Dosage form design and in vitro/ in vivo evaluation of cevimeline extended-release tablet formulations
The objective of the present work is to develop an extended-release dosage form of cevimeline. Two types of extended-release tablets (simple matrix tablets and press-coated tablets) were prepared and their potential as extended-release dosage forms were assessed. Simple matrix tablets have a large a...
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| Veröffentlicht in: | International journal of pharmaceutics 2010-01, Vol.383 (1), p.99-105 |
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| container_title | International journal of pharmaceutics |
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| creator | Tajiri, Shinichiro Kanamaru, Taro Makoto, Kamada Konno, Tsutomu Nakagami, Hiroaki |
| description | The objective of the present work is to develop an extended-release dosage form of cevimeline. Two types of extended-release tablets (simple matrix tablets and press-coated tablets) were prepared and their potential as extended-release dosage forms were assessed. Simple matrix tablets have a large amount of hydroxypropylcellulose as a rate-controlling polymer and the matrix is homogeneous throughout the tablet. The press-coated tablets consisted of a matrix core tablet, which was completely surrounded by an outer shell containing a large amount of hydroxypropylcellulose. The simple matrix tablets could not sustain the release of cevimeline effectively. In contrast, the press-coated tablets showed a slower dissolution rate compared with simple matrix tablets and the release curve was nearly linear. The dissolution of cevimeline from the press-coated tablets was not markedly affected by the pH of the dissolution medium or by a paddle rotating speed over the range of 50–200
rpm. Furthermore, cevimeline was constantly released from the press-coated tablets in the gastrointestinal tract and the steady-state plasma drug levels were maintained in beagle dogs. These results suggested that the designed PC tablets have a potential for extended-release dosage forms. |
| doi_str_mv | 10.1016/j.ijpharm.2009.09.007 |
| format | Article |
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rpm. Furthermore, cevimeline was constantly released from the press-coated tablets in the gastrointestinal tract and the steady-state plasma drug levels were maintained in beagle dogs. These results suggested that the designed PC tablets have a potential for extended-release dosage forms.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2009.09.007</identifier><identifier>PMID: 19747964</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Animals ; Biological and medical sciences ; Cevimeline ; Chemistry, Pharmaceutical - methods ; Delayed-Action Preparations - administration & dosage ; Delayed-Action Preparations - chemistry ; Delayed-Action Preparations - metabolism ; Dogs ; Dosage Forms ; Drug Design ; Drug Evaluation, Preclinical - methods ; Extended-release tablets ; General pharmacology ; Hydroxypropylcellulose ; Male ; Medical sciences ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Press-coated tablets ; Quinuclidines - administration & dosage ; Quinuclidines - chemistry ; Quinuclidines - metabolism ; Tablets ; Tablets, Enteric-Coated ; Thiophenes - administration & dosage ; Thiophenes - chemistry ; Thiophenes - metabolism</subject><ispartof>International journal of pharmaceutics, 2010-01, Vol.383 (1), p.99-105</ispartof><rights>2009 Elsevier B.V.</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c394t-608cc07979eadb6531ee188a2ffdc33819a4aff9b7809149fb86d780c30376ac3</citedby><cites>FETCH-LOGICAL-c394t-608cc07979eadb6531ee188a2ffdc33819a4aff9b7809149fb86d780c30376ac3</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.2009.09.007$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27929,27930,46000</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22271752$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19747964$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tajiri, Shinichiro</creatorcontrib><creatorcontrib>Kanamaru, Taro</creatorcontrib><creatorcontrib>Makoto, Kamada</creatorcontrib><creatorcontrib>Konno, Tsutomu</creatorcontrib><creatorcontrib>Nakagami, Hiroaki</creatorcontrib><title>Dosage form design and in vitro/ in vivo evaluation of cevimeline extended-release tablet formulations</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The objective of the present work is to develop an extended-release dosage form of cevimeline. Two types of extended-release tablets (simple matrix tablets and press-coated tablets) were prepared and their potential as extended-release dosage forms were assessed. Simple matrix tablets have a large amount of hydroxypropylcellulose as a rate-controlling polymer and the matrix is homogeneous throughout the tablet. The press-coated tablets consisted of a matrix core tablet, which was completely surrounded by an outer shell containing a large amount of hydroxypropylcellulose. The simple matrix tablets could not sustain the release of cevimeline effectively. In contrast, the press-coated tablets showed a slower dissolution rate compared with simple matrix tablets and the release curve was nearly linear. The dissolution of cevimeline from the press-coated tablets was not markedly affected by the pH of the dissolution medium or by a paddle rotating speed over the range of 50–200
