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Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics

The availability of liquid oral preparations compounded by pharmacists is essential to meet paediatric needs which remain unanswered by the pharmaceutical industry. Unfortunately, compendial monographs are often not available and, in many cases, pre-formulation studies (e.g., compatibility with othe...

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Autores principales: Casiraghi, Antonella, Centin, Giorgio, Selmin, Francesca, Picozzi, Claudia, Minghetti, Paola, Zanon, Davide
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8618881/
https://www.ncbi.nlm.nih.gov/pubmed/34834378
http://dx.doi.org/10.3390/pharmaceutics13111963
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author Casiraghi, Antonella
Centin, Giorgio
Selmin, Francesca
Picozzi, Claudia
Minghetti, Paola
Zanon, Davide
author_facet Casiraghi, Antonella
Centin, Giorgio
Selmin, Francesca
Picozzi, Claudia
Minghetti, Paola
Zanon, Davide
author_sort Casiraghi, Antonella
collection PubMed
description The availability of liquid oral preparations compounded by pharmacists is essential to meet paediatric needs which remain unanswered by the pharmaceutical industry. Unfortunately, compendial monographs are often not available and, in many cases, pre-formulation studies (e.g., compatibility with other excipients and solubility evaluations) are not performed in-depth, leading, in some rare cases, to the inadvertent administration of a toxic dose. In this study, the preparation of an oral liquid formulation for paediatric use, containing flecainide acetate at different strengths, was considered, taking into account the possible effects of conventionally used excipients. First, the optimal vehicle was selected based on a solubility study, evidencing some unexpected formations of precipitates. As a matter of fact, the buffers commonly used for oral solutions significantly reduced flecainide solubility, and the concomitant presence of citrate buffer and methylparaben even caused the formation of non-resuspendable crystals. Then, chemical, physical, and microbiological stability were assessed. Solutions at strengths of 10 and 20 mg/mL flecainide acetate were stable up to 8 weeks when compounded by using a 40% sucrose solution as a vehicle. Microbiological data showed that the use of methylparaben was not necessary over this time period.
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spelling pubmed-86188812021-11-27 Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics Casiraghi, Antonella Centin, Giorgio Selmin, Francesca Picozzi, Claudia Minghetti, Paola Zanon, Davide Pharmaceutics Article The availability of liquid oral preparations compounded by pharmacists is essential to meet paediatric needs which remain unanswered by the pharmaceutical industry. Unfortunately, compendial monographs are often not available and, in many cases, pre-formulation studies (e.g., compatibility with other excipients and solubility evaluations) are not performed in-depth, leading, in some rare cases, to the inadvertent administration of a toxic dose. In this study, the preparation of an oral liquid formulation for paediatric use, containing flecainide acetate at different strengths, was considered, taking into account the possible effects of conventionally used excipients. First, the optimal vehicle was selected based on a solubility study, evidencing some unexpected formations of precipitates. As a matter of fact, the buffers commonly used for oral solutions significantly reduced flecainide solubility, and the concomitant presence of citrate buffer and methylparaben even caused the formation of non-resuspendable crystals. Then, chemical, physical, and microbiological stability were assessed. Solutions at strengths of 10 and 20 mg/mL flecainide acetate were stable up to 8 weeks when compounded by using a 40% sucrose solution as a vehicle. Microbiological data showed that the use of methylparaben was not necessary over this time period. MDPI 2021-11-19 /pmc/articles/PMC8618881/ /pubmed/34834378 http://dx.doi.org/10.3390/pharmaceutics13111963 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Casiraghi, Antonella
Centin, Giorgio
Selmin, Francesca
Picozzi, Claudia
Minghetti, Paola
Zanon, Davide
Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics
title Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics
title_full Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics
title_fullStr Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics
title_full_unstemmed Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics
title_short Critical Aspects in the Preparation of Extemporaneous Flecainide Acetate Oral Solution for Paediatrics
title_sort critical aspects in the preparation of extemporaneous flecainide acetate oral solution for paediatrics
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8618881/
https://www.ncbi.nlm.nih.gov/pubmed/34834378
http://dx.doi.org/10.3390/pharmaceutics13111963
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