Gastro-floating tablets of cephalexin: Preparation and in vitro/in vivo evaluation
Gastro-floating tablets of cephalexin were developed to prolong the residence time in major absorption sites. Gastro-floating tablets were prepared and optimized using hydroxypropyl methylcellulose (HPMC K100M) as matrix and sodium bicarbonate as a gas-forming agent. The properties of the tablets in...
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| Veröffentlicht in: | International journal of pharmaceutics 2013-08, Vol.452 (1-2), p.241-248 |
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| container_end_page | 248 |
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| container_title | International journal of pharmaceutics |
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| creator | Yin, Lifang Qin, Chao Chen, Kaisheng Zhu, Chunli Cao, Hui Zhou, Jianping He, Wei Zhang, Qiang |
| description | Gastro-floating tablets of cephalexin were developed to prolong the residence time in major absorption sites. Gastro-floating tablets were prepared and optimized using hydroxypropyl methylcellulose (HPMC K100M) as matrix and sodium bicarbonate as a gas-forming agent. The properties of the tablets in terms of floating lag time, floating time and in vitro release were evaluated. Furthermore, in vivo pharmacokinetic study in fed and fasted beagle dogs was performed. The gastro-floating tablets had short floating lag time and exhibited a satisfactory sustained-release profile in vitro. Compared with conventional capsules, the gastro-floating tablets presented a sustained-release behavior with a relative bioavailability of 99.4%, while the reference sustained-release tablets gave a relative bioavailability of only 39.3%. Meanwhile, the food had significant effect on the pharmacokinetics of sustained-release tablets. It was concluded that the gastro-floating tablets had a sustained-release effect in vitro and in vivo, as well as desired pharmacokinetic properties in both fed and fasted conditions. |
| doi_str_mv | 10.1016/j.ijpharm.2013.05.011 |
| format | Article |
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Gastro-floating tablets were prepared and optimized using hydroxypropyl methylcellulose (HPMC K100M) as matrix and sodium bicarbonate as a gas-forming agent. The properties of the tablets in terms of floating lag time, floating time and in vitro release were evaluated. Furthermore, in vivo pharmacokinetic study in fed and fasted beagle dogs was performed. The gastro-floating tablets had short floating lag time and exhibited a satisfactory sustained-release profile in vitro. Compared with conventional capsules, the gastro-floating tablets presented a sustained-release behavior with a relative bioavailability of 99.4%, while the reference sustained-release tablets gave a relative bioavailability of only 39.3%. Meanwhile, the food had significant effect on the pharmacokinetics of sustained-release tablets. It was concluded that the gastro-floating tablets had a sustained-release effect in vitro and in vivo, as well as desired pharmacokinetic properties in both fed and fasted conditions.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2013.05.011</identifier><identifier>PMID: 23680730</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Absorption study ; Administration, Oral ; Animals ; Anti-Bacterial Agents - blood ; Anti-Bacterial Agents - chemistry ; Anti-Bacterial Agents - pharmacokinetics ; Bioavailability ; Biological Availability ; Cephalexin ; Cephalexin - blood ; Cephalexin - chemistry ; Cephalexin - pharmacokinetics ; Delayed-Action Preparations - chemistry ; Delayed-Action Preparations - pharmacokinetics ; Dogs ; Drug Compounding ; Drug Delivery Systems ; Fasting - metabolism ; Female ; Food-Drug Interactions ; Gastro-floating ; Intestinal Absorption ; Male ; Sustained-release ; Tablets</subject><ispartof>International journal of pharmaceutics, 2013-08, Vol.452 (1-2), p.241-248</ispartof><rights>2013 Elsevier B.V.