Application of image-based particle size and shape characterization systems in the development of small molecule pharmaceuticals.

abstract：:Knowledge of slip or cleavage planes can facilitate the fundamental understanding of mechanical properties of organic crystals important to pharmaceutical operations, such as tableting and milling. Slip/cleavage planes were frequently assigned based on attachment energy calculation. These crystallographic planes can a...

journal_title：Journal of pharmaceutical sciences

authors： Sun CC,Kiang YH

更新日期：2008-08-01 00:00:00

abstract：:Nasal mucosa excised from dogs or rabbits was mounted as a flat sheet in an in vitro chamber. The permeability was assessed by measuring the unidirectional flux of the radiolabeled tracer compounds, water, sucrose, polyethylene glycol, and cholecystokinin octapeptide. The permeability coefficients calculated from the ...

journal_title：Journal of pharmaceutical sciences

authors： Hersey SJ,Jackson RT

更新日期：1987-12-01 00:00:00

abstract：:The present work employs recent advances in high-resolution real-time magnetic resonance imaging (MRI) to investigate the disintegration process of tablets containing disintegrants. A temporal resolution of 75 ms and a spatial resolution of 80 × 80 µm with a section thickness of only 600 µm were achieved. The histogra...

journal_title：Journal of pharmaceutical sciences

authors： Quodbach J,Moussavi A,Tammer R,Frahm J,Kleinebudde P

更新日期：2014-01-01 00:00:00

abstract：:A conventional atomistic approach of estimating molecular hydrophobicity (log P) was improved by taking into account the proximity effect of substituent groups as well as the importance of solute-solvent interaction in the partition phenomena. The new method reassigns atomic parameters when the molecule is fully expos...

journal_title：Journal of pharmaceutical sciences

authors： Masuda T,Jikihara T,Nakamura K,Kimura A,Takagi T,Fujiwara H

更新日期：1997-01-01 00:00:00

abstract：:The in vitro antifungal activity of a novel series of cis- and trans-5-([aryl or aryloxy (or thio)]methyl)-3-(1H-imidazol-1-ylmethyl)-3- (2-thienyl)-2-methylisoxazolidines (13-24) was evaluated and compared with ketoconazole. The title series of compounds was prepared via a 1,3-dipolar cycloaddition reaction of 1-(2-t...

journal_title：Journal of pharmaceutical sciences

authors： Mullen GB,Mitchell JT,Allen SD,St Georgiev V

更新日期：1988-12-01 00:00:00

abstract：:Alginate microparticles incorporating hydrocortisone hemisuccinate were produced by aerosolization and homogenization methods to investigate their potential for colonic drug delivery. Microparticle stabilization was achieved by CaCl2 crosslinking solution (0.5 M and 1 M), and drug loading was accomplished by diffusion...

journal_title：Journal of pharmaceutical sciences

authors： Samak YO,El Massik M,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:The aim of this work was to optimize the absorption of parathyroid hormone 1-34 (PTH) from the lungs by determining factors favoring its transport from the air spaces into the bloodstream. We simultaneously conducted pharmacokinetic and regional lung deposition studies in vivo in the rat following intratracheal admini...

journal_title：Journal of pharmaceutical sciences

authors： Codrons V,Vanderbist F,Ucakar B,Préat V,Vanbever R

更新日期：2004-05-01 00:00:00

abstract：:A confocal Raman microscopic technique was optimized to more efficiently detect amorphous-amorphous phase separation in freeze-dried protein formulations. A Renishaw Raman inVia confocal microscope was used to collect 100-200 μm line maps (2 μm step size) of freeze-dried protein-excipient formulations. At each point a...

journal_title：Journal of pharmaceutical sciences

authors： Forney-Stevens KM,Pelletier MJ,Shalaev EY,Pikal MJ,Bogner RH

更新日期：2014-09-01 00:00:00

abstract：:This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original q...

