized as a bioactive flavonoid shown to possess anti-inflammatory, antioxidant and anticancer properties. Epidemiologic studies suggest that a diet rich in flavones is related to a decreased risk of certain cance...

journal_title：Pharmaceutical research

authors： Shukla S,Gupta S

更新日期：2010-06-01 00:00:00

abstract：PURPOSE:The purpose of this study was to investigate the effects of formulation factors including varying wax concentration, drug loading and drug particle size, on drug release characteristics from both pure oil and gel formulations prepared with a combination of derivatized vegetable oil (Labrafil 1944 CS) and glycer...

journal_title：Pharmaceutical research

authors： Gao ZH,Shukla AJ,Johnson JR,Crowley WR

更新日期：1995-06-01 00:00:00

abstract：PURPOSE:Nine common excipients were examined to determine their ability to cause disproportionation of the HCl salt of a a weakly basic compound. The goal was to determine which excipients were problematic and correlate the results to known properties such as surface pH, slurry pH, or molecular structure. Such a correl...

journal_title：Pharmaceutical research

authors： John CT,Xu W,Lupton LK,Harmon PA

更新日期：2013-06-01 00:00:00

abstract：:A 1H-NMR spectroscopic method for the determination of the optical purity of threo-methylphenidate hydrochloride is presented. Complexation of the free-base form of the substrate with a chiral Eu(III) shift reagent resulted in two distinct enantiomeric ester methyl proton signals of utility for quantitative work. The ...

journal_title：Pharmaceutical research

authors： Hanna GM,Lau-Cam CA

更新日期：1990-07-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate whether biodegradable nanocapsules could be obtained by the emulsification-diffusion technique. METHODS:This technique consists of emulsifying an organic solution containing an oil, a polymer, and a drug in an aqueous solution of a stabilizing agent. The subsequent addi...

journal_title：Pharmaceutical research

authors： Quintanar-Guerrero D,Allémann E,Doelker E,Fessi H

更新日期：1998-07-01 00:00:00

abstract：:The molecular environment of sucrose and mineral oil within sucrose and mineral oil solid state emulsions was investigated by NMR techniques. The 13C and 1H chemical shifts of sucrose and mineral oil to those observed in solid state emulsions (comprised of sucrose and mineral oil) were equivalent, indicating that the ...

journal_title：Pharmaceutical research

authors： Shively ML,Dec SF

更新日期：1994-09-01 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：:The Office of Generic Drugs has ensured the high quality of generic products based upon two requirements: pharmaceutical equivalence and bioequivalence to the reference listed drug (RLD). This paradigm has been used with success toward ensuring quality generic drug products that provide the same therapeutic benefit as...

journal_title：Pharmaceutical research

authors： Raw AS,Lionberger R,Yu LX

更新日期：2011-07-01 00:00:00

abstract：PURPOSE:Understanding the mechanism of protein-excipient interaction and illuminating the influencing factors on protein stability are key steps in the rational design of protein formulations. The objective of this study was to assess effects of preferential interaction type of excipient and surface aromatic hydrophobi...

journal_title：Pharmaceutical research

authors： Wen L,Zheng X,Wang X,Lan H,Yin Z

更新日期：2017-07-01 00:00:00

abstract：PURPOSE:VLPs displaying tumor targeting single-chain variable fragments (VLP-rscFvs) which targets tumor-associated glycoprotein-72 (TAG-72) marker protein have a potential for immunotherapy against colon carcinoma tumors. In this study, scFvs anchored on VLPs using glycosylphosphatidylinositol (GPI) were prepared to t...

journal_title：Pharmaceutical research

authors： Deo VK,Yui M,Alam J,Yamazaki M,Kato T,Park EY

更新日期：2014-08-01 00:00:00

abstract：PURPOSE:This study was conducted to investigate in vivo the impact of interferon-alpha (IFN)-alpha on P-glycoprotein (P-gp) activity in rats by studying how its administration modifies the bioavailability of digoxin, a fairly pure P-gp substrate. METHODS:Human recombinant IFN-alpha was given to rats (n = 5-7 per group...

journal_title：Pharmaceutical research

authors： Ben Reguiga M,Bonhomme-Faivre L,Orbach-Arbouys S,Farinotti R

更新日期：2005-11-01 00:00:00

abstract：PURPOSE:The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED. METHODS:The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed b...

journal_title：Pharmaceutical research

authors： Zhang A,Sun R,Ran M,Deng Y,Ge Y,Zhu Y,Tao X,Shang L,Gou J,He H,Yin T,Wang Y,Zhang Y,Tang X

更新日期：2020-07-14 00:00:00

abstract：PURPOSE:We have shown that the three human prostate xenograft tumors, i.e. the androgen-dependent CWR22 tumor, and the androgen-resistant CWR22R and CWR91 tumors, are comparable to patient tumors in their expression of prostate specific antigen, multidrug resistance p-glycoprotein, p53 and Bcl-2 and in their sensitivit...

journal_title：Pharmaceutical research

authors： Gan Y,Au JL,Lu J,Wientjes MG

更新日期：1998-11-01 00:00:00

abstract：:An on-line simultaneous assay for the enantiomers of verapamil (VA) and its three metabolites in plasma was developed with column-switching HPLC. This system consists of an ovomucoid protein chiral stationary phase coupled to an achiral reversed-phase column via a dilution tube and a trapping column. The reversed-phas...

