Título:	Hot-melt extrusion as an advantageous technology to obtain effervescent drug products
Autor(es):	Lima, Ana Luiza Pinho, Ludmila Alvim Gomes Chaker, Juliano Alexandre Pinho, Ludmila Alvim Gomes Barreto, Livia Cristina Lira de Sá Gratieri, Taís Gelfuso, Guilherme Martins Cunha Filho, Marcilio Sérgio Soares da
ORCID:	https://orcid.org/0000-0002-2177-8941 https://orcid.org/0000-0002-4801-2145 https://orcid.org/0000-0002-1924-7885 https://orcid.org/0000-0002-9167-6852
Afiliação do autor:	University of Brasilia, School of Health Sciences, Laboratory of Food, Drug, and Cosmetics University of Brasilia, School of Health Sciences, Laboratory of Food, Drug, and Cosmetics University of Brasília, Faculty of Ceilândia University of Brasília, Faculty of Ceilândia Federal University of Goiás, School of Pharmacy, Laboratory of Nanosystems and Drug Delivery Devices University of Brasilia, School of Health Sciences, Laboratory of Food, Drug, and Cosmetics University of Brasilia, School of Health Sciences, Laboratory of Food, Drug, and Cosmetics University of Brasilia, School of Health Sciences, Laboratory of Food, Drug, and Cosmetics
Assunto:	Extrusão por fusão a quente Medicamentos efervescentes
Data de publicação:	17-Ago-2020
Editora:	MDPI
Referência:	LIMA, Ana Luiza et al. Hot-melt extrusion as an advantageous technology to obtain effervescent drug products. Pharmaceutics, [S. l.], v. 12, n. 8, 799, 2020. DOI: https://doi.org/10.3390/pharmaceutics12080779. Disponível em: https://www.mdpi.com/1999-4923/12/8/779. Acesso em: 15 nov. 2023.
Abstract:	Here, we assessed the feasibility of hot-melt extrusion (HME) to obtain effervescent drug products for the first time. For this, a combined mixture design was employed using paracetamol as a model drug. Extrudates were obtained under reduced torque (up to 0.3 Nm) at 100 ◦C to preserve the stability of the effervescent salts. Formulations showed vigorous and rapid effervescent disintegration (<3 min), adequate flow characteristics, and complete solubilization of paracetamol instantly after the effervescent reaction. Formulations containing PVPVA in the concentration range of 15–20% m/m were demonstrated to be sensitive to accelerated aging conditions, undergoing marked microstructural changes, since the capture of water led to the agglomeration and loss of their functional characteristics. HPMC matrices, in contrast, proved to be resistant to storage conditions in high relative humidity, showing superior performance to controls, including the commercial product. Moreover, the combined mixture design allowed us to identify significant interactions between the polymeric materials and the disintegrating agents, showing the formulation regions in which the responses are kept within the required levels. In conclusion, this study demonstrates that HME can bring important benefits to the elaboration of effervescent drug products, simplifying the production process and obtaining formulations with improved characteristics, such as faster disintegration, higher drug solubilization, and better stability.
Unidade Acadêmica:	Faculdade de Ciências da Saúde (FS) Departamento de Farmácia (FS FAR) Faculdade UnB Ceilândia (FCE) Colegiado de Bases Biológicas e da Saúde (FCE-BASES)
Licença:	© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
DOI:	https://doi.org/10.3390/pharmaceutics12080779
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