Further improvement of orally disintegrating tablets using micronized ethylcellulose
The aim of this study is to design a new orally disintegrating tablet (ODT) containing micronized ethylcellulose (MEC). The new ODT was prepared by physical mixing of rapidly disintegrating granules (RDGs) with MEC. To obtain RDGs, mannitol was spray-coated with a suspension of corn starch and crosp...
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| Veröffentlicht in: | International journal of pharmaceutics 2012-02, Vol.423 (2), p.351-359 |
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| creator | Okuda, Yutaka Irisawa, Yosuke Okimoto, Kazuto Osawa, Takashi Yamashita, Shinji |
| description | The aim of this study is to design a new orally disintegrating tablet (ODT) containing micronized ethylcellulose (MEC). The new ODT was prepared by physical mixing of rapidly disintegrating granules (RDGs) with MEC. To obtain RDGs, mannitol was spray-coated with a suspension of corn starch and crospovidone (9:1, w/w ratio) using a fluidized-bed granulator (suspension spray-coating method). The new ODTs were evaluated for their hardness, friability, thickness, internal structure (X-ray-CT scanning), in vivo disintegration time, and water absorption rate. Since MEC increases tablet hardness by increasing the contact frequency between the granules, the new ODTs could obtain high hardness (>50N) and low friability ( |
| doi_str_mv | 10.1016/j.ijpharm.2011.10.050 |
| format | Article |
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In conclusion, the new ODTs containing MEC developed in this study possessed superior properties for clinical use and are expected to be applied for a wide range of functionally released drugs for bitter taste masking, sustained release, and controlled release (pH-dependent film coating, matrix, and microcapsule).</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2011.10.050</identifier><identifier>PMID: 22138608</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Absorption ; Administration, Oral ; Capillary channels ; Cellulose - analogs & derivatives ; Cellulose - chemistry ; Chemistry, Pharmaceutical ; Drug Compounding ; Excipients - chemistry ; Hardness ; Hardness Tests ; Humidity ; Kinetics ; Mannitol - chemistry ; Micronized ethylcellulose ; Models, Chemical ; Orally disintegrating tablet ; Physical strength ; Povidone - chemistry ; Solubility ; Starch - chemistry ; Suspension spray-coating method ; Tablets ; Technology, Pharmaceutical - methods ; Tomography, X-Ray Computed ; Water - chemistry ; Wettability ; Wicking action</subject><ispartof>International journal of pharmaceutics, 2012-02, Vol.423 (2), p.351-359</ispartof><rights>2011 Elsevier B.V.</rights><rights>Copyright © 2011 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c430t-a440a6ed4914e4665806f91d8472aa7e2eca8a2fcc1841449d20a06afdfde5c93</citedby><cites>FETCH-LOGICAL-c430t-a440a6ed4914e4665806f91d8472aa7e2eca8a2fcc1841449d20a06afdfde5c93</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ijpharm.2011.10.050$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,778,782,3539,27911,27912,45982</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22138608$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Okuda, Yutaka</creatorcontrib><creatorcontrib>Irisawa, Yosuke</creatorcontrib><creatorcontrib>Okimoto, Kazuto</creatorcontrib><creatorcontrib>Osawa, Takashi</creatorcontrib><creatorcontrib>Yamashita, Shinji</creatorcontrib><title>Further improvement of orally disintegrating tablets using micronized ethylcellulose</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The aim of this study is to design a new orally disintegrating tablet (ODT) containing micronized ethylcellulose (MEC). The new ODT was prepared by physical mixing of rapidly disintegrating granules (RDGs) with MEC. To obtain RDGs, mannitol was spray-coated with a suspension of corn starch and crospovidone (9:1, w/w ratio) using a fluidized-bed granulator (suspension spray-coating method). The new ODTs were evaluated for their hardness, friability, thickness, internal structure (X-ray-CT scanning), in vivo disintegration time, and water absorption rate. Since MEC increases tablet hardness by increasing the contact frequency between the granules, the new ODTs could obtain high hardness (>50N) and low friability (<0.5%) with relatively low compression force. In addition, fine capillary channels formed in ODTs facilitated the wicking action and enabled rapid disintegration in vivo (<30s). On the other hand, since MEC has low hygroscopicity, the tablet hardness of ODTs containing MEC remained high for 1 month in high-humidity conditions.
