Development and tableting of directly compressible powder from electrospun nanofibrous amorphous solid dispersion

Démuth, Balázs; Farkas, Attila; Szabó, Bence; Balogh, Attila; Nagy, Brigitta; Vágó, Emese; Vígh, Tamás; Tinke, A.P.; Kazsu, Z.; Demeter, Ádám; Bertels, Johny; Mensch, J.; Dijck, A. Van; Verreck, Geert; Assche, Ivo Van; Marosi, György; Nagy, Zsombor Kristóf

doi:10.1016/j.apt.2017.03.026

Cited by 31 publications

(19 citation statements)

References 39 publications

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“…Therefore, the addition of flowability aiding excipients is necessary. Interestingly, the powder mixture consisting of ASD of SPIR and PVPVA64 and the tableting excipients had much improved flowability, which is surprising considering results of similar subject in the literature [59]. (Hausner ratio: 1.12, Carr index: 11%; according to the U.S. Pharmacopeia, powder blends with Hausner ratios between 1.12 and 1.18 and Carr indices between 11 and 15% receive the second best, 'good' classification for flowability).…”

Section: Tabletingmentioning

confidence: 85%

Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

Szabó

Démuth

Nagy

et al. 2018

Express Polym. Lett.

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Section: Tabletingmentioning

confidence: 85%

Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

Szabó

Démuth

Nagy

et al. 2018

Express Polym. Lett.

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“…Related to the downstream processing of electrospun material, tableting was successfully performed from protein-type drug-loaded [34] and from acetaminophen-loaded electrospun fibers [35]. Since then, a minitablet formulation from electrospun nanofibers has been published in the literature [36], and tableting of itraconazole containing electrospun ASDs with other excipients also was scrutinized [37]. The latter one seems to be curiously promising in the industrial application because a scaled-up electrospinning method with high productivity and a rotary tablet machine were applied during the experiments.…”

Section: Preparation Of Polymer-based Amorphous Solid Dispersionsmentioning

confidence: 99%

“…However, powder properties of the electrospun samples are fairly weak, which can make the formulation process difficult. Therefore, the milling of these products might be needed if tablet forms are planned to be achieved [37]. On the other hand, other formulation strategies such as dry coating or granulation also may be appropriate to increase the flow properties of the fiber-based powders.…”

Section: Improvement Of the Flowability Of Asds For Continuous Feedingmentioning

confidence: 99%

Continuous Formulation Approaches of Amorphous Solid Dispersions: Significance of Powder Flow Properties and Feeding Performance

et al. 2019

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Preparation and formulation of amorphous solid dispersions (ASDs) are becoming more and more popular in the pharmaceutical field because the dissolution of poorly water-soluble drugs can be effectively improved this way, which can lead to increased bioavailability in many cases. During downstream processing of ASDs, technologists need to keep in mind both traditional challenges and the newest trends. In the last decade, the pharmaceutical industry began to display considerable interest in continuous processing, which can be explained with their potential advantages such as smaller footprint, easier scale-up, and more consistent product, better quality and quality assurance. Continuous downstream processing of drug-loaded ASDs opens new ways for automatic operation. Therefore, the formulation of poorly water-soluble drugs may be more effective and safe. However, developments can be challenging due to the poor flowability and feeding properties of ASDs. Consequently, this review pays special attention to these characteristics since the feeding of the components greatly influences the content uniformity in the final dosage form. The main purpose of this paper is to summarize the most important steps of the possible ASD-based continuous downstream processes in order to give a clear overview of current course lines and future perspectives.

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“…The application of this MCC subtype was preferable since ES products are hygroscopic. The adoption of both materials was desirable since (as it was described in our previous work [ 48 ]) the electrospun samples can adhere to their surfaces. Ultimately, this phenomenon sets the foundation to achieve proper homogenization.…”

Section: Resultsmentioning

confidence: 99%

Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation

et al. 2018

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Low-dose tablet formulations were produced with excellent homogeneity based on drug-loaded electrospun fibers prepared by single-needle as well as scaled-up electrospinning (SNES and HSES). Carvedilol (CAR), a BCS II class compound, served as the model drug while poly (vinylpyrrolidone-co-vinyl acetate) (PVPVA64) was adopted as the fiber-forming polymer. Scanning electron microscopy (SEM) imaging was used to study the morphology of HSES and SNES samples. Different homogenization techniques were compared to maximize homogeneity: mixing in plastic bags and in a high-shear granulator resulting in low-shear mixing (LSM) and high-shear mixing (HSM). Drug content and homogeneity of the tablets were measured by UV-Vis spectrometry, the results revealed acceptably low-dose fluctuations especially with formulations homogenized with HSM. Sieve analysis was used on the final LSM and HSM powder mixtures in order to elucidate the observed differences between tablet homogeneity. Tablets containing drug-loaded electrospun fibers were also studied by Raman mapping demonstrating evenly distributed CAR within the corpus.

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Development and tableting of directly compressible powder from electrospun nanofibrous amorphous solid dispersion

Cited by 31 publications

References 39 publications

Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

Continuous Formulation Approaches of Amorphous Solid Dispersions: Significance of Powder Flow Properties and Feeding Performance

Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation

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