Manufacture and Performance Evaluation of a Stable Amorphous Complex of an Acidic Drug Molecule and Neusilin
In this paper, we explore the use of Neusilin, an inorganic magnesium aluminometasilicate, to stabilize the amorphous form of an acidic drug Sulindac. Both cryomilling and ball milling of the drug with Neusilin were found to produce the amorphous phase. However, the ball‐milled (BM) material exhibit...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 2011-08, Vol.100 (8), p.3332-3344 |
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| creator | Maclean, Jenifer Medina, Cesar Daurio, Dominick Alvarez‐Nunez, Fernando Jona, Janan Munson, Eric Nagapudi, Karthik |
| description | In this paper, we explore the use of Neusilin, an inorganic magnesium aluminometasilicate, to stabilize the amorphous form of an acidic drug Sulindac. Both cryomilling and ball milling of the drug with Neusilin were found to produce the amorphous phase. However, the ball‐milled (BM) material exhibited superior physical stability when compared with the cryomilled material at 40°C/75% relative humidity. 13C solid‐state nuclear magnetic resonance investigation of the BM material revealed an acid–base reaction between Sulindac and Neusilin. Optimal milling conditions and the kinetics of salt formation were also established. As benchtop milling is a laboratory‐scale process, a scalable process was developed to make Sulindac–Neusilin amorphous drug complex using hot‐melt extrusion (HME). The dissolution properties of the resulting HME material was found to have been improved over the material made by benchtop milling while maintaining similar physical stability. The HME material was used to make tablets using a direct compression method. The HME tablets were found to have better dissolution properties than tablets made from crystalline Sulindac. For the broad class of acidic drugs containing the carboxyl moiety, inorganic silicates such as Neusilin would offer a better choice than organic polymers to stabilize the amorphous phase. © 2011 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3332–3344, 2011 |
| doi_str_mv | 10.1002/jps.22583 |
| format | Article |
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Both cryomilling and ball milling of the drug with Neusilin were found to produce the amorphous phase. However, the ball‐milled (BM) material exhibited superior physical stability when compared with the cryomilled material at 40°C/75% relative humidity. 13C solid‐state nuclear magnetic resonance investigation of the BM material revealed an acid–base reaction between Sulindac and Neusilin. Optimal milling conditions and the kinetics of salt formation were also established. As benchtop milling is a laboratory‐scale process, a scalable process was developed to make Sulindac–Neusilin amorphous drug complex using hot‐melt extrusion (HME). The dissolution properties of the resulting HME material was found to have been improved over the material made by benchtop milling while maintaining similar physical stability. The HME material was used to make tablets using a direct compression method. The HME tablets were found to have better dissolution properties than tablets made from crystalline Sulindac. For the broad class of acidic drugs containing the carboxyl moiety, inorganic silicates such as Neusilin would offer a better choice than organic polymers to stabilize the amorphous phase. © 2011 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3332–3344, 2011</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.22583</identifier><identifier>PMID: 21520086</identifier><identifier>CODEN: JPMSAE</identifier><language>eng</language><publisher>Hoboken: Elsevier Inc</publisher><subject>Acids ; Aluminum Compounds ; Aluminum Silicates - chemistry ; amorphous ; Biological and medical sciences ; Compressive Strength ; Drug Stability ; extrusion ; General pharmacology ; Magnesium - chemistry ; Magnesium Compounds ; Medical sciences ; milling ; Molecular Structure ; Neusilin ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Phase Transition ; Salts ; Silicates ; solid-state NMR ; Solubility ; Sulindac - chemistry ; Technology, Pharmaceutical - methods ; Transition Temperature</subject><ispartof>Journal of pharmaceutical sciences, 2011-08, Vol.100 (8), p.3332-3344</ispartof><rights>2011 Wiley-Liss, Inc.</rights><rights>Copyright © 2011 Wiley‐Liss, Inc.</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2011 Wiley-Liss, Inc.