In vivo evaluation of enteric-coated naproxen tablets using gamma scintigraphy.

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 Res

journal_title

Pharmaceutical research

authors

Wilding IR,Hardy JG,Sparrow RA,Davis SS,Daly PB,English JR

doi

10.1023/a:1015858829187

subject

Has Abstract

pub_date

1992-11-01 00:00:00

pages

1436-41

issue

11

eissn

0724-8741

issn

1573-904X

journal_volume

9

pub_type

临床试验,杂志文章,随机对照试验
  • Protein spray-freeze drying. Effect of atomization conditions on particle size and stability.

    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

    authors: Costantino HR,Firouzabadian L,Hogeland K,Wu C,Beganski C,Carrasquillo KG,Córdova M,Griebenow K,Zale SE,Tracy MA

    更新日期:2000-11-01 00:00:00

  • Hyaluronic Acid-Based Nanogels Produced by Microfluidics-Facilitated Self-Assembly Improves the Safety Profile of the Cationic Host Defense Peptide Novicidin.

    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

    authors: Water JJ,Kim Y,Maltesen MJ,Franzyk H,Foged C,Nielsen HM

    更新日期:2015-08-01 00:00:00

  • Photokinetic Drug Delivery: Near infrared (NIR) Induced Permeation Enhancement of Bevacizumab, Ranibizumab and Aflibercept through Human Sclera.

    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

    authors: Giannos SA,Kraft ER,Zhao ZY,Merkley KH,Cai J

    更新日期:2018-03-29 00:00:00

  • A floating controlled-release drug delivery system: in vitro-in vivo evaluation.

    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

    authors: Desai S,Bolton S

    更新日期:1993-09-01 00:00:00

  • Production of ultrafine sumatriptan succinate particles for pulmonary delivery.

    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

    authors: Yang ZY,Le Y,Hu TT,Shen Z,Chen JF,Yun J

    更新日期:2008-09-01 00:00:00

  • Oxaliplatin degradation in the presence of chloride: identification and cytotoxicity of the monochloro monooxalato complex.

    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

    authors: Jerremalm E,Hedeland M,Wallin I,Bondesson U,Ehrsson H

    更新日期:2004-05-01 00:00:00

  • Local Radiation Treatment of HER2-Positive Breast Cancer Using Trastuzumab-Modified Gold Nanoparticles Labeled with 177Lu.

    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

    authors: Cai Z,Yook S,Lu Y,Bergstrom D,Winnik MA,Pignol JP,Reilly RM

    更新日期:2017-03-01 00:00:00

  • A novel one-step drug-loading procedure for water-soluble amphiphilic nanocarriers.

    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

    authors: Fournier E,Dufresne MH,Smith DC,Ranger M,Leroux JC

    更新日期:2004-06-01 00:00:00

  • Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo.

    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

    authors: Collett A,Tanianis-Hughes J,Hallifax D,Warhurst G

    更新日期:2004-05-01 00:00:00

  • Utilization of Liver Microsomes to Estimate Hepatic Intrinsic Clearance of Monoamine Oxidase Substrate Drugs in Humans.

    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

    authors: Masuo Y,Nagamori S,Hasegawa A,Hayashi K,Isozumi N,Nakamichi N,Kanai Y,Kato Y

    更新日期:2017-06-01 00:00:00

  • Grapefruit juice activates P-glycoprotein-mediated drug transport.

    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

    authors: Soldner A,Christians U,Susanto M,Wacher VJ,Silverman JA,Benet LZ

    更新日期:1999-04-01 00:00:00

  • Contribution of monoamine oxidase (MAO) to the binding of tertiary basic drugs in lung mitochondria.

    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

    authors: Yoshida H,Kamiya A,Okumura K,Hori R

    更新日期:1989-10-01 00:00:00

  • Bioadhesion of lectin-latex conjugates to rat intestinal mucosa.

    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

    authors: Irache JM,Durrer C,Duchêne D,Ponchel G

    更新日期:1996-11-01 00:00:00

  • pGlu-L-Dopa-Pro: a tripeptide prodrug targeting the intestinal peptide transporter for absorption and tissue enzymes for conversion.