journal_title：Journal of pharmaceutical sciences

authors： Sahoo NG,Kakran M,Shaal LA,Li L,Müller RH,Pal M,Tan LP

更新日期：2011-06-01 00:00:00

abstract：:The purpose of this study was to evaluate the cardiovascular effects of two potential beta-hydroxylase inhibitors, a dithiocarbamate and a thiourea derivative of d-amphetamine, 1 and 2, respectively. These compounds when given intravenously elicited a significant dose-dependent depressor effect in normotensive rats an...

journal_title：Journal of pharmaceutical sciences

authors： Venugopalan CS,Jenkins HJ

更新日期：1985-06-01 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：:Insoluble (visible) aggregates of a homodimer fusion glycoprotein, consisting of the first extracellular domain of a human protein, fused to the hinge, C(H)2, and C(H)3 domains of a human immunoglobulin G(1) (IgG(1)), were observed during early formulation development. The soluble fraction of the fusion protein was co...

journal_title：Journal of pharmaceutical sciences

authors： Souillac PO

更新日期：2005-09-01 00:00:00

abstract：:Eighteen healthy adult volunteers completed an open-label, four-way crossover study designed to determine the bioequivalency of 160-mg cibenzoline [2-(2,2-diphenylcyclopropyl)-4,5-dihydro-1H-imidazole] capsules and tablets, their relative bioavailability compared with an oral solution of the drug, as well as the absol...

journal_title：Journal of pharmaceutical sciences

authors： Massarella J,Silvestri T,Lin A

更新日期：1986-09-01 00:00:00

abstract：:Vaults, at 13 MDa, are the largest ribonucleoprotein particles known. In vitro, expression of the major vault protein (MVP) alone in Sf9 insect cells results in the production of recombinant particles with characteristic vault structure. With the ultimate goal of using recombinant vaults as nanocapsules for the delive...

journal_title：Journal of pharmaceutical sciences

authors： Esfandiary R,Kickhoefer VA,Rome LH,Joshi SB,Middaugh CR

更新日期：2009-04-01 00:00:00

abstract：:The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the comp...

journal_title：Journal of pharmaceutical sciences

authors： Nordström J,Alderborn G

更新日期：2015-06-01 00:00:00

abstract：:Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

journal_title：Journal of pharmaceutical sciences

authors： Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

更新日期：2013-10-01 00:00:00

abstract：:The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...

journal_title：Journal of pharmaceutical sciences

authors： Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

更新日期：2015-10-01 00:00:00

abstract：:Understanding the coating unit operation is imperative to improve product quality and reduce output risks for coated solid dosage forms. Three batches of sustained-release tablets coated with the same process parameters (pan speed, spray rate, etc.) were subjected to terahertz pulsed imaging (TPI) analysis followed by...

journal_title：Journal of pharmaceutical sciences

authors： Ho L,Müller R,Gordon KC,Kleinebudde P,Pepper M,Rades T,Shen Y,Taday PF,Zeitler JA

更新日期：2009-12-01 00:00:00

abstract：:Three dissolution apparatus, the rotating basket, the rotating paddle, and the rotating filter--stationary basket, were evaluated for their suitability as production control tools and their relation to blood level studies in dogs. The rotating basket and rotating paddle assemblies were easier to use and less variable ...

journal_title：Journal of pharmaceutical sciences

authors： Hardwidge EA,Sarapu AC,Laughlin WC

更新日期：1978-12-01 00:00:00

abstract：:Chitosan salts are being investigated as materials for bacterially triggered colonic drug delivery, via the oral route, based on the assumption that they will be degraded by the enzymes produced by the human colonic bacteria. The actual susceptibility of chitosan to these enzymes is, however, unclear. The digestion of...

journal_title：Journal of pharmaceutical sciences

authors： McConnell EL,Murdan S,Basit AW

更新日期：2008-09-01 00:00:00

abstract：:Alpha-Hydroxyaryl ketones such as 2-hydroxypropiophenone and 1-(2,4-difluorophenyl)-2-hydroxy-1-propanone, the key intermediates in the preparation of antifungal agents, decompose into oxidized, rearranged, and condensed products. These products were isolated and characterized. The possible mechanisms for the formatio...