rpm. Furthermore, cevimeline was constantly released from the press-coated tablets in the gastrointestinal tract and the steady-state plasma drug levels were maintained in beagle dogs. These results suggested that the designed PC tablets have a potential for extended-release dosage forms.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cevimeline</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Delayed-Action Preparations - administration & dosage</subject><subject>Delayed-Action Preparations - chemistry</subject><subject>Delayed-Action Preparations - metabolism</subject><subject>Dogs</subject><subject>Dosage Forms</subject><subject>Drug Design</subject><subject>Drug Evaluation, Preclinical - methods</subject><subject>Extended-release tablets</subject><subject>General pharmacology</subject><subject>Hydroxypropylcellulose</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Press-coated tablets</subject><subject>Quinuclidines - administration & dosage</subject><subject>Quinuclidines - chemistry</subject><subject>Quinuclidines - metabolism</subject><subject>Tablets</subject><subject>Tablets, Enteric-Coated</subject><subject>Thiophenes - administration & dosage</subject><subject>Thiophenes - chemistry</subject><subject>Thiophenes - metabolism</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkMFu1DAQhi1ERZeFRwD5gnrK1o6zdnxCqJSCVIkLnK2JPS5eOfFiJxF9e7LdCI6VRvIcvn888xHyjrMdZ1xeH3bhcPwFud_VjOndqZh6QTa8VaISjZIvyYYJ1VZ7rsQleV3KgTEmay5ekUuuVaO0bDbEf04FHpD6lHvqsISHgcLgaBjoHMacrs_dnCjOECcYQxpo8tTiHHqMYUCKf0YcHLoqY0QoSEfoIo5PI6f4lChvyIWHWPDt-m7Jzy-3P26-Vvff777dfLqvrNDNWEnWWsuUVhrBdXIvOCJvW6i9d1aIlmtowHvdqZZp3mjftdItvRXLqRKs2JKr89xjTr8nLKPpQ7EYIwyYpmKUaPi-Flou5P5M2pxKyejNMYce8qPhzJwMm4NZDZuTYXMqppbc-_WHqevR_U-tShfgwwpAsRB9hsGG8o-r61pxteywJR_PHC4-5oDZFBtwsOhCRjsal8Izq_wFpoOdug</recordid><startdate>20100104</startdate><enddate>20100104</enddate><creator>Tajiri, Shinichiro</creator><creator>Kanamaru, Taro</creator><creator>Makoto, Kamada</creator><creator>Konno, Tsutomu</creator><creator>Nakagami, Hiroaki</creator><general>Elsevier B.V</general><general>Elsevier</general><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>7X8</scope></search><sort><creationdate>20100104</creationdate><title>Dosage form design and in vitro/ in vivo evaluation of cevimeline extended-release tablet formulations</title><author>Tajiri, Shinichiro ; Kanamaru, Taro ; Makoto, Kamada ; Konno, Tsutomu ; Nakagami, Hiroaki</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c394t-608cc07979eadb6531ee188a2ffdc33819a4aff9b7809149fb86d780c30376ac3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cevimeline</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Delayed-Action Preparations - administration & dosage</topic><topic>Delayed-Action Preparations - chemistry</topic><topic>Delayed-Action Preparations - metabolism</topic><topic>Dogs</topic><topic>Dosage Forms</topic><topic>Drug Design</topic><topic>Drug Evaluation, Preclinical - methods</topic><topic>Extended-release tablets</topic><topic>General pharmacology</topic><topic>Hydroxypropylcellulose</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Press-coated tablets</topic><topic>Quinuclidines - administration & dosage</topic><topic>Quinuclidines - chemistry</topic><topic>Quinuclidines - metabolism</topic><topic>Tablets</topic><topic>Tablets, Enteric-Coated</topic><topic>Thiophenes - administration & dosage</topic><topic>Thiophenes - chemistry</topic><topic>Thiophenes - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tajiri, Shinichiro</creatorcontrib><creatorcontrib>Kanamaru, Taro</creatorcontrib><creatorcontrib>Makoto, Kamada</creatorcontrib><creatorcontrib>Konno, Tsutomu</creatorcontrib><creatorcontrib>Nakagami, Hiroaki</creatorcontrib><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>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tajiri, Shinichiro</au><au>Kanamaru, Taro</au><au>Makoto, Kamada</au><au>Konno, Tsutomu</au><au>Nakagami, Hiroaki</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Dosage form design and in vitro/ in vivo evaluation of cevimeline extended-release tablet formulations</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2010-01-04</date><risdate>2010</risdate><volume>383</volume><issue>1</issue><spage>99</spage><epage>105</epage><pages>99-105</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The objective of the present work is to develop an extended-release dosage form of cevimeline. Two types of extended-release tablets (simple matrix tablets and press-coated tablets) were prepared and their potential as extended-release dosage forms were assessed. Simple matrix tablets have a large amount of hydroxypropylcellulose as a rate-controlling polymer and the matrix is homogeneous throughout the tablet. The press-coated tablets consisted of a matrix core tablet, which was completely surrounded by an outer shell containing a large amount of hydroxypropylcellulose. The simple matrix tablets could not sustain the release of cevimeline effectively. In contrast, the press-coated tablets showed a slower dissolution rate compared with simple matrix tablets and the release curve was nearly linear. The dissolution of cevimeline from the press-coated tablets was not markedly affected by the pH of the dissolution medium or by a paddle rotating speed over the range of 50–200
rpm. Furthermore, cevimeline was constantly released from the press-coated tablets in the gastrointestinal tract and the steady-state plasma drug levels were maintained in beagle dogs. These results suggested that the designed PC tablets have a potential for extended-release dosage forms.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>19747964</pmid><doi>10.1016/j.ijpharm.2009.09.007</doi><tpages>7</tpages></addata></record> |
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| subjects | Animals Biological and medical sciences Cevimeline Chemistry, Pharmaceutical - methods Delayed-Action Preparations - administration & dosage Delayed-Action Preparations - chemistry Delayed-Action Preparations - metabolism Dogs Dosage Forms Drug Design Drug Evaluation, Preclinical - methods Extended-release tablets General pharmacology Hydroxypropylcellulose Male Medical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Press-coated tablets Quinuclidines - administration & dosage Quinuclidines - chemistry Quinuclidines - metabolism Tablets Tablets, Enteric-Coated Thiophenes - administration & dosage Thiophenes - chemistry Thiophenes - metabolism |
| title | Dosage form design and in vitro/ in vivo evaluation of cevimeline extended-release tablet formulations |
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