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4903-6d61502f7c1acf85c27f3366a730f00c1bac50d8544e442a4dec94cdcae35bc13</citedby><cites>FETCH-LOGICAL-c4903-6d61502f7c1acf85c27f3366a730f00c1bac50d8544e442a4dec94cdcae35bc13</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.22583$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.22583$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,778,782,1414,27907,27908,45557,45558</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=24354491$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21520086$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Maclean, Jenifer</creatorcontrib><creatorcontrib>Medina, Cesar</creatorcontrib><creatorcontrib>Daurio, Dominick</creatorcontrib><creatorcontrib>Alvarez‐Nunez, Fernando</creatorcontrib><creatorcontrib>Jona, Janan</creatorcontrib><creatorcontrib>Munson, Eric</creatorcontrib><creatorcontrib>Nagapudi, Karthik</creatorcontrib><title>Manufacture and Performance Evaluation of a Stable Amorphous Complex of an Acidic Drug Molecule and Neusilin</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>In this paper, we explore the use of Neusilin, an inorganic magnesium aluminometasilicate, to stabilize the amorphous form of an acidic drug Sulindac. Both cryomilling and ball milling of the drug with Neusilin were found to produce the amorphous phase. However, the ball‐milled (BM) material exhibited superior physical stability when compared with the cryomilled material at 40°C/75% relative humidity. 13C solid‐state nuclear magnetic resonance investigation of the BM material revealed an acid–base reaction between Sulindac and Neusilin. Optimal milling conditions and the kinetics of salt formation were also established. As benchtop milling is a laboratory‐scale process, a scalable process was developed to make Sulindac–Neusilin amorphous drug complex using hot‐melt extrusion (HME). The dissolution properties of the resulting HME material was found to have been improved over the material made by benchtop milling while maintaining similar physical stability. The HME material was used to make tablets using a direct compression method. The HME tablets were found to have better dissolution properties than tablets made from crystalline Sulindac. For the broad class of acidic drugs containing the carboxyl moiety, inorganic silicates such as Neusilin would offer a better choice than organic polymers to stabilize the amorphous phase. © 2011 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3332–3344, 2011</description><subject>Acids</subject><subject>Aluminum Compounds</subject><subject>Aluminum Silicates - chemistry</subject><subject>amorphous</subject><subject>Biological and medical sciences</subject><subject>Compressive Strength</subject><subject>Drug Stability</subject><subject>extrusion</subject><subject>General pharmacology</subject><subject>Magnesium - chemistry</subject><subject>Magnesium Compounds</subject><subject>Medical sciences</subject><subject>milling</subject><subject>Molecular Structure</subject><subject>Neusilin</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Phase Transition</subject><subject>Salts</subject><subject>Silicates</subject><subject>solid-state NMR</subject><subject>Solubility</subject><subject>Sulindac - chemistry</subject><subject>Technology, Pharmaceutical - methods</subject><subject>Transition Temperature</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kU9v1DAQxSMEokvhwBdAlhBCHNL6b5w9rpZ2oWpLUUFws7zOGLw4cbCT0n57vM22SAhOc5jfvHkzryieE3xAMKaHmz4dUCpq9qCYEUFxWWEiHxaz3KMlE3y-VzxJaYMxrrAQj4s9uqVwXc0Kf6a70WozjBGQ7hp0AdGG2OrOADq60n7UgwsdChZpdDnotQe0aEPsv4cxoWVoew_Xt90OLYxrnEFv4_gNnQUPZvST5jmMyXnXPS0eWe0TPNvV_eLz8dGn5bvy9MPq_XJxWho-x6ysmooITK00RBtbC0OlZayqtGTYYmzIWhuBm1pwDpxTzRswc24ao4GJtSFsv3g96fYx_BwhDap1yYD3uoNsW9WSEioZ3ZIv_yI3YYxdNqeIIJLVUlYyU28mysSQUgSr-uhaHW8UwWqbgMoJqNsEMvtipziuW2juybuXZ-DVDtDJaG9jfrVLfzieA-PzrbXDifvlPNz8f6M6ubi8W11OEy4NcH0_oeMPlY-QQn05Xyn6sf56fEJqtco8m3jIWVw5iCoZBzn4xkUwg2qC-8eBvwFQyLy7</recordid><startdate>201108</startdate><enddate>201108</enddate><creator>Maclean, Jenifer</creator><creator>Medina, Cesar</creator><creator>Daurio, Dominick</creator><creator>Alvarez‐Nunez, Fernando</creator><creator>Jona, Janan</creator><creator>Munson, Eric</creator><creator>Nagapudi, Karthik</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><general>Wiley</general><general>American Pharmaceutical Association</general><general>Elsevier Limited</general><scope>BSCLL</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>RC3</scope><scope>7X8</scope></search><sort><creationdate>201108</creationdate><title>Manufacture