Optimization of Premix Powders for Tableting Use
Direct compression is a popular choice as it provides the simplest way to prepare the tablet. It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prep...
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Veröffentlicht in: | Chemical & pharmaceutical bulletin 2018/07/01, Vol.66(7), pp.748-756 |
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creator | Todo, Hiroaki Sato, Kazuki Takayama, Kozo Sugibayashi, Kenji |
description | Direct compression is a popular choice as it provides the simplest way to prepare the tablet. It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prepared in advance for tableting use. The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using statistical techniques. Based on the “Quality by Design” concept, a (3,3)-simplex lattice design consisting of three components, LAC, CS, and MCC was employed to prepare the model premix powders. Response surface method incorporating a thin-plate spline interpolation (RSM-S) was applied for estimation of the optimum premix powders for tableting use. The effect of tablet shape identified by the surface curvature on the optimization was investigated. The optimum premix powder was effective when the premix was applied to a small quantity of API, although the function of premix was limited in the case of the formulation of large amount of API. Statistical techniques are valuable to exploit new functions of well-known materials such as LAC, CS, and MCC. |
doi_str_mv | 10.1248/cpb.c18-00213 |
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It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prepared in advance for tableting use. The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using statistical techniques. Based on the “Quality by Design” concept, a (3,3)-simplex lattice design consisting of three components, LAC, CS, and MCC was employed to prepare the model premix powders. Response surface method incorporating a thin-plate spline interpolation (RSM-S) was applied for estimation of the optimum premix powders for tableting use. The effect of tablet shape identified by the surface curvature on the optimization was investigated. The optimum premix powder was effective when the premix was applied to a small quantity of API, although the function of premix was limited in the case of the formulation of large amount of API. Statistical techniques are valuable to exploit new functions of well-known materials such as LAC, CS, and MCC.</description><identifier>ISSN: 0009-2363</identifier><identifier>EISSN: 1347-5223</identifier><identifier>DOI: 10.1248/cpb.c18-00213</identifier><identifier>PMID: 29743471</identifier><language>eng</language><publisher>Japan: The Pharmaceutical Society of Japan</publisher><subject>Cellulose ; Cellulose - chemistry ; Compression ; Crystalline cellulose ; Curvature ; direct compression ; Drug Compounding ; Drying ; Interpolation ; Lactose ; Lactose - chemistry ; Lattice design ; Optimization ; Powder ; Powders - chemical synthesis ; Powders - chemistry ; premix powder ; quality by design ; Response surface methodology ; Shape effects ; simplex lattice design ; Starch - chemistry ; Statistical analysis ; Statistical methods ; Surface Properties ; tablet ; Tablets - chemical synthesis ; Tablets - chemistry ; Tensile Strength ; thin-plate spline</subject><ispartof>Chemical and Pharmaceutical Bulletin, 2018/07/01, Vol.66(7), pp.748-756</ispartof><rights>2018 The Pharmaceutical Society of Japan</rights><rights>Copyright Japan Science and Technology Agency 2018</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c697t-521202c694a6d01766d964c1227d8c5c1b7c6284f3aa021de7fe4baf91c360c23</citedby><cites>FETCH-LOGICAL-c697t-521202c694a6d01766d964c1227d8c5c1b7c6284f3aa021de7fe4baf91c360c23</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1883,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/29743471$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Todo, Hiroaki</creatorcontrib><creatorcontrib>Sato, Kazuki</creatorcontrib><creatorcontrib>Takayama, Kozo</creatorcontrib><creatorcontrib>Sugibayashi, Kenji</creatorcontrib><creatorcontrib>Department of Pharmaceutical Sciences</creatorcontrib><creatorcontrib>Faculty of Pharmacy and Pharmaceutical Sciences</creatorcontrib><creatorcontrib>Josai University</creatorcontrib><title>Optimization of Premix Powders for Tableting Use</title><title>Chemical & pharmaceutical bulletin</title><addtitle>Chem. Pharm. Bull.</addtitle><description>Direct compression is a popular choice as it provides the simplest way to prepare the tablet. It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prepared in advance for tableting use. The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using statistical techniques. Based on the “Quality by Design” concept, a (3,3)-simplex lattice design consisting of three components, LAC, CS, and MCC was employed to prepare the model premix powders. Response surface method incorporating a thin-plate spline interpolation (RSM-S) was applied for estimation of the optimum premix powders for tableting use. The effect of tablet shape identified by the surface curvature on the optimization was investigated. The optimum premix powder was effective when the premix was applied to a small quantity of API, although the function of premix was limited in the case of the formulation of large amount of API. Statistical techniques are valuable to exploit new functions of well-known materials such as LAC, CS, and MCC.