    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

    authors: Bai JP

    更新日期:1995-07-01 00:00:00

  • High variability in drug pharmacokinetics complicates determination of bioequivalence: experience with verapamil.

    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

    authors: Tsang YC,Pop R,Gordon P,Hems J,Spino M

    更新日期:1996-06-01 00:00:00

  • Area/moment and compartmental modeling of pharmacokinetics during pregnancy: applications to maternal/fetal exposures to corticosteroids in sheep and rats.

    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

    authors: Samtani MN,Schwab M,Nathanielsz PW,Jusko WJ

    更新日期:2004-12-01 00:00:00

  • Application of fractal kinetics for carrier-mediated transport of drugs across intestinal epithelial membrane.

    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

    authors: Ogihara T,Tamai I,Tsuji A

    更新日期:1998-04-01 00:00:00

  • Cyclosporine inhibition of hepatic and intestinal CYP3A4, uptake and efflux transporters: application of PBPK modeling in the assessment of drug-drug interaction potential.

    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

    authors: Gertz M,Cartwright CM,Hobbs MJ,Kenworthy KE,Rowland M,Houston JB,Galetin A

    更新日期:2013-03-01 00:00:00

  • Brushed block copolymer micelles with pH-sensitive pendant groups for controlled drug delivery.

    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

    authors: Lee HJ,Bae Y

    更新日期:2013-08-01 00:00:00

  • Cumulative organic anion transporter-mediated drug-drug interaction potential of multiple components in salvia miltiorrhiza (danshen) preparations.

    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

    authors: Wang L,Venitz J,Sweet DH

    更新日期:2014-12-01 00:00:00

  • Location-dependent analysis of porosity and pore direction in tablets.

    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

    authors: Wu YS,Frijlink HW,van Vliet LJ,Stokroos I,van der Voort Maarschalk K

    更新日期:2005-08-01 00:00:00

  • Transport screening of drug cocktails through an in vitro blood-brain barrier: is it a good strategy for increasing the throughput of the discovery pipeline?

    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

    authors: Berezowski V,Landry C,Lundquist S,Dehouck L,Cecchelli R,Dehouck MP,Fenart L

    更新日期:2004-05-01 00:00:00

  • Pharmacokinetics of multiple daily transdermal doses of nicotine in healthy smokers.

    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

    authors: Ross HD,Chan KK,Piraino AJ,John VA

    更新日期:1991-03-01 00:00:00

  • Insights into Spray Development from Metered-Dose Inhalers Through Quantitative X-ray Radiography.

    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

    authors: Mason-Smith N,Duke DJ,Kastengren AL,Stewart PJ,Traini D,Young PM,Chen Y,Lewis DA,Soria J,Edgington-Mitchell D,Honnery D

    更新日期:2016-05-01 00:00:00

  • Multi-compartmental nanoparticles-in-emulsion formulation for macrophage-specific anti-inflammatory gene delivery.

    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

    authors: Attarwala H,Amiji M

    更新日期:2012-06-01 00:00:00

  • Recrystallization and Water Absorption Properties of Vitrified Trehalose Near Room Temperature.

    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

    authors: Shirakashi R,Takano K

    更新日期:2018-05-10 00:00:00

  • Analytical approaches to the study of monoclonal antibody stability.

    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

    authors: Jiskoot W,Beuvery EC,de Koning AA,Herron JN,Crommelin DJ

    更新日期:1990-12-01 00:00:00

  • Metabolite formation pharmacokinetics: rate and extent of metabolite formation determined by deconvolution.

    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

    authors: Karol MD,Goodrich S

    更新日期:1988-06-01 00:00:00

  • Cyclodextrins as mucosal absorption promoters of insulin. II. Effects of beta-cyclodextrin derivatives on alpha-chymotryptic degradation and enteral absorption of insulin in rats.

    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

    authors: Shao Z,Li Y,Chermak T,Mitra AK

    更新日期:1994-08-01 00:00:00

  • Controlled Endolysosomal Release of Agents by pH-responsive Polymer Blend Particles.

    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

    authors: Zhan X,Tran KK,Wang L,Shen H

    更新日期:2015-07-01 00:00:00