Evaluation of New Chemical Entities as Substrates of Liver Transporters in the Pharmaceutical Industry: Response to Regulatory Requirements and Future Steps.

abstract：:Recently developed techniques were applied in a preformulation program to select a compound and a suitable salt for use in a one-month toxicological test. The program showed that valuable information can be obtained prior to the choice of a compound as a candidate for a solid-dosage form. Information about the physica...

journal_title：Journal of pharmaceutical sciences

authors： Graffner C,Johansson ME,Nicklasson M,Nyqvist H

更新日期：1985-01-01 00:00:00

abstract：:Fibril formation (aggregation) of human and bovine insulin and six human insulin mutants in hydrochloric acid were investigated by visual inspection, Thioflavin T fluorescence spectroscopy, transmission electron microscopy (TEM), and Fourier transform infrared (FTIR) spectroscopy. The fibrillation tendencies of the wi...

journal_title：Journal of pharmaceutical sciences

authors： Garriques LN,Frokjaer S,Carpenter JF,Brange J

更新日期：2002-12-01 00:00:00

abstract：:The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However...

journal_title：Journal of pharmaceutical sciences

authors： Welling PG,Elliott RL,Pitterle ME,Corrick-West HP,Lyons LL

更新日期：1979-02-01 00:00:00

abstract：:Drug stability studies are expensive and time consuming. Multiple batches are studied to ensure that a product will consistently remain within specifications for its entire expiration dating period. Some of these studies involve the same drug products in similar packages or in multiple strengths. Application of sound ...

journal_title：Journal of pharmaceutical sciences

authors： Fairweather WR,Lin TY,Kelly R

更新日期：1995-11-01 00:00:00

abstract：:The chemical shifts of the methyl groups of 2,4-dimethylbenzo[g]quinoline are defined with respect to concentration, showing that the methyl resonances are reversed from their expected positions in concentrations normally used in NMR spectroscopy. The phenomenon is explained in terms of the probably "fixation" of bond...

journal_title：Journal of pharmaceutical sciences

authors： Born JL,Harsin CE

更新日期：1977-08-01 00:00:00

abstract：:The purpose of this study was to examine the role of multidrug resistance-associated protein-1 and -2 (Mrp1 and Mrp2) in the efflux transport of organic anions across the blood-cerebrospinal fluid (CSF) barrier. The CSF concentration of estradiol-17beta-glucuronide (E(2)17betaG) and 2,4-dinitrophenyl-S-glutathione (DN...

journal_title：Journal of pharmaceutical sciences

authors： Lee YJ,Kusuhara H,Sugiyama Y

更新日期：2004-01-01 00:00:00

abstract：:Site I of human serum albumin is an important and complex region for high-affinity binding of drugs. Equilibrium dialysis showed independent binding of dansyl-L-asparagine (DNSA) and n-alkyl p-aminobenzoates (p-ABEs) to regions Ib and Ic, respectively, in the pH range 6.0-9.0. However, individual binding of DNSA incre...

journal_title：Journal of pharmaceutical sciences

authors： Yamasaki K,Maruyama T,Takadate A,Suenaga A,Kragh-Hansen U,Otagiri M

更新日期：2004-12-01 00:00:00

abstract：:15-Lipoxygenase (15-LOX) is one of the key enzymes responsible for the formation of oxidized low-density lipoprotein, a major causal factor for atherosclerosis. Δ(9)-Tetrahydrocannabinol (Δ(9)-THC), a major component of marijuana, has suggested to suppress atherosclerosis. Although Δ(9)-THC seems to be attractive for ...

journal_title：Journal of pharmaceutical sciences

authors： Takeda S,Jiang R,Aramaki H,Imoto M,Toda A,Eyanagi R,Amamoto T,Yamamoto I,Watanabe K

更新日期：2011-03-01 00:00:00

abstract：:The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...

journal_title：Journal of pharmaceutical sciences

authors： Nagy ZK,Balogh A,Drávavölgyi G,Ferguson J,Pataki H,Vajna B,Marosi G

更新日期：2013-02-01 00:00:00

abstract：:The correlation between dynamic surface properties of drug molecules and drug absorption in two common in vitro models of the intestinal wall (Caco-2 monolayers and rat intestinal segments) has been investigated. A homologous series of beta-adrenoreceptor antagonists were used as model compounds. Dynamic molecular sur...

