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 solid dispersions (SDSDs) and therefore to guarantee appropriate carrier and drug-loading (DL) selection. A DoE approach was conducted to optimize process conditions of ProCept 4M8-TriX spray-drying to maximize the yield from a 100 mg batch of Itraconazole/HPMCAS-LF and Itraconazole/Soluplus 40:60 (w/w). Optimized process parameters include: inlet temperature, pump speed, drying and atomizing airflows. Identified process conditions derived from the DoE analysis were further (i) tested with Itraconazole, Naproxen and seven polymers, (ii) adapted for small cyclone use, (iii) downscaled to 20 mg batch production. Drug-polymer miscibility was systematically characterized using modulated differential scanning calorimetry (mDSC). Spray-drying was identified as a well-suited screening approach: mean yield of 10.1 to 40.6% and 51.1 to 81.0% were obtained for 20 and 100 mg ASD productions, respectively. Additionally, this work demonstrates the interest to move beyond conventional screening approaches and integrate spray-drying during screening phases so that a greater prediction accuracy in terms of SDSDs miscibility and performance can be obtained.

journal_name

Pharm Dev Technol

authors

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

doi

10.1080/10837450.2018.1534861

subject

Has Abstract

pub_date

2019-06-01 00:00:00

pages

560-574

issue

5

eissn

1083-7450

issn

1097-9867

journal_volume

24

pub_type

杂志文章
  • A measurement of the unstirred aqueous boundary layer in a Franz diffusion cell.

    abstract::The unstirred aqueous boundary layer (ABL) thickness was determined for modified Franz diffusion cells using three test compounds--parathion, 4-hexylresorcinol, and 2,4-dinitrochlorobenzene (DNCB). Steady-state fluxes through one, two, and three dialysis membranes in series were achieved in donor-saturated, infinite-d...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2011.572895

    authors: Miller MA,Kasting G

    更新日期:2012-11-01 00:00:00

  • Effect of solid state transition on the physical stability of suspensions containing bupivacaine lipid microparticles.

    abstract::Bupivacaine lipid microparticles were prepared and evaluated as a parenteral sustained-release dosage form for postoperative pain management. Bupivacaine free base was incorporated into a molten tristearin matrix and lipid micro-particles were subsequently formed from this molten mixture by a spray-congealing process....

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-54475

    authors: Li LC,Zhu L,Song JF,Deng JS,Bandopadhyay R,Wurster DE

    更新日期:2005-01-01 00:00:00

  • Development of an effective liposomal cholesterol ester transfer protein (CETP) vaccine for protecting against atherosclerosis in rabbit model.

    abstract::Clinical trials of cholesterol ester transfer protein (CETP) peptide vaccine were stopped after disappointing results in humans due to the inadequacy of adjuvant aluminum hydroxide in stimulating the immune response against the self-antigen of CETP. To increase the efficacy of the CETP vaccine, we developed a novel li...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1706181

    authors: Aghebati T,Arabsalmani M,Mohammadpour AH,Afshar M,Jaafari MR,Abnous K,Nazemi S,Badiee A

    更新日期:2020-04-01 00:00:00

  • Doxorubicin hydrochloride loaded nanotextured films as a novel drug delivery platform for ovarian cancer treatment.

    abstract::An approach for cancer treatment is modulation of tumor microenvironment. Based on the role of extracellular matrix in cell modulation, fabrication of textured materials mimicking extracellular matrix could provide novel opportunities such as determining cancer cell behaviour. With this background, in this work, we ha...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1823992

    authors: Yaşayan G,Mega Tiber P,Orun O,Alarçin E

    更新日期:2020-12-01 00:00:00

  • Novel organogels for topical delivery of naproxen: design, physicochemical characteristics and in vitro drug permeation.

    abstract::Taking into account possible irritation of the skin upon contact with naproxen (NPX) crystals and lower bioavailability after administration of the suspended or ionized drug, the aim of the work was to design and characterize novel and easy-to-formulate gels with the entirely dissolved drug in the acidic form. The for...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1135342

    authors: Osmałek T,Milanowski B,Froelich A,Górska S,Białas W,Szybowicz M,Kapela M

