Abstract:
:Seven healthy, male volunteers were entered into a randomized, open crossover study of the gastrointestinal transit of two enteric-coated 500-mg naproxen tablets. Two radiolabeled tablets were given to each volunteer on two occasions separated by 7 days, once in the fasted state and once after breakfast. Radiolabeling of tablets was achieved by the incorporation of samarium-152 oxide during manufacture, followed by neutron activation of the tablet to produce the gamma-emitting isotope samarium-153. No loss of tablet integrity was seen in the stomach and all tablets disintegrated in the small intestine. Onset of tablet disintegration was controlled predominantly by gastric emptying. Time in the small intestine prior to tablet disintegration was independent of food intake. Naproxen blood levels with time were consistent with the delayed release of naproxen from the tablets. Overall, transit, disintegration, and absorption were as expected from an enteric-coated tablet.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Wilding IR,Hardy JG,Sparrow RA,Davis SS,Daly PB,English JRdoi
10.1023/a:1015858829187subject
Has Abstractpub_date
1992-11-01 00:00:00pages
1436-41issue
11eissn
0724-8741issn
1573-904Xjournal_volume
9pub_type
临床试验,杂志文章,随机对照试验abstract:PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007570030368
更新日期:2000-11-01 00:00:00
abstract:PURPOSE:Cationic host defence peptides constitute a promising class of therapeutic drug leads with a wide range of therapeutic applications, including anticancer therapy, immunomodulation, and antimicrobial activity. Although potent and efficacious, systemic toxicity and low chemical stability have hampered their comme...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1658-6
更新日期:2015-08-01 00:00:00
abstract:PURPOSE:Permeation studies, with near infrared (NIR) light and anti-aggregation antibody formulation, were used to investigate the in vitro permeation of bevacizumab, ranibizumab and aflibercept through human sclera. METHODS:A vertical, spherical Franz cell diffusion apparatus was used for this scleral tissue permeati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2392-7
更新日期:2018-03-29 00:00:00
abstract::A novel floating controlled-release drug delivery system was formulated in an effort increase the gastric retention time of the dosage form and to control drug release. The buoyancy was attributed to air and oil entrapped in the agar gel network. A floating controlled-release 300-mg theophylline tablet having a densit...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018921830385
更新日期:1993-09-01 00:00:00
abstract:PURPOSE:Drug particle physical properties are critical for the efficiency of a drug delivered to the lung. The purpose of this study was to produce ultrafine sumatriptan succinate particles for inhalation. METHODS:Sumatriptan succinate particles were produced via reactive precipitation without any surfactants. Several...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9586-3
更新日期:2008-09-01 00:00:00
abstract:PURPOSE:To study the degradation of oxaliplatin in chloride media and evaluate the cytotoxicity of oxaliplatin in normal and chloride-deficient medium. METHODS:The products of the reaction of oxaliplatin with chloride were separated on a Hypercarb S column with a mobile phase containing 40% methanol in 0.05 M ammonia ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000026444.67883.83
更新日期:2004-05-01 00:00:00
abstract:PURPOSE:To compare the effectiveness of trastuzumab-modified gold nanoparticles (AuNP) labeled with 177Lu (trastuzumab-AuNP-177Lu) targeted to HER2 with non-targeted AuNP-177Lu for killing HER2-overexpressing breast cancer (BC) cells in vitro and inhibiting tumor growth in vivo following intratumoral (i.t.) injection. ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2082-2
更新日期:2017-03-01 00:00:00
abstract:PURPOSE:The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000029284.40637.69
更新日期:2004-06-01 00:00:00
abstract:PURPOSE:Cell-based permeability screens are widely used to identify drug-P-glycoprotein (PGP) interaction in vitro. However, their reliability in predicting the impact of PGP on human drug pharmacokinetics is poorly defined. The aim was to determine whether a quantitative relationship exists between PGP-mediated altera...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000026434.82855.69
更新日期:2004-05-01 00:00:00
abstract:PURPOSE:Monoamine oxidases (MAOs) are non-CYP enzymes that contribute to systemic elimination of therapeutic agents, and localized on mitochondrial membranes. The aim of the present study was to validate quantitative estimation of metabolic clearance of MAO substrate drugs using human liver microsomes (HLMs). METHODS:...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2140-4
更新日期:2017-06-01 00:00:00
abstract:PURPOSE:Grapefruit juice (GJ) is known to increase the oral bioavailability of many CYP3A-substrates by inhibiting intestinal phase-I metabolism. However, the magnitude of AUC increase is often insignificant and highly variable. Since we earlier suggested that CYP3A and P-glycoprotein (P-gp) form a concerted barrier to...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011902625609
更新日期:1999-04-01 00:00:00
abstract::The effects of tertiary amine-containing basic drugs on the enzymes located in the mitochondria and the effect of monoamine oxidase inhibitors (MAOIs) on drug accumulation in lung mitochondria have been studied. Various basic drugs inhibited MAO activity but not other mitochondrial marker enzymes. The potency of MAO i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015964623098
更新日期:1989-10-01 00:00:00
