Synthesis of 8-(3-Carboxy-l-methyl-propylammo)-6-methoxyquinoline: A Newly Characterized Primaquine Metabolite.

abstract：PURPOSE:The clinical utility of anthracyclines like idarubicin (IDA) is limited by the occurrence of multidrug resistance and cardiotoxicity. Previous studies have demonstrated that the multidrug transporter P-glycoprotein (P-gp) is present in the heart and have suggested that it exerts a protective function. We sought...

journal_title：Pharmaceutical research

authors： Kang W,Weiss M

更新日期：2001-11-01 00:00:00

abstract：PURPOSE:A key step of delivering extracellular agents to its intracellular target is to escape from endosomal/lysosomal compartments, while minimizing the release of digestive enzymes that may compromise cellular functions. In this study, we examined the intracellular distribution of both fluorecent cargoes and enzymes...

journal_title：Pharmaceutical research

authors： Zhan X,Tran KK,Wang L,Shen H

更新日期：2015-07-01 00:00:00

abstract：:Various carboxylic acid esters of the N-hydroxymethyl derivative of N-benzyloxycarbonylglycine benzylamide, used as a peptide-like model, were prepared and their decomposition kinetics studied in aqueous solution and in human plasma solutions. These N-acyloxymethylamide derivatives were found to undergo a facile decom...

journal_title：Pharmaceutical research

authors： Bundgaard H,Rasmussen GJ

更新日期：1991-10-01 00:00:00

abstract：PURPOSE:Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compou...

journal_title：Pharmaceutical research

authors： Chou SC,Kaur M,Thompson JA,Agarwal R,Agarwal C

更新日期：2010-04-01 00:00:00

abstract：:HPLC analyses of GM-CSF in solution mixtures containing both GM-CSF and HSA showed losses of GM-CSF which could not be accounted for using conventional electrophoretic and/or RP-HPLC techniques. Further investigation of these mixtures by immunoblotting and by immunoaffinity chromatography demonstrated the presence of ...

journal_title：Pharmaceutical research

authors： Kumarasamy R,Bausch J,Kopcha D,Patel S,McGonigle E

更新日期：1994-03-01 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：:The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...

journal_title：Pharmaceutical research

authors： Shao Z,Li Y,Chermak T,Mitra AK

更新日期：1994-08-01 00:00:00

abstract：PURPOSE:To identify the mechanism behind the unexpected bio-performance of two amorphous solid dispersions: BMS-A/PVP-VA and BMS-A/HPMC-AS. METHODS:Solubility of crystalline BMS-A in PVP-VA and HPMC-AS was measured by DSC. Drug-polymer interaction parameters were obtained by Flory-Huggins model fitting. Drug dissoluti...

journal_title：Pharmaceutical research

authors： Qian F,Wang J,Hartley R,Tao J,Haddadin R,Mathias N,Hussain M

更新日期：2012-10-01 00:00:00

abstract：PURPOSE:The aim of the study is to determine the effect of experimental parameters on microinfusion through hollow microneedles into skin to optimize drug delivery protocols and identify rate-limiting barriers to flow. METHODS:Glass microneedles were inserted to a depth of 720-1080 microm into human cadaver skin to mi...

journal_title：Pharmaceutical research

authors： Martanto W,Moore JS,Kashlan O,Kamath R,Wang PM,O'Neal JM,Prausnitz MR

更新日期：2006-01-01 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：:Alpha- and beta-cyclodextrins and their hydroxypropyl derivatives were converted by the reaction with chlorosulfonic acid in pyridine to the corresponding sulfates. Cyclodextrin sulfates were shown by fast-atom bombardment mass spectrometry (negative ion mode, triethanolamine matrix) to be mixtures with nearly symmetr...

journal_title：Pharmaceutical research

authors： Pitha J,Mallis LM,Lamb DJ,Irie T,Uekama K

更新日期：1991-09-01 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：PURPOSE:To measure aggregate and particle formation in tumor necrosis factor-alpha (TNF-α) inhibitors etanercept, adalimumab and certolizumab pegol product samples after exposure to freezing temperature conditions similar to storage conditions previously observed in patients' homes. METHODS:TNF-α inhibitors in their o...

