Study of drug-protein binding by affinity chromatography: interaction of bovine serum albumin and salicylic acid.

abstract：:Polysorbate 80, a surfactant often assumed to be inert, was found to bind a number of biochemically important ions (K+, Na+, NH4+, Ca2+) and transport them through a model membrane (CH2Cl2). The rates and fluxes of potassium ions were found to depend on the initial concentration of potassium ion, the polysorbate 80 co...

journal_title：Journal of pharmaceutical sciences

authors： Thoman CJ

更新日期：1986-10-01 00:00:00

abstract：:Surface adsorption of two monoclonal antibodies (mAb1 and mAb2), with widely different hydrophobicity and self-association behavior in solution, was examined by quartz crystal microbalance with dissipation monitoring to understand how adsorption and protein self-interactions near the surface are impacted by their intr...

journal_title：Journal of pharmaceutical sciences

authors： Oom A,Poggi M,Wikström J,Sukumar M

更新日期：2012-02-01 00:00:00

abstract：:The rising popularity of microwaves for drying, material processing and quality sensing has fuelled the need for knowledge concerning dielectric properties of common pharmaceutical materials. This article represents one of the few reports on the density and moisture content dependence of the dielectric properties of p...

journal_title：Journal of pharmaceutical sciences

authors： Heng PW,Loh ZH,Liew CV,Lee CC

更新日期：2010-02-01 00:00:00

abstract：:The stereochemistries of geometric isomers of 4-(2-bromo-1,2-diphenylvinyl)phenol, 4-(2-bromo-1,2-diphenylvinyl)anisole, and 2-[p-(2-bromo-1,2-diphenylvinyl)phenoxy]triethylamine were determined by conversion of the phenolic analog to the ethers and subsequent comparison of physical properties with those of 2-[p-(2-ch...

journal_title：Journal of pharmaceutical sciences

authors： Richardson A Jr,Benson HD,Hite G

更新日期：1976-10-01 00:00:00

abstract：:There is a growing clinical interest in developing and commercializing pharmaceutical-grade cannabinoid products, containing primarily tetrahydrocannabinol (THC) and cannabidiol (CBD). The oral bioavailability of THC and CBD is very low due to extensive "first-pass" metabolism. A novel oral THC and CBD formulation, PT...

journal_title：Journal of pharmaceutical sciences

authors： Atsmon J,Cherniakov I,Izgelov D,Hoffman A,Domb AJ,Deutsch L,Deutsch F,Heffetz D,Sacks H

更新日期：2018-05-01 00:00:00

abstract：:A stability-indicating high-performance liquid chromatographic assay has been used to investigate the stability of solutions of melphalan under conditions that pertain to setting up in vitro chemosensitivity assays. Melphalan (1 and 20 micrograms/mL) was found to be 30% more stable in 150 mM NaCl solution (normal sali...

journal_title：Journal of pharmaceutical sciences

authors： Bosanquet AG

更新日期：1985-03-01 00:00:00

abstract：:Modified cyclodextrins (CDs) have shown great promise as non-viral gene and siRNA delivery vectors in a range of in vitro and in vivo studies. In the current study, structural and biophysical characterisation of selected CDs was carried out to enhance our understanding of their interaction with nucleic acids. The meth...

journal_title：Journal of pharmaceutical sciences

authors： O'Mahony AM,Cronin MF,McMahon A,Evans JC,Daly K,Darcy R,O'Driscoll CM

更新日期：2014-05-01 00:00:00

abstract：:This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

journal_title：Journal of pharmaceutical sciences

authors： Xu H,Wang W,Shi Y,Gao P

更新日期：2019-01-01 00:00:00

abstract：:Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...

journal_title：Journal of pharmaceutical sciences

authors： Sanvordeker DR,Chien YW,Lin TK,Lambert HJ

更新日期：1975-11-01 00:00:00

abstract：:Pelrinone HCl is essentially nonhygroscopic. The pH-solubility profile exhibits a U-shaped curve, while the octanol-water partition coefficient-pH profile shows a bell-shaped curve. Two ionizable functions, with a pKa1 value of 4.71 and a pKa2 value of 8.94, produce the cationic and anionic forms, respectively. A weak...

