QbD approach to downstream processing of spray-dried amorphous solid dispersions - a case study.

Abstract:

:In the current study, we demonstrate a structured approach to downstream process development for spray dried amorphous solid dispersions. Direct compression is generally not suitable due to typically poor flow of spray dried powders in tablets. Roller compaction (RC) is therefore the method of choice to enable spray dried dispersion downstream processing. Here, a structured experimental design of RC process parameters was used. The objective was to identify process conditions that lead to improved powder flow without compromising tablet robustness. Ten blends were compacted using different process parameters, and subsequently compressed into tablets. The impact of process parameters on granules and tablet properties was analyzed. We demonstrate that compaction force, gap and mesh aperture have major impact on RC outcomes. A combination of large gap and low force was identified as optimum combination of RC process parameters leading to powder flow improvement that could guarantee low tablet weight variation and at the same prevented loss of blend compressibility.

journal_name

Pharm Dev Technol

authors

Henriques J,Moreira J,Doktorovová S

doi

10.1080/10837450.2020.1863985

subject

Has Abstract

pub_date

2021-01-04 00:00:00

pages

1-9

eissn

1083-7450

issn

1097-9867

pub_type

杂志文章
  • The impact of solid-state form, water content and surface area of magnesium stearate on lubrication efficiency, tabletability, and dissolution.

    abstract::Magnesium stearate (MgSt) is a widely used pharmaceutical lubricant in tablet manufacturing. However, batch-to-batch variability in hydrate form and surface area can lead to inconsistency in tablet performance. In this work, several unique MgSt samples were studied: traditional monohydrate samples with high surface ar...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1839763

    authors: Calahan JL,Paul S,Yanez EG,DeNeve D,Sun CC,Munson EJ

    更新日期:2021-02-01 00:00:00

  • Effect of sample preparation method on quantification of polymorphs using PXRD.

    abstract::The purpose of this study was to improve the sensitivity and accuracy of quantitative analysis of polymorphic mixtures. Various techniques such as hand grinding and mixing (in mortar and pestle), air jet milling and ball milling for micronization of particle and mixing were used to prepare binary mixtures. Using these...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903286511

    authors: Alam S,Patel S,Bansal AK

    更新日期:2010-09-01 00:00:00

  • Development of a small-scale spray-drying approach for amorphous solid dispersions (ASDs) screening in early drug development.

    abstract::The present study details the development of a small-scale spray-drying approach for the routine screening of amorphous solid dispersions (ASDs). This strategy aims to overcome the limitations of standard screening methodologies like solvent casting and quench cooling to predict drug-polymer miscibility of spray-dried...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1534861

    authors: Ousset A,Bassand C,Chavez PF,Meeus J,Robin F,Schubert MA,Somville P,Dodou K

    更新日期:2019-06-01 00:00:00

  • Waxy corn starch: a potent cofiller in pellets produced by extrusion-spheronization.

    abstract::The purpose of this study was to assess the usefulness of waxy corn (maize) starch as a cofiller and diluent in pellets produced by aqueous extrusion-spheronization. Waxy corn starch was combined with microcrystalline cellulose (MCC) in the range of 20-50% of the entire composition. Pellets containing ordinary corn st...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100100521

    authors: Junnila R,Palviainen P,Heinämäki J,Myllärinen P,Forssell P,Yliruusi J

    更新日期:2000-01-01 00:00:00

  • Identification of physical-chemical variables affecting particle size following precipitation using a supercritical fluid.

    abstract::The physical-chemical processing variables affecting particle size following precipitation using the supercritical antisolvent (SAS) method were investigated by varying both the composition of the feed solvent and the structure of the solute, using a series of steroids. The key factor influencing particle size in thes...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450600561299

    authors: Sacha GA,Schmitt WJ,Nail SL

    更新日期:2006-01-01 00:00:00

  • The absorption of (99m)Tc-alendronate given by rectal route in rabbits.

    abstract::Alendronate sodium (ALD) is a bisphosphonate medication used in the treatment and prevention of osteoporosis. Absorption of ALD as oral formulation is very poor (0.5%-1%). Its bioavailability can decrease with food effect. It has some gastrointestinal adverse effects such as gastritis, gastric ulcer, and esophagitis. ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450801949509

    authors: Asikoğlu M,Ozguney I,Ozcan I,Orumlu O,Guneri T,Koseoğlu K,Ozkilic H

    更新日期:2008-01-01 00:00:00

  • About the equivalence between different batches of a glycopeptide drug.