journal_title：Pharmaceutical research

authors： Vlieland ND,Nejadnik MR,Gardarsdottir H,Romeijn S,Sediq AS,Bouvy ML,Egberts ACG,van den Bemt BJF,Jiskoot W

更新日期：2018-02-05 00:00:00

abstract：PURPOSE:The purpose of this study was to evaluate glucose responsiveness in HepG2 human hepatoma cells transduced by a recombinant adeno-associated virus (rAAV) vector containing the insulin gene promoter. and to investigate the effect of protamine sulfate on rAAV-mediated gene delivery. METHODS:Recombinant AAV vector...

journal_title：Pharmaceutical research

authors： Yang YW,Hsieh YC

更新日期：2001-07-01 00:00:00

abstract：PURPOSE:To investigate, for the first time, the performance of a dry powder inhaler (DPI, Aerolizer(®)) in the case of a model drug (i.e. albuterol sulphate) formulated with spray dried mannitol carrier particles with homogeneous shape and solid-state form but different sizes. METHODS:Spray dried mannitol (SDM) partic...

journal_title：Pharmaceutical research

authors： Kaialy W,Hussain T,Alhalaweh A,Nokhodchi A

更新日期：2014-01-01 00:00:00

abstract：:Excessive production of reactive oxygen species by alveolar macrophages (AMs) in response to inhaled toxic substances is a major cause of oxidative lung injury. Therapeutic approaches designed to protect the lungs from oxidative injury by administering native antioxidant enzymes such as catalase and superoxide dismuta...

journal_title：Pharmaceutical research

authors： Harrison J,Shi X,Wang L,Ma JK,Rojanasakul Y

更新日期：1994-08-01 00:00:00

abstract：:The pharmacokinetics of trilostane and one of its metabolites ketotrilostane are described and characterized in the rat following the separate intravenous administration of trilostane and ketotrilostane. It was noted during these studies that the parent compound and its metabolite undergo metabolic interconversion-tri...

journal_title：Pharmaceutical research

authors： McGee JP,Shaw PN

更新日期：1992-04-01 00:00:00

abstract：PURPOSE:Solid dispersions (SDs) represent the most common formulation technique used to increase the dissolution rate of a drug. In this work, the three most common methods used to prepare SDs, namely spray-drying, solvent-casting and freeze-drying, have been compared in order to investigate their effect on increasing ...

journal_title：Pharmaceutical research

authors： De Mohac LM,Caruana R,Cavallaro G,Giammona G,Licciardi M

更新日期：2020-02-19 00:00:00

abstract：PURPOSE:To evaluate the effect of re-directing the uptake mechanism of polyplexes containing oligodeoxynucleotide (ODN) decoys to nuclear factor kappa B (NF-kappaB) from absorptive-mediated to receptor-mediated endocytosis. MATERIALS AND METHODS:Complexes of ODNs and a co-polymer of biotin-polyethylenglycol and polyet...

journal_title：Pharmaceutical research

authors： Bhattacharya R,Osburg B,Fischer D,Bickel U

更新日期：2008-03-01 00:00:00

abstract：PURPOSE:Drug transfer into milk is a general concern during lactation. Because data are limited in human subjects, particularly for new drugs, experimental animal models of lactational drug transfer are critical. This study analyzed drug transfer into milk in a mouse model, as well as the contribution of similar and di...

journal_title：Pharmaceutical research

authors： Ito N,Ito K,Koshimichi H,Hisaka A,Honma M,Igarashi T,Suzuki H

更新日期：2013-09-01 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:In vitro in vivo correlation (IVIVC) is a biopharmaceutical tool recommended for use in formulation development. When validated, IVIVC can be used to set dissolution limits and, based on the dissolution limits, as a surrogate for an in vivo study. The purpose of this paper is to study the various methods used t...

