Agglomeration of mesoporous silica by melt and steam granulation. part II: screening of steam granulation process variables using a factorial design.


:The objectives of this study were to identify the key process parameters during steam granulation of disordered mesoporous silica material Syloid® 244 FP (244) and to compare two different binders: polyvinylpyrrolidone (PVP) K25 and hydroxypropylmethyl cellulose (HPMC). Itraconazole (ITZ) was selected as the model compound for the development of an oral dosage form for enhanced release. Six factors: binder content, steam amount, mixing time, impeller speed, spray pause time, and filler content were investigated using a two-level quarter-fraction factorial design of experiment (DOE) for each binder type. As experimental responses, characteristics correlating to both granules and tablets were selected. Granules prepared from PVP resulted in an overall higher bulk density, granule size, increased flow properties, and better compression and compaction behavior. Although granulation with PVP resulted in the most ITZ to extract from the pores during processing, the premature drug release was less than 5%. The results of the DOE indicate that the risk of extracting the drug from the pores during processing is governed both by the process parameters and the binder properties. Centerpoint replicates of granules prepared with HPMC were highly variable.


J Pharm Sci


Vialpando M,Albertini B,Passerini N,Vander Heyden Y,Rombaut P,Martens JA,Van Den Mooter G




Has Abstract


2013-11-01 00:00:00














  • Numerical modelling of transdermal delivery from matrix systems: parametric study and experimental validation with silicone matrices.

    abstract::A model is presented for transdermal drug delivery from single-layered silicone matrix systems. The work is based on our previous results that, in particular, extend the well-known Higuchi model. Recently, we have introduced a numerical transient model describing matrix systems where the drug dissolution can be non-in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Snorradóttir BS,Jónsdóttir F,Sigurdsson ST,Másson M

    更新日期:2014-08-01 00:00:00

  • Effect of tumor necrosis factor-alpha and interferon-gamma on intestinal P-glycoprotein expression, activity, and localization in Caco-2 cells.

    abstract::The P-glycoprotein (Pgp), a drug efflux pump, is expressed in intestinal epithelial cells, where it constitutes a barrier against xenobiotics. In inflammatory bowel disease, a dysregulation in the production of tumor necrosis factor (TNF)alpha and interferon (IFN)gamma, and an alteration of Pgp expression and activity...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Belliard AM,Lacour B,Farinotti R,Leroy C

    更新日期:2004-06-01 00:00:00

  • Compatibility, physical stability, and characterization of an IgG4 monoclonal antibody after dilution into different intravenous administration bags.

    abstract::The physical stability of an immunoglobulin G4 monoclonal antibody (mAb) upon dilution into intravenous (i.v.) bags containing 0.9% saline was examined. Soluble aggregates and subvisible particles were observed by size-exclusion high-performance liquid chromatography (SE-HPLC) and light obscuration when formulated wit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kumru OS,Liu J,Ji JA,Cheng W,Wang YJ,Wang T,Joshi SB,Middaugh CR,Volkin DB

    更新日期:2012-10-01 00:00:00

  • Controlled and complete release of a model poorly water-soluble drug, prednisolone, from hydroxypropyl methylcellulose matrix tablets using (SBE)(7m)-beta-cyclodextrin as a solubilizing agent.

    abstract::Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-beta-cyclodextrins ((SBE)(7M)-beta-CDs...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Rao VM,Haslam JL,Stella VJ

    更新日期:2001-07-01 00:00:00

  • Interaction of L-tryptophan with alpha-cyclodextrin: studies with calorimetry and proton nuclear magnetic resonance spectroscopy.

    abstract::The interaction of L-tryptophan with alpha-cyclodextrin was investigated in a 0.1 M phosphate buffer at pH 7.4 with a LKB 2277 microcalorimeter, using flow mixed mode at 25 degrees C. The thermodynamic parameters for inclusion complex formation obtained are as follows; DeltaG(0) = - 7.03 kJ/mol (K = 17.0), DeltaH(0) =...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Nishijo J,Tsuchitani M

    更新日期:2001-02-01 00:00:00

  • Binding of (+)- and (-)-isomers and racemate of etomoxir to human serum albumin and effect of stearic acid and stanozolol.

    abstract::Binding of (+)- and (-)-isomers and the racemate of sodium 2[6-(4-chlorophenoxy)-hexyl]-oxiran-2-carboxylate dihydrat (etomoxir) to the human serum albumin (HSA) was studied by the gel filtration method. The experimental results are presented graphically using the method of Scatchard. Measurements revealed the followi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Vestemar V,Medic-Saric M,Rendic S

    更新日期:1994-04-01 00:00:00

  • Simultaneous determination of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations by gas chromatography.

    abstract::An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schieffer GW,Palermo PJ,Pollard-Walker S

    更新日期:1984-01-01 00:00:00

  • Molecular modeling of beta-cyclodextrin complexes with nootropic drugs.

