Development of new laboratory tools for assessment of granulation behavior during bulk active pharmaceutical ingredient drying.

Abstract:

:Approximately 30% of active pharmaceutical ingredients (APIs) experience agglomeration, granulation, and breakage during agitated drying. Currently, there is no small-scale bench tool to help assess and observe granulation behavior of APIs in the laboratory and subsequently lead to the development of a robust drying method. As a result, more conservative drying methods are usually used at scale and much longer drying times are needed. In this work, we build on work reported in the literature and demonstrate that a mixer torque rheometer (MTR) can be a useful small-scale tool to flag potentially problematic granulation behavior of APIs under different conditions. The results from the MTR were confirmed using a second new tool involving the use of an acoustic mixer to verify and observe the granulation behavior on a small scale. We also show consistency between the data collected at the laboratory and the pilot plant scales.

journal_name

J Pharm Sci

authors

Zhang S,Lamberto DJ

doi

10.1002/jps.23762

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

152-60

issue

1

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)30749-8

journal_volume

103

pub_type

杂志文章
  • Detection of a minor amorphous phase in crystalline etoricoxib by dynamic mechanical analysis: comparison with Raman spectroscopy and modulated differential scanning calorimetry.

    abstract::Detection and quantification of the amorphous phase of etoricoxib bulk drug substances, a selective cycloogenase-2 inhibitor used for the treatment of osteoarthritis, rheumatoid arthritis, and dental pain, was carried out using modulated differential scanning calorimetry (MDSC), dynamic mechanical analysis (DMA), and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22774

    authors: Clas SD,Lalonde K,Khougaz K,Dalton CR,Bilbeisi R

    更新日期:2012-02-01 00:00:00

  • High-performance frontal analysis-high-performance liquid chromatographic system for stereoselective determination of unbound ketoprofen enantiomers in plasma after direct sample injection.

    abstract::An on-line, high-performance frontal analysis (HPFA)-high-performance liquid chromatographic system was developed for the enantioselective determination of a low level of unbound ketoprofen (KP) that is in equilibrium with KP that is bound to protein. The system consists of three subsystems (HPFA system, preconcentrat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810725

    authors: Shibukawa A,Terakita A,He JY,Nakagawa T

    更新日期:1992-07-01 00:00:00

  • Utilising Magnetically Isolated Lysosomes for Direct Quantification of Intralysosomal Drug Concentrations by LC-MS/MS Analysis: An Investigatory Study With Imipramine.

    abstract::Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.05.026

    authors: Francis L,Harrell A,Hallifax D,Galetin A

    更新日期:2020-09-01 00:00:00

  • Potency of synthetic luteinizing hormone releasing hormone preparations in rat anterior pituitary cell cultures.

    abstract::Selected synthetic luteinizing hormone releasing hormone preparations were assayed, and their potencies were determined relative to one sample utilizing primary cultures of enzymatically dispersed rat anterior pituitary cells. Preliminary cell culture experiments indicated that luteinizing hormone releasing hormone ha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660319

    authors: Dermody WC,Pastushok CA,Sakowski R,Vaitkus JW,Reel JR

    更新日期:1977-03-01 00:00:00

  • Focused Ultrasound-Triggered Release of Tyrosine Kinase Inhibitor From Thermosensitive Liposomes for Treatment of Renal Cell Carcinoma.

    abstract::This study reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.01.027

    authors: Abshire C,Murad HY,Arora JS,Liu J,Mandava SH,John VT,Khismatullin DB,Lee BR

    更新日期:2017-05-01 00:00:00

  • Synthesis and biological evaluation of p-bromospiperone as potential neuroleptic drug.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.2600690835

    authors: Huang CC,Friedman AM,So R,Simonovic M,Meltzer HY

    更新日期:1980-08-01 00:00:00

  • Sustained release of isomazole from matrix tablets administered to dogs.

    abstract::Isomazole matrix tablet formulations, with various concentrations of hydroxypropyl methylcellulose (HPMC) hydrogel, were prepared and tested for sustained-release activity. Sustained-release activity was determined by administering isomazole test formulations orally to conscious dogs, instrumented with an indwelling l...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780715

    authors: Wilson HC,Cuff GW

    更新日期:1989-07-01 00:00:00

  • Preservative and Irritant Capacity of Biosurfactants From Different Sources: A Comparative Study.

    abstract::One of the most important challenges for pharmaceutical and cosmetic industries is solubilization and preservation of their active ingredients. Therefore, most of these formulations contain irritant chemical additives to improve their shelf-life and the solubility of hydrophobic ingredients. An interesting alternative...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.02.010

    authors: Rodríguez-López L,Rincón-Fontán M,Vecino X,Cruz JM,Moldes AB

    更新日期:2019-07-01 00:00:00

  • Distribution of gacyclidine enantiomers after experimental spinal cord injury in rats: possible involvement of an active transport system.

    abstract::The pharmacokinetics of gacyclidine enantiomers, a noncompetitive N-methyl-D-aspartate (NMDA) antagonist, were studied in plasma and spinal cord extracellular fluid (ECF) after experimental spinal cord injury in rats. Spinal cord trauma was produced by introducing an inflatable balloon in the dorsal subdural space. Up...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/1520-6017(200101)90:1<70::aid-jps8>3.0.co;

    authors: Hoizey G,Kaltenbach ML,Dukic S,Lamiable D,Lallemand A,Millart H,D'Arbigny P,Vistelle R

    更新日期:2001-01-01 00:00:00

  • Particle shape: a new design parameter for passive targeting in splenotropic drug delivery.

    abstract::The role of particle size and surface modification on biodistribution of nanocarriers is widely reported. We report for the first time the role of nanoparticle shape on biodistribution. Our study demonstrates that irregular shaped polymer lipid nanoparticles (LIPOMER) evade kupffer cells and localize in the spleen. We...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22052

    authors: Devarajan PV,Jindal AB,Patil RR,Mulla F,Gaikwad RV,Samad A

    更新日期:2010-06-01 00:00:00

  • Influence of ambient moisture on the compaction behavior of microcrystalline cellulose powder undergoing uni-axial compression and roller-compaction: a comparative study using near-infrared spectroscopy.

    abstract::This study evaluates the effect of variation in the ambient moisture on the compaction behavior of microcrystalline cellulose (MCC) powder. The study was conducted by comparing the physico-mechanical properties of, and the near infrared (NIR) spectra collected on, compacts prepared by roller compaction with those coll...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20430

    authors: Gupta A,Peck GE,Miller RW,Morris KR

    更新日期:2005-10-01 00:00:00

  • Drying-induced variations in physico-chemical properties of amorphous pharmaceuticals and their impact on stability (I): stability of a monoclonal antibody.

    abstract::The present study was conducted to investigate the impact of drying method and formulation on the storage stability of IgG1. Formulations of IgG1 with varying levels of sucrose with and without surfactant were dried by different methods, namely freeze drying, spray drying, and foam drying. Dried powders were character...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20859

    authors: Abdul-Fattah AM,Truong-Le V,Yee L,Nguyen L,Kalonia DS,Cicerone MT,Pikal MJ

    更新日期:2007-08-01 00:00:00

  • New potent topical anti-inflammatory steroids with reduced side effects: derivatives of steroid-16-carboxy esters.

    abstract::Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790716

    authors: Heiman AS,Taraporewala IB,McLean HM,Hong D,Lee HJ

    更新日期:1990-07-01 00:00:00

  • Development of a Novel Lung Slice Methodology for Profiling of Inhaled Compounds.

    abstract::The challenge of defining the concentration of unbound drug at the lung target site after inhalation limits the possibility to optimize target exposure by compound design. In this study, a novel rat lung slice methodology has been developed and applied to study drug uptake in lung tissue, and the mechanisms by which t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24575

    authors: Bäckström E,Lundqvist A,Boger E,Svanberg P,Ewing P,Hammarlund-Udenaes M,Fridén M

    更新日期:2016-02-01 00:00:00

  • Kinetics and mechanism of the equilibrium reaction of triazolam in aqueous solution.

    abstract::The equilibrium kinetics of triazolam in aqueous solution was investigated in the pH range of 1-11 at body temperature. The quantitative study indicated that it forms equilibrium mixtures consisting of ring-opened and closed forms with the composition being dependent on pH. The equilibrium constants of the two species...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600711206

    authors: Konishi M,Hirai K,Mori Y

    更新日期:1982-12-01 00:00:00

  • Pilocarpine prodrugs. II. Synthesis, stability, bioconversion, and physicochemical properties of sequentially labile pilocarpine acid diesters.

    abstract::Various novel diesters of pilocarpic acid were synthesized and evaluated as prodrug forms for pilocarpine with the aim of improving the ocular delivery characteristics of the drug. The pilocarpic acid monoesters previously studied cyclized spontaneously to pilocarpine in aqueous solution and although they showed enhan...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600750811

    authors: Bundgaard H,Falch E,Larsen C,Mosher GL,Mikkelson TJ

    更新日期:1986-08-01 00:00:00

  • Isomeric benzoylpyrroleacetic acids: some structural aspects for aldose reductase inhibitory and anti-inflammatory activities.

    abstract::A number of isomeric benzoylpyrroleacetic acids (1-6) were prepared and tested in vitro for rat lenses aldose reductase activity. These pyrrole derivatives are structurally related to the acidic nonsteroidal anti-inflammatory drugs. Therefore, their anti-inflammatory properties were also evaluated in the carrageenan-i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840119

    authors: Demopoulos VJ,Rekka E

    更新日期:1995-01-01 00:00:00

  • Synthesis and evaluation of 3-halocyclophosphamides and analogous compounds as novel anticancer "pro-prodrugs".

    abstract::3-Fluoro-, 3-chloro-, and 3-bromocyclophosphamide were prepared from the reaction of trifluoromethylhypofluorite, sodium hypochlorite, and bromine with the anticancer drug cyclophosphamide. Treatment of cis- and trans-4-phenylcyclophosphamide and 5,6-benzocyclophosphamide with sodium hypochlorite afforded cis- and tra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720622

    authors: Zon G,Ludeman SM,Ozkan G,Chandrasegaran S,Hammer CF,Dickerson R,Mizuta K,Egan W

    更新日期:1983-06-01 00:00:00

  • Solubility and mass and nuclear magnetic resonance spectroscopic studies on interaction of cyclosporin A with dimethyl-alpha- and -beta-cyclodextrins in aqueous solution.

    abstract::The interaction of cyclosporin A (CsA) with dimethyl-alpha- and -beta-cyclodextrins (DM-alpha-CyD and DM-beta-CyD) was investigated by the solubility method, electrospray ionization mass spectrometry (ESI-MS) and 1H-nuclear magnetic resonance spectroscopy (1H NMR). The extremely low solubility (1.9 x 10(-5) M at 25 de...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980284+

    authors: Miyake K,Hirayama F,Uekama K

    更新日期:1999-01-01 00:00:00

  • Fluoride remineralization of demineralized bovine tooth enamel and hydroxyapatite pellets.

    abstract::Both bovine enamel and hydroxyapatite pellets were remineralized in a fluoride-containing remineralization solution after prior demineralization for various lengths of time. In both the enamel and pellet systems, the degree of remineralization attainable was directly related to the extent of prior demineralization, al...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700818

    authors: Yonese M,Fox JL,Nambu N,Hefferren JJ,Higuchi WI

    更新日期:1981-08-01 00:00:00

  • Prediction of the relaxation behavior of amorphous pharmaceutical compounds. I. Master curves concept and practice.

    abstract::Variability in the time to crystallization is a major technical and economic hurdle in using amorphous solids in dosage forms. It is hypothesized that amorphous solids "age", and that the older they are, the more relaxed they are and the higher the probability of crystallization. At present, there is no method that al...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10404

    authors: Hilden LR,Morris KR

    更新日期:2003-07-01 00:00:00

  • A procedure to optimize scale-up for the primary drying phase of lyophilization.

    abstract::This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21430

    authors: Kramer T,Kremer DM,Pikal MJ,Petre WJ,Shalaev EY,Gatlin LA

    更新日期:2009-01-01 00:00:00

  • High-performance liquid chromatographic assay of sulfapyridine and acetylsulfapyridine in biological fluids.

    abstract::A high-pressure liquid chromatographic method for the sensitive, rapid, and specific determination of sulfapyridine and its N-acetyl derivative in plasma and saliva was developed. A cyano-bonded, reversed-phase, high efficiency column was used. The system detected these sulfonamides in serum to 0.25 mg/liter and withi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670916

    authors: Owerbach J,Johnson NF,Bates TR,Pieniaszek HJ Jr,Jusko WJ

    更新日期:1978-09-01 00:00:00

  • Finding the Needle in the Haystack: High-Resolution Techniques for Characterization of Mixed Protein Particles Containing Shed Silicone Rubber Particles Generated During Pumping.

    abstract::During the manufacturing process of biopharmaceuticals, peristaltic pumps are employed at different stages for transferring and dosing of the final product. Commonly used silicone tubings are known for particle shedding from the inner tubing surface due to friction in the pump head. These nanometer sized silicone rubb...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.12.002

    authors: Deiringer N,Haase C,Wieland K,Zahler S,Haisch C,Friess W

    更新日期:2020-12-09 00:00:00

  • Thermochemical investigations of associated solutions: calculation of solute--solvent equilibrium constants from solubility measurements.

    abstract::A simple solution model that has lead to successful predictive equations for the partial molar excess properties of a solute in simple binary solvent mixtures containing only nonspecific interactions is extended to include association between the solute and one of the solvent components. An expression is derived and t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720822

    authors: Acree WE Jr,McHan DR,Rytting JH

    更新日期:1983-08-01 00:00:00

  • Preparation of liposomes encapsulating water-soluble compounds using supercritical carbon dioxide.

    abstract::In this paper the development of a new preparation method of liposomes containing a water soluble marker (fluorescein isothiocyanate-dextran (FITC-dextran) or zinc phthalocyanine tetrasulfonic acid (TSZnPc) using supercritical carbon dioxide (called "the supercritical liposome method") is described. The apparatus used...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js960403q

    authors: Frederiksen L,Anton K,van Hoogevest P,Keller HR,Leuenberger H

    更新日期:1997-08-01 00:00:00

  • Comparison of granule strength and tablet tensile strength.

    abstract::The granule strength (crushing load) of lactose granulated with 1-9% povidone was measured initially and at intervals during a 1-year period. The granule strengths of dibasic calcium phosphate dihydrate granulated with various concentrations of starch and povidone were measured. The axial and radial tensile strengths ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720513

    authors: Jarosz PJ,Parrott EL

    更新日期:1983-05-01 00:00:00

  • Finite dose pharmacokinetics of skin penetration.

    abstract::A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600741018

    authors: Cooper ER,Berner B

    更新日期:1985-10-01 00:00:00

  • Preparation and characterization of the micelle-forming polymeric drug indomethacin-incorporated poly(ethylene oxide)-poly(beta-benzyl L-aspartate) block copolymer micelles.

    abstract::To estimate the feasibility of novel containers for drugs, poly(ethylene oxide)-poly(beta-benzyl L-aspartate) (PEO-PBLA) micelles were prepared by dialysis against water using different solvents. The solvent selected is very important because it drastically affects the stability of polymeric micelles. The critical mic...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js950204r

    authors: La SB,Okano T,Kataoka K

    更新日期:1996-01-01 00:00:00

  • Time-dependent changes in the activation of RhoA/ROCK and ERM/p-ERM in the increased expression of intestinal P-glycoprotein by repeated oral treatment with etoposide.

    abstract::Previously, we reported that repeated oral treatment with etoposide (ETP) increased ileal membrane localization of P-glycoprotein (P-gp) and that this was possibly mediated by increased expression of the ezrin/radixin/moesin (ERM)/phosphorylated ERM (p-ERM) via activation of RhoA/ROCK. These changes caused decreases i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23503

    authors: Kobori T,Harada S,Nakamoto K,Tokuyama S

    更新日期:2013-05-01 00:00:00