Formulation Development of Sustained-Release Hydrophilic Matrix Tablets of Zileuton
ABSTRACT The purpose of this paper was to develop a hydrophilic matrix system for extended oral delivery of zileuton, and study the effects of certain formulation, processing, and dissolution variables on in vitro drug release. Tablet formulations with 60-70% drug and varying release rates were prep...
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| Veröffentlicht in: | Pharmaceutical development and technology 1997, Vol.2 (3), p.197-204 |
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| container_title | Pharmaceutical development and technology |
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| creator | Qiu, Yihong Hui, Ho-Wah Cheskin, Howard |
| description | ABSTRACT
The purpose of this paper was to develop a hydrophilic matrix system for extended oral delivery of zileuton, and study the effects of certain formulation, processing, and dissolution variables on in vitro drug release. Tablet formulations with 60-70% drug and varying release rates were prepared by wet granulation using low and medium viscosity grades of hydroxypropylmethocellulose. In vitro drug release was evaluated using USP apparatus I. The in vitro drug release from all formulations followed zero-order kinetics and was independent of compression force. In general, the release rate decreased with increasing drug load and higher polymer concentration or viscosity. High-shear granulation also resulted in lower release rate. Accelerated release was observed with increased agitation as well as in the dissolution media with higher surfactant concentration and/or ionic strength. No stereoselective release from the matrix system was observed. The hydrophilic matrix system effectively controlled the in vitro release of zileuton. Matrix tablets with desired release rates can be prepared by adjusting various formulation and processing parameters. The matrix system also has the advantage of simple processing and relatively low cost. |
| doi_str_mv | 10.3109/10837459709031439 |
| format | Article |
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The purpose of this paper was to develop a hydrophilic matrix system for extended oral delivery of zileuton, and study the effects of certain formulation, processing, and dissolution variables on in vitro drug release. Tablet formulations with 60-70% drug and varying release rates were prepared by wet granulation using low and medium viscosity grades of hydroxypropylmethocellulose. In vitro drug release was evaluated using USP apparatus I. The in vitro drug release from all formulations followed zero-order kinetics and was independent of compression force. In general, the release rate decreased with increasing drug load and higher polymer concentration or viscosity. High-shear granulation also resulted in lower release rate. Accelerated release was observed with increased agitation as well as in the dissolution media with higher surfactant concentration and/or ionic strength. No stereoselective release from the matrix system was observed. The hydrophilic matrix system effectively controlled the in vitro release of zileuton. Matrix tablets with desired release rates can be prepared by adjusting various formulation and processing parameters. The matrix system also has the advantage of simple processing and relatively low cost.</description><identifier>ISSN: 1083-7450</identifier><identifier>EISSN: 1097-9867</identifier><identifier>DOI: 10.3109/10837459709031439</identifier><identifier>PMID: 9552447</identifier><language>eng</language><publisher>England: Informa UK Ltd</publisher><subject>5-lipoxygenase inhibitor ; Biological Availability ; Chemistry, Pharmaceutical ; Compressive Strength ; Delayed-Action Preparations ; Humans ; Hydroxyurea - analogs & derivatives ; Hydroxyurea - pharmacokinetics ; In vitro release ; Lipoxygenase Inhibitors - pharmacokinetics ; Matrix formulation ; Osmolar Concentration ; Polymers ; Rotation ; Solubility ; Surface-Active Agents ; Sustained-release ; Tablets ; Viscosity ; Water - chemistry ; Zileuton</subject><ispartof>Pharmaceutical development and technology, 1997, Vol.2 (3), p.197-204</ispartof><rights>1997 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1997</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c316t-ad3c5c1757a8ff93e67acf2fbca77ced4b5135034fe2261993d5fcfe95d97b0e3</citedby><cites>FETCH-LOGICAL-c316t-ad3c5c1757a8ff93e67acf2fbca77ced4b5135034fe2261993d5fcfe95d97b0e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/10837459709031439$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/10837459709031439$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,776,780,4010,27900,27901,27902,59620,59726,60409,60515,61194,61229,61375,61410</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9552447$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Qiu, Yihong</creatorcontrib><creatorcontrib>Hui, Ho-Wah</creatorcontrib><creatorcontrib>Cheskin, Howard</creatorcontrib><title>Formulation Development of Sustained-Release Hydrophilic Matrix Tablets of Zileuton</title><title>Pharmaceutical development and technology</title><addtitle>Pharm Dev Technol</addtitle><description>ABSTRACT
The purpose of this paper was to develop a hydrophilic matrix system for extended oral delivery of zileuton, and study the effects of certain formulation, processing, and dissolution variables on in vitro drug release. Tablet formulations with 60-70% drug and varying release rates were prepared by wet granulation using low and medium viscosity grades of hydroxypropylmethocellulose. In vitro drug release was evaluated using USP apparatus I. The in vitro drug release from all formulations followed zero-order kinetics and was independent of compression force. In general, the release rate decreased with increasing drug load and higher polymer concentration or viscosity. High-shear granulation also resulted in lower release rate. Accelerated release was observed with increased agitation as well as in the dissolution media with higher surfactant concentration and/or ionic strength. No stereoselective release from the matrix system was observed. The hydrophilic matrix system effectively controlled the in vitro release of zileuton. Matrix tablets with desired release rates can be prepared by adjusting various formulation and processing parameters. The matrix system also has the advantage of simple processing and relatively low cost.</description><subject>5-lipoxygenase inhibitor</subject><subject>Biological Availability</subject><subject>Chemistry, Pharmaceutical</subject><subject>Compressive Strength</subject><subject>Delayed-Action Preparations</subject><subject>Humans</subject><subject>Hydroxyurea - analogs & derivatives</subject><subject>Hydroxyurea - pharmacokinetics</subject><subject>In vitro release</subject><subject>Lipoxygenase Inhibitors - pharmacokinetics</subject><subject>Matrix formulation</subject><subject>Osmolar Concentration</subject><subject>Polymers</subject><subject>Rotation</subject><subject>Solubility</subject><subject>Surface-Active Agents</subject><subject>Sustained-release</subject><subject>Tablets</subject><subject>Viscosity</subject><subject>Water - chemistry</subject><subject>Zileuton</subject><issn>1083-7450</issn><issn>1097-9867</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1997</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtL7DAUx4MoXl8fwIXQ1d1Vk6aZNOjm4hsUwcfGTTlNT5hI2oxJqs63t8MMF0R0dQ7n_-DwI2Sf0UPOqDpitOKyFEpSRTkruVojW-Nd5qqayPXFXvF8NNA_ZDvGF0pZpajYJJtKiKIs5RZ5uPChGxwk6_vsDN_Q-VmHfcq8yR6GmMD22Ob36BAiZlfzNvjZ1Dqrs1tIwX5kj9A4THHhf7YOh-T7XbJhwEXcW80d8nRx_nh6ld_cXV6f_rvJNWeTlEPLtdBMCgmVMYrjRII2hWk0SKmxLRvBuKC8NFgUE6YUb4XRBpVolWwo8h3yd9k7C_51wJjqzkaNzkGPfoi1VEIWkonRyJZGHXyMAU09C7aDMK8ZrRcg628gx8zBqnxoOmz_J1bkRv1kqdvejAjh3QfX1gnmzgcToNc2Lqp_rj_-Ep8iuDTVELB-8UPoR26_PPcJGoiU2Q</recordid><startdate>1997</startdate><enddate>1997</enddate><creator>Qiu, Yihong</creator><creator>Hui, Ho-Wah</creator><creator>Cheskin, Howard</creator><general>Informa UK Ltd</general><general>Taylor & Francis</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>1997</creationdate><title>Formulation