Screening of several excipients for direct compression of tablets: A new perspective based on functional properties
ABSTRACT: Excipients are widely used to formulate solid drug forms by direct compression. However, the powder-forming and tableting properties of these excipients are affected by the presence of lubricants and active ingredients. In this study, a screening methodology was employed to test the perfor...
- Autores:
-
Rojas Camargo, John Jairo
Aristizábal, Julián
Henao, Manuel
- Tipo de recurso:
- Article of investigation
- Fecha de publicación:
- 2013
- Institución:
- Universidad de Antioquia
- Repositorio:
- Repositorio UdeA
- Idioma:
- eng
- OAI Identifier:
- oai:bibliotecadigital.udea.edu.co:10495/38192
- Acceso en línea:
- https://hdl.handle.net/10495/38192
https://rcfba.fcfar.unesp.br/index.php/ojs/article/view/230
- Palabra clave:
- Lubricantes
Lubricants
Tamizaje Masivo
Mass Screening
Comprimidos
Tablets
Dilución
Dilution
https://id.nlm.nih.gov/mesh/D054327
https://id.nlm.nih.gov/mesh/D008403
https://id.nlm.nih.gov/mesh/D013607
- Rights
- openAccess
- License
- http://creativecommons.org/licenses/by/2.5/co/
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Screening of several excipients for direct compression of tablets: A new perspective based on functional properties |
| dc.title.translated.spa.fl_str_mv |
Triagem de vários excipientes para compressão direta: Uma nova perspectiva com base nas propriedades funcionais |
| title |
Screening of several excipients for direct compression of tablets: A new perspective based on functional properties |
| spellingShingle |
Screening of several excipients for direct compression of tablets: A new perspective based on functional properties Lubricantes Lubricants Tamizaje Masivo Mass Screening Comprimidos Tablets Dilución Dilution https://id.nlm.nih.gov/mesh/D054327 https://id.nlm.nih.gov/mesh/D008403 https://id.nlm.nih.gov/mesh/D013607 |
| title_short |
Screening of several excipients for direct compression of tablets: A new perspective based on functional properties |
| title_full |
Screening of several excipients for direct compression of tablets: A new perspective based on functional properties |
| title_fullStr |
Screening of several excipients for direct compression of tablets: A new perspective based on functional properties |
| title_full_unstemmed |
Screening of several excipients for direct compression of tablets: A new perspective based on functional properties |
| title_sort |
Screening of several excipients for direct compression of tablets: A new perspective based on functional properties |
| dc.creator.fl_str_mv |
Rojas Camargo, John Jairo Aristizábal, Julián Henao, Manuel |
| dc.contributor.author.none.fl_str_mv |
Rojas Camargo, John Jairo Aristizábal, Julián Henao, Manuel |
| dc.contributor.researchgroup.spa.fl_str_mv |
Diseño y Formulación de Medicamentos Cosméticos y Afines |
| dc.subject.decs.none.fl_str_mv |
Lubricantes Lubricants Tamizaje Masivo Mass Screening Comprimidos Tablets Dilución Dilution |
| topic |
Lubricantes Lubricants Tamizaje Masivo Mass Screening Comprimidos Tablets Dilución Dilution https://id.nlm.nih.gov/mesh/D054327 https://id.nlm.nih.gov/mesh/D008403 https://id.nlm.nih.gov/mesh/D013607 |
| dc.subject.meshuri.none.fl_str_mv |
https://id.nlm.nih.gov/mesh/D054327 https://id.nlm.nih.gov/mesh/D008403 https://id.nlm.nih.gov/mesh/D013607 |
| description |
ABSTRACT: Excipients are widely used to formulate solid drug forms by direct compression. However, the powder-forming and tableting properties of these excipients are affected by the presence of lubricants and active ingredients. In this study, a screening methodology was employed to test the performance of an excipient for direct compression. The effects of three lubricants (magnesium stearate, stearic acid and talc) on the compressibility and compaction of these excipients were assessed by the compressibility index and lubricant sensitivity ratio, respectively. Likewise, the dilution potential in blends with a poorly compactible drug such as acetaminophen was also assessed. Finally, the elastic recovery of tablets was evaluated five days after production. All lubricants increased the compressibility of these excipients and improved their flowability. However, hydrophobic lubricants such as magnesium stearate had a marked negative effect on compactibility, especially in plastic-deforming and more regularly-shaped materials with a smooth surface such as Starch 1500. Alginic acid, rice and cassava starches had the largest elastic recovery (>5%), indicating a tendency to cap. Moreover, highly plastic deforming materials such as sorbitol and polyvinylpyrrolidone (PVP-K30) exhibited the best dilution potential (~10%), whereas alginic acid showed a very high value (~70%). In terms of performance, sorbitol, PVP-K30, Avicel PH-101, sodium alginate and pregelatinized starch were the most appropriate excipients for the direct compression of drugs. |
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2013 |
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2013 |
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2024-02-17T20:58:08Z |
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2024-02-17T20:58:08Z |
| dc.type.spa.fl_str_mv |
Artículo de investigación |
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http://purl.org/coar/resource_type/c_2df8fbb1 |
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https://purl.org/redcol/resource_type/ART |
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http://purl.org/coar/version/c_970fb48d4fbd8a85 |
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info:eu-repo/semantics/article |