journal_title：Journal of pharmaceutical sciences

authors： Hajdu J,Adams G,Lee HK

更新日期：1988-11-01 00:00:00

abstract：:Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. Surveys have revealed that a sufficient lack of therapeutically efficient CBZ transbuccal formulation exists. Therefore, this investigation was directed toward designing multiparticulate composite construct (MCC) for the transbuccal delivery of C...

journal_title：Journal of pharmaceutical sciences

authors： Adeleke OA,Choonara YE,Du Toit LC,Pillay V

更新日期：2014-04-01 00:00:00

abstract：:Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...

journal_title：Journal of pharmaceutical sciences

authors： Kim D,Hong S,Jung S,Jung Y,Kim YM

更新日期：2009-11-01 00:00:00

abstract：:Interaction between nonsteroidal anti-inflammatory drugs (NSAIDs) and other drugs occurs relatively frequently because of the wide use of NSAIDs. Such interactions with drugs of narrow therapeutic index used in serious disease states may lead to toxicity. Gentamicin toxicity is based on its concentration in serum, and...

journal_title：Journal of pharmaceutical sciences

authors： Shivprakash,Gandhi TP,Patel RB,Sheikh MA,Jhala A,Santani DD

更新日期：1994-04-01 00:00:00

abstract：:Protein aggregates are a potential risk factor for immunogenicity. The measurement, characterization, and control of protein aggregates in drug products are indispensable for the development of biopharmaceuticals, including therapeutic mAbs. In this study, Fcγ receptor (FcγR)-expressing reporter cell lines were used t...

journal_title：Journal of pharmaceutical sciences

authors： Tada M,Aoyama M,Ishii-Watabe A

更新日期：2020-01-01 00:00:00

abstract：:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

journal_title：Journal of pharmaceutical sciences

authors： van de Waterbeemd H,van Bakel P,Jansen A

更新日期：1981-09-01 00:00:00

abstract：:4,5-Dimethoxykynuramine was synthesized in a three-step sequence originating with veratrole. Indirect evidence indicates that the drug was converted in vivo to the hypotensive agent 6,7-dimethoxy-4-quinolinol by the action of monoamine oxidase. ...

journal_title：Journal of pharmaceutical sciences

authors： Schwan TJ,Honkomp LJ,Snyder HR Jr,Watson EJ

更新日期：1978-03-01 00:00:00

abstract：:Cyclosporin A (CyA) is a good candidate for incorporation in colloidal carriers such as nanoparticles (NP) that would diminish the adverse effects associated with its use under conventional pharmaceutical dosage forms and improve bioavailability after oral administration. In this study a composite rotational experimen...

journal_title：Journal of pharmaceutical sciences

authors： Molpeceres J,Guzman M,Aberturas MR,Chacon M,Berges L

更新日期：1996-02-01 00:00:00

abstract：:Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Hoffman L,Bongers J,Tao L,Huang Y,Slaney T,Das TK,Leone A,Kar SR

更新日期：2019-06-01 00:00:00

abstract：:From a consideration of the basic processes involved in drug elimination, the fraction of drug cleared by the gut and by the liver were described as functions of availability and hepatic clearance. For a drug given orally, a plot of the fraction of drug cleared by the gut or liver against alpha, a proportionality cons...

journal_title：Journal of pharmaceutical sciences

authors： Minchin RF,Ilett KF

更新日期：1982-04-01 00:00:00

abstract：:2,2'-Anhydro-1-beta-D-arabinofuranosylcytosine (I) is a more potent and less toxic antineoplastic agent than is cytarabine (1-beta-D-arabinofuranosylcytosine) (II). The anhydronucleoside (I) was found to be readily transformed by hydrogen peroxide into 2,2'-anhydro-5-hydroxy-1-beta-D-arabinofuranosylcytosine (III) by ...

journal_title：Journal of pharmaceutical sciences

authors： Kikugawa K

更新日期：1975-03-01 00:00:00

abstract：:N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...

