Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets

The formulation of active pharmaceutical ingredients (APIs) in amorphous solid dispersions (ASDs) is a promising approach to improve the bioavailability of poorly soluble compounds. However, problems often arise in the production of tablets from ASDs regarding the compressibility and recrystallizati...

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Autores principales:	Lena Ritters, Yuanyuan Tian, Stephan Reichl
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	amorphous solid dispersion tablet recrystallization drug release Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/64bd75fd28ac467fbe9ae31bcf67a369
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spelling	oai:doaj.org-article:64bd75fd28ac467fbe9ae31bcf67a3692021-11-25T18:42:11ZSpray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets10.3390/pharmaceutics131119381999-4923https://doaj.org/article/64bd75fd28ac467fbe9ae31bcf67a3692021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1938https://doaj.org/toc/1999-4923The formulation of active pharmaceutical ingredients (APIs) in amorphous solid dispersions (ASDs) is a promising approach to improve the bioavailability of poorly soluble compounds. However, problems often arise in the production of tablets from ASDs regarding the compressibility and recrystallization of the API. In the present study, the preparation of spray-dried ASDs of paracetamol (PCM) and four different types of polyvinylpyrrolidone (PVP) and their further processing into tablets were investigated. The influence of PVP type on the glass transition temperature (T<sub>g</sub>) and the physical stability of ASD powders were characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). ASD powders with 10 to 30% PCM were stable for at least 48 weeks. PCM contents of 40 to 50% led to recrystallization of the amorphous PCM within a few days or weeks. ASD with PVP/vinyl acetate (VA) copolymer (PVP/VA) was the most unstable and tended to recrystallize in PCM polymorphic form II. This formulation was therefore used for tablet studies. The influence of compression force on recrystallization, crushing strength, and drug release was investigated. Even high compression forces did not affect the stability of the ASD. However, the ASD tablets led to slow release of the API.Lena RittersYuanyuan TianStephan ReichlMDPI AGarticleamorphous solid dispersiontabletrecrystallizationdrug releasePharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1938, p 1938 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	amorphous solid dispersion tablet recrystallization drug release Pharmacy and materia medica RS1-441
spellingShingle	amorphous solid dispersion tablet recrystallization drug release Pharmacy and materia medica RS1-441 Lena Ritters Yuanyuan Tian Stephan Reichl Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets
description	The formulation of active pharmaceutical ingredients (APIs) in amorphous solid dispersions (ASDs) is a promising approach to improve the bioavailability of poorly soluble compounds. However, problems often arise in the production of tablets from ASDs regarding the compressibility and recrystallization of the API. In the present study, the preparation of spray-dried ASDs of paracetamol (PCM) and four different types of polyvinylpyrrolidone (PVP) and their further processing into tablets were investigated. The influence of PVP type on the glass transition temperature (T<sub>g</sub>) and the physical stability of ASD powders were characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). ASD powders with 10 to 30% PCM were stable for at least 48 weeks. PCM contents of 40 to 50% led to recrystallization of the amorphous PCM within a few days or weeks. ASD with PVP/vinyl acetate (VA) copolymer (PVP/VA) was the most unstable and tended to recrystallize in PCM polymorphic form II. This formulation was therefore used for tablet studies. The influence of compression force on recrystallization, crushing strength, and drug release was investigated. Even high compression forces did not affect the stability of the ASD. However, the ASD tablets led to slow release of the API.
format	article
author	Lena Ritters Yuanyuan Tian Stephan Reichl
author_facet	Lena Ritters Yuanyuan Tian Stephan Reichl
author_sort	Lena Ritters
title	Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets
title_short	Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets
title_full	Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets
title_fullStr	Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets
title_full_unstemmed	Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets
title_sort	spray-dried paracetamol/polyvinylpyrrolidone amorphous solid dispersions: part i—stability of powders and tablets
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/64bd75fd28ac467fbe9ae31bcf67a369
work_keys_str_mv	AT lenaritters spraydriedparacetamolpolyvinylpyrrolidoneamorphoussoliddispersionspartistabilityofpowdersandtablets AT yuanyuantian spraydriedparacetamolpolyvinylpyrrolidoneamorphoussoliddispersionspartistabilityofpowdersandtablets AT stephanreichl spraydriedparacetamolpolyvinylpyrrolidoneamorphoussoliddispersionspartistabilityofpowdersandtablets
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Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I—Stability of Powders and Tablets

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