    abstract:CONTEXT:Teicoplanin is a glycopeptide antibiotic consisting of a combination of different active components. Clinical equivalence between different batches of this drug is not guaranteed by the present pharmacopeial specification of chemical composition based on an HPLC chromatogram. OBJECTIVE:To test a modification o...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1035726

    authors: Boix-Montañes A,Garcia-Arieta A

    更新日期:2016-08-01 00:00:00

  • The solution, solid state stability and kinetic investigation in degradation studies of lercanidipine: study of excipients compatibility of lercanidipine.

    abstract::The objectives of this research were to evaluate the stability of lercanidipine in solution state and solid state and explore the compatibility of drug with oils, surfactants and cosurfactants as excipients. The effect of pH on the degradation in solution state was studied through pH-rate profile of lercanidipine in c...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2011.580758

    authors: Parmar N,Amin S,Singla N,Kohli K

    更新日期:2012-11-01 00:00:00

  • Estimation of initial dissolution rate of drug substance by thermal analysis: application for carbamazepine hydrate.

    abstract::We have proposed a theory indicating the correlation between the dissolution rate and the heat of solution of drug substances. The initial dissolution rates of the drug substances containing amorphous were predicted accurately from their heats of solution. In this report, the possibility for the theory to estimate the...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120002234

    authors: Yoshihashi Y,Yonemochi E,Terada K

    更新日期:2002-01-01 00:00:00

  • "Prevention of structural perturbation and aggregation of hepatitis B surface antigen: screening of various additives".

    abstract::The instability of protein and antigen(s) during encapsulation in biodegradable polymers by water-in-oil-in-water (w/o/w) encapsulation is well established. The aim of present study is to screen various additives to prevent the inactivation and loss of immunogenicity of HBsAg upon its exposure to the water/CH(2)Cl(2) ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.546408

    authors: Tomar P,Giri N,Karwasara VS,Pandey RS,Dixit VK

    更新日期:2012-07-01 00:00:00

  • Drug-polymer mixed coating: a new approach for controlling drug release rates in pellets.

    abstract::A new approach to developing a drug-polymer mixed coat for highly water-soluble diltiazem pellets was investigated at different coating levels. Drug layering and the coating procedures were performed using a bottom spray fluidized bed coater. Drug pellets were coated with Eudragit NE40 (NE40) alone and in combination ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450500464008

    authors: Nisar ur Rahman,Yuen KH,Khan NA,Wong JW

    更新日期:2006-02-01 00:00:00

  • A novel approach to increase oral drug absorption.

    abstract::A comprehensive analytical solution that accounts for many factors and assumptions affecting drug concentration profile in the gastrointestinal tract was presented. A sensitivity analysis approach was utilized in order to investigate the importance of different parameters in the model. The partition coefficient is fou...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100000741

    authors: Idkaidek NM,Abdel-Jabbar N

    更新日期:2001-01-01 00:00:00

  • Improvement of solubility and oral bioavailability of rutin by complexation with 2-hydroxypropyl-beta-cyclodextrin.

    abstract::The object of this study was to enhance the solubility, dissolution rate, and oral bioavailability of rutin by complexation with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD). The interaction of rutin with cyclodextrins (CyDs) was evaluated by the solubility, and ultraviolet (UV) and circular dichroism (CD) spectrop...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100100556

    authors: Miyake K,Arima H,Hirayama F,Yamamoto M,Horikawa T,Sumiyoshi H,Noda S,Uekama K

    更新日期:2000-01-01 00:00:00

  • The prediction of variability occurring in fluidized bed coating equipment. I. The measurement of particle circulation rates in a bottom-spray fluidized bed coater.

    abstract::The purpose of this work was to investigate the effect that changes in design and process variables had on the movement of particles around a fluidized bed coating apparatus. To measure the mean and variance of the particle cycle time distribution (CTD), the number of passages taken by a magnetic tracer particle throu...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100100546

    authors: Cheng XX,Turton R

    更新日期:2000-01-01 00:00:00

  • Use of scoring to induce reproducible drug delivery from osmotic pulsatile tablets.