journal_title：Journal of pharmaceutical sciences

authors： Zera RT,Nagasawa HT

更新日期：1980-09-01 00:00:00

abstract：:It is shown that a suitable dosage interval, tau, can be estimated by a factor times the sum of the mean residence time (MRT) of the central compartment (MRTC) and the MRT of the absorption site (MRTA). This value of tau will provide a ratio, maximum steady-state plasma concentration: minimum steady-state plasma conce...

journal_title：Journal of pharmaceutical sciences

authors： Wagner JG

更新日期：1987-01-01 00:00:00

abstract：:The metabolic fate of aprophen hydrochloride (2-diethylaminoethyl 2,2-diphenylpropionate) was studied in rats after intravenous administration. Both 14C-labeled and unlabeled aprophen were used in these studies. Blood samples were collected and analyzed to determine the identities of the metabolites formed. Utilizing ...

journal_title：Journal of pharmaceutical sciences

authors： Brown ND,Smejkal RM,Breuer E,Doctor BP,Chiang PK

更新日期：1988-02-01 00:00:00

abstract：:Baclofen, a widely used antispastic agent, has been found to exist in two crystalline forms, the anhydrate and monohydrate. The aim of this study was (1) to identify and characterize these two solid phases of baclofen, and (2) to examine the processing-induced phase transformations associated with wet granulation of b...

journal_title：Journal of pharmaceutical sciences

authors： Mirza S,Miroshnyk I,Rantanen J,Aaltonen J,Harjula P,Kiljunen E,Heinämäki J,Yliruusi J

更新日期：2007-09-01 00:00:00

abstract：:Many pathophysiological circumstances vary during 24 h periods. Many physiologic processes undergo biological rhythms, including the sleep-wake rhythm and metabolism. Disruptive effect in the 24 h variations can manifest as the emergence or exacerbation of pathological conditions. So, chronotherapeutics is gaining inc...

journal_title：Journal of pharmaceutical sciences

authors： Ohdo S,Koyanagi S,Matsunaga N,Hamdan A

更新日期：2011-09-01 00:00:00

abstract：:Upon exposure to shaking stress, an IgG1 mAb formulation in both the liquid and lyophilized state formed subvisible particles. Because freeze-drying was expected to minimize protein physical instability under these conditions, the extent and nature of aggregate formation in the lyophilized preparation were examined us...

journal_title：Journal of pharmaceutical sciences

authors： Telikepalli S,Kumru OS,Kim JH,Joshi SB,O'Berry KB,Blake-Haskins AW,Perkins MD,Middaugh CR,Volkin DB

更新日期：2015-02-01 00:00:00

abstract：:p-Bromospiperone was prepared from the reaction of spiperone with bromine. It was tested for dopamine receptor binding affinity in vitro and its ability to stimulate prolactin secretion in vivo. The results indicate no significant change of biological activities due to the bromination of spiperone. ...

journal_title：Journal of pharmaceutical sciences

authors： Huang CC,Friedman AM,So R,Simonovic M,Meltzer HY

更新日期：1980-08-01 00:00:00

abstract：:The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2004-01-01 00:00:00

abstract：:A quantitative high-pressure liquid chromatographic method, using a reversed-phase column coupled to a fluorescence detector, was developed to determine salicylic acid in bulk aspirin and plain and buffered aspirin tablets. The aspirin was dissolved, filtered, and injected into the chromatograph; the fluorescence of t...

journal_title：Journal of pharmaceutical sciences

authors： Kirchhoefer RD,Juhl WE

更新日期：1980-05-01 00:00:00

abstract：:The clearance (Cl) and volume of distribution (V(ss)) of a lipophilic, lymphatically transported drug, halofantrine (Hf) have been evaluated after intravenous delivery to the systemic circulation in ex vivo lymph and plasma, and compared with the data obtained after administration of a lipid-based emulsion and a lipid...

journal_title：Journal of pharmaceutical sciences

authors： Caliph SM,Trevaskis NL,Charman WN,Porter CJ

更新日期：2012-09-01 00:00:00