Development of Sustained-Release Hydrophilic Matrix Tablets of Zileuton</title><author>Qiu, Yihong ; Hui, Ho-Wah ; Cheskin, Howard</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c316t-ad3c5c1757a8ff93e67acf2fbca77ced4b5135034fe2261993d5fcfe95d97b0e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1997</creationdate><topic>5-lipoxygenase inhibitor</topic><topic>Biological Availability</topic><topic>Chemistry, Pharmaceutical</topic><topic>Compressive Strength</topic><topic>Delayed-Action Preparations</topic><topic>Humans</topic><topic>Hydroxyurea - analogs & derivatives</topic><topic>Hydroxyurea - pharmacokinetics</topic><topic>In vitro release</topic><topic>Lipoxygenase Inhibitors - pharmacokinetics</topic><topic>Matrix formulation</topic><topic>Osmolar Concentration</topic><topic>Polymers</topic><topic>Rotation</topic><topic>Solubility</topic><topic>Surface-Active Agents</topic><topic>Sustained-release</topic><topic>Tablets</topic><topic>Viscosity</topic><topic>Water - chemistry</topic><topic>Zileuton</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Qiu, Yihong</creatorcontrib><creatorcontrib>Hui, Ho-Wah</creatorcontrib><creatorcontrib>Cheskin, Howard</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>Pharmaceutical development and technology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Qiu, Yihong</au><au>Hui, Ho-Wah</au><au>Cheskin, Howard</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Formulation Development of Sustained-Release Hydrophilic Matrix Tablets of Zileuton</atitle><jtitle>Pharmaceutical development and technology</jtitle><addtitle>Pharm Dev Technol</addtitle><date>1997</date><risdate>1997</risdate><volume>2</volume><issue>3</issue><spage>197</spage><epage>204</epage><pages>197-204</pages><issn>1083-7450</issn><eissn>1097-9867</eissn><abstract>ABSTRACT
The purpose of this paper was to develop a hydrophilic matrix system for extended oral delivery of zileuton, and study the effects of certain formulation, processing, and dissolution variables on in vitro drug release. Tablet formulations with 60-70% drug and varying release rates were prepared by wet granulation using low and medium viscosity grades of hydroxypropylmethocellulose. In vitro drug release was evaluated using USP apparatus I. The in vitro drug release from all formulations followed zero-order kinetics and was independent of compression force. In general, the release rate decreased with increasing drug load and higher polymer concentration or viscosity. High-shear granulation also resulted in lower release rate. Accelerated release was observed with increased agitation as well as in the dissolution media with higher surfactant concentration and/or ionic strength. No stereoselective release from the matrix system was observed. The hydrophilic matrix system effectively controlled the in vitro release of zileuton. Matrix tablets with desired release rates can be prepared by adjusting various formulation and processing parameters. The matrix system also has the advantage of simple processing and relatively low cost.</abstract><cop>England</cop><pub>Informa UK Ltd</pub><pmid>9552447</pmid><doi>10.3109/10837459709031439</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1083-7450 |
| ispartof | Pharmaceutical development and technology, 1997, Vol.2 (3), p.197-204 |
| issn | 1083-7450 1097-9867 |
| language | eng |
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| source | MEDLINE; Taylor & Francis Medical Library - CRKN; Taylor & Francis Journals Complete |
| subjects | 5-lipoxygenase inhibitor Biological Availability Chemistry, Pharmaceutical Compressive Strength Delayed-Action Preparations Humans Hydroxyurea - analogs & derivatives Hydroxyurea - pharmacokinetics In vitro release Lipoxygenase Inhibitors - pharmacokinetics Matrix formulation Osmolar Concentration Polymers Rotation Solubility Surface-Active Agents Sustained-release Tablets Viscosity Water - chemistry Zileuton |
| title | Formulation Development of Sustained-Release Hydrophilic Matrix Tablets of Zileuton |
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