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Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions
Grapiprant is a new analgesic and anti-inflammatory drug belonging to the piprant class, approved in 2016 by the FDA Veterinary Medicine Center for the treatment of pain and inflammation associated with osteoarthritis in dogs. It acts as a highly selective antagonist of the EP4 receptor, one of the...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9687689/ https://www.ncbi.nlm.nih.gov/pubmed/36359341 http://dx.doi.org/10.3390/biomedicines10112821 |
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author | Gumułka, Paweł Tarsa, Monika Dąbrowska, Monika Starek, Małgorzata |
author_facet | Gumułka, Paweł Tarsa, Monika Dąbrowska, Monika Starek, Małgorzata |
author_sort | Gumułka, Paweł |
collection | PubMed |
description | Grapiprant is a new analgesic and anti-inflammatory drug belonging to the piprant class, approved in 2016 by the FDA Veterinary Medicine Center for the treatment of pain and inflammation associated with osteoarthritis in dogs. It acts as a highly selective antagonist of the EP4 receptor, one of the four prostaglandin E2 (PGE2) receptor subtypes. It has been shown to have anti-inflammatory effects in rat models of acute and chronic inflammation and clinical studies in people with osteoarthritis. The current state of knowledge suggests the possibility of using it in oncological therapy. The manuscript presents the development of conditions for the identification and quantitative determination of grapiprant by thin-layer chromatography with densitometric detection. The optimal separation of the substance occurs using silica gel 60F(254) chromatographic plates and the mobile phase containing ethyl acetate-toluene-butylamine. Validation (according to ICH requirements) showed that the developed method is characterized by straightness of results in a wide concentration range with the limit of detection of 146.65 µg/mL. The %RSD values of the precision and accuracy confirm the sensitivity and reliability of the developed procedure. Next, the method was used for quantification of grapiprant in a pharmaceutical preparation, and for stability studies under various environmental conditions. Additionally, the mass studies were carried out on the stressed samples using the UPLC-MS/MS method. The degradation products were primarily characterized by comparing their mass fragmentation profiles with those of the drug. The results indicated a potential degradation pathway for grapiprant. |
format | Online Article Text |
id | pubmed-9687689 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-96876892022-11-25 Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions Gumułka, Paweł Tarsa, Monika Dąbrowska, Monika Starek, Małgorzata Biomedicines Article Grapiprant is a new analgesic and anti-inflammatory drug belonging to the piprant class, approved in 2016 by the FDA Veterinary Medicine Center for the treatment of pain and inflammation associated with osteoarthritis in dogs. It acts as a highly selective antagonist of the EP4 receptor, one of the four prostaglandin E2 (PGE2) receptor subtypes. It has been shown to have anti-inflammatory effects in rat models of acute and chronic inflammation and clinical studies in people with osteoarthritis. The current state of knowledge suggests the possibility of using it in oncological therapy. The manuscript presents the development of conditions for the identification and quantitative determination of grapiprant by thin-layer chromatography with densitometric detection. The optimal separation of the substance occurs using silica gel 60F(254) chromatographic plates and the mobile phase containing ethyl acetate-toluene-butylamine. Validation (according to ICH requirements) showed that the developed method is characterized by straightness of results in a wide concentration range with the limit of detection of 146.65 µg/mL. The %RSD values of the precision and accuracy confirm the sensitivity and reliability of the developed procedure. Next, the method was used for quantification of grapiprant in a pharmaceutical preparation, and for stability studies under various environmental conditions. Additionally, the mass studies were carried out on the stressed samples using the UPLC-MS/MS method. The degradation products were primarily characterized by comparing their mass fragmentation profiles with those of the drug. The results indicated a potential degradation pathway for grapiprant. MDPI 2022-11-05 /pmc/articles/PMC9687689/ /pubmed/36359341 http://dx.doi.org/10.3390/biomedicines10112821 Text en © 2022 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 Gumułka, Paweł Tarsa, Monika Dąbrowska, Monika Starek, Małgorzata Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions |
title | Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions |
title_full | Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions |
title_fullStr | Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions |
title_full_unstemmed | Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions |
title_short | Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions |
title_sort | quantification of grapiprant and its stability testing under changing environmental conditions |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9687689/ https://www.ncbi.nlm.nih.gov/pubmed/36359341 http://dx.doi.org/10.3390/biomedicines10112821 |
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