In conclusion, the new ODTs containing MEC developed in this study possessed superior properties for clinical use and are expected to be applied for a wide range of functionally released drugs for bitter taste masking, sustained release, and controlled release (pH-dependent film coating, matrix, and microcapsule).</description><subject>Absorption</subject><subject>Administration, Oral</subject><subject>Capillary channels</subject><subject>Cellulose - analogs & derivatives</subject><subject>Cellulose - chemistry</subject><subject>Chemistry, Pharmaceutical</subject><subject>Drug Compounding</subject><subject>Excipients - chemistry</subject><subject>Hardness</subject><subject>Hardness Tests</subject><subject>Humidity</subject><subject>Kinetics</subject><subject>Mannitol - chemistry</subject><subject>Micronized ethylcellulose</subject><subject>Models, Chemical</subject><subject>Orally disintegrating tablet</subject><subject>Physical strength</subject><subject>Povidone - chemistry</subject><subject>Solubility</subject><subject>Starch - chemistry</subject><subject>Suspension spray-coating method</subject><subject>Tablets</subject><subject>Technology, Pharmaceutical - methods</subject><subject>Tomography, X-Ray Computed</subject><subject>Water - chemistry</subject><subject>Wettability</subject><subject>Wicking action</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE9PwzAMxSMEgjH4CKDeOHU4aZq2J4QQA6RJXMY5yhJ3y9Q_I0mRxqcn1QZXTpat9-znHyE3FGYUqLjfzux2t1GunTGgNM5mkMMJmdCyyNKMF-KUTCAryjSnRXZBLr3fAoBgNDsnFyyWUkA5Icv54MIGXWLbneu_sMUuJH2d9E41zT4x1tsu4NqpYLt1EtSqweCTwY9da7XrO_uNJsGw2Tcam2Zoeo9X5KxWjcfrY52Sj_nz8uk1Xby_vD09LlLNMwip4hyUQMMrypELkZcg6oqakhdMqQIZalUqVmtNS045rwwDBULVpjaY6yqbkrvD3hj9c0AfZGv9mEJ12A9eVgxYFo08KvODMib23mEtd862yu0lBTnylFt55ClHnuM48oy-2-OFYdWi-XP9AoyCh4MA459fFp302mKn0ViHOkjT239O_ABhCYuO</recordid><startdate>20120228</startdate><enddate>20120228</enddate><creator>Okuda, Yutaka</creator><creator>Irisawa, Yosuke</creator><creator>Okimoto, Kazuto</creator><creator>Osawa, Takashi</creator><creator>Yamashita, Shinji</creator><general>Elsevier B.V</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>7X8</scope></search><sort><creationdate>20120228</creationdate><title>Further improvement of orally disintegrating tablets using micronized ethylcellulose</title><author>Okuda, Yutaka ; Irisawa, Yosuke ; Okimoto, Kazuto ; Osawa, Takashi ; Yamashita, Shinji</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c430t-a440a6ed4914e4665806f91d8472aa7e2eca8a2fcc1841449d20a06afdfde5c93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Absorption</topic><topic>Administration, Oral</topic><topic>Capillary channels</topic><topic>Cellulose - analogs & derivatives</topic><topic>Cellulose - chemistry</topic><topic>Chemistry, Pharmaceutical</topic><topic>Drug Compounding</topic><topic>Excipients - chemistry</topic><topic>Hardness</topic><topic>Hardness Tests</topic><topic>Humidity</topic><topic>Kinetics</topic><topic>Mannitol - chemistry</topic><topic>Micronized ethylcellulose</topic><topic>Models, Chemical</topic><topic>Orally disintegrating tablet</topic><topic>Physical strength</topic><topic>Povidone - chemistry</topic><topic>Solubility</topic><topic>Starch - chemistry</topic><topic>Suspension spray-coating method</topic><topic>Tablets</topic><topic>Technology, Pharmaceutical - methods</topic><topic>Tomography, X-Ray Computed</topic><topic>Water - chemistry</topic><topic>Wettability</topic><topic>Wicking action</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Okuda, Yutaka</creatorcontrib><creatorcontrib>Irisawa, Yosuke</creatorcontrib><creatorcontrib>Okimoto, Kazuto</creatorcontrib><creatorcontrib>Osawa, Takashi</creatorcontrib><creatorcontrib>Yamashita, Shinji</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Okuda, Yutaka</au><au>Irisawa, Yosuke</au><au>Okimoto, Kazuto</au><au>Osawa, Takashi</au><au>Yamashita, Shinji</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Further improvement of orally disintegrating tablets using micronized ethylcellulose</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2012-02-28</date><risdate>2012</risdate><volume>423</volume><issue>2</issue><spage>351</spage><epage>359</epage><pages>351-359</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>The aim of this study is to design a new orally disintegrating tablet (ODT) containing micronized ethylcellulose (MEC). The new ODT was prepared by physical mixing of rapidly disintegrating granules (RDGs) with MEC. To obtain RDGs, mannitol was spray-coated with a suspension of corn starch and crospovidone (9:1, w/w ratio) using a fluidized-bed granulator (suspension spray-coating method). The new ODTs were evaluated for their hardness, friability, thickness, internal structure (X-ray-CT scanning), in vivo disintegration time, and water absorption rate. Since MEC increases tablet hardness by increasing the contact frequency between the granules, the new ODTs could obtain high hardness (>50N) and low friability (<0.5%) with relatively low compression force. In addition, fine capillary channels formed in ODTs facilitated the wicking action and enabled rapid disintegration in vivo (<30s). On the other hand, since MEC has low hygroscopicity, the tablet hardness of ODTs containing MEC remained high for 1 month in high-humidity conditions.
In conclusion, the new ODTs containing MEC developed in this study possessed superior properties for clinical use and are expected to be applied for a wide range of functionally released drugs for bitter taste masking, sustained release, and controlled release (pH-dependent film coating, matrix, and microcapsule).</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>22138608</pmid><doi>10.1016/j.ijpharm.2011.10.050</doi><tpages>9</tpages></addata></record> |
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| subjects | Absorption Administration, Oral Capillary channels Cellulose - analogs & derivatives Cellulose - chemistry Chemistry, Pharmaceutical Drug Compounding Excipients - chemistry Hardness Hardness Tests Humidity Kinetics Mannitol - chemistry Micronized ethylcellulose Models, Chemical Orally disintegrating tablet Physical strength Povidone - chemistry Solubility Starch - chemistry Suspension spray-coating method Tablets Technology, Pharmaceutical - methods Tomography, X-Ray Computed Water - chemistry Wettability Wicking action |
| title | Further improvement of orally disintegrating tablets using micronized ethylcellulose |
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