Impact of blend properties on die filling during tableting.

Abstract:

:Based on characterization of a wide range of fillers and APIs, thirty divergent blends were composed and subsequently compressed on a rotary tablet press, varying paddle speed and turret speed. The tablet weight variability was determined of 20 grab samples consisting of each 20 tablets. Additionally, the bulk residence time, ejection force, pre-compression displacement, main compression force, die fill fraction and feed frame fill fraction were determined during each run. Multivariate data analysis was applied to investigate the relation between the process parameters, blend characteristics, product and process responses. Blends with metoprolol tartrate as API showed high ejection forces. This behavior could be linked to the high wall friction value of metoprolol tartrate. The main responses related to the die filling could be predicted via a PLS model based on blend characteristics. Tablet weight variability was highly correlated with the variability on pre-compression displacement and main compression force. A good predictive model for tablet weight variability was obtained taking the porosity, wall friction angle, flowability, density, compressibility and permeability into account. Additionally, turret speed and paddle speed were included in the calibration of the model. The applied approach can save resources (material, time) during early drug product development.

journal_name

Int J Pharm

authors

Van Snick B,Grymonpré W,Dhondt J,Pandelaere K,Di Pretoro G,Remon JP,De Beer T,Vervaet C,Vanhoorne V

doi

10.1016/j.ijpharm.2018.08.015

subject

Has Abstract

pub_date

2018-10-05 00:00:00

pages

476-488

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(18)30575-1

journal_volume

549

pub_type

杂志文章
  • Controlled release from hydrogel-based solid matrices. A model accounting for water up-take, swelling and erosion.

    abstract::Design and realization of drug delivery systems based on polymer matrices could be greatly improved by modeling the phenomena which take place after the systems administration. Availability of a reliable mathematical model, able to predict the release kinetic from drug delivery systems, could actually replace the reso...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.01.023

    authors: Lamberti G,Galdi I,Barba AA

    更新日期:2011-04-04 00:00:00

  • Development of a controlled release formulation based on SLN and NLC for topical clotrimazole delivery.

    abstract::Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) are colloidal carrier systems providing controlled release profiles for many substances. Clotrimazole-loaded SLN and NLC were prepared by the hot high pressure homogenization technique in order to evaluate the physical stability of these particles...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.02.032

    authors: Souto EB,Wissing SA,Barbosa CM,Müller RH

    更新日期:2004-06-18 00:00:00

  • Synthesis, characterization, in vitro and in vivo evaluation of PEGylated oridonin conjugates.

    abstract::Oridonin (ORI), a diterpenoid compound with promising antitumor activity, was proved to possess potent antileukemia efficacies in vitro and in vivo recently. However, the development and application of ORI was limited by its poor solubility and rapid plasma clearance. The purpose of this study was to solve these probl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.08.014

    authors: Shen J,Zhang D,Zhao Z,Jia L,Zheng D,Liu G,Hao L,Zhang Q,Tian X,Li C,Guo H

    更新日期:2013-11-01 00:00:00

  • Formulation parameters governing sustained protein delivery from degradable viscous liquid aliphatic polycarbonates.

    abstract::Viscous liquid degradable polymers have advantages as drug depots for sustained protein delivery. We have created a new aliphatic polycarbonate for this purpose, poly(trimethylene carbonate-co-5-hydroxy trimethylene carbonate), which upon degradation retains a near neutral micro-environmental pH. As such, this copolym...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119965

    authors: Mohajeri S,Burke-Kleinman J,Maurice DH,Amsden BG

    更新日期:2020-11-30 00:00:00

  • In vitro and in vivo evaluation of mucoadhesive microspheres consisting of dextran derivatives and cellulose acetate butyrate.

    abstract::The objective of this study was to evaluate mucoadhesive properties and gastrointestinal transit of microspheres made of oppositely charged dextran derivatives and cellulose acetate butyrate (CAB). The microspheres were prepared by emulsion solvent evaporation method. A reference microsphere was made of lactose instea...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(03)00159-5

    authors: Miyazaki Y,Ogihara K,Yakou S,Nagai T,Takayama K

    更新日期:2003-06-04 00:00:00

  • Influence of methyl-beta-cyclodextrin and liposomes on rheological properties of Carbopol 974P NF gels.

    abstract::The influence of positively-charged and sterically stabilized liposomes and/or methyl-beta-cyclodextrin on rheological properties of Carbopol 974P NF hydrogels was investigated. All formulations have displayed a shear-thinning behavior of Carbopol gels, and the rate stress as a function of the shear rate was fitted us...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00683-x

    authors: Boulmedarat L,Grossiord JL,Fattal E,Bochot A

    更新日期:2003-03-18 00:00:00

  • 1H NMR quantification of spray dried and spray freeze-dried saccharide carriers in dry powder inhaler formulations.