    abstract::An osmotic-controlled pulsatile delivery technology was developed for targeted drug delivery. This novel system consists of a tablet core surrounded by an osmotic coating that has been mechanically compromised in strategic locations to facilitate reliable drug release at a given time point after administration. The ta...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450902838692

    authors: Rahemba TR,Bell S,Connolly EK,Waterman KC

    更新日期:2009-01-01 00:00:00

  • Spray coating of foley urinary catheter by chlorhexidine-loadedpoly(ε-caprolactone) nanospheres: effect of lyoprotectants, characteristics, and antibacterial activity evaluation.

    abstract::In this study, chlorhexidine-loaded poly(ε-caprolactone) nanospheres (CHX-NS) were prepared and successfully coated on the urinary catheters. Properties of CHX-NS were evaluated including drug loading content and the nanosphere size. Effects of different lyoprotectants for long-term storage of CHX-NS were also investi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1502317

    authors: Srisang S,Nasongkla N

    更新日期:2019-04-01 00:00:00

  • The effect of composition on the tableting indices of binary powder mixtures.

    abstract::The purpose of this study was to investigate the effect of the composition of a binary powder mixture on the bonding index, the brittle fracture index, and the strain index, as defined by Hiestand. The studies involved tensile strength and dynamic indentation hardness determinations of square compacts, the solid fract...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459709022630

    authors: Majuru S,Wurster DE

    更新日期:1997-11-01 00:00:00

  • Transdermal delivery of diclofenac using water-in-oil microemulsion: formulation and mechanistic approach of drug skin permeation.

    abstract::The objective of the present investigation was to enhance skin permeation of diclofenac using water-in-oil microemulsion and to elucidate its skin permeation mechanism. The w/o microemulsion formulations were selected based on constructed pseudoternary phase diagrams depending on water solubilization capacity and ther...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.788658

    authors: Thakkar PJ,Madan P,Lin S

    更新日期:2014-05-01 00:00:00

  • Relating formulation variables to in vitro dissolution using an artificial neural network.

    abstract::The purpose of this paper was to investigate the effect of several experimental variables on the ability of a neural network to predict in vitro dissolution rate as a function of product formulation changes. Neural network software was trained with sets of hypothetical and experimental data consisting of 4-15 formulat...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459709031442

    authors: Ebube NK,McCall T,Chen Y,Meyer MC

    更新日期:1997-08-01 00:00:00

  • Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs.

    abstract::The main purpose of this work was to develop a supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) of carbamazepine (CBZ). S-SMEDDS of CBZ was prepared and drug precipitation behavior, dissolution rate in vitro and particle size distribution were evaluated. The relative bioavailability of S-SMEDDS f...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837451003774419

    authors: Zhang N,Zhang W,Jin Y,Quan DQ

    更新日期:2011-08-01 00:00:00

  • Novel microemulsion-based gel formulation of tazarotene for therapy of acne.

    abstract::The objective of this study was to develop and evaluate a novel microemulsion based gel formulation containing tazarotene for targeted topical therapy of acne. Psudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and co-surfactant for microemulsion formation. The optimized...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1081610

    authors: Patel MR,Patel RB,Parikh JR,Patel BG

    更新日期:2016-12-01 00:00:00

  • Influence of the type of vegetable oil on the drug release profile from lipid-core nanocapsules and in vivo genotoxicity study.

    abstract::The use of rice bran (RB), soybean (SB) or sunflower seed (SF) oils to prepare lipid-core nanocapsules (LNCs) as controlled drug delivery systems was investigated. LNCs were prepared by interfacial deposition using the preformed polymer method. All formulations showed negative zeta potential and adequate nanotechnolog...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.829097

    authors: Rigo LA,Frescura V,Fiel L,Coradini K,Ourique AF,Emanuelli T,Quatrin A,Tedesco S,Silva CB,Guterres SS,Pohlmann AR,Beck RC

    更新日期:2014-11-01 00:00:00

  • Understanding the mechanism for paradoxical effect of ionized and unionized chitosan: Orodispersible tablets of Ondansetron Hydrochloride.