</description><subject>Cellulose</subject><subject>Cellulose - chemistry</subject><subject>Compression</subject><subject>Crystalline cellulose</subject><subject>Curvature</subject><subject>direct compression</subject><subject>Drug Compounding</subject><subject>Drying</subject><subject>Interpolation</subject><subject>Lactose</subject><subject>Lactose - chemistry</subject><subject>Lattice design</subject><subject>Optimization</subject><subject>Powder</subject><subject>Powders - chemical synthesis</subject><subject>Powders - chemistry</subject><subject>premix powder</subject><subject>quality by design</subject><subject>Response surface methodology</subject><subject>Shape effects</subject><subject>simplex lattice design</subject><subject>Starch - chemistry</subject><subject>Statistical analysis</subject><subject>Statistical methods</subject><subject>Surface Properties</subject><subject>tablet</subject><subject>Tablets - chemical synthesis</subject><subject>Tablets - chemistry</subject><subject>Tensile Strength</subject><subject>thin-plate spline</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkE1P3DAQhq2KChbKsdcqEhcugRnbsTdHtCofEhIc4Gw5jgNeJfHWzgraX99hFxaJi8fSPHrn1cPYT4Qz5HJ-7lbNmcN5CcBRfGMzFFKXFedij80AoC65UOKAHea8JKQCLfbZAa-1JA5nDO5WUxjCPzuFOBaxK-6TH8JrcR9fWp9y0cVUPNim91MYn4rH7H-w753tsz9-n0fs8fL3w-K6vL27ullc3JZO1XqiBsiB019a1QJqpdpaSYec63buKoeNdorPZSespeat152Xje1qdEKB4-KInW5zVyn-Wfs8mSFk5_vejj6us-EgNFRaaST05Au6jOs0UjtDHrhEqVRFVLmlXIo5J9-ZVQqDTX8NgnlTaUilIZVmo5L4X--p62bw7Y7-cEfA1RagbXC2j2MfRv9522XtnkkmVd2EKgWaRm1A0zHQlRKIqGqgpMU2aZkn--R3p2yaguv9pphSRr89u4Kf22ebjB_Ff5O5mrE</recordid><startdate>20180701</startdate><enddate>20180701</enddate><creator>Todo, Hiroaki</creator><creator>Sato, Kazuki</creator><creator>Takayama, Kozo</creator><creator>Sugibayashi, Kenji</creator><general>The Pharmaceutical Society of Japan</general><general>Pharmaceutical Society of Japan</general><general>Japan Science and Technology Agency</general><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>7TK</scope><scope>7TM</scope><scope>7U9</scope><scope>H94</scope><scope>7X8</scope></search><sort><creationdate>20180701</creationdate><title>Optimization of Premix Powders for Tableting Use</title><author>Todo, Hiroaki ; Sato, Kazuki ; Takayama, Kozo ; Sugibayashi, Kenji</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c697t-521202c694a6d01766d964c1227d8c5c1b7c6284f3aa021de7fe4baf91c360c23</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Cellulose</topic><topic>Cellulose - chemistry</topic><topic>Compression</topic><topic>Crystalline cellulose</topic><topic>Curvature</topic><topic>direct compression</topic><topic>Drug Compounding</topic><topic>Drying</topic><topic>Interpolation</topic><topic>Lactose</topic><topic>Lactose - chemistry</topic><topic>Lattice design</topic><topic>Optimization</topic><topic>Powder</topic><topic>Powders - chemical synthesis</topic><topic>Powders - chemistry</topic><topic>premix powder</topic><topic>quality by design</topic><topic>Response surface methodology</topic><topic>Shape effects</topic><topic>simplex lattice design</topic><topic>Starch - chemistry</topic><topic>Statistical analysis</topic><topic>Statistical methods</topic><topic>Surface Properties</topic><topic>tablet</topic><topic>Tablets - chemical synthesis</topic><topic>Tablets - chemistry</topic><topic>Tensile Strength</topic><topic>thin-plate spline</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Todo, Hiroaki</creatorcontrib><creatorcontrib>Sato, Kazuki</creatorcontrib><creatorcontrib>Takayama, Kozo</creatorcontrib><creatorcontrib>Sugibayashi, Kenji</creatorcontrib><creatorcontrib>Department of Pharmaceutical Sciences</creatorcontrib><creatorcontrib>Faculty of Pharmacy and Pharmaceutical Sciences</creatorcontrib><creatorcontrib>Josai University</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Todo, Hiroaki</au><au>Sato, Kazuki</au><au>Takayama, Kozo</au><au>Sugibayashi, Kenji</au><aucorp>Department of Pharmaceutical Sciences</aucorp><aucorp>Faculty of Pharmacy and Pharmaceutical Sciences</aucorp><aucorp>Josai University</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Optimization of Premix Powders for Tableting Use</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem. Pharm. Bull.</addtitle><date>2018-07-01</date><risdate>2018</risdate><volume>66</volume><issue>7</issue><spage>748</spage><epage>756</epage><pages>748-756</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><abstract>Direct compression is a popular choice as it provides the simplest way to prepare the tablet. It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prepared in advance for tableting use. The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using statistical techniques. Based on the “Quality by Design” concept, a (3,3)-simplex lattice design consisting of three components, LAC, CS, and MCC was employed to prepare the model premix powders. Response surface method incorporating a thin-plate spline interpolation (RSM-S) was applied for estimation of the optimum premix powders for tableting use. The effect of tablet shape identified by the surface curvature on the optimization was investigated. The optimum premix powder was effective when the premix was applied to a small quantity of API, although the function of premix was limited in the case of the formulation of large amount of API. Statistical techniques are valuable to exploit new functions of well-known materials such as LAC, CS, and MCC.</abstract><cop>Japan</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>29743471</pmid><doi>10.1248/cpb.c18-00213</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Cellulose Cellulose - chemistry Compression Crystalline cellulose Curvature direct compression Drug Compounding Drying Interpolation Lactose Lactose - chemistry Lattice design Optimization Powder Powders - chemical synthesis Powders - chemistry premix powder quality by design Response surface methodology Shape effects simplex lattice design Starch - chemistry Statistical analysis Statistical methods Surface Properties tablet Tablets - chemical synthesis Tablets - chemistry Tensile Strength thin-plate spline |
title | Optimization of Premix Powders for Tableting Use |
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