    abstract::Quantitative analysis using proton NMR (1H qNMR) has been employed in various areas such as pharmaceutical analysis (e.g., dissolution study), vaccines, natural products analysis, metabolites, and macrolide antibiotics in agriculture industry. However, it is not routinely used in the quantification of saccharides in d...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.03.030

    authors: Babenko M,Peron JR,Kaialy W,Calabrese G,Alany RG,ElShaer A

    更新日期:2019-06-10 00:00:00

  • A novel treatment strategy for preterm birth: Intra-vaginal progesterone-loaded fibrous patches.

    abstract::Progesterone-loaded poly(lactic) acid fibrous polymeric patches were produced using electrospinning and pressurized gyration for intra-vaginal application to prevent preterm birth. The patches were intravaginally inserted into rats in the final week of their pregnancy, equivalent to the third trimester of human pregna...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119782

    authors: Cam ME,Hazar-Yavuz AN,Cesur S,Ozkan O,Alenezi H,Turkoglu Sasmazel H,Sayip Eroglu M,Brako F,Ahmed J,Kabasakal L,Ren G,Gunduz O,Edirisinghe M

    更新日期:2020-10-15 00:00:00

  • Simultaneous determination of amiloride and furosemide in pharmaceutical formulations by first digital derivative spectrophotometry.

    abstract::This work presents a simple and fast method for the simultaneous determination of amiloride and furosemide by digital derivative spectrophotometry. HCl 1 x 10(-2) mol/l dissolved in ethanol was used as solvent and to extract drugs from formulations. Subsequently the samples were evaluated directly by first digital der...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00482-9

    authors: Inés Toral M,Pope S,Quintanilla S,Richter P

    更新日期:2002-12-05 00:00:00

  • Interactions between a poorly soluble cationic drug and sodium dodecyl sulfate in dissolution medium and their impact on in vitro dissolution behavior.

    abstract::In the pharmaceutical industry, in vitro dissolution testing ofsolid oral dosage forms is a very important tool for drug development and quality control. However, ion-pairing interaction between the ionic drugand surfactants in dissolution medium often occurs, resulting in inconsistent and incomplete drug release. The...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.10.063

    authors: Huang Z,Parikh S,Fish WP

    更新日期:2018-01-15 00:00:00

  • Antioxidant activity of gamma-oryzanol: mechanism of action and its effect on oxidative stability of pharmaceutical oils.

    abstract::Gamma-oryzanol, a phytosteryl ferulate mixture extracted from rice bran oil, has a wide spectrum of biological activities; in particular, it has antioxidant properties and is often used in cosmetic formulations as a sunscreen. The first objective of the present investigation was to elucidate the molecular mechanism(s)...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.05.018

    authors: Juliano C,Cossu M,Alamanni MC,Piu L

    更新日期:2005-08-11 00:00:00

  • Controlled release injectable liposomal gel of ibuprofen for epidural analgesia.

    abstract::The epidural administration is used commonly in the treatment of pain. Nonsteroidal anti-inflammatory drugs, especially ibuprofen, would have potential in epidural use. Like many epidurally useful drugs it, however, has a short duration of action, which is a limiting factor. To improve epidural pain treatment, a long-...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(00)00376-8

    authors: Paavola A,Kilpeläinen I,Yliruusi J,Rosenberg P

    更新日期:2000-04-10 00:00:00

  • Controlled-release implant system formulated using biodegradable hemostatic gauze as scaffold.

    abstract::A unique polymer-based sustained-release implant was formulated using biodegradable hemostatic gauze as the scaffold. A piece of commercial gauze, Surgicel was coated with a poly(lactic-co-glycolic) acid (PLGA) solution in which drugs were loaded, followed by evaporating the solvent. Drug release kinetics from the PLG...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.12.019

    authors: Xu L,Wu F,Yuan W,Jin T

    更新日期:2008-05-01 00:00:00

  • Measurement of residence time distributions and material tracking on three continuous manufacturing lines.

    abstract::Over the recent decade, benefits of continuous manufacturing (CM) of pharmaceutical products have been acknowledged widely. In contrast to batch processes, the product is not physically separated into batches in CM, which creates a few challenges. Product release is done for batches that should have a uniform quality ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.03.058

    authors: Karttunen AP,Hörmann TR,De Leersnyder F,Ketolainen J,De Beer T,Hsiao WK,Korhonen O