    更新日期:2017-06-01 00:00:00

  • Investigation of propellant-free aqueous foams as pharmaceutical carrier systems.

    abstract::Due to their light consistency and good spreadability, aqueous foams are considered as convenient and highly accepted drug carrier systems that are of great importance in the field of topical drug delivery. The production of a stable, easy to dose, preferably environmentally harmless foam formulation is challenging. T...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1863426

    authors: Farkas D,Kállai-Szabó N,Sárádi-Kesztyűs Á,Lengyel M,Magramane S,Kiss É,Antal I

    更新日期:2020-12-27 00:00:00

  • Preparation, preliminary pharmacokinetics and brain tissue distribution of Tanshinone IIA and Tetramethylpyrazine composite nanoemulsions.

    abstract::Objective: Tanshinone IIA (TSN) and Tetramethylpyrazine (TMP) were combined in a composite, oil-in-water nanoemulsions (TSN/TMP O/W NEs) was prepared to prolong in vitro and vivo circulation time, and enhance the bioavailability of TSN. Material and methods: Physicochemical characterization of TSN/TMP O/W NEs was char...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1656237

    authors: Wang B,Hong L,Liu Y,Bedingfield SK,Zhang C,Peng C,Qian J,Zha L

    更新日期:2019-12-01 00:00:00

  • Stability of Octastatin, a somatostatin analog cyclic octapeptide, in aqueous solution.

    abstract::In this study, the degradation of Octastatin, a cyclic octapeptide analog of somatostatin, was examined as a function of pH, temperature, buffer, and ionic strength by reversed-phase gradient high-performance liquid chromatography. Degradation of Octastatin followed a first-order kinetics. Various buffer species such ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459709022640

    authors: Jang SW,Woo BH,Lee JT,Moon SC,Lee KC,DeLuca PP

    更新日期:1997-11-01 00:00:00

  • Dual drug nanocrystals loaded microparticles for fixed dose combination of simvastatin and ezetimibe.

    abstract::Dual drug nanocrystals loaded nano embedded microparticles (DNEMs) were prepared for fixed dose combination of simvastatin (SIM) and ezetimibe (EZE) using NanoCrySP technology. The purpose was to generate nanonized SIM and EZE dispersed in matrix of single crystallization inducing excipient and investigate their in vi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1669181

    authors: Nandi S,Kaur A,Bansal AK

    更新日期:2020-01-01 00:00:00

  • Controlled release of DSBP from genipin-crosslinked gelatin thin films.

    abstract::Controlled release of a marker drug, 4,4'-bis(2-sulfostyryl) biphenyl (DSBP) from genipin crosslinked gelatin thin films, with application to drug delivery by transdermal patches is studied in this paper. A simple method for fabrication of nano-thin films, using basic lab equipment is introduced. This method consists ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802309679

    authors: Abbasi A,Eslamian M,Heyd D,Rousseau D

    更新日期:2008-01-01 00:00:00

  • Characterization of a backbone cleavage product of BMS-196854 (Oncostatin M), a recombinant anti-inflammatory cytokine.

    abstract:PURPOSE:BMS-196843 (Oncostatin M) is a therapeutic recombinant protein in development. Scale-up process changes led to unexpected instability of the bulk drug substance solution during storage. A product with an apparent higher MW than the parent protein was observed by the size-exclusion chromatography (SEC). This stu...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100002202

    authors: Zhao F,Stein DJ,Paborji M,Cash PW,Root BJ,Wei Z,Knupp CJ

    更新日期:2001-01-01 00:00:00

  • Effect of the degree of phosphate substitution in aluminum hydroxide adjuvant on the adsorption of phosphorylated proteins.