abstract:PURPOSE:The specific interactions between three lectin-latex conjugates and different structures of rat intestinal mucosa have been studied ex vivo. METHODS:These systems were prepared by covalent coupling of different ligands, i.e., tomato lectin (TL), asparagus pea lectin (AL), mycoplasma gallisepticum lectin (ML), ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016405126656
更新日期:1996-11-01 00:00:00
abstract:PURPOSE:The purpose of this study is to investigate the characteristics of pGlu-L-Dopa-Pro as a prodrug of L-Dopa. METHODS:pGlu-L-Dopa-Pro and L-Dopa-Pro were synthesized using the standard procedures of peptide synthesis. The conversion of pGlu-L-Dopa-Pro to L-Dopa was studied using pyroglutamyl aminopeptidase I and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016239321494
更新日期:1995-07-01 00:00:00
abstract:PURPOSE:For the assessment of bioequivalence it is assumed that drug clearance in each subject on each of the study days is the same and any observed differences in AUC and/or Cmax between a brand and generic formulation are due to differences in bioavailability. We hypothesized that this assumption was invalid for hig...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章
doi:10.1023/a:1016040825844
更新日期:1996-06-01 00:00:00
abstract:PURPOSE:The pharmacokinetics of corticosteroids in pregnancy were analyzed to assess maternal/fetal disposition and factors controlling fetal exposure. Area/Moment equations and compartmental models for estimating pharmacokinetic parameters from single dose data during pregnancy were developed. METHODS:Betamethasone i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-7681-7
更新日期:2004-12-01 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
pub_type: 杂志文章
doi:10.1023/a:1011994230346
更新日期:1998-04-01 00:00:00
abstract:PURPOSE:To apply physiologically-based pharmacokinetic (PBPK) modeling to investigate the consequences of reduction in activity of hepatic and intestinal uptake and efflux transporters by cyclosporine and its metabolite AM1. METHODS:Inhibitory potencies of cyclosporine and AM1 against OATP1B1, OATP1B3 and OATP2B1 were...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0918-y
更新日期:2013-03-01 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
pub_type: 杂志文章
doi:10.1007/s11095-013-1060-1
更新日期:2013-08-01 00:00:00
abstract:PURPOSE:To evaluate organic anion transporter-mediated drug-drug interaction (DDI) potential for individual active components of Danshen (Salvia miltiorrhiza) vs. combinations using in vitro and in silico approaches. METHODS:Inhibition profiles for single Danshen components and combinations were generated in stably-ex...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1437-9
更新日期:2014-12-01 00:00:00
abstract:PURPOSE:Several phenomena in tablets indicate that an inhomogeneous pore distribution is formed during the compaction process. Examples are lamination and the capping of corners. In order to gain an understanding of the relation between structure and compact properties, analyzing the structure in a location dependent m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-5280-x
更新日期:2005-08-01 00:00:00
abstract:PURPOSE:The objective of the current study was to investigate whether blood-brain barrier (BBB) permeability studies in vitro could be accelerated by running several compounds together in the same experiment. METHODS:To address this question, we compared the transport of six compounds run separately with the results o...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000026424.78528.11
更新日期:2004-05-01 00:00:00
abstract::The plasma concentration-time profiles and pharmacokinetics were characterized for nicotine and its major metabolite, cotinine, after multiple daily application of a nicotine user-activated transdermal therapeutic system (UATTS) to nine healthy smokers. The volunteers abstained from smoking 24 hr prior to and during t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015810019076
更新日期:1991-03-01 00:00:00
abstract:PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1869-5
更新日期:2016-05-01 00:00:00
abstract:PURPOSE:To develop a safe and effective non-viral vector for gene delivery and transfection in macrophages for potential anti-inflammatory therapy. METHODS:Solid nanoparticles-in-emulsion (NiE) multi-compartmental delivery system was designed using plasmid DNA-encapsulated type B gelatin nanoparticles suspended in the...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0677-9
更新日期:2012-06-01 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
pub_type: 杂志文章
doi:10.1007/s11095-018-2420-7
更新日期:2018-05-10 00:00:00
abstract::The stability of two purified monoclonal antibodies, MN12 and WT31, was investigated. The monoclonal antibodies were incubated for 32 days at different pH values (ranging from 3.0 to 10.0) at 4 and 37 degrees C. Various analytical methods were used to assess changes in physicochemical properties of the proteins. The m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015925519154
更新日期:1990-12-01 00:00:00
abstract::A two-step analytic procedure to determine the rate and extent of metabolite production following administration of the parent compound is described. The procedure provides the rate and extent of metabolite production as a function of time by application of the general model independent approach of deconvolution. The ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015951426191
更新日期:1988-06-01 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
pub_type: 杂志文章
doi:10.1023/a:1018997101542
更新日期:1994-08-01 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
pub_type: 杂志文章
doi:10.1007/s11095-015-1619-0
更新日期:2015-07-01 00:00:00