    更新日期:2019-05-30 00:00:00

  • Secondary structure alterations in insulin and growth hormone water-in-oil emulsions.

    abstract::Water-in-oil (w/o) emulsions have shown a promising release profile of small drug molecules and proteins. However, the major concerns are the structural stability, the retention of the activity and to avoid unwanted immunological reactions caused by the changes in protein structure. In the present study, the secondary...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00668-3

    authors: Jørgensen L,Vermehren C,Bjerregaard S,Froekjaer S

    更新日期:2003-03-18 00:00:00

  • Use of ultrasound to prepare lipid emulsions of lorazepam for intravenous injection.

    abstract::Lipid emulsions can be used as a vehicle for the production of low-volume injectable preparations with minimally water-soluble active ingredients. First, we focus on the galenic and technological conditions established by ultrasound techniques. A 2(5) factorial design was used to optimize the carrier emulsion. The stu...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(00)00664-5

    authors: Medina J,Salvadó A,del Pozo A

    更新日期:2001-03-23 00:00:00

  • Thermal dose as a universal tool to evaluate nanoparticle-induced photothermal therapy.

    abstract::Thermal isoeffect dose (TID) is a widely applied concept to evaluate the safety of medical devices that can expose patients to heat. However, it has rarely been used in photothermal therapy (PTT), where nanoparticles are used as light absorbers. Utilizing TID in an appropriate way would make it feasible to compare the...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119657

    authors: Happonen E,Tamarov K,Martikainen MV,Ketola K,Roponen M,Lehto VP,Xu W

    更新日期:2020-09-25 00:00:00

  • Determination of acetaminophen's solubility in poly(ethylene oxide) by rheological, thermal and microscopic methods.

    abstract::A drug's solubility in a polymeric excipient is an important parameter that dictates the process window of hot-melt extrusion (HME) and product stability during storage. However, it is rather challenging to experimentally determine the solubility and there is very few published work in this field. In this study, the s...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.10.026

    authors: Yang M,Wang P,Suwardie H,Gogos C

    更新日期:2011-01-17 00:00:00

  • Effect of preparation technique on the properties of liposomes encapsulating ketoprofen-cyclodextrin complexes aimed for transdermal delivery.

    abstract::The combined approach of cyclodextrin complexation and entrapment in liposomes was investigated in order to develop an effective topical formulation of ketoprofen. Equimolar complex of drug and hydroxypropyl-beta-cyclodextrin (HPbetaCyd) was added at different concentrations to the aqueous phase of liposomes consistin...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.12.047

    authors: Maestrelli F,González-Rodríguez ML,Rabasco AM,Mura P

    更新日期:2006-04-07 00:00:00

  • Effect of medium-chain triglycerides on the release behavior of Endostar encapsulated PLGA microspheres.

    abstract::The incomplete release of Endostar from PLGA microspheres was observed in our previous study. In the present study, we focused on the effect of medium-chain triglycerides (MCT) on the in vitro/in vivo release behavior of Endostar encapsulated PLGA microspheres, which were prepared by a water-in-oil-in-water (W/O/W) do...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.07.018

    authors: Meng B,Li L,Hua S,Wang Q,Liu C,Xu X,Yin X

    更新日期:2010-09-15 00:00:00

  • Chitosan/o-carboxymethyl chitosan nanoparticles for efficient and safe oral anticancer drug delivery: in vitro and in vivo evaluation.

    abstract::The present study investigated the ability of a polyelectrolyte complex (CS/CMCS-NPs), composed of chitosan (CS) and o-carboxymeymethy chitosan (CMCS) as a pH responsive carrier for oral delivery of doxorubicin hydrochloride (DOX). The obtained CS/CMCS-NPs were characterized for various parameters including morphology...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.07.079

    authors: Feng C,Wang Z,Jiang C,Kong M,Zhou X,Li Y,Cheng X,Chen X

    更新日期:2013-11-30 00:00:00

  • Solid dispersion of acetaminophen and poly(ethylene oxide) prepared by hot-melt mixing.

    abstract::In this study, a model drug, acetaminophen (APAP), was melt mixed with poly(ethylene oxide) (PEO) using a Brabender mixer. APAP was found to recrystallize upon cooling to room temperature for all the drug loadings investigated. Higher drug loading leads to faster recrystallization rate. However, the morphology of the ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.04.033

    authors: Yang M,Wang P,Huang CY,Ku MS,Liu H,Gogos C

    更新日期:2010-08-16 00:00:00

  • BCNU-loaded poly(D, L-lactide-co-glycolide) wafer and antitumor activity against XF-498 human CNS tumor cells in vitro.