journal_title：Journal of pharmaceutical sciences

authors： Gala D,Puar MS,Das PR,Kugelman M,DiBenedetto DJ

更新日期：1992-12-01 00:00:00

abstract：:Product temperature (Tb) and drying time constitute critical material attributes and process parameters in the lyophilization process and especially during the primary drying stage. In the study, we performed a temperature measurement by the sublimation rate (TMbySR) to monitor the Tb value and determine the end point...

journal_title：Journal of pharmaceutical sciences

authors： Kawasaki H,Shimanouchi T,Sawada H,Hosomi H,Hamabe Y,Kimura Y

更新日期：2019-07-01 00:00:00

abstract：:A high-pressure liquid chromatographic method suitable for determining plasma metoclopramide levels at normal (10-20 mg) doses is described. Eight metabolites as well as metclopramide were isolated and identified in rat, dog. and human urine. The only common metabolite in these species is 2-[(4-amino-5-chloro-2-metho...

journal_title：Journal of pharmaceutical sciences

authors： Teng L,Bruce RB,Dunning LK

更新日期：1977-11-01 00:00:00

abstract：:The recently introduced four-parameter extended Hansen approach was used to study the solubility of p-hydroxybenzoic acid and methyl p-hydroxybenzoate in 32 and 35 individual solvents, respectively. The results are compared with those for benzoic acid in 40 solvents. Seventeen of the thirty-two or 53% of the calculate...

journal_title：Journal of pharmaceutical sciences

authors： Martin A,Wu PL,Beerbower A

更新日期：1984-02-01 00:00:00

abstract：:Co-amorphous drug-amino acid systems have gained growing interest as an alternative to common amorphous formulations which contain polymers as stabilizers. Several preparation methods have recently been investigated, including vibrational ball milling on a laboratory scale or spray drying in a larger scale. In this st...

journal_title：Journal of pharmaceutical sciences

authors： Lenz E,Löbmann K,Rades T,Knop K,Kleinebudde P

更新日期：2017-01-01 00:00:00

abstract：:The cyclopropyl amine moiety in GSK2879552 (1) degrades hydrolytically in high pH conditions. This degradation pathway was observed during long-term stability studies and impacted the shelf life of the drug product. This article describes the work to identify the degradation impurities, elucidate the degradation mecha...

journal_title：Journal of pharmaceutical sciences

authors： Campbell JM,Lee M,Clawson J,Kennedy-Gabb S,Bethune S,Janiga A,Kindon L,Leach KP

更新日期：2019-09-01 00:00:00

abstract：:A GLC method for determining theophylline, hydroxyethyltheophylline, and diphenylpyraline hydrochloride is presented. The method permits the separation and quantitative determination of the therapeutically active ingredients with a single injection in an overall time of approximately 2.5 hr. ...

journal_title：Journal of pharmaceutical sciences

authors： de Fabrizio F

更新日期：1979-04-01 00:00:00

abstract：:Anthralin and its decomposition products were separated by both column chromatographic and TLC techniques. Two decomposition products were characterized by TLC, melting-point data, and UV and IR spectroscopy. Pure anthralin and its decomposition products also were determined quantitatively. ...

journal_title：Journal of pharmaceutical sciences

authors： Elsabbagh HM,Whitworth CW,Schramm LC

更新日期：1979-03-01 00:00:00

abstract：:The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

journal_title：Journal of pharmaceutical sciences

authors： Hudgins PM,Stubbins JF

更新日期：1975-08-01 00:00:00

abstract：:We report a programed drug delivery system that can tailor the release of anesthetic bupivacaine in a spatiotemporally controlled manner. The drug delivery system was developed through the combination of a collagen-based injectable hydrogel and 2 types of poly(lactic-co-glycolic acid) (PLGA) particles. As a rapid-rele...

journal_title：Journal of pharmaceutical sciences

authors： Dinh VV,Suh YS,Yang HK,Lim YT

更新日期：2016-12-01 00:00:00