Cross-linking of poly (vinyl alcohol) films under acidic and thermal stress
| Autor: | George Crull, Ipsit Kundu, Balvinder S. Vig, Varia Sailesh Amilal, Salil D. Desai, Hemant Bhutani, Narayana P. Swamy, Ravi P. Shah, Chiranjeevi Venkatesh, Sridhar Desikan, Sherif Badawy, Duohai Pan, Junshu Zhao |
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| Rok vydání: | 2020 |
| Předmět: |
Vinyl alcohol
Materials science Polymers Pharmaceutical Science Ether Hydrochloric acid 02 engineering and technology engineering.material 030226 pharmacology & pharmacy Excipients 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Coating Dissolution chemistry.chemical_classification Aqueous solution Polymer 021001 nanoscience & nanotechnology Acid strength chemistry Chemical engineering Polyvinyl Alcohol engineering 0210 nano-technology Tablets |
| Zdroj: | European Journal of Pharmaceutical Sciences. 152:105429 |
| ISSN: | 0928-0987 |
| DOI: | 10.1016/j.ejps.2020.105429 |
| Popis: | Poly (vinyl alcohol), PVA, a commonly used excipient to coat tablets, forms insoluble films in the presence of acids and thermal stress. This may lead to drug products failing to meet dissolution specifications over time. Studies were conducted to understand the effect of acid strength, processing conditions, and storage stress on the mechanism of insoluble film formation using PVA and OpadryⓇ II as model systems. Aqueous cast films, prepared by incorporating hydrochloric acid (HCl) into the coating solutions or exposing pre-cast "as is" films to HCl vapors, were used as surrogates to develop analytical methods. To understand effect of acid and processing on coatings, acidified OpadryⓇ II was spray coated onto inert cores under "wet" or "dry" conditions. Samples stored at 50-60 °C were analyzed for film disintegration to understand physical/chemical changes in the polymer. Rate and extent of insoluble films formation was dependent on the acid concentration and thermal stress. Analysis of the films indicated significant de-acetylation and ether bond formation in insoluble aqueous cast films. In contrast, acidified coated films showed only ether bond formation, which increased on stress, forming insoluble films. The reduction in the time to form insoluble films for "wet" versus "dry" coated films was rationalized by considering effect of coating, drying, and storage on the microstructure of acidified PVA and ether bond propagation. The results highlight the need to develop an in-depth understanding of the design space for PVA coated products and storage conditions in presence of acids. |
| Databáze: | OpenAIRE |
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