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Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters
Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address so...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779791/ https://www.ncbi.nlm.nih.gov/pubmed/35057045 http://dx.doi.org/10.3390/pharmaceutics14010149 |
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author | Choi, Michael Porter, Stuart C. Meisen, Axel |
author_facet | Choi, Michael Porter, Stuart C. Meisen, Axel |
author_sort | Choi, Michael |
collection | PubMed |
description | Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address solubility issues, spray coating of the APIs onto beads and tablets offers another option for producing amorphous drug products. High-level comparisons between bead and tablet coating technologies have the potential for simpler equipment and operation that can reduce the cost of development and manufacturing. However, spray coating directly onto tablets is not without challenges, especially with respect to meeting uniformity acceptance value (AV) criteria, comprising accuracy (mean) and precision (variance) objectives. The feasibility of meeting AV criteria is examined, based on mathematical models for accuracy and precision. The results indicate that the main difficulty in manufacturing satisfactory drug-layered tablets by spray coating is caused by the practical limitations of achieving the necessary coating precision. Despite this limitation, it is shown that AV criteria can be consistently met by appropriate materials monitoring and control as well as processing equipment setup, operation, and maintenance. |
format | Online Article Text |
id | pubmed-8779791 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-87797912022-01-22 Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters Choi, Michael Porter, Stuart C. Meisen, Axel Pharmaceutics Article Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address solubility issues, spray coating of the APIs onto beads and tablets offers another option for producing amorphous drug products. High-level comparisons between bead and tablet coating technologies have the potential for simpler equipment and operation that can reduce the cost of development and manufacturing. However, spray coating directly onto tablets is not without challenges, especially with respect to meeting uniformity acceptance value (AV) criteria, comprising accuracy (mean) and precision (variance) objectives. The feasibility of meeting AV criteria is examined, based on mathematical models for accuracy and precision. The results indicate that the main difficulty in manufacturing satisfactory drug-layered tablets by spray coating is caused by the practical limitations of achieving the necessary coating precision. Despite this limitation, it is shown that AV criteria can be consistently met by appropriate materials monitoring and control as well as processing equipment setup, operation, and maintenance. MDPI 2022-01-08 /pmc/articles/PMC8779791/ /pubmed/35057045 http://dx.doi.org/10.3390/pharmaceutics14010149 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Choi, Michael Porter, Stuart C. Meisen, Axel Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters |
title | Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters |
title_full | Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters |
title_fullStr | Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters |
title_full_unstemmed | Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters |
title_short | Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters |
title_sort | application of mathematical models to determine the feasibility of amorphous drug layering in pan coaters |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779791/ https://www.ncbi.nlm.nih.gov/pubmed/35057045 http://dx.doi.org/10.3390/pharmaceutics14010149 |
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