Investigation of the gastrointestinal transit and in vivo drug release of isosorbide-5-nitrate pellets.

abstract：:A method is described for the assay of phenobarbital N-glucosylation using UDP-D-[6-3H]glucose. The radioactive phenobarbital N-glucoside conjugates [(5R)-PBG, (5S)-PBG] formed during the incubations were resolved from each other and from uncharacterized radioactive products by semipreparative HPLC. The product ratio ...

journal_title：Pharmaceutical research

authors： Soine WH,Safi H,Westkaemper RB

更新日期：1992-05-01 00:00:00

abstract：PURPOSE:Recently identified organic solute transporter (Ost) alpha and beta are located on the basolateral membrane of enterocytes and may be responsible for the intestinal absorption of many substrates including bile acids. In the present study, the mechanism governing the transcriptional regulation of their expressio...

journal_title：Pharmaceutical research

authors： Okuwaki M,Takada T,Iwayanagi Y,Koh S,Kariya Y,Fujii H,Suzuki H

更新日期：2007-02-01 00:00:00

abstract：PURPOSE:To identify the aggregation mechanism and the stability characteristics of three different monoclonal antibodies under acidic conditions. METHODS:The aggregation kinetics is analyzed by a combination of light scattering, size exclusion chromatography and fluorescence techniques and the aggregation data are cor...

journal_title：Pharmaceutical research

authors： Arosio P,Rima S,Morbidelli M

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:Adenoviruses are being developed for diseases of the gastrointestinal tract. Several in vitro assays were used to predict stability of PEGylated adenovirus along the GI tract and determine in vivo gene transfer after oral administration. METHODS:Recombinant adenovirus was modified with monomethoxypoly(ethylene...

journal_title：Pharmaceutical research

authors： Cheng X,Ming X,Croyle MA

更新日期：2003-09-01 00:00:00

abstract：PURPOSE:Hydroxylation of the antidepressant and smoking deterrent drug bupropion is a clinically important bioactivation and elimination pathway. Bupropion hydroxylation is catalyzed selectively by cytochrome P4502B6 (CYP2B6). CYP2B6-catalyzed bupropion hydroxylation has been used as an in vitro and in vivo phenotypic ...

journal_title：Pharmaceutical research

authors： Coles R,Kharasch ED

更新日期：2008-06-01 00:00:00

abstract：:This study utilized different statistical techniques to evaluate the reliability (internal consistency) and the discriminant validity of the most widely used measures of organizational commitment and intention to quit (the employing organization). Data were obtained from a national mail survey of members of the Americ...

journal_title：Pharmaceutical research

authors： Kong SX,Wertheimer AI,Serradell J,McGhan WF

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:To investigate the effects of small aliphatic pendent groups conjugated through an acid-sensitive linker to the core of brushed block copolymer micelles on particle properties. METHODS:The brushed block copolymers were synthesized by conjugating five types of 2-alkanone (2-butanone, 2-hexanone, 2-octanone, 2-d...

journal_title：Pharmaceutical research

authors： Lee HJ,Bae Y

更新日期：2013-08-01 00:00:00

abstract：:A novel application of attenuated total reflectance IR spectroscopy (ATR-IR) was used to monitor the outer several microns of the stratum corneum (SC) and, thereby, demonstrate enhanced percutaneous absorption in vivo in man. 4-Cyanophenol (CP) as a model permeant yielded a unique IR signal, distinct from those of the...

journal_title：Pharmaceutical research

authors： Mak VH,Potts RO,Guy RH

更新日期：1990-08-01 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：:This review describes the design and current development of leukotriene biosynthesis inhibitors as potential antiinflammatory agents. Knowledge of the enzymatic mechanism of 5-lipoxygenase led to specific inhibitors of this enzyme which catalyzes a key step in the leukotriene pathway. Competitive inhibitors include ir...

journal_title：Pharmaceutical research

authors： Cashman JR

更新日期：1985-11-01 00:00:00

abstract：PURPOSE:A novel bioequivalence limit is proposed taking into account the therapeutic window. METHODS:The therapeutic range is introduced as the ratios maximum tolerated dose/therapeutic dose (MTD/D) and the therapeutic dose/lowest effective dose. The performance of the new acceptance range was compared with the method...

journal_title：Pharmaceutical research

authors： Jacobs T,De Ridder F,Rusch S,Van Peer A,Molenberghs G,Bijnens L

更新日期：2008-11-01 00:00:00

abstract：PURPOSE:To provide the physicochemical properties of vitrified trehalose for predicting its recrystallization. METHODS:Thin films of vitrified trehalose solutions were prepared at room temperature and exposed to various humid and temperature atmospheres. The in-situ amount of retained water in the vacuum-dried trehalo...

journal_title：Pharmaceutical research

authors： Shirakashi R,Takano K

更新日期：2018-05-10 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 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：: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:This study uses high drug content solid dispersions for dose window extension beyond current demonstrations using fused deposition modelling (FDM) to; i) accommodate pharmaceutically relevant doses of drugs of varying potencies at acceptable dosage form sizes and ii) enable enhanced dose flexibility via modular...

journal_title：Pharmaceutical research

authors： Govender R,Abrahmsén-Alami S,Folestad S,Larsson A

更新日期：2019-12-17 00:00:00

abstract：PURPOSE:To evaluate the effects of several buffers and excipients on the stability of glucagon during freeze-drying and storage as dried powder formulations. METHODS:The chemical and physical stability of glucagon in freeze-dried solid formulations was evaluated by a variety of techniques including mass spectrometry (...