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1808-4532 |
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https://hdl.handle.net/10495/38192 |
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2179-443X |
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https://rcfba.fcfar.unesp.br/index.php/ojs/article/view/230 |
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1808-4532 2179-443X |
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https://hdl.handle.net/10495/38192 https://rcfba.fcfar.unesp.br/index.php/ojs/article/view/230 |
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eng |
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Rev. Ciênc. Farm. Básica Apl. |
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1 |
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34 |
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Revista de Ciencias Farmacéuticas Básica e Aplicada |
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application/pdf |
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Universidade Estadual Paulista |
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Araraquara, Brasil |
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Universidad de Antioquia |
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Rojas Camargo, John JairoAristizábal, JuliánHenao, ManuelDiseño y Formulación de Medicamentos Cosméticos y Afines2024-02-17T20:58:08Z2024-02-17T20:58:08Z20131808-4532https://hdl.handle.net/10495/381922179-443Xhttps://rcfba.fcfar.unesp.br/index.php/ojs/article/view/230ABSTRACT: Excipients are widely used to formulate solid drug forms by direct compression. However, the powder-forming and tableting properties of these excipients are affected by the presence of lubricants and active ingredients. In this study, a screening methodology was employed to test the performance of an excipient for direct compression. The effects of three lubricants (magnesium stearate, stearic acid and talc) on the compressibility and compaction of these excipients were assessed by the compressibility index and lubricant sensitivity ratio, respectively. Likewise, the dilution potential in blends with a poorly compactible drug such as acetaminophen was also assessed. Finally, the elastic recovery of tablets was evaluated five days after production. All lubricants increased the compressibility of these excipients and improved their flowability. However, hydrophobic lubricants such as magnesium stearate had a marked negative effect on compactibility, especially in plastic-deforming and more regularly-shaped materials with a smooth surface such as Starch 1500. Alginic acid, rice and cassava starches had the largest elastic recovery (>5%), indicating a tendency to cap. Moreover, highly plastic deforming materials such as sorbitol and polyvinylpyrrolidone (PVP-K30) exhibited the best dilution potential (~10%), whereas alginic acid showed a very high value (~70%). In terms of performance, sorbitol, PVP-K30, Avicel PH-101, sodium alginate and pregelatinized starch were the most appropriate excipients for the direct compression of drugs.RESUMO: Os excipientes são materiais amplamente utilizados para formular fármacos através de compressão direta. No entanto, as propriedades do pó e compressão desses materiais são afetadas pela presença de lubrificantes e ingredientes ativos. Este estudo utilizou uma metodologia para avaliar a eficácia destes materiais como agentes de compressão direta. O efeito de três lubrificantes (estearato de magnésio, ácido esteárico e talco) na compressibilidade e compactação dos materiais foi avaliado pelo índice de compressibilidade e sensibilidade do lubrificante, respectivamente. Da mesma forma, a capacidade da diluição foi avaliada com um fármaco pouco compressível como o acetaminofeno. Finalmente, a recuperação elástica dos comprimidos foi avaliada aos cinco dias após a produção. Todos os lubrificantes aumentaram a compressibilidade destes materiais e a sua fluidez. No entanto, os lubrificantes hidrofóbicos, tais como o estearato de magnésio tem um efeito negativo sobre a compactação, em especial em materiais plásticos com uma superfície lisa, como o amido 1500. O amido de arroz e de mandioca e ácido algínico apresentaram a maior recuperação elástica (> 5%), indicando uma elevada tendência para a laminação. Além disso, os materiais plásticos com alta deformação, tais como o sorbitol, e polivinilpirrolidona (PVP-K30), exibiram a melhor potencial de diluição (~10%), enquanto que o ácido algínico mostrou um valor muito elevado (~ 70%). Em termos de desempenho, o sorbitol, o PVP-K30, alginato de sódio, Avicel PH101, e de amido pré-gelatinizado são os materiais mais adequados para a compressão direta de fármacos.COL00036237 páginasapplication/pdfengUniversidade Estadual PaulistaAraraquara, Brasilhttp://creativecommons.org/licenses/by/2.5/co/https://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccesshttp://purl.org/coar/access_right/c_abf2Screening of several excipients for direct compression of tablets: A new perspective based on functional propertiesTriagem de vários excipientes para compressão direta: Uma nova perspectiva com base nas propriedades funcionaisArtículo de investigaciónhttp://purl.org/coar/resource_type/c_2df8fbb1https://purl.org/redcol/resource_type/ARThttp://purl.org/coar/version/c_970fb48d4fbd8a85info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionLubricantesLubricantsTamizaje MasivoMass ScreeningComprimidosTabletsDiluciónDilutionhttps://id.nlm.nih.gov/mesh/D054327https://id.nlm.nih.gov/mesh/D008403https://id.nlm.nih.gov/mesh/D013607Rev. Ciênc. Farm. 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