</rights><rights>Copyright © 2013 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c431t-5c40a9c1c41e25eb301d6cab5b7f1cd174e84f249df584675ff58698c116e8b63</citedby><cites>FETCH-LOGICAL-c431t-5c40a9c1c41e25eb301d6cab5b7f1cd174e84f249df584675ff58698c116e8b63</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.2013.05.011$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,27922,27923,45993</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23680730$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yin, Lifang</creatorcontrib><creatorcontrib>Qin, Chao</creatorcontrib><creatorcontrib>Chen, Kaisheng</creatorcontrib><creatorcontrib>Zhu, Chunli</creatorcontrib><creatorcontrib>Cao, Hui</creatorcontrib><creatorcontrib>Zhou, Jianping</creatorcontrib><creatorcontrib>He, Wei</creatorcontrib><creatorcontrib>Zhang, Qiang</creatorcontrib><title>Gastro-floating tablets of cephalexin: Preparation and in vitro/in vivo evaluation</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>Gastro-floating tablets of cephalexin were developed to prolong the residence time in major absorption sites. Gastro-floating tablets were prepared and optimized using hydroxypropyl methylcellulose (HPMC K100M) as matrix and sodium bicarbonate as a gas-forming agent. The properties of the tablets in terms of floating lag time, floating time and in vitro release were evaluated. Furthermore, in vivo pharmacokinetic study in fed and fasted beagle dogs was performed. The gastro-floating tablets had short floating lag time and exhibited a satisfactory sustained-release profile in vitro. Compared with conventional capsules, the gastro-floating tablets presented a sustained-release behavior with a relative bioavailability of 99.4%, while the reference sustained-release tablets gave a relative bioavailability of only 39.3%. Meanwhile, the food had significant effect on the pharmacokinetics of sustained-release tablets. It was concluded that the gastro-floating tablets had a sustained-release effect in vitro and in vivo, as well as desired pharmacokinetic properties in both fed and fasted conditions.</description><subject>Absorption study</subject><subject>Administration, Oral</subject><subject>Animals</subject><subject>Anti-Bacterial Agents - blood</subject><subject>Anti-Bacterial Agents - chemistry</subject><subject>Anti-Bacterial Agents - pharmacokinetics</subject><subject>Bioavailability</subject><subject>Biological Availability</subject><subject>Cephalexin</subject><subject>Cephalexin - blood</subject><subject>Cephalexin - chemistry</subject><subject>Cephalexin - pharmacokinetics</subject><subject>Delayed-Action Preparations - chemistry</subject><subject>Delayed-Action Preparations - pharmacokinetics</subject><subject>Dogs</subject><subject>Drug Compounding</subject><subject>Drug Delivery Systems</subject><subject>Fasting - metabolism</subject><subject>Female</subject><subject>Food-Drug Interactions</subject><subject>Gastro-floating</subject><subject>Intestinal Absorption</subject><subject>Male</subject><subject>Sustained-release</subject><subject>Tablets</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkMtKxDAUhoMoOl4eQenSTWtO01zGjcjgDQRFdB3S9FQzdJox6Qz69mYuunV1Auf7z08-Qk6BFkBBXEwLN51_mDArSgqsoLygADtkBEqynFVS7JIRZVLlHCQ7IIcxTimlogS2Tw5KJhSVjI7Iy52JQ_B523kzuP49G0zd4RAz32YWU0GHX66_zJ4Dzk1IiO8z0zeZ67OlS8GL9WPpM1yabrHeH5O91nQRT7bziLzd3rxO7vPHp7uHyfVjbisGQ85tRc3Ygq0AS441o9AIa2peyxZsA7JCVbVlNW5arioheZumGCsLIFDVgh2R883defCfC4yDnrlosetMj34RNTAJpVAKeEL5BrXBxxiw1fPgZiZ8a6B6pVNP9VanXunUlOukM-XOthWLeobNX-rXXwKuNgCmjy4dBh2tw95i4wLaQTfe_VPxA6xHiWc</recordid><startdate>20130816</startdate><enddate>20130816</enddate><creator>Yin, Lifang</creator><creator>Qin, Chao</creator><creator>Chen, Kaisheng</creator><creator>Zhu, Chunli</creator><creator>Cao, Hui</creator><creator>Zhou, Jianping</creator><creator>He, Wei</creator><creator>Zhang, Qiang</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>20130816</creationdate><title>Gastro-floating tablets of cephalexin: Preparation and in vitro/in vivo evaluation</title><author>Yin, Lifang ; Qin, Chao ; Chen, Kaisheng ; Zhu, Chunli ; Cao, Hui ; Zhou, Jianping ; He, Wei ; Zhang, Qiang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c431t-5c40a9c1c41e25eb301d6cab5b7f1cd174e84f249df584675ff58698c116e8b63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Absorption study</topic><topic>Administration, Oral</topic><topic>Animals</topic><topic>Anti-Bacterial Agents - blood</topic><topic>Anti-Bacterial Agents - chemistry</topic><topic>Anti-Bacterial Agents - pharmacokinetics</topic><topic>Bioavailability</topic><topic>Biological Availability</topic><topic>Cephalexin</topic><topic>Cephalexin - blood</topic><topic>Cephalexin - chemistry</topic><topic>Cephalexin - pharmacokinetics</topic><topic>Delayed-Action Preparations - chemistry</topic><topic>Delayed-Action Preparations - pharmacokinetics</topic><topic>Dogs</topic><topic>Drug Compounding</topic><topic>Drug Delivery Systems</topic><topic>Fasting - metabolism</topic><topic>Female</topic><topic>Food-Drug Interactions</topic><topic>Gastro-floating</topic><topic>Intestinal Absorption</topic><topic>Male</topic><topic>Sustained-release</topic><topic>Tablets</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yin, Lifang</creatorcontrib><creatorcontrib>Qin, Chao</creatorcontrib><creatorcontrib>Chen, Kaisheng</creatorcontrib><creatorcontrib>Zhu, Chunli</creatorcontrib><creatorcontrib>Cao, Hui</creatorcontrib><creatorcontrib>Zhou, Jianping</creatorcontrib><creatorcontrib>He, Wei</creatorcontrib><creatorcontrib>Zhang, Qiang</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>Yin, Lifang</au><au>Qin, Chao</au><au>Chen, Kaisheng</au><au>Zhu, Chunli</au><au>Cao, Hui</au><au>Zhou, Jianping</au><au>He, Wei</au><au>Zhang, Qiang</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Gastro-floating tablets of cephalexin: Preparation and in vitro/in vivo evaluation</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2013-08-16</date><risdate>2013</risdate><volume>452</volume><issue>1-2</issue><spage>241</spage><epage>248</epage><pages>241-248</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>Gastro-floating tablets of cephalexin were developed to prolong the residence time in major absorption sites. Gastro-floating tablets were prepared and optimized using hydroxypropyl methylcellulose (HPMC K100M) as matrix and sodium bicarbonate as a gas-forming agent. The properties of the tablets in terms of floating lag time, floating time and in vitro release were evaluated. Furthermore, in vivo pharmacokinetic study in fed and fasted beagle dogs was performed. The gastro-floating tablets had short floating lag time and exhibited a satisfactory sustained-release profile in vitro. Compared with conventional capsules, the gastro-floating tablets presented a sustained-release behavior with a relative bioavailability of 99.4%, while the reference sustained-release tablets gave a relative bioavailability of only 39.3%. Meanwhile, the food had significant effect on the pharmacokinetics of sustained-release tablets. It was concluded that the gastro-floating tablets had a sustained-release effect in vitro and in vivo, as well as desired pharmacokinetic properties in both fed and fasted conditions.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>23680730</pmid><doi>10.1016/j.ijpharm.2013.05.011</doi><tpages>8</tpages></addata></record> |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Absorption study Administration, Oral Animals Anti-Bacterial Agents - blood Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacokinetics Bioavailability Biological Availability Cephalexin Cephalexin - blood Cephalexin - chemistry Cephalexin - pharmacokinetics Delayed-Action Preparations - chemistry Delayed-Action Preparations - pharmacokinetics Dogs Drug Compounding Drug Delivery Systems Fasting - metabolism Female Food-Drug Interactions Gastro-floating Intestinal Absorption Male Sustained-release Tablets |
| title | Gastro-floating tablets of cephalexin: Preparation and in vitro/in vivo evaluation |
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