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Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients
Crystal form can be crucial to the performance of a dosage form. This is especially true for compounds that have intrinsic barriers to drug delivery, such as low aqueous solubility, slow dissolution in gastrointestinal media, low permeability and first-pass metabolism. The nature of the physical for...
Autores principales: | , , , , |
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Formato: | Texto |
Lenguaje: | English |
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Medknow Publications
2009
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2865806/ https://www.ncbi.nlm.nih.gov/pubmed/20502540 http://dx.doi.org/10.4103/0250-474X.57283 |
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author | Yadav, A. V. Shete, A. S. Dabke, A. P. Kulkarni, P. V. Sakhare, S. S. |
author_facet | Yadav, A. V. Shete, A. S. Dabke, A. P. Kulkarni, P. V. Sakhare, S. S. |
author_sort | Yadav, A. V. |
collection | PubMed |
description | Crystal form can be crucial to the performance of a dosage form. This is especially true for compounds that have intrinsic barriers to drug delivery, such as low aqueous solubility, slow dissolution in gastrointestinal media, low permeability and first-pass metabolism. The nature of the physical form and formulation tends to exhibit the greatest effect on bioavailability parameters of water insoluble compounds that need to be given orally in high doses. An alternative approach available for the enhancement of drug solubility, dissolution and bioavailability is through the application of crystal engineering of co-crystals. The physicochemical properties of the active pharmaceutical ingredients and the bulk material properties can be modified, whilst maintaining the intrinsic activity of the drug molecule. This article covers the advantages of co-crystals over salts, solvates (hydrates), solid dispersions and polymorphs, mechanism of formation of co-crystals, methods of preparation of co-crystals and application of co-crystals to modify physicochemical characteristics of active pharmaceutical ingredients along with the case studies. The intellectual property implications of creating co-crystals are also highly relevant. |
format | Text |
id | pubmed-2865806 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2009 |
publisher | Medknow Publications |
record_format | MEDLINE/PubMed |
spelling | pubmed-28658062010-05-25 Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients Yadav, A. V. Shete, A. S. Dabke, A. P. Kulkarni, P. V. Sakhare, S. S. Indian J Pharm Sci Review Article Crystal form can be crucial to the performance of a dosage form. This is especially true for compounds that have intrinsic barriers to drug delivery, such as low aqueous solubility, slow dissolution in gastrointestinal media, low permeability and first-pass metabolism. The nature of the physical form and formulation tends to exhibit the greatest effect on bioavailability parameters of water insoluble compounds that need to be given orally in high doses. An alternative approach available for the enhancement of drug solubility, dissolution and bioavailability is through the application of crystal engineering of co-crystals. The physicochemical properties of the active pharmaceutical ingredients and the bulk material properties can be modified, whilst maintaining the intrinsic activity of the drug molecule. This article covers the advantages of co-crystals over salts, solvates (hydrates), solid dispersions and polymorphs, mechanism of formation of co-crystals, methods of preparation of co-crystals and application of co-crystals to modify physicochemical characteristics of active pharmaceutical ingredients along with the case studies. The intellectual property implications of creating co-crystals are also highly relevant. Medknow Publications 2009 /pmc/articles/PMC2865806/ /pubmed/20502540 http://dx.doi.org/10.4103/0250-474X.57283 Text en © Indian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Review Article Yadav, A. V. Shete, A. S. Dabke, A. P. Kulkarni, P. V. Sakhare, S. S. Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients |
title | Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients |
title_full | Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients |
title_fullStr | Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients |
title_full_unstemmed | Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients |
title_short | Co-Crystals: A Novel Approach to Modify Physicochemical Properties of Active Pharmaceutical Ingredients |
title_sort | co-crystals: a novel approach to modify physicochemical properties of active pharmaceutical ingredients |
topic | Review Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2865806/ https://www.ncbi.nlm.nih.gov/pubmed/20502540 http://dx.doi.org/10.4103/0250-474X.57283 |
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