and Performance Evaluation of a Stable Amorphous Complex of an Acidic Drug Molecule and Neusilin</title><author>Maclean, Jenifer ; Medina, Cesar ; Daurio, Dominick ; Alvarez‐Nunez, Fernando ; Jona, Janan ; Munson, Eric ; Nagapudi, Karthik</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4903-6d61502f7c1acf85c27f3366a730f00c1bac50d8544e442a4dec94cdcae35bc13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Acids</topic><topic>Aluminum Compounds</topic><topic>Aluminum Silicates - chemistry</topic><topic>amorphous</topic><topic>Biological and medical sciences</topic><topic>Compressive Strength</topic><topic>Drug Stability</topic><topic>extrusion</topic><topic>General pharmacology</topic><topic>Magnesium - chemistry</topic><topic>Magnesium Compounds</topic><topic>Medical sciences</topic><topic>milling</topic><topic>Molecular Structure</topic><topic>Neusilin</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Phase Transition</topic><topic>Salts</topic><topic>Silicates</topic><topic>solid-state NMR</topic><topic>Solubility</topic><topic>Sulindac - chemistry</topic><topic>Technology, Pharmaceutical - methods</topic><topic>Transition Temperature</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Maclean, Jenifer</creatorcontrib><creatorcontrib>Medina, Cesar</creatorcontrib><creatorcontrib>Daurio, Dominick</creatorcontrib><creatorcontrib>Alvarez‐Nunez, Fernando</creatorcontrib><creatorcontrib>Jona, Janan</creatorcontrib><creatorcontrib>Munson, Eric</creatorcontrib><creatorcontrib>Nagapudi, Karthik</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Maclean, Jenifer</au><au>Medina, Cesar</au><au>Daurio, Dominick</au><au>Alvarez‐Nunez, Fernando</au><au>Jona, Janan</au><au>Munson, Eric</au><au>Nagapudi, Karthik</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Manufacture and Performance Evaluation of a Stable Amorphous Complex of an Acidic Drug Molecule and Neusilin</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>2011-08</date><risdate>2011</risdate><volume>100</volume><issue>8</issue><spage>3332</spage><epage>3344</epage><pages>3332-3344</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><coden>JPMSAE</coden><abstract>In this paper, we explore the use of Neusilin, an inorganic magnesium aluminometasilicate, to stabilize the amorphous form of an acidic drug Sulindac. Both cryomilling and ball milling of the drug with Neusilin were found to produce the amorphous phase. However, the ball‐milled (BM) material exhibited superior physical stability when compared with the cryomilled material at 40°C/75% relative humidity. 13C solid‐state nuclear magnetic resonance investigation of the BM material revealed an acid–base reaction between Sulindac and Neusilin. Optimal milling conditions and the kinetics of salt formation were also established. As benchtop milling is a laboratory‐scale process, a scalable process was developed to make Sulindac–Neusilin amorphous drug complex using hot‐melt extrusion (HME). The dissolution properties of the resulting HME material was found to have been improved over the material made by benchtop milling while maintaining similar physical stability. The HME material was used to make tablets using a direct compression method. The HME tablets were found to have better dissolution properties than tablets made from crystalline Sulindac. For the broad class of acidic drugs containing the carboxyl moiety, inorganic silicates such as Neusilin would offer a better choice than organic polymers to stabilize the amorphous phase. © 2011 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3332–3344, 2011</abstract><cop>Hoboken</cop><pub>Elsevier Inc</pub><pmid>21520086</pmid><doi>10.1002/jps.22583</doi><tpages>13</tpages></addata></record> |
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| subjects | Acids Aluminum Compounds Aluminum Silicates - chemistry amorphous Biological and medical sciences Compressive Strength Drug Stability extrusion General pharmacology Magnesium - chemistry Magnesium Compounds Medical sciences milling Molecular Structure Neusilin Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Phase Transition Salts Silicates solid-state NMR Solubility Sulindac - chemistry Technology, Pharmaceutical - methods Transition Temperature |
| title | Manufacture and Performance Evaluation of a Stable Amorphous Complex of an Acidic Drug Molecule and Neusilin |
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