journal_title：Pharmaceutical research

authors： Oda Y,Asakawa N,Kajima T,Yoshida Y,Sato T

更新日期：1991-08-01 00:00:00

abstract：PURPOSE:To evaluate organic anion transporter-mediated drug-drug interaction (DDI) potential for individual active components of Danshen (Salvia miltiorrhiza) vs. combinations using in vitro and in silico approaches. METHODS:Inhibition profiles for single Danshen components and combinations were generated in stably-ex...

journal_title：Pharmaceutical research

authors： Wang L,Venitz J,Sweet DH

更新日期：2014-12-01 00:00:00

abstract：PURPOSE:The objective of this study was to determine the pharmacokinetics and safety for NX1838 following injection into the vitreous humor of rhesus monkeys. METHODS:Plasma and vitreous humor pharmacokinetics were determined following a single bilateral 0.25, 0.50, 1.0, 1.5, or 2.0 mg/eye dose. In addition, the pharm...

journal_title：Pharmaceutical research

authors： Drolet DW,Nelson J,Tucker CE,Zack PM,Nixon K,Bolin R,Judkins MB,Farmer JA,Wolf JL,Gill SC,Bendele RA

更新日期：2000-12-01 00:00:00

abstract：PURPOSE:Excipients are added to lyophilized protein drug formulations to protect the protein during processing and storage, but the mechanisms are poorly understood. Here, hydrogen/deuterium (H/D) exchange with mass spectrometry was used to assess protein conformation and excipient interactions in lyophilized solids. ...

journal_title：Pharmaceutical research

authors： Li Y,Williams TD,Topp EM

更新日期：2008-02-01 00:00:00

abstract：PURPOSE:In this study, we developed and evaluated a novel method to produce insulin-loaded hydrophilic microspheres allowing high encapsulation efficiency and the preservation of peptide stability during particle processing. The preparation method used the diffusion of water by an excess of solvent starting from a wate...

journal_title：Pharmaceutical research

authors： Trotta M,Chirio D,Cavalli R,Peira E

更新日期：2004-08-01 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:We recently showed that the perfusion of isolated rat livers with perfusates containing bovine serum albumin (BSA) would significantly stimulate the release of tumor necrosis factor (TNF)-alpha. Here, we hypothesize that BSA-induced increase in the release of TNF-alpha, and possibly other cytokines, would affec...

journal_title：Pharmaceutical research

authors： Vuppugalla R,Shah RB,Chimalakonda AP,Fisher CW,Mehvar R

更新日期：2003-01-01 00:00:00

abstract：:The release of lithium carbonate incorporated into polymethylmethacrylate, polyvinyl chloride, hydrogenated vegetable oil, and carbomer matrix tablets was studied in vitro. The formulation containing 10% carbomer showed a sustained-release profile comparable to that of a standard, commercially available, sustained-rel...

journal_title：Pharmaceutical research

authors： Ciftçi K,Capan Y,Oztürk O,Hincal AA

更新日期：1990-04-01 00:00:00

abstract：PURPOSE:To better understand the nature of drug-excipient interactions we have studied the phase behavior of amorphous binary and ternary mixtures of citric acid, indomethacin and PVP, as model systems. METHODS:We have prepared amorphous mixtures by co-melting or coprecipitation from solvents, and have measured glass ...

journal_title：Pharmaceutical research

authors： Lu Q,Zografi G

更新日期：1998-08-01 00:00:00

abstract：PURPOSE:Polyesters with hydrophilic domains, i.e., poly(D,L-lactic-co-glycolic-co-hydroxymethyl glycolic acid) (PLGHMGA) and a multiblock copolymer of poly(ε-caprolactone)-PEG-poly(ε-caprolactone) and poly(L-lactide) ((PC-PEG-PC)-(PL)) are expected to cause less acylation of encapsulated peptides than fully hydrophobic...

journal_title：Pharmaceutical research

authors： Shirangi M,Hennink WE,Somsen GW,van Nostrum CF

更新日期：2015-09-01 00:00:00

abstract：PURPOSE:To characterize the electrochemical behavior of the photodegradation product of nifedipine, i.e., 2,6-dimethyl-4-(2-nitrosophenyl)-3,5-pyridine-carboxylic acid dimethyl ester (NPD) in different electrolytic media. We also evaluated the interaction between free radicals generated from NPD and xeno/endobiotics. ...

journal_title：Pharmaceutical research

authors： Núñez-Vergara LJ,Bollo S,Fuentealba J,Sturm JC,Squella JA

更新日期：2002-04-01 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：:A number of substituted phthalimide, 1, 8-naphthalimide, succinimide and glutarimide derivatives demonstrated significant hypolipidemic activity at 20 mg/kg/ day, I.P. after 16 days dosing. The N-(n-pentyl) succinimide proved to be the most potent analogue of the new compounds, lowering serum triglyceride levels 51 % ...

journal_title：Pharmaceutical research

authors： Chapman JM Jr,Wyrick SD,Maguire JH,Cocolas GH,Hall IH

更新日期：1984-11-01 00:00:00

abstract：PURPOSE:One of the drawbacks of polycationic and cationic liposomal gene transfer is its sensitivity to serum. Gene therapy requires the transfectant-DNA complex to be resistant to serum as well as blood. Since Ca2+ has proved to be an efficient cofactor of polycationic gene transfer, we decided to investigate its effe...

journal_title：Pharmaceutical research

authors： Haberland A,Knaus T,Zaitsev SV,Buchberger B,Lun A,Haller H,Böttger M

更新日期：2000-02-01 00:00:00