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Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization
Purpose: To enhance the dissolution rate of the poorly soluble drug atorvastatin calcium (ATC) by cocrystallization with selected coformers. Enhancement of the dissolution rate and solubility of the drug, which is classified as Class II of the Biopharmaceutical Classification System (BCS), is expect...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Tabriz University of Medical Sciences
2019
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6912187/ https://www.ncbi.nlm.nih.gov/pubmed/31857959 http://dx.doi.org/10.15171/apb.2019.064 |
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author | Al-Kazemi, Reham Al-Basarah, Yacoub Nada, Aly |
author_facet | Al-Kazemi, Reham Al-Basarah, Yacoub Nada, Aly |
author_sort | Al-Kazemi, Reham |
collection | PubMed |
description | Purpose: To enhance the dissolution rate of the poorly soluble drug atorvastatin calcium (ATC) by cocrystallization with selected coformers. Enhancement of the dissolution rate and solubility of the drug, which is classified as Class II of the Biopharmaceutical Classification System (BCS), is expected to enhance the bioavailability. Methods: Two methods were used for preparing the cocrystals, solvent drop grinding (SDG) and solvent evaporation (SE) method using 1:1, 1:3, and 1:10 drug-coformer molar ratios. Glucosamine hydrochloride (GluN) and nicotinamide (NIC) were investigated as coformers. The cocrystals, their physical mixtures, and the raw ATC were characterized by fourier transform infrared (FTIR spectroscopy), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), mass spectroscopy (MS), scanning electron microscopy (SEM), solubility, and dissolution rate studies. Results: SDG and SE were effective in improving the dissolution rate of ATC with both coformers. Drug: coformer ratio 1:3 was optimum. The solubility values for ATC, GluN-, and NIC-cocrystals were 26, to 35 and 50 µg/mL, respectively. The dissolution rate of ATC from cocrystals was > 90% after 5 minutes, compared to 41% untreated ATC. Conclusion: Cocrystallization significantly improved the solubility and dissolution, in comparison to the untreated ATC. |
format | Online Article Text |
id | pubmed-6912187 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Tabriz University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-69121872019-12-19 Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization Al-Kazemi, Reham Al-Basarah, Yacoub Nada, Aly Adv Pharm Bull Research Article Purpose: To enhance the dissolution rate of the poorly soluble drug atorvastatin calcium (ATC) by cocrystallization with selected coformers. Enhancement of the dissolution rate and solubility of the drug, which is classified as Class II of the Biopharmaceutical Classification System (BCS), is expected to enhance the bioavailability. Methods: Two methods were used for preparing the cocrystals, solvent drop grinding (SDG) and solvent evaporation (SE) method using 1:1, 1:3, and 1:10 drug-coformer molar ratios. Glucosamine hydrochloride (GluN) and nicotinamide (NIC) were investigated as coformers. The cocrystals, their physical mixtures, and the raw ATC were characterized by fourier transform infrared (FTIR spectroscopy), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), mass spectroscopy (MS), scanning electron microscopy (SEM), solubility, and dissolution rate studies. Results: SDG and SE were effective in improving the dissolution rate of ATC with both coformers. Drug: coformer ratio 1:3 was optimum. The solubility values for ATC, GluN-, and NIC-cocrystals were 26, to 35 and 50 µg/mL, respectively. The dissolution rate of ATC from cocrystals was > 90% after 5 minutes, compared to 41% untreated ATC. Conclusion: Cocrystallization significantly improved the solubility and dissolution, in comparison to the untreated ATC. Tabriz University of Medical Sciences 2019-10 2019-10-24 /pmc/articles/PMC6912187/ /pubmed/31857959 http://dx.doi.org/10.15171/apb.2019.064 Text en © 2019 The Author (s) http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution (CC BY), which permits unrestricted use, distribution, and reproduction in any medium, as long as the original authors and source are cited. No permission is required from the authors or the publishers. |
spellingShingle | Research Article Al-Kazemi, Reham Al-Basarah, Yacoub Nada, Aly Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization |
title | Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization |
title_full | Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization |
title_fullStr | Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization |
title_full_unstemmed | Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization |
title_short | Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization |
title_sort | dissolution enhancement of atorvastatin calcium by cocrystallization |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6912187/ https://www.ncbi.nlm.nih.gov/pubmed/31857959 http://dx.doi.org/10.15171/apb.2019.064 |
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