journal_title：Pharmaceutical research

authors： Roudier B,Davit BM,Beyssac E,Cardot JM

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:To investigate the effect of benzofusion on NO donor properties and related biological activities of the furoxan system. The biological properties considered were the ability to increase the cytosolic levels of cGMP in C6 cells and vasodilation. METHODS:NO donor properties were investigated either in the prese...

journal_title：Pharmaceutical research

authors： Medana C,Di Stilo A,Visentin S,Fruttero R,Gasco A,Ghigo D,Bosia A

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:Formulate phospho-sulindac (P-S, OXT-328) in a Pluronic hydrogel to be used as a topical anti-inflammatory agent and study its efficacy, safety and pharmacokinetics in an arthritis model. METHODS:LEW/crlBR rats with Freund's adjuvant-induced arthritis were treated with P-S formulated in Pluronic hydrogel (PSH)...

journal_title：Pharmaceutical research

authors： Mattheolabakis G,Mackenzie GG,Huang L,Ouyang N,Cheng KW,Rigas B

更新日期：2013-06-01 00:00:00

abstract：PURPOSE:To group microcrystalline celluloses (MCCs) using a combination of artificial neural network (ANN) and data clustering. METHODS:Radial basis function (RBF) network was used to model the torque measurements of the various MCCs. Output from the RBF network was used to group the MCCs using a data clustering techn...

journal_title：Pharmaceutical research

authors： Soh JL,Chen F,Liew CV,Shi D,Heng PW

更新日期：2004-12-01 00:00:00

abstract：PURPOSE:To investigate the possible pathways for transport of wheat germ agglutinin conjugated PEG-PLA nanoparticles (WGA-NP) into the brain after nasal administration. METHODS:The nose-to-brain pathways were investigated using WGA-NP containing 6-coumarin (as a fluorescent marker) and (125)I-labeled WGA-NP. Ex vivo i...

journal_title：Pharmaceutical research

authors： Liu Q,Shen Y,Chen J,Gao X,Feng C,Wang L,Zhang Q,Jiang X

更新日期：2012-02-01 00:00:00

abstract：PURPOSE:To determine by pharmacokinetic (PK) means the role of erythropoietin-receptor (EPO-R) upregulation in fetuses on the elimination of erythropoietin (EPO). MATERIALS AND METHODS:Six fetal sheep were catheterized at a gestational age of 125-127 days and phlebotomized daily for 6 days. Paired tracer PK studies us...

journal_title：Pharmaceutical research

authors： Freise KJ,Widness JA,Segar JL,Schmidt RL,Veng-Pedersen P

更新日期：2007-09-01 00:00:00

abstract：:A rapid quantitative, enantioselective HPLC method for the analysis of the four stereoisomers, (+) and (-) erythro and (+) and (-) threo forms, of mefloquine has been developed using a Chiralpak Ad analytical column containing amylose tris-3,5-dimethylphenyl carbonate coated on silica gel and hexane/ethanol/diethylami...

journal_title：Pharmaceutical research

authors： Qiu Y,Kitamura S,Guillory JK

更新日期：1992-12-01 00:00:00

abstract：PURPOSE:The Caco-2 association of lectin-grafted PLGA-nanospheres was investigated compared to plain and BSA-coated spheres. METHODS:Nanospheres made from fluorescent-labeled PLGA were coated with wheat germ agglutinin (WGA) or BSA and incubated with Caco-2 monolayers varying the concentration of nanospheres, the time...

journal_title：Pharmaceutical research

authors： Weissenboeck A,Bogner E,Wirth M,Gabor F

更新日期：2004-10-01 00:00:00

abstract：:Transdermal drug delivery of ionized drugs can be enhanced by iontophoresis. Drug in the ionic form, contained in some reservoir, can be "phoresed" through the skin with a small current across two electrodes, one above the reservoir and one at a distal skin location. Positive ions can be introduced from the positive p...

journal_title：Pharmaceutical research

authors： Tyle P

更新日期：1986-12-01 00:00:00