journal_title：Journal of pharmaceutical sciences

authors： Palm K,Luthman K,Ungell AL,Strandlund G,Artursson P

更新日期：1996-01-01 00:00:00

abstract：:The growing interest of pharmaceutical companies toward the crystal morphology prediction of active pharmaceutical ingredients is a consequence of the dramatic effect of the crystal habit on the tableting behavior of drugs. In order to help the optimization of the industrial process, molecular mechanics calculations t...

journal_title：Journal of pharmaceutical sciences

authors： Li Destri G,Marrazzo A,Rescifina A,Punzo F

更新日期：2013-01-01 00:00:00

abstract：:A set of nonionic cellulose ethers with varying hydrophobicity and molecular weight has been investigated by principal component analysis (PCA). Several experimental variables such as dynamic surface tension, diffusion coefficient, microviscosity as monitored by a fluorescence probe technique, and intrinsic viscosity ...

journal_title：Journal of pharmaceutical sciences

authors： Persson B,Evertsson H,Bergman R,Sundelöf LO

更新日期：1999-08-01 00:00:00

abstract：:The hydrolytic degradation of pirbuterol was investigated under saturated oxygen conditions over a wide range of pH values and at different temperatures. Two of the five observed breakdown products were positively identified. The first-order decomposition rate appeared to depend on the rate constants of the four disso...

journal_title：Journal of pharmaceutical sciences

authors： Bansal PC,Monkhouse DC

更新日期：1977-06-01 00:00:00

abstract：:During the drying process of a wet granulate, water-soluble compounds can migrate to the outer layers of the granule with the evaporating solvent. This migration can affect structural and mechanical characteristics of the granules as the solute accumulates on the granule's outer crust. The objective of this study was ...

journal_title：Journal of pharmaceutical sciences

authors： Poutiainen S,Honkanen M,Becker J,Nachtweide D,Järvinen K,Ketolainen J

更新日期：2012-04-01 00:00:00

abstract：:The physicochemical properties of A-75998, a synthetic antagonist of luteinizing hormone releasing hormone with potential for treatment of hormone-sensitive cancers and endometriosis, are described. An accelerated solution stability study indicated that the compound is relatively stable and showed a U-shaped pH-rate p...

journal_title：Journal of pharmaceutical sciences

authors： Cannon JB,Krill SL,Porter WR

更新日期：1995-08-01 00:00:00

abstract：:The objective of this study is to understand the underlying mechanisms responsible for the superior stability of indomethacin (INM)-Eudragit® E PO (E PO) system by exploring the miscibility and intermolecular interactions through the combination of thermal, rheological, and spectroscopic analysis. The zero shear-rate ...

journal_title：Journal of pharmaceutical sciences

authors： Liu H,Zhang X,Suwardie H,Wang P,Gogos CG

更新日期：2012-06-01 00:00:00

abstract：:The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...

journal_title：Journal of pharmaceutical sciences

authors： Nagata O,Terasaki T,Yada E,Sato H,Tamai I,Tsuji A

更新日期：1989-01-01 00:00:00

abstract：:The intracellular delivery of small interfering RNA (siRNA) is a therapeutic strategy to transiently block gene expression. Two silencing RNA strategies utilize either synthetic double stranded RNA or plasmid DNA encoding a short hairpin RNA (shRNA). In the present study, we have quantitatively compared the potency of...

journal_title：Journal of pharmaceutical sciences

authors： McAnuff MA,Rettig GR,Rice KG

更新日期：2007-11-01 00:00:00

abstract：:Aliphatic polyesters have great utility as temporary prosthetics and surgical aids, and in drug delivery systems. Knowledge of the mechanism and pathways of hydrolysis can form a basis for the design and selection of a controlled-release system. Because of the importance of hydrolysis to the properties of such a syste...

journal_title：Journal of pharmaceutical sciences

authors： Maniar ML,Kalonia DS,Simonelli AP

更新日期：1991-08-01 00:00:00

abstract：:A highly sensitive and specific electron-capture GLC assay capable of detecting picogram quantities of metoclopramide, a procaine derivative, in biological fluids was developed. This assay consisted of extracting metoclopramide from an alkalinized aqueous layer into benzene. A portion of the organic phase was derivati...

journal_title：Journal of pharmaceutical sciences

authors： Tam YK,Axelson JE

更新日期：1978-08-01 00:00:00

abstract：:The adsorption of quinidine onto kaolin was studied as a function of pH in aqueous solutions in which the ionic strength was adjusted to 0.1. The interaction of quinidine with pectin also was investigated in water and in phosphate buffer; the buffer pH and ionic strength were adjusted to 6.5 and 0.1, respectively. The...

journal_title：Journal of pharmaceutical sciences

authors： Bucci AJ,Myre SA,Tan HS,Shenouda LS

更新日期：1981-09-01 00:00:00

abstract：:The aim of this review is to describe the theoretical background lying behind the solid drug mechanochemical activation by cogrinding pointing out its advantages and drawbacks. A brief historical introduction precedes the discussion about the mechanisms leading to solid drug activation. This allows to clarify the conc...

journal_title：Journal of pharmaceutical sciences

authors： Colombo I,Grassi G,Grassi M

更新日期：2009-11-01 00:00:00

abstract：:A combination of coformer screening and modeling, followed by characterization using calorimetry, structure elucidation, and solubility led to the identification of novel crystalline forms of the hepatitis C protease inhibitor, telaprevir. The lead crystalline form, a cocrystalline solid of telaprevir with 4-aminosaly...

journal_title：Journal of pharmaceutical sciences

authors： Stavropoulos K,Johnston SC,Zhang Y,Rao BG,Hurrey M,Hurter P,Topp EM,Kadiyala I

更新日期：2015-10-01 00:00:00

abstract：:A rapid, sensitive, and specific determination of ketoprofen in human and animal deproteinized body fluids by reversed-phase high-pressure liquid chromatography is presented. The acid is detectable in amounts as low as 0.1 microgram/ml. Limits of error are in the range of +/- 5.1% of the sample mean. ...

journal_title：Journal of pharmaceutical sciences

authors： Ballerini R,Cambi A,Del Soldato P,Melani F,Meli A

更新日期：1979-03-01 00:00:00

abstract：:A rapid approach for estimating the pK(a) value of small organic molecules was developed using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection. The VAMCE method employed a 96-capillary array, arranged in a standard 8 x 12 microtiter plate configuration, with each row of capilla...

journal_title：Journal of pharmaceutical sciences

authors： Zhou C,Jin Y,Kenseth JR,Stella M,Wehmeyer KR,Heineman WR

更新日期：2005-03-01 00:00:00

abstract：:Systematic structural modifications were performed on the natural sesquiterpene lactone tenulin to define those groupings essential to, or significant in, its in vivo antitumor activity. Accordingly, the following tenulin analogs were prepared: dihydrotenulin, 2,3-epoxytenulin, isotenulin, dihydroisotenulin, 2,3-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Waddell TG,Austin AM,Cochran JW,Gerhart KG,Hall IH,Lee KH

更新日期：1979-06-01 00:00:00

abstract：:The release kinetics of a polymeric-controlled release device are determined by its geometry and dimensions. A method to calculate the required size and shape of diffusion-controlled dosage forms to achieve a particular release profile is presented. The diffusion parameters are determined for various drugs (theophylli...

journal_title：Journal of pharmaceutical sciences

authors： Siepmann J,Ainaoui A,Vergnaud JM,Bodmeier R

更新日期：1998-07-01 00:00:00

abstract：:A crossover experiment was utilized to compare the pharmacokinetics of a 1-g dose of cephalexin tablets, cephalexin capsules, or cephradine capsules in nine normal human volunteers. These antibiotics were administered as three formulations: two 500-mg capsulin every 6 hr for five doses, and one 1000-mg tablet of cepha...

journal_title：Journal of pharmaceutical sciences

authors： Finkelstein E,Quintiliani R,Lee R,Bracci A,Nightingale CH

更新日期：1978-10-01 00:00:00

abstract：:Cationic antimicrobial peptides are good candidates for new diagnostics and antimicrobial agents. They can rapidly kill a broad range of microbes and have additional activities that have impact on the quality and effectiveness of innate responses and inflammation. Furthermore, the challenge of bacterial resistance to ...

journal_title：Journal of pharmaceutical sciences

authors： Brouwer CP,Wulferink M,Welling MM

更新日期：2008-05-01 00:00:00

abstract：:Tablet characteristics of tensile strength and disintegration time were predicted using residual stress distribution, simulated by the finite element method (FEM). The Drucker-Prager Cap (DPC) model was selected as the method for modeling the mechanical behavior of pharmaceutical powders composed of lactose (LAC), cor...

journal_title：Journal of pharmaceutical sciences

authors： Hayashi Y,Miura T,Shimada T,Onuki Y,Obata Y,Takayama K

更新日期：2013-10-01 00:00:00