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Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation

Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The purpose of this study was to characterize the solid state of cocrystalline phas...

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Autores principales: Yuliandra, Yori, Zaini, Erizal, Syofyan, Syofyan, Pratiwi, Wenny, Putri, Lidiya Novita, Pratiwi, Yuti Sahra, Arifin, Helmi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6027666/
https://www.ncbi.nlm.nih.gov/pubmed/29867030
http://dx.doi.org/10.3390/scipharm86020023
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author Yuliandra, Yori
Zaini, Erizal
Syofyan, Syofyan
Pratiwi, Wenny
Putri, Lidiya Novita
Pratiwi, Yuti Sahra
Arifin, Helmi
author_facet Yuliandra, Yori
Zaini, Erizal
Syofyan, Syofyan
Pratiwi, Wenny
Putri, Lidiya Novita
Pratiwi, Yuti Sahra
Arifin, Helmi
author_sort Yuliandra, Yori
collection PubMed
description Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The purpose of this study was to characterize the solid state of cocrystalline phase of ibuprofen-nicotinamide, determine the solubility, and evaluate its in vivo analgesic activity. The cocrystal of ibuprofen-nicotinamide was prepared by a slow evaporation method. The solid-state characterization was conducted by powder X-ray diffraction (PXRD) analysis, differential thermal analysis (DTA), and scanning electron microscopy (SEM). To investigate the in vivo analgesic activity, 28 male Swiss-Webster mice were injected with acetic acid 0.5% following oral administration of intact ibuprofen, physical mixture, and its cocrystalline phase with nicotinamide (equivalent to 26 mg/kg ibuprofen). The number of writhes was counted, and pain inhibition was calculated. All data were analyzed with one-way ANOVA followed by Duncan’s Multiple Range Test (95% confidence interval). The results revealed that a new cocrystalline phase was successfully formed. The solubility testing showed that the cocrystal formation enhanced the solubility significantly as compared with the physical mixture and intact ibuprofen. A significant increase in the analgesic activity of cocrystal ibuprofen-nicotinamide was also confirmed.
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spelling pubmed-60276662018-07-02 Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation Yuliandra, Yori Zaini, Erizal Syofyan, Syofyan Pratiwi, Wenny Putri, Lidiya Novita Pratiwi, Yuti Sahra Arifin, Helmi Sci Pharm Article Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The purpose of this study was to characterize the solid state of cocrystalline phase of ibuprofen-nicotinamide, determine the solubility, and evaluate its in vivo analgesic activity. The cocrystal of ibuprofen-nicotinamide was prepared by a slow evaporation method. The solid-state characterization was conducted by powder X-ray diffraction (PXRD) analysis, differential thermal analysis (DTA), and scanning electron microscopy (SEM). To investigate the in vivo analgesic activity, 28 male Swiss-Webster mice were injected with acetic acid 0.5% following oral administration of intact ibuprofen, physical mixture, and its cocrystalline phase with nicotinamide (equivalent to 26 mg/kg ibuprofen). The number of writhes was counted, and pain inhibition was calculated. All data were analyzed with one-way ANOVA followed by Duncan’s Multiple Range Test (95% confidence interval). The results revealed that a new cocrystalline phase was successfully formed. The solubility testing showed that the cocrystal formation enhanced the solubility significantly as compared with the physical mixture and intact ibuprofen. A significant increase in the analgesic activity of cocrystal ibuprofen-nicotinamide was also confirmed. MDPI 2018-06-04 2018 /pmc/articles/PMC6027666/ /pubmed/29867030 http://dx.doi.org/10.3390/scipharm86020023 Text en © 2018 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/).
spellingShingle Article
Yuliandra, Yori
Zaini, Erizal
Syofyan, Syofyan
Pratiwi, Wenny
Putri, Lidiya Novita
Pratiwi, Yuti Sahra
Arifin, Helmi
Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation
title Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation
title_full Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation
title_fullStr Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation
title_full_unstemmed Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation
title_short Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation
title_sort cocrystal of ibuprofen–nicotinamide: solid-state characterization and in vivo analgesic activity evaluation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6027666/
https://www.ncbi.nlm.nih.gov/pubmed/29867030
http://dx.doi.org/10.3390/scipharm86020023
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