Upscaling of the hot-melt extrusion process: Comparison between laboratory scale and pilot scale production of solid dispersions with miconazole and Kollicoat® IR

Guns, Sandra; Mathot, Vincent; Martens, Johan A.; Mooter, Guy Van den

doi:10.1016/j.ejpb.2012.03.020

Cited by 26 publications

(16 citation statements)

References 21 publications

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“…However, the scale-up of these laboratory-scale processes is essential during product development. (98,(109)(110)(111). The scale-up of batch processes is one of the most critical functions in the pharmaceutical industries.…”

Section: Scale-up Of Hme Processesmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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Abstract. Hot-melt extrusion (HME) is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. In drug discovery and development, industry estimates that more than 50% of active pharmaceutical ingredients currently used belong to the biopharmaceutical classification system II (BCS class II), which are characterized as poorly water-soluble compounds and result in formulations with low bioavailability. Therefore, there is a critical need for the pharmaceutical industry to develop formulations that will enhance the solubility and ultimately the bioavailability of these compounds. HME technology also offers an opportunity to earn intellectual property, which is evident from an increasing number of patents and publications that have included it as a novel pharmaceutical formulation technology over the past decades. This review had a threefold objective. First, it sought to provide an overview of HME principles and present detailed engineered extrusion equipment designs. Second, it included a number of published reports on the application of HME techniques that covered the fields of solid dispersions, microencapsulation, taste masking, targeted drug delivery systems, sustained release, films, nanotechnology, floating drug delivery systems, implants, and continuous manufacturing using the wet granulation process. Lastly, this review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology.

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Section: Scale-up Of Hme Processesmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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“…Guns et al . also used 200 rpm for 1 min recirculation to prepare glass solutions, even though they did not provide a systematic evaluation of the process variables …”

Section: Resultsmentioning

confidence: 99%

“…However, the Leistritz Nano‐16, ThermoScientific TSG16 and Three‐Tec ZE 16 models have too large a scale to conduct formulation screening with tiny amounts of material in the early development stage. Especially in the field of HME for solid‐dispersion screening within the scale of 10 g per batch, it has been reported that glass solutions, glass suspensions and solid solutions can be prepared using the HAAKE Minilab or the DSM Xplore extruders . However, there is no report concerning the preparation of other types of solid dispersions with these machines.…”

Section: Introductionmentioning

confidence: 99%

Investigation into mixing capability and solid dispersion preparation using the DSM Xplore Pharma Micro Extruder

Sakai

Thommes

2014

Journal of Pharmacy and Pharmacology

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“…Crystallinity was not observed in either case, and thus the researchers deduced that processing was comparable for both extruders. Guns et al (2012) discussed scale-up aspects of melt extrusion and made a comparative assessment of miconazole and Kollicoat ® IR solid dispersion prepared by laboratory scale and pilot-scale extrusion, respectively. The properties of the final dosage forms were influenced by the processing parameters (screw speed, processing temperature, and feed rate) of the melt extrusion process.…”

Section: Late-stage Development: Scale-up Considerations and Qbd-basementioning

confidence: 99%

Melt Extrusion in Drug Delivery: Three Decades of Progress

Shah

Repka

2013

AAPS Advances in the Pharmaceutical Sciences Series

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This chapter appraises the role of melt extrusion as a solubilization and bioavailability enhancement technique. The introductory chapter highlights major aspects of hot melt extrusion (HME) technology as applied in the pharmaceutical industry, particularly processing techniques, material considerations, recent innovative applications of melt extrusion in drug delivery system design, and a review of current HME-based formulations (marketed or under commercial development). The chapter also focuses on key development aspects of HME processes, such as material sparing screening approaches, process formulation relationships, and stability evaluation of prototype formulations, which emphasize the clinical and biological significance of this technique. In addition, it displays the journey and evolution of this important processing technology into an established pharmaceutical manufacturing platform. The chapter describes several case studies wherein melt extrusion has been utilized to develop commercial drug products.Early-stage development in melt extrusion encompasses various critically interdependent areas involving process considerations, stability assessment of prototype formulations, and performance evaluation (with respect to intended applications) of prototype formulations. Processing ConsiderationsProcessing considerations is a rather broad terminology covering material properties, instrument considerations, and process-formulation interplay. Systematic research over the last couple of decades has revealed that critical product quality attributes are directly dependent on both "formulation" and the "process" employed. It is important to note that the interplay between these determines the finished product attributes. Material PropertiesAll of the materials used in melt extrusion (drugs, carriers, processing aids, release modifiers, etc.) should meet certain minimal pharmaceutical criteria, which

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Upscaling of the hot-melt extrusion process: Comparison between laboratory scale and pilot scale production of solid dispersions with miconazole and Kollicoat® IR

Cited by 26 publications

References 21 publications

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

Investigation into mixing capability and solid dispersion preparation using the DSM Xplore Pharma Micro Extruder

Melt Extrusion in Drug Delivery: Three Decades of Progress

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