Developing HME-Based Drug Products Using Emerging Science: a Fast-Track Roadmap from Concept to Clinical Batch

Matić, Josip; Paudel, Amrit; Bauer, Hannes; García, Raymar Andreína Lara; Biedrzycka, Kinga; Khinast, Johannes

doi:10.1208/s12249-020-01713-0

Cited by 21 publications

(15 citation statements)

References 107 publications

(122 reference statements)

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“…The Noxafil® and Nucynta® ER products listed in Table 5 are manufactured by melt extrusion [119,120]. HME is listed as alternative manufacturing method for sublingual films which are commonly manufactured by wet casting techniques [23,24].…”

Section: Bioavailability Enhancement and Melt Extrusionmentioning

confidence: 99%

Applications of polymer blends in drug delivery

Nyamweya¹

2021

Futur J Pharm Sci

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Background Polymers are essential components of many drug delivery systems and biomedical products. Despite the utility of many currently available polymers, there exists a demand for materials with improved characteristics and functionality. Due to the extensive safety testing required for new excipient approval, the introduction and use of new polymers is considerably limited. The blending of currently approved polymers provides a valuable solution by which the limitations of individual polymers can be addressed. Main body Polymer blends combine two or more polymers resulting in improved, augmented, or customized properties and functionality which can result in significant advantages in drug delivery applications. This review discusses the rationale for the use of polymer blends and blend polymer-polymer interactions. It provides examples of their use in commercially marketed products and drug delivery systems. Examples of polymer blends in amorphous solid dispersions and biodegradable systems are also discussed. A classification scheme for polymer blends based on the level of material processing and interaction is presented. Conclusion The use of polymer blends represents a valuable and under-utilized resource in addressing a diverse range of drug delivery challenges. It is anticipated that new drug molecule development challenges such as bioavailability enhancement and the demand for enabling excipients will lead to increased applications of polymer blends in pharmaceutical products. Graphical abstract

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Section: Bioavailability Enhancement and Melt Extrusionmentioning

confidence: 99%

Applications of polymer blends in drug delivery

Nyamweya¹

2021

Futur J Pharm Sci

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“…The HME process is flexible and allows for the screw configuration to be tailored to the specific requirements of the processed formulation [15,16]. In addition, HME offers the possibility of implementing PAT, real-time quality monitoring [15,17,18], and other tools for advanced process control [18][19][20][21]. Recently, in silico process development and scale-up has shown successful cases of reducing the overall process development time and material waste [21][22][23][24].…”

Section: Introductionmentioning

confidence: 99%

SEDEX—Self-Emulsifying Delivery Via Hot Melt Extrusion: A Continuous Pilot-Scale Feasibility Study

et al. 2022

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The aim of this study was to develop a continuous pilot-scale solidification and characterization of self-emulsifying drug delivery systems (SEDDSs) via hot melt extrusion (HME) using Soluplus® and Kollidon® VA-64. First, an oil-binding capacity study was performed to estimate the maximal amount of SEDDSs that the polymers could bind. Then, HME was conducted using a Coperion 18 mm ZSK18 pilot plant-scale extruder with split-feeding of polymer and SEDDS in 10, 20, and 30% w/w SEDDSs was conducted. The prepared extrudates were characterized depending on appearance, differential scanning calorimetry, wide-angle X-ray scattering, emulsification time, droplet size, polydispersity index, and cloud point. The oil-binding studies showed that the polymers were able to bind up to 50% w/w of liquid SEDDSs. The polymers were processed via HME in a temperature range between 110 and 160 °C, where a plasticizing effect of the SEDDSs was observed. The extrudates were found to be stable in the amorphous state and self-emulsified in demineralized water at 37 °C with mean droplet sizes between 50 and 300 nm. A cloud point and phase inversion were evident in the Soluplus® samples. In conclusion, processing SEDDSs with HME could be considered a promising alternative to the established solidification techniques as well as classic amorphous solid dispersions for drug delivery.

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“…Technologies to produce solid dispersion includes spray drying, hot melt extrusion, co-precipitation, fluid bed granulation, and recently the Kinetisol process and others have been reported ( Friesen et al, 2008 ; Hughey et al, 2015 ; Mendonsa et al, 2020 ; Sandhu et al, 2014 ). However commercial products mostly rely on spray drying and hot melt extrusion technology ( Matić et al, 2020 ; Solanki et al, 2019 ; Zhang et al, 2018 ). Spray drying is one of the preferred technology for formulating amorphous solid dispersion with HPMCAS.…”

Section: Introductionmentioning

confidence: 99%

Downstream processing of spray-dried ASD with hypromellose acetate succinate – Roller compaction and subsequent compression into high ASD load tablets

Sauer¹,

Warashina

Mishra³

et al. 2021

International Journal of Pharmaceutics: X

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Despite wide commercial application of hypromellose acetate succinate (HPMCAS) in spray-dried amorphous solid dispersion (ASD) drug products, little information is available in the references on downstream processing of spray-dried dispersions with HPMCAS. Poor flow and high dilution factor are a challenge in formulating spray-dried ASDs into tablets, leaving little space for other excipients facilitating binding and disintegration. Direct compression is not possible due to the poor powder flow of spray-dried ASDs. Moisture has to be avoided due to the plasticizing properties of water on the ASD, resulting in reduced stability of the amorphous state. Thus, dry granulation by roller compaction and subsequent tablet compression is the preferred downstream process. We report the investigation of downstream processing by roller compaction and tablet compression of a high load formulation with 75% of spray-dried amorphous solid dispersion (Nifedipine:HPMCAS 1:2). A head to head comparison of microcrystalline cellulose/croscarmellose (MCC/cl-NaCMC) as binder/disintegrant vs. MCC and low-substituted hydroxypropyl cellulose (L-HPC) as excipient for binding and disintegration showed improved re-workability of the formulation with MCC/L-HPC after roller compaction. Upon transfer to the rotary press, a 45% higher tensile strength of tablets is observed after dry granulation with MCC/L-HPC.

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Developing HME-Based Drug Products Using Emerging Science: a Fast-Track Roadmap from Concept to Clinical Batch

Cited by 21 publications

References 107 publications

Applications of polymer blends in drug delivery

Applications of polymer blends in drug delivery

SEDEX—Self-Emulsifying Delivery Via Hot Melt Extrusion: A Continuous Pilot-Scale Feasibility Study

Downstream processing of spray-dried ASD with hypromellose acetate succinate – Roller compaction and subsequent compression into high ASD load tablets

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