Downstream processing of polymer-based amorphous solid dispersions to generate tablet formulations

2015 ◽  
Vol 486 (1-2) ◽  
pp. 268-286 ◽  
Author(s):  
B. Démuth ◽  
Z.K. Nagy ◽  
A. Balogh ◽  
T. Vigh ◽  
G. Marosi ◽  
...  
Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 654 ◽  
Author(s):  
Edina Szabó ◽  
Balázs Démuth ◽  
Dorián László Galata ◽  
Panna Vass ◽  
Edit Hirsch ◽  
...  

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.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 655
Author(s):  
Wei Qiang ◽  
Korbinian Löbmann ◽  
Colin P. McCoy ◽  
Gavin P. Andrews ◽  
Min Zhao

The thermodynamically unstable nature of amorphous drugs has led to a persistent stability issue of amorphous solid dispersions (ASDs). Lately, microwave-induced in situ amorphization has been proposed as a promising solution to this problem, where the originally loaded crystalline drug is in situ amorphized within the final dosage form using a household microwave oven prior to oral administration. In addition to circumventing issues with physical stability, it can also simplify the problematic downstream processing of ASDs. In this review paper, we address the significance of exploring and developing this novel technology with an emphasis on systemically reviewing the currently available literature in this pharmaceutical arena and highlighting the underlying mechanisms involved in inducing in situ amorphization. Specifically, in order to achieve a high drug amorphicity, formulations should be composed of drugs with high solubility in polymers, as well as polymers with high hygroscopicity and good post-plasticized flexibility of chains. Furthermore, high microwave energy input is considered to be a desirable factor. Lastly, this review discusses challenges in the development of this technology including chemical stability, selection criteria for excipients and the dissolution performance of the microwave-induced ASDs.


2021 ◽  
Vol 159 ◽  
pp. 105700
Author(s):  
Sergey A. Zolotov ◽  
Natalia B. Demina ◽  
Anna S. Zolotova ◽  
Natalia V. Shevlyagina ◽  
Grigorii A. Buzanov ◽  
...  

Author(s):  
Valentyn Mohylyuk ◽  
Thomas Pauly ◽  
Oleksandr Dobrovolnyi ◽  
Nathan Scott ◽  
David S. Jones ◽  
...  

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