QbD approach to downstream processing of spray-dried amorphous solid dispersions – a case study

This study aimed to elucidate the impact of a common anionic surfactant, sodium dodecyl sulfate (SDS), along with hydroxypropyl cellulose (HPC) and Soluplus (Sol) on the release of griseofulvin (GF), a poorly soluble drug, from amorphous solid dispersions (ASDs). Solutions of 2.5% GF and 2.5%–12.5% HPC/Sol with 0.125% SDS/without SDS were prepared in acetone–water and spray-dried. The solid-state characterization of the ASDs suggests that GF–Sol had better miscibility and stronger interactions than GF–HPC and formed XRPD-amorphous GF, whereas HPC-based ASDs, especially the ones with a lower HPC loading, had crystalline GF. The dissolution tests show that without SDS, ASDs provided limited GF supersaturation (max. 250%) due to poor wettability of Sol-based ASDs and extensive GF recrystallization in HPC-based ASDs (max. 50%). Sol-based ASDs with SDS exhibited a dramatic increase in supersaturation (max. 570%), especially at a higher Sol loading, whereas HPC-based ASDs with SDS did not. SDS did not interfere with Sol’s ability to inhibit GF recrystallization, as confirmed by the precipitation from the supersaturated state and PLM imaging. The favorable use of SDS in a ternary ASD was attributed to both the wettability enhancement and its inability to promote GF recrystallization when used as a minor component along with Sol.

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Influence of Preparation Methods on Solid State Supersaturation of Amorphous Solid Dispersions: A Case Study with Itraconazole and Eudragit E100

Pharmaceutical Research ◽

10.1007/s11095-010-0069-y ◽

2010 ◽

Vol 27 (5) ◽

pp. 775-785 ◽

Cited By ~ 89

Author(s):

Sandrien Janssens ◽

Ann De Zeure ◽

Amrit Paudel ◽

Jan Van Humbeeck ◽

Patrick Rombaut ◽

...

Keyword(s):

Solid State ◽

Solid Dispersions ◽

Amorphous Solid ◽

Amorphous Solid Dispersions ◽

Preparation Methods ◽

Eudragit E100

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Development of spray-dried amorphous solid dispersions of tadalafil using glycyrrhizin for enhanced dissolution and aphrodisiac activity in male rats

Saudi Pharmaceutical Journal ◽

10.1016/j.jsps.2020.11.007 ◽

2020 ◽

Vol 28 (12) ◽

pp. 1817-1826

Author(s):

Mohammed Muqtader Ahmed ◽

Farhat Fatima ◽

Mohd Abul Kalam ◽

Aws Alshamsan ◽

Gamal A. Soliman ◽

...

Keyword(s):

Solid Dispersions ◽

Amorphous Solid ◽

Male Rats ◽

Amorphous Solid Dispersions ◽

Enhanced Dissolution ◽

Spray Dried

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

Pharmaceutics ◽

10.3390/pharmaceutics11120654 ◽

2019 ◽

Vol 11 (12) ◽

pp. 654 ◽

Cited By ~ 4

Author(s):

Edina Szabó ◽

Balázs Démuth ◽

Dorián László Galata ◽

Panna Vass ◽

Edit Hirsch ◽

...

Keyword(s):

Solid Dispersions ◽

Scale Up ◽

Amorphous Solid ◽

Downstream Processing ◽

Water Soluble ◽

Content Uniformity ◽

Amorphous Solid Dispersions ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble

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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