Cargando…
Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals
Purpose: Novel cocrystals of nevirapine (NP) were designed and prepared with salicylamide and 3-hydroxy benzoic acid (3-HBA). Methods: The cocrystals were prepared by solvent drop grinding method by adding few drops of acetone to enhance the solubility and dissolution. The drug and cocrystals were c...
Autores principales: | , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Tabriz University of Medical Sciences
2021
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8642792/ https://www.ncbi.nlm.nih.gov/pubmed/34888225 http://dx.doi.org/10.34172/apb.2021.087 |
_version_ | 1784609744244178944 |
---|---|
author | Panzade, Prabhakar Shendarkar, Giridhar Kulkarni, Deepak Shelke, Santosh |
author_facet | Panzade, Prabhakar Shendarkar, Giridhar Kulkarni, Deepak Shelke, Santosh |
author_sort | Panzade, Prabhakar |
collection | PubMed |
description | Purpose: Novel cocrystals of nevirapine (NP) were designed and prepared with salicylamide and 3-hydroxy benzoic acid (3-HBA). Methods: The cocrystals were prepared by solvent drop grinding method by adding few drops of acetone to enhance the solubility and dissolution. The drug and cocrystals were characterized by differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD). The solubility of NP, its wet ground form, and cocrystals were investigated at different pH. Moreover, the effect of surfactant on solubility of cocrystals was also studied. Finally, intrinsic dissolution rate (IDR) and stability of cocrystals was examined. Results: The characterization of cocrystals by DSC and PXRD revealed formation of new solid forms due to changes in thermogram and PXRD pattern. The cocrystal of NP with 3-HBA showed 4.5 folds greater solubility in pH 1.2 buffer and 5.5 folds in 1% Tween 80 as compared to original drug. IDR of cocrystals was higher than the pure drug in 0.1 N hydrochloric acid (HCl). Moreover, cocrystals were found physically stable after 3 months as evident from unchanged IDR. Conclusion: Hence, the present research indicates the new stable solid forms of NP with improved dissolution rate than pure drug. |
format | Online Article Text |
id | pubmed-8642792 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Tabriz University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-86427922021-12-08 Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals Panzade, Prabhakar Shendarkar, Giridhar Kulkarni, Deepak Shelke, Santosh Adv Pharm Bull Short Communication Purpose: Novel cocrystals of nevirapine (NP) were designed and prepared with salicylamide and 3-hydroxy benzoic acid (3-HBA). Methods: The cocrystals were prepared by solvent drop grinding method by adding few drops of acetone to enhance the solubility and dissolution. The drug and cocrystals were characterized by differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD). The solubility of NP, its wet ground form, and cocrystals were investigated at different pH. Moreover, the effect of surfactant on solubility of cocrystals was also studied. Finally, intrinsic dissolution rate (IDR) and stability of cocrystals was examined. Results: The characterization of cocrystals by DSC and PXRD revealed formation of new solid forms due to changes in thermogram and PXRD pattern. The cocrystal of NP with 3-HBA showed 4.5 folds greater solubility in pH 1.2 buffer and 5.5 folds in 1% Tween 80 as compared to original drug. IDR of cocrystals was higher than the pure drug in 0.1 N hydrochloric acid (HCl). Moreover, cocrystals were found physically stable after 3 months as evident from unchanged IDR. Conclusion: Hence, the present research indicates the new stable solid forms of NP with improved dissolution rate than pure drug. Tabriz University of Medical Sciences 2021-09 2020-09-22 /pmc/articles/PMC8642792/ /pubmed/34888225 http://dx.doi.org/10.34172/apb.2021.087 Text en © 2021 The Authors. https://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 | Short Communication Panzade, Prabhakar Shendarkar, Giridhar Kulkarni, Deepak Shelke, Santosh Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals |
title | Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals |
title_full | Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals |
title_fullStr | Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals |
title_full_unstemmed | Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals |
title_short | Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals |
title_sort | solid state characterization and dissolution enhancement of nevirapine cocrystals |
topic | Short Communication |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8642792/ https://www.ncbi.nlm.nih.gov/pubmed/34888225 http://dx.doi.org/10.34172/apb.2021.087 |
work_keys_str_mv | AT panzadeprabhakar solidstatecharacterizationanddissolutionenhancementofnevirapinecocrystals AT shendarkargiridhar solidstatecharacterizationanddissolutionenhancementofnevirapinecocrystals AT kulkarnideepak solidstatecharacterizationanddissolutionenhancementofnevirapinecocrystals AT shelkesantosh solidstatecharacterizationanddissolutionenhancementofnevirapinecocrystals |