    abstract::Aluminum hydroxide adjuvant was pretreated with six concentrations of potassium dihydrogen phosphate to produce a series of adjuvants with various degrees of phosphate substitution for surface hydroxyl. The adsorption of three phosphorylated proteins (alpha casein, dephosphorylated alpha casein, and ovalbumin) by the ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120017526

    authors: Iyer S,HogenEsch H,Hem SL

    更新日期:2003-01-01 00:00:00

  • The impact of crystallinity on Brequinar sodium hygroscopicity.

    abstract::The hygroscopicity of Brequinar sodium, an organ transplant immunosuppressant, at 75% relative humidity highly depends on the crystal form or crystallinity of the drug substance. Hygroscopicity and ease of water uptake of three lots of Brequinar sodium were investigated. Those lots contained different impurities at le...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459609031417

    authors: Wu LS,Pang J,Hussain MA

    更新日期:1996-04-01 00:00:00

  • Solid-state characterization of fluconazole.

    abstract::Two polymorphs and three solvates of fluconazole were isolated and characterized by x-ray powder diffractometry, IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetry, and their dissolution rates. The different forms were prepared by crystallization of the original powder in different solvents at ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120015052

    authors: Alkhamis KA,Obaidat AA,Nuseirat AF

    更新日期:2002-11-01 00:00:00

  • Fabrication and evaluation of Phytomenadione as a nanostructure lipid carrier for enhancement of bioavailability.

    abstract::Owing to its limited aqueous solubility, Phytomenadione (vitamin K) undergoes a low bioavailability (50%) with a large inter-individual variability after oral administration. Therefore, the aim of this work was to incorporate vitamin K into nanostructure lipid carrier systems to improve its aqueous solubility and bioa...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1312440

    authors: Aljaeid BM,Hosny KM

    更新日期:2018-04-01 00:00:00

  • Prolonged injectable formulation of Nafarelin using in situ gel combination delivery system.

    abstract::The principal purpose of the present study was to prepare and characterize a complex drug delivery system consisting of Nafarelin-poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanoparticles (NPs) in combination with sodium alginate/poloxamer 407 in situ gel. Nafarelin-loaded PHBV NPs were prepared via double em...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1321662

    authors: Alizadeh B,Bahari Javan N,Akbari Javar H,Khoshayand MR,Dorkoosh F

    更新日期:2018-02-01 00:00:00

  • Multivariate analysis in the pharmaceutical industry: enabling process understanding and improvement in the PAT and QbD era.

    abstract::In the pharmaceutical industry, chemometrics is rapidly establishing itself as a tool that can be used at every step of product development and beyond: from early development to commercialization. This set of multivariate analysis methods allows the extraction of information contained in large, complex data sets thus ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章,评审

    doi:10.3109/10837450.2014.898656

    authors: Ferreira AP,Tobyn M

    更新日期:2015-01-01 00:00:00

  • Action of carriers on Carbamazepine dissolution.

    abstract::It is well known that carriers can affect the dissolution of poorly soluble drugs. In this study, our aim was to investigate the dissolution enhancement of carbamazepine solid dispersed or mixed at different loading ratios in crospovidone, polyvinylpyrrolidone, and sodium starch glycolate. The physical state of the dr...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120005725

    authors: Moneghini M,Voinovich D,Perissutti B,Princivalle F

    更新日期:2002-01-01 00:00:00

  • Novel potential drug against T. cruzi and its interaction with surfactant micelles.

    abstract::The interaction of 5-nitro-2-furfurilylidene benzhydrazide (5NFB), potential anti-trypanosomal compound, with micellar solutions was studied. The results indicated that 50 mug of 5NFB completely kills 20 million T. cruzi epimastigote cells within 3 days, whereas the same amount of benznidazole kills 30% of the cells a...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450701212727

    authors: Rangel-Yagui CO,Hsu HW,Barbosa LR,Caetano W,Pessoa A Jr,Tavares LC,Itri R

    更新日期:2007-01-01 00:00:00

  • Iontophoretic enhancement of leuprolide acetate by fatty acids, limonene, and depilatory lotions through porcine epidermis.

