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Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State?

In this study a solid dispersion and a physical mixture of cilazapril (CIL) with a biopolymer - polyvinylpyrrolidone (PVP) as a carrier were prepared so as to investigate the effect of PVP on the stability of CIL. CIL is unstable in solid state and decomposes rapidly under humid conditions. It requi...

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Autores principales: Regulska, Katarzyna, Regulski, Miosz, Wzgarda, Anna, Kotowska, Aleksandra, Ignasiak, Aleksandra, Ćwiertnia, Barbara, Stanisz, Beata
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6706751/
https://www.ncbi.nlm.nih.gov/pubmed/31531043
http://dx.doi.org/10.22037/ijpr.2019.1100640
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author Regulska, Katarzyna
Regulski, Miosz
Wzgarda, Anna
Kotowska, Aleksandra
Ignasiak, Aleksandra
Ćwiertnia, Barbara
Stanisz, Beata
author_facet Regulska, Katarzyna
Regulski, Miosz
Wzgarda, Anna
Kotowska, Aleksandra
Ignasiak, Aleksandra
Ćwiertnia, Barbara
Stanisz, Beata
author_sort Regulska, Katarzyna
collection PubMed
description In this study a solid dispersion and a physical mixture of cilazapril (CIL) with a biopolymer - polyvinylpyrrolidone (PVP) as a carrier were prepared so as to investigate the effect of PVP on the stability of CIL. CIL is unstable in solid state and decomposes rapidly under humid conditions. It requires stabilization to ensure safety of its use. The studied CIL/PVP formulations were prepared by milling and evaporation technique. Their identity was confirmed by FT-IR method. The stability of CIL in the CIL/PVP formulations was assessed by forced ageing test under isothermic conditions using RP-HPLC. The influence of temperature (experimental conditions: RH 76.4% and T = 70, 75, 80, 85, and 90 (o)C) and the effect of relative humidity (experimental conditions: RH 25.0%, 50.9%, 60.9%, 66.5%, 76.4%, T = 90 °C) on the rate of CIL degradation were examined. It was established that the process of CIL decay in the studied forms followed first-order kinetics with the formation of one degradation product - cilazaprilat. The degradation rate constant of this reaction was lower than that for pure CIL. The energy of activation of the CIL degradation in the presence of PVP was higher than that of pure CIL. Furthermore, CIL incorporated into PVP exhibited lower sensitivity to moisture. Based on these data PVP was considered as a potential stabilizing substance for CIL-containing dosage forms.
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spelling pubmed-67067512019-09-17 Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State? Regulska, Katarzyna Regulski, Miosz Wzgarda, Anna Kotowska, Aleksandra Ignasiak, Aleksandra Ćwiertnia, Barbara Stanisz, Beata Iran J Pharm Res Original Article In this study a solid dispersion and a physical mixture of cilazapril (CIL) with a biopolymer - polyvinylpyrrolidone (PVP) as a carrier were prepared so as to investigate the effect of PVP on the stability of CIL. CIL is unstable in solid state and decomposes rapidly under humid conditions. It requires stabilization to ensure safety of its use. The studied CIL/PVP formulations were prepared by milling and evaporation technique. Their identity was confirmed by FT-IR method. The stability of CIL in the CIL/PVP formulations was assessed by forced ageing test under isothermic conditions using RP-HPLC. The influence of temperature (experimental conditions: RH 76.4% and T = 70, 75, 80, 85, and 90 (o)C) and the effect of relative humidity (experimental conditions: RH 25.0%, 50.9%, 60.9%, 66.5%, 76.4%, T = 90 °C) on the rate of CIL degradation were examined. It was established that the process of CIL decay in the studied forms followed first-order kinetics with the formation of one degradation product - cilazaprilat. The degradation rate constant of this reaction was lower than that for pure CIL. The energy of activation of the CIL degradation in the presence of PVP was higher than that of pure CIL. Furthermore, CIL incorporated into PVP exhibited lower sensitivity to moisture. Based on these data PVP was considered as a potential stabilizing substance for CIL-containing dosage forms. Shaheed Beheshti University of Medical Sciences 2019 /pmc/articles/PMC6706751/ /pubmed/31531043 http://dx.doi.org/10.22037/ijpr.2019.1100640 Text en This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Regulska, Katarzyna
Regulski, Miosz
Wzgarda, Anna
Kotowska, Aleksandra
Ignasiak, Aleksandra
Ćwiertnia, Barbara
Stanisz, Beata
Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State?
title Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State?
title_full Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State?
title_fullStr Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State?
title_full_unstemmed Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State?
title_short Does Polyvinylpyrrolidone Improve the Chemical Stability of Cilazapril in Solid State?
title_sort does polyvinylpyrrolidone improve the chemical stability of cilazapril in solid state?
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6706751/
https://www.ncbi.nlm.nih.gov/pubmed/31531043
http://dx.doi.org/10.22037/ijpr.2019.1100640
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