    abstract::The geometry and structural features of the inclusion complexes of beta-cyclodextrin (beta-CD) with the chiral antiamnesic drugs (+/-)-1-benzyl-4-hydroxymethylpyrrolidin-2-one (WEB-1868). (+/-)-1-benzenesulfonyl-5-ethoxypyrrolidin-2-one (RU-35929), and (+/-)-1-(3-pyridinlysulfonyl)-5-ethoxypyrrolidin-2-one (RU-47010) ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Amato ME,Djedaïni F,Pappalardo GC,Perly B,Scarlata G

    更新日期:1992-12-01 00:00:00

  • Expression of Carboxylesterase Isozymes and Their Role in the Behavior of a Fexofenadine Prodrug in Rat Skin.

    abstract::The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

    更新日期:2016-02-01 00:00:00

  • Effect of symmetrical tetraalkylammonium salts on cloud point on nonionic surfactants.

    abstract::The salting in and salting out of the nonionic surfactant octoxynol NF by halides of ammonium and the four lowest symmetrical tetraalkylammonium cations were investigated by measuring their effect on the cloud point at various salt concentrations. The chloride anion tended to salt the surfactant out, lowering its clou...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schott H,Han SK

    更新日期:1977-02-01 00:00:00

  • α-Lipoic Acid in Soluplus(®) Polymeric Nanomicelles for Ocular Treatment of Diabetes-Associated Corneal Diseases.

    abstract::α-Lipoic acid (ALA) is a powerful antioxidant valuable for prevention and treatment of ophthalmic complications such as diabetic keratopathy and retinopathy. The aim of this work was to develop micelle-based formulations that can enhance the solubility, stability, and corneal permeability of ALA. Compared to a convent...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Alvarez-Rivera F,Fernández-Villanueva D,Concheiro A,Alvarez-Lorenzo C

    更新日期:2016-09-01 00:00:00

  • Achieving continuous manufacturing for final dosage formation: challenges and how to meet them. May 20-21, 2014 Continuous Manufacturing Symposium.

    abstract::We describe the key issues and possibilities for continuous final dosage formation, otherwise known as downstream processing or drug product manufacturing. A distinction is made between heterogeneous processing and homogeneous processing, the latter of which is expected to add more value to continuous manufacturing. W...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Byrn S,Futran M,Thomas H,Jayjock E,Maron N,Meyer RF,Myerson AS,Thien MP,Trout BL

    更新日期:2015-03-01 00:00:00

  • Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems.

    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

    pub_type: 杂志文章


    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

  • Determination of drug plasma protein binding by solid phase microextraction.

    abstract::The plasma protein binding of drugs has been shown to have significant effects on the quantitative relationship between clinical pharmacokinetics and pharmacodynamics. In many clinical situations, measurement of the total drug concentration does not provide the needed information concerning the unbound fraction of dru...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Musteata FM,Pawliszyn J,Qian MG,Wu JT,Miwa GT

    更新日期:2006-08-01 00:00:00

  • Kinetics of drug action in disease states. XXXVI: Effect of cyclosporine on the pharmacodynamics and pharmacokinetics of a barbiturate (heptabarbital) in rats.

    abstract::Pretreatment with cyclosporine reportedly prolongs the effect of certain general anesthetics in humans and the sleeping time of mice after pentobarbital administration. This investigation was designed to determine the mechanism(s) of the cyclosporine-barbiturate interaction. Adult female Wistar rats received cyclospor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hoffman A,Levy G

    更新日期:1990-01-01 00:00:00

  • Monitoring the film coating unit operation and predicting drug dissolution using terahertz pulsed imaging.

    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

    pub_type: 杂志文章


    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

  • Transport in quantitative structure-activity relationships. VI: Relationship between transport rate constants and partition coefficients.

    abstract::The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: van de Waterbeemd H,van Bakel P,Jansen A

    更新日期:1981-09-01 00:00:00

  • Antiradiation compounds XV: condensations of carbon disulfide with amino, chloro, cyanomethyl, and sulfonamido heterocycles.

    abstract::Condensations of carbon disulfide were carried out with amino, chloro, and diamino heterocycles to give condensed ring thiazoline-2-thiones and imidazoline-2-thiones, with cyanomethyl heterocycles to give dithio acid derivatives, and with heterocyclic sulfonamides to give sulfonyldithiocarbamates. Of several examples ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Foye WO,Kauffman JM,Lanzillo JJ,LaSala EF

    更新日期:1975-08-01 00:00:00

  • Synthesis of 4,5-dimethoxykynuramine and its in vivo conversion to 6,7-dimethoxy-4-quinolinol.

    abstract::4,5-Dimethoxykynuramine was synthesized in a three-step sequence originating with veratrole. Indirect evidence indicates that the drug was converted in vivo to the hypotensive agent 6,7-dimethoxy-4-quinolinol by the action of monoamine oxidase. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schwan TJ,Honkomp LJ,Snyder HR Jr,Watson EJ

    更新日期:1978-03-01 00:00:00

  • Anti-plasticizing effect of amorphous indomethacin induced by specific intermolecular interactions with PVA copolymer.

    abstract::The mechanism of how poly(vinyl alcohol-co-acrylic acid-co-methyl methacrylate) (PVA copolymer) stabilizes an amorphous drug was investigated. Solid dispersions of PVA copolymer, poly(vinyl pyrrolidone) (PVP), and poly(vinyl pyrrolidone-co-vinyl acetate) (PVPVA) with indomethacin (IMC) were prepared. The glass transit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ueda H,Aikawa S,Kashima Y,Kikuchi J,Ida Y,Tanino T,Kadota K,Tozuka Y

    更新日期:2014-09-01 00:00:00

  • Effects of taraxacum mongolicum on the bioavailability and disposition of ciprofloxacin in rats.

    abstract::Taraxacum mongolicum (TM), also known as dandelion, is a herb widely used in the East for its antibacterial activity. The high mineral content of TM presents a potential problem for the absorption of quinolone antibiotics. This study was undertaken to discern the significance of a drug-drug interaction between TM and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zhu M,Wong PY,Li RC

    更新日期:1999-06-01 00:00:00

  • Combined use of pharmacokinetic modeling and a steady-state delivery approach allows early assessment of IkappaB kinase-2 (IKK-2) target safety and efficacy.

    abstract::NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chiang PC,Kishore NN,Thompson DC

    更新日期:2010-03-01 00:00:00

  • Apparent absorption kinetics of micronized griseofulvin after its oral administration on single- and multiple-dose regimens to rats as a corn oil-in-water emulsion and aqueous suspension.

    abstract::This investigation was designed to quantitate and compare in the rat the oral absorption characteristics of micronized griseofulvin from a corn oil-in-water emulsion dosage form containing suspended drug and a control aqueous suspension after single-dose (50 mg/kg) and multiple-dose (50 mg/kg every 12 hr for five dose...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bates TR,Carrigan PJ

    更新日期:1975-09-01 00:00:00

  • Dietary polyphenols (-)-epicatechin and chrysin inhibit intestinal glucuronidation metabolism to increase drug absorption.

    abstract::The effect of dietary polyphenols on the intestinal glucuronidation and absorption of a model phenolic drug, alpha-naphthol (alpha-NA), was studied in isolated rat small intestine. (-)-Epicatechin significantly inhibited the glucuronidation of alpha-NA. Chrysin, (-)-epigallocatechin galleate (EGCG), and quercetin decr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mizuma T,Awazu S

    更新日期:2004-09-01 00:00:00

  • Modified NF method for quantitative determination of pentaerythritol tetranitrate.

    abstract::A modified NF method for the quantitative determination of pentaerythritol tetranitrate is reported. A solution of powder is made directly from the dosage form in glacial acetic acid and is then reacted with phenoldisulfonic acid TS. The proposed method saves approximately 75% of the time required with the NF method. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Gupta VD

    更新日期:1978-05-01 00:00:00

  • Moisture sorption kinetics for water-soluble substances. I: Theoretical considerations of heat transport control.

    abstract::A model based on heat transport control was developed to describe the uptake of water on a deliquescent solid in an atmosphere of pure water vapor. The model assumes the presence of a saturated liquid film on the surface of the solid. The decrease in the vapor pressure of water over the surface, brought about by the c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Van Campen L,Amidon GL,Zografi G

    更新日期:1983-12-01 00:00:00

  • Verification and validation of computational models used in biopharmaceutical manufacturing: Potential application of the ASME Verification and Validation 40 standard and FDA proposed AI/ML model life cycle management framework.

    abstract::A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

    更新日期:2021-01-22 00:00:00

  • Inulin hydrogels as carriers for colonic drug targeting. Rheological characterization of the hydrogel formation and the hydrogel network.

    abstract::Free radical polymerization converts aqueous solutions of methacrylated inulin into cross-linked hydrogels. The purpose of this work was to study the hydrogel formation and to characterize the fully cured hydrogels. The gelation process of aqueous solutions of methacrylated inulin was monitored as a function of time b...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Vervoort L,Vinckier I,Moldenaers P,Van den Mooter G,Augustijns P,Kinget R

    更新日期:1999-02-01 00:00:00

  • Simultaneous determination of unlabeled and carbon-13-labeled etoricoxib, a new cyclooxygenase-2 inhibitor, in human plasma using HPLC-MS/MS.

    abstract::A method for the simultaneous determination of etoricoxib and its carbon-13 analog ((13)C(6)-etoricoxib) from human plasma has been developed and used to support bioavailability studies. Plasma samples (0.5 mL) were extracted by using a 3M Empore 96-well plate (C(8)) and the resulting extracts were analyzed by using a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Rose MJ,Agrawal N,Woolf EJ,Matuszewski BK

    更新日期:2002-02-01 00:00:00

  • Effect of pH on injection phlebitis.

    abstract::Formulation pH has been reported to be responsible for the incidence of phlebitis. In this study, the effect of pH on injection phlebitis is investigated. Buffers of varying pHs were examined for their ability to produce phlebitis in rabbits. Thermal measurements as well as visual evaluations were used for phlebitis q...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Simamora P,Pinsuwan S,Alvarez JM,Myrdal PB,Yalkowsky SH

    更新日期:1995-04-01 00:00:00