    abstract::The effect of chemical enhancers (e.g., fatty acids, limonene, depilatory lotions) and iontophoresis was investigated on the in vitro permeability of leuprolide acetate through porcine epidermis. Franz diffusion cells and Scepter iontophoretic power source were used for the percutaneous absorption studies. Anodal iont...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-200032986

    authors: Rastogi SK,Singh J

    更新日期:2004-11-01 00:00:00

  • Phase transition of a microemulsion upon addition of cyclodextrin - applications in drug delivery.

    abstract::This study reports on the impact of cyclodextrin addition on the phase behavior of microemulsion systems. Three distinct oil-in-water microemulsions were formulated and subjected to increasing concentrations of various cyclodextrins. The prepared formulations underwent visual, textural and microscopic characterization...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1371191

    authors: Thakur SS,Solloway J,Stikkelman A,Seyfoddin A,Rupenthal ID

    更新日期:2018-02-01 00:00:00

  • Production of microparticles by high-pressure homogenization.

    abstract::A high-pressure homogenization method for the production of aqueous suspensions of poly(D,L-lactide) and poly(D,L-lactide-co-glycolide) was investigated. Depending on the production conditions it was possible to produce micro--as well as nanoparticulate systems without the use of organic solvents. The influence of dif...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459809009857

    authors: Calvör A,Müller BW

    更新日期:1998-08-01 00:00:00

  • Prediction of tablet hardness and porosity using near-infrared diffuse reflectance spectroscopy as a nondestructive method.

    abstract::The main objective of this research is to use the near-infrared diffuse reflectance method to evaluate and quantify the effects of hardness and porosity on the near-infrared spectras of tablets. To develop a model equation, validate the model and test the model predictive ability. Seven theophylline tablet formulation...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120024689

    authors: Donoso M,Kildsig DO,Ghaly ES

    更新日期:2003-01-01 00:00:00

  • Bioavailability testing of a newly developed clindamycin oral suspension in a pediatric porcine model.

    abstract::Background: Clindamycin's bitter taste and odor is known to affect treatment adherence in children. Recently, a formulation of clindamycin HCl complexed with ion exchange resin IRP 69 was shown to mask the bitter taste. Because of the potential benefit of this formulation for children, a pilot study using a porcine mo...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章,随机对照试验

    doi:10.1080/10837450.2019.1624771

    authors: Goode GA,Wagh SJ,Irby DJ,Ma D,Jacobs RF,Kearns GL,Almoazen H

    更新日期:2019-10-01 00:00:00

  • Buccal delivery of acyclovir from films based on chitosan and polyacrylic acid.

    abstract::The aim of the present work was to investigate the possibility of achieving buccal delivery of a problematic drug, acyclovir, from films based on chitosan hydrochloride (HCS) and polyacrylic acid sodium salt (PAA). At first, the ionic interaction between HCS and PAA in distilled water was investigated by means of rheo...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120018490

    authors: Rossi S,Sandri G,Ferrari F,Bonferoni MC,Caramella C

    更新日期:2003-01-01 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

  • 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

  • Novel metrics to compare dissolution profiles.

    abstract:PURPOSE:To evaluate four novel metrics that compare dissolution profiles and assess their performance characteristics by comparing dissolution profiles of FAST and SLOW immediate release metoprolol tartrate tablets. METHODS:The four novel metrics (rho, rho m, delta a, and delta s), along with f2, were applied to disso...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120003493

    authors: Seo PR,Shah VP,Polli JE

    更新日期:2002-05-01 00:00:00

  • Rapid formulation screening with a Multipart Microscale Fluid bed Powder processor.

    abstract::The aim of this study was to investigate early formulation screening in small scale with a miniaturized fluid bed device. Altogether eight different batches were granulated in a Multipart Microscale Fluid bed Powder processor (MMFP) with constant process conditions using electrostatic atomization. Atomization voltage ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837451003739271

    authors: Kivikero N,Murtomaa M,Antikainen O,Hatara J,Juppo AM,Sandler N

    更新日期:2011-08-01 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