    abstract::The objective of the present investigation was to formulate and evaluate orodispersible tablets (ODTs) of ondansetron HCl possessing sufficient mechanical strength by wet granulation or direct compression method. A combination of glycine and chitosan was employed for providing a sweet tasting disintegrating system. Th...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450902749279

    authors: Goel H,Vora N,Tiwary AK,Rana V

    更新日期:2009-01-01 00:00:00

  • Formulation, development, and in-vitro/ex-vivo evaluation of vaginal bioadhesive salbutamol sulfate tablets for preterm labor.

    abstract::Preterm labor is the main cause of death and serious illness of both infants and pregnant women in Africa and worldwide. Parenteral and oral salbutamol sulfate as a B2 antagonist has been used for the treatment of preterm labor. The study aims are to formulate salbutamol sulfate non-invasive vaginal bioadhesive tablet...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1767129

    authors: El-Enin ASMA,Elbakry AM,Hosary RE,Lotfy MAF

    更新日期:2020-10-01 00:00:00

  • Silk fibroin nanoparticles for enhanced bio-macromolecule delivery to the retina.

    abstract::The aim of this study was to investigate intravitreal injection of silk fibroin nanoparticles (SFNs) encapsulating bio-macromolecules, achieving enhanced drug bioavailability, and extended retention in retina. SFNs were prepared with regenerated silk fibroin using desolvation method with fluorescein isothiocyanate lab...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1545236

    authors: Yang P,Dong Y,Huang D,Zhu C,Liu H,Pan X,Wu C

    更新日期:2019-06-01 00:00:00

  • Evaluation of co-processed excipients used for direct compression of orally disintegrating tablets (ODT) using novel disintegration apparatus.

    abstract::The compendial method of evaluation of orodispersible tablets (ODT) is the same disintegration test as for conventional tablets. Since it does not reflect the disintegration process in the oral cavity, alternative methods are proposed that are more related to in vivo conditions, e.g. modified dissolution paddle appara...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2012.710238

    authors: Brniak W,Jachowicz R,Krupa A,Skorka T,Niwinski K

    更新日期:2013-03-01 00:00:00

  • Characterization of acid modified Dioscorea starches as direct compression excipient.

    abstract::Starches obtained from four different Dioscorea species namely White (D. rotundata), Bitter (D. dumetorum), Chinese (D. oppositifolia) and Water yam (D. alata), were modified by acid hydrolysis and the physicochemical, material and tablet formation properties of the starches were investigated with the aim of determini...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802572367

    authors: Odeku OA,Picker-Freyer KM

    更新日期:2009-01-01 00:00:00

  • Development of a novel physico-chemically and microbiologically stable oral solution of flecainide for pediatrics.

    abstract::There is as yet no commercialized preparation for oral administration of flecainide acetate (FA) to children. In such cases, manipulation of commercial tablets is the usual practice in pharmacy services of hospitals and compounding pharmacies, to provide a suitable dosage form for this vulnerable pediatric population ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2016.1238484

    authors: Santoveña A,Charola I,Suárez-González J,Teigell-Pérez N,García-van Nood S,Soriano M,Fariña JB

    更新日期:2018-12-01 00:00:00

  • Starch-quercetin conjugate by radical grafting: synthesis and biological characterization.

    abstract::A novel flavonoid-polysaccharide conjugate was synthesized by free radical grafting of quercetin on starch. The covalent insertion of quercetin in the polymeric chain was confirmed by FT-IR, DSC and fluorescence analyses, while an estimation of the amount of quercetin bound per g of polymer was obtained by the Folin-C...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.546413

    authors: Cirillo G,Puoci F,Iemma F,Curcio M,Parisi OI,Spizzirri UG,Altimari I,Picci N

    更新日期:2012-07-01 00:00:00

  • Dynamic rheology as a quantitative method for real-time tracking of excipient solvation in non-aqueous hydroxypropylcellulose topical gels.

    abstract::This article describes a method to quantitatively track the solvation of HPC in a non-aqueous solvent system during topical gel manufacture. Where visual observation and microscopy could not establish a trend, straight-forward rheological profiling demonstrated a correlation between increased solvation of hydroxypropy...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1502319

    authors: Potuck A,Leming R,Lam S

    更新日期:2019-04-01 00:00:00