journal_title：Pharmaceutical research

authors： Fang WJ,Qi W,Kinzell J,Prestrelski S,Carpenter JF

更新日期：2012-12-01 00:00:00

abstract：PURPOSE:To determine whether a Protected Graft Copolymer (PGC) containing fatty acid can be used as a stabilizing excipient for GLP-1 and whether PGC/GLP-1 given once a week can be an effective treatment for diabetes. METHODS:To create a PGC excipient, polylysine was grafted with methoxypolyethyleneglycol and fatty ac...

journal_title：Pharmaceutical research

authors： Castillo GM,Reichstetter S,Bolotin EM

更新日期：2012-01-01 00:00:00

abstract：:The pharmacokinetics of 2',3'-dideoxyinosine (ddI) were examined in rats given intravenous doses of 8, 40, or 200 mg/kg. The concentrations of ddI in whole blood and plasma were identical. The concentration decline was multiexponential, with mean half-lives of 2 and 20 min for the first and second phases, respectively...

journal_title：Pharmaceutical research

authors： Wientjes MG,Mukherji E,Au JL

更新日期：1992-08-01 00:00:00

abstract：PURPOSE:Covalent binding between N-acetyl-L-cysteine (NAC) and albumin was evaluated kinetically by conducting in vitro experiments. METHOD:After 14C-NAC was incubated with human or rat serum, the solution was analyzed by anion-exchange HPLC. The albumin-bound 14C-NAC was quantified by measuring the radioactivity in t...

journal_title：Pharmaceutical research

authors： Harada D,Naito S,Otagiri M

更新日期：2002-11-01 00:00:00

abstract：PURPOSE:S-(4-Nitrobenzyl)-6-thioinosine (NBMPR) is routinely used at concentrations of 0.10 μM and 0.10 mM to specifically inhibit transport of nucleosides mediated by equilibrative nucleoside transporters 1 (ENT1) and 2 (ENT2), respectively. We recently showed that NBMPR (0.10 mM) might also inhibit placental active e...

journal_title：Pharmaceutical research

authors： Karbanova S,Sorf A,Jiraskova L,Lalinska A,Ptackova Z,Staud F,Cerveny L

更新日期：2020-02-21 00:00:00

abstract：:A physical-chemical analysis of the extent of sorption of water by tablets containing superdisintegrants was carried out following the aqueous film coating of formulated tablets. Characterization of the uncoated and coated tablet properties was conducted using thermogravimetric analysis, differential scanning calorime...

journal_title：Pharmaceutical research

authors： Pourkavoos N,Peck GE

更新日期：1993-08-01 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：PURPOSE:Fractal kinetics was used for the analysis of the carrier-mediated transport for drugs across the intestinal epithelial cells. METHODS:The transport was examined under various agitation rates using a monolayer of Caco-2 cells and rabbit ileum sheets. RESULTS:The passive transport of antipyrine across Caco-2 c...

journal_title：Pharmaceutical research

authors： Ogihara T,Tamai I,Tsuji A

更新日期：1998-04-01 00:00:00

abstract：PURPOSE:To develop an isolated perfused rat liver (IPRL) model with low baseline levels of tumor necrosis factor (TNF)-alpha in the outlet perfusate to study the effects of immunostimulants and immunosuppressants on the release of TNF-alpha from this organ. METHODS:Isolated rat livers were perfused with a buffer conta...

journal_title：Pharmaceutical research

authors： Mehvar R,Zhang X

更新日期：2002-01-01 00:00:00

abstract：:Published permeability coefficient (Kp) data for the transport of a large group of compounds through mammalian epidermis were analyzed by a simple model based upon permeant size [molecular volume (MV) or molecular weight (MW)] and octanol/water partition coefficient (Koct). The analysis presented is a facile means to ...

journal_title：Pharmaceutical research

authors： Potts RO,Guy RH

更新日期：1992-05-01 00:00:00

abstract：PURPOSE:The purpose of this work was to study the influence of cell differentiation on the mRNA expression of transporters and channels in Caco-2 cells and to assess Caco-2 cells as a model for carrier-mediated drug transport in the intestines. METHOD:Gene mRNA expression was measured using a custom-designed microarra...

journal_title：Pharmaceutical research

authors： Anderle P,Rakhmanova V,Woodford K,Zerangue N,Sadée W

更新日期：2003-01-01 00:00:00

abstract：:The hair follicle, hair shaft, and sebaceous gland collectively form what is recognized as the pilosebaceous unit. This complex, three-dimensional structure within the skin possesses a unique biochemistry, metabolism and immunology. Recent studies have focused on the hair follicle as a potential pathway for both local...

journal_title：Pharmaceutical research

authors： Lauer AC,Lieb LM,Ramachandran C,Flynn GL,Weiner ND

更新日期：1995-02-01 00:00:00

abstract：PURPOSE:To prepare a thermoreversible gel system able to work as a medium for crystallization at around 20°C, allowing easy retrieval of crystals by simply decreasing the gel temperature. Lactose was selected has model substance for crystallization. METHODS:Water solutions with different% of poloxamer 407, α-Lactose m...

journal_title：Pharmaceutical research

authors： Cespi M,Bonacucina G,Casettari L,Mencarelli G,Palmieri GF

更新日期：2012-03-01 00:00:00

abstract：PURPOSE:Recombinant human serum albumin (rHSA), secreted by a Pichia pastoris expression system, was purified by a fast and efficient method, the essential feature of which is strong but reversible binding of the protein to Blue Sepharose. The structural characteristics, stability, and ligand-binding properties of the ...

journal_title：Pharmaceutical research

authors： Watanabe H,Yamasaki K,Kragh-Hansen U,Tanase S,Harada K,Suenaga A,Otagiri M

更新日期：2001-12-01 00:00:00