Bioavailability of ibuprofen from matrix mini-tablets based on a mixture of starch and microcrystalline wax
The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers ( n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow ®...
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Veröffentlicht in: | International journal of pharmaceutics 2000-11, Vol.208 (1), p.81-86 |
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creator | De ∣Brabander, C Vervaet, C Görtz, J.P Remon, J.P Berlo, J.A |
description | The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers (
n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow
® 600) or as mini-tablets (filled into hard gelatin capsules). The mini-tablets consisted of 60% ibuprofen, 15% Paracera
® M (wax), 22.5% DDWM (starch) and 2.5% triacetin (lubricant).
t
50% of the in vitro release was 4.5 and 5 h for the mini-tablet and Ibu-slow
® formulations, respectively. Both formulations behaved in vivo as sustained-release formulation; their HVD
t50%
Cmax
value was determined at 5.6 and 5.1 h for the mini-tablet and Ibu-slow
® formulations, respectively. A significantly higher value of
C
max was seen for the mini-tablet formulation, resulting in a relative bioavailability of 116±22.6% compared to the Ibu-slow
® matrix. These data demonstrate that the experimental mini-tablets can be used to formulate sustained-release dosage forms. |
doi_str_mv | 10.1016/S0378-5173(00)00549-4 |
format | Article |
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n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow
® 600) or as mini-tablets (filled into hard gelatin capsules). The mini-tablets consisted of 60% ibuprofen, 15% Paracera
® M (wax), 22.5% DDWM (starch) and 2.5% triacetin (lubricant).
t
50% of the in vitro release was 4.5 and 5 h for the mini-tablet and Ibu-slow
® formulations, respectively. Both formulations behaved in vivo as sustained-release formulation; their HVD
t50%
Cmax
value was determined at 5.6 and 5.1 h for the mini-tablet and Ibu-slow
® formulations, respectively. A significantly higher value of
C
max was seen for the mini-tablet formulation, resulting in a relative bioavailability of 116±22.6% compared to the Ibu-slow
® matrix. These data demonstrate that the experimental mini-tablets can be used to formulate sustained-release dosage forms.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/S0378-5173(00)00549-4</identifier><identifier>PMID: 11203270</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Adult ; Anti-Inflammatory Agents, Non-Steroidal - blood ; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics ; Bioavailability ; Biological and medical sciences ; Biological Availability ; Bones, joints and connective tissue. Antiinflammatory agents ; Cross-Over Studies ; General pharmacology ; Humans ; Ibuprofen ; Ibuprofen - blood ; Ibuprofen - pharmacokinetics ; Male ; Matrix ; Medical sciences ; Middle Aged ; Mini-tablet ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Starch - pharmacokinetics ; Statistics, Nonparametric ; Sustained release ; Tablets ; Waxes - pharmacokinetics</subject><ispartof>International journal of pharmaceutics, 2000-11, Vol.208 (1), p.81-86</ispartof><rights>2000 Elsevier Science B.V.</rights><rights>2000 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c390t-e650d2345e3bec0f234ef94b6cd70fc8851e7b9629965ff4d638f498778dc953</citedby><cites>FETCH-LOGICAL-c390t-e650d2345e3bec0f234ef94b6cd70fc8851e7b9629965ff4d638f498778dc953</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517300005494$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1523816$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11203270$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>De ∣Brabander, C</creatorcontrib><creatorcontrib>Vervaet, C</creatorcontrib><creatorcontrib>Görtz, J.P</creatorcontrib><creatorcontrib>Remon, J.P</creatorcontrib><creatorcontrib>Berlo, J.A</creatorcontrib><title>Bioavailability of ibuprofen from matrix mini-tablets based on a mixture of starch and microcrystalline wax</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers (
n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow
® 600) or as mini-tablets (filled into hard gelatin capsules). The mini-tablets consisted of 60% ibuprofen, 15% Paracera
® M (wax), 22.5% DDWM (starch) and 2.5% triacetin (lubricant).
t
50% of the in vitro release was 4.5 and 5 h for the mini-tablet and Ibu-slow
® formulations, respectively. Both formulations behaved in vivo as sustained-release formulation; their HVD
t50%
Cmax
value was determined at 5.6 and 5.1 h for the mini-tablet and Ibu-slow
® formulations, respectively. A significantly higher value of
C
max was seen for the mini-tablet formulation, resulting in a relative bioavailability of 116±22.6% compared to the Ibu-slow
® matrix. These data demonstrate that the experimental mini-tablets can be used to formulate sustained-release dosage forms.</description><subject>Adult</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - blood</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</subject><subject>Bioavailability</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Cross-Over Studies</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Ibuprofen</subject><subject>Ibuprofen - blood</subject><subject>Ibuprofen - pharmacokinetics</subject><subject>Male</subject><subject>Matrix</subject><subject>Medical sciences</subject><subject>Middle Aged</subject><subject>Mini-tablet</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Starch - pharmacokinetics</subject><subject>Statistics, Nonparametric</subject><subject>Sustained release</subject><subject>Tablets</subject><subject>Waxes - pharmacokinetics</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM1u1DAURi1ERYfCI4C8QAgWgev4N6sKKmiRKrGge8txroXBSYqdlJm3x9MZ0WVXtj6dz773EPKKwQcGTH38AVybRjLN3wG8B5Cia8QTsmFG84YLrZ6SzX_klDwv5RcAqJbxZ-SUsRZ4q2FDfn-Os7tzMbk-prjs6Bxo7NfbPAecaMjzSEe35LilY5xis7g-4VJo7woOdJ6oq_l2WTPui2Vx2f-kbhpq6vPs865GKcUJ6V-3fUFOgksFXx7PM3Lz9cvNxVVz_f3y28Wn68bzDpYGlYSh5UIi79FDqFcMneiVHzQEb4xkqPtOtV2nZAhiUNwE0RmtzeA7yc_I28OzdYk_K5bFjrF4TMlNOK_F6lYoqYSpoDyAddRSMgZ7m-Po8s4ysHvJ9l6y3Ru0APZeshW19_r4wdqPODy0jlYr8OYIuOJdCtlNPpYHTrbcMFWx8wOGVcZdxGyLjzh5HGJGv9hhjo9M8g9Kd5n0</recordid><startdate>20001104</startdate><enddate>20001104</enddate><creator>De ∣Brabander, C</creator><creator>Vervaet, C</creator><creator>Görtz, J.P</creator><creator>Remon, J.P</creator><creator>Berlo, J.A</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>20001104</creationdate><title>Bioavailability of ibuprofen from matrix mini-tablets based on a mixture of starch and microcrystalline wax</title><author>De ∣Brabander, C ; Vervaet, C ; Görtz, J.P ; Remon, J.P ; Berlo, J.A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-e650d2345e3bec0f234ef94b6cd70fc8851e7b9629965ff4d638f498778dc953</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Adult</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - blood</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</topic><topic>Bioavailability</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Cross-Over Studies</topic><topic>General pharmacology</topic><topic>Humans</topic><topic>Ibuprofen</topic><topic>Ibuprofen - blood</topic><topic>Ibuprofen - pharmacokinetics</topic><topic>Male</topic><topic>Matrix</topic><topic>Medical sciences</topic><topic>Middle Aged</topic><topic>Mini-tablet</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Starch - pharmacokinetics</topic><topic>Statistics, Nonparametric</topic><topic>Sustained release</topic><topic>Tablets</topic><topic>Waxes - pharmacokinetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>De ∣Brabander, C</creatorcontrib><creatorcontrib>Vervaet, C</creatorcontrib><creatorcontrib>Görtz, J.P</creatorcontrib><creatorcontrib>Remon, J.P</creatorcontrib><creatorcontrib>Berlo, J.A</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>De ∣Brabander, C</au><au>Vervaet, C</au><au>Görtz, J.P</au><au>Remon, J.P</au><au>Berlo, J.A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Bioavailability of ibuprofen from matrix mini-tablets based on a mixture of starch and microcrystalline wax</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2000-11-04</date><risdate>2000</risdate><volume>208</volume><issue>1</issue><spage>81</spage><epage>86</epage><pages>81-86</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers (
n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow
® 600) or as mini-tablets (filled into hard gelatin capsules). The mini-tablets consisted of 60% ibuprofen, 15% Paracera
® M (wax), 22.5% DDWM (starch) and 2.5% triacetin (lubricant).
t
50% of the in vitro release was 4.5 and 5 h for the mini-tablet and Ibu-slow
® formulations, respectively. Both formulations behaved in vivo as sustained-release formulation; their HVD
t50%
Cmax
value was determined at 5.6 and 5.1 h for the mini-tablet and Ibu-slow
® formulations, respectively. A significantly higher value of
C
max was seen for the mini-tablet formulation, resulting in a relative bioavailability of 116±22.6% compared to the Ibu-slow
® matrix. These data demonstrate that the experimental mini-tablets can be used to formulate sustained-release dosage forms.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>11203270</pmid><doi>10.1016/S0378-5173(00)00549-4</doi><tpages>6</tpages></addata></record> |
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source | MEDLINE; Elsevier ScienceDirect Journals |
subjects | Adult Anti-Inflammatory Agents, Non-Steroidal - blood Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Bioavailability Biological and medical sciences Biological Availability Bones, joints and connective tissue. Antiinflammatory agents Cross-Over Studies General pharmacology Humans Ibuprofen Ibuprofen - blood Ibuprofen - pharmacokinetics Male Matrix Medical sciences Middle Aged Mini-tablet Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Starch - pharmacokinetics Statistics, Nonparametric Sustained release Tablets Waxes - pharmacokinetics |
title | Bioavailability of ibuprofen from matrix mini-tablets based on a mixture of starch and microcrystalline wax |
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