Improvement of solubility and oral bioavailability of a poorly water‐soluble drug, TAS‐301, by its melt‐adsorption on a porous calcium silicate
The aim of the present study was to improve the solubility and oral bioavailability of a poorly water‐soluble drug, 3‐bis(4‐methoxyphenyl) methylene‐2‐indolinone (TAS‐301), by its melt‐adsorption on a porous calcium silicate, Florite® RE (FLR), without any solvents. The melt‐adsorbed products were p...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 2002-02, Vol.91 (2), p.362-370 |
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| container_title | Journal of pharmaceutical sciences |
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| creator | Kinoshita, Masahiro Baba, Kazuhiko Nagayasu, Atushi Yamabe, Kanoo Shimooka, Takashi Takeichi, Yoh'ichiro Azuma, Mami