    abstract::Implantable polymeric device that can release chemotherapeutic agent directly into central nervous system (CNS) has had an impact on malignant glioma therapy. The purpose of our study was to develop an implantable polymeric device, which can release intact 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) for long-term peri...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00543-4

    authors: Seong H,An TK,Khang G,Choi SU,Lee CO,Lee HB

    更新日期:2003-01-30 00:00:00

  • Amino Acid-functionalized hollow mesoporous silica nanospheres as efficient biocompatible drug carriers for anticancer applications.

    abstract::Herein, a series of new amino acid-functionalized hollow mesoporous silica nanospheres (HMSNs) by post-grafting methods were prepared. These new materials were characterized by different techniques and were studied as matrices for the antineoplastic drug (cisplatin) transport and delivery. The results demonstrate that...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118709

    authors: Ezzati N,Mahjoub AR,Abolhosseini Shahrnoy A,Syrgiannis Z

    更新日期:2019-12-15 00:00:00

  • An in vitro kinetic method for detection of precipitation of poorly soluble drugs.

    abstract::A simple in vitro method for the detection of precipitation using 96-well microplates and a SpectraMax Plus microtiter plate reader has been developed and described. The method requires only small amount of drug and is, therefore, potentially applicable in early pre-formulation. The method is based on opacity changes ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.08.012

    authors: Wu Z,Tucker IG,Razzak M,Medlicott NJ

    更新日期:2005-11-04 00:00:00

  • Characterization and monitoring of pseudo-polymorphs in manufacturing process by NIR.

    abstract::Moisture-sensitive pseudo-polymorphs with different stabilities were characterized, and their polymorphisms were monitored in the process of tableting and film coating by near-infrared (NIR) spectroscopy. In this study, we proved that we could successfully maintain the crystal form ratio in the tablet by controlling t...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.10.010

    authors: Kamada K,Yoshimura S,Murata M,Murata H,Nagai H,Ushio H,Terada K

    更新日期:2009-02-23 00:00:00

  • Effects of carriers and storage of formulation on the lung deposition of a hydrophobic and hydrophilic drug from a DPI.

    abstract::The effects of carriers, the drug:carrier ratio and a 1 month storage period of a formulation in permeable polystyrene tube at 40 degrees C/75% RH on the in vitro pulmonary deposition of model drugs from dry powder inhaler (DPI) were evaluated. Budesonide (hydrophobic) and salbutamol sulphate (hydrophilic) were used a...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(03)00357-0

    authors: Harjunen P,Lankinen T,Salonen H,Lehto VP,Järvinen K

    更新日期:2003-09-16 00:00:00

  • Partially hydrolyzed polyvinyl alcohol for fusion-based pharmaceutical formulation processes: Evaluation of suitable plasticizers.

    abstract::The present study evaluates the effect of several pharmaceutical plasticizers on the thermo-physical and physicochemical properties of partially hydrolyzed poly(vinyl alcohol) (PVA) used in fusion-based pharmaceutical formulation processes. Specifically, the effect of mannitol (MAN), sorbitol (SOR), sucrose (SUC), anh...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119121

    authors: Katopodis K,Kapourani A,Vardaka E,Karagianni A,Chorianopoulou C,Kontogiannopoulos KN,Bikiaris DN,Kachrimanis K,Barmpalexis P

    更新日期:2020-03-30 00:00:00

  • Evaluation of in vitro percutaneous absorption of lorazepam and clonazepam from hydro-alcoholic gel formulations.

    abstract::Clonazepam and lorazepam are two anxiolytics, antidepressant agents, having suitable features for transdermal delivery. The objectives of this study were to evaluate the in vitro percutaneous absorption of these drugs through excised human skin (stratum corneum and epidermis, SCE) and to determine their in vitro perme...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(01)00806-7

    authors: Puglia C,Bonina F,Trapani G,Franco M,Ricci M

    更新日期:2001-10-09 00:00:00

  • Formulation of self-microemulsifying drug delivery system (SMEDDS) by D-optimal mixture design to enhance the oral bioavailability of a new cathepsin K inhibitor (HL235).

    abstract::HL235 is a new cathepsin K inhibitor designed and synthesized to treat osteoporosis. Since HL235 has poor aqueous solubility, a self-microemulsifying drug delivery system (SMEDDS) was formulated to enhance its oral bioavailability. A solubility study of HL235 was performed to select a suitable oil, surfactant and cosu...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118772

    authors: Visetvichaporn V,Kim KH,Jung K,Cho YS,Kim DD

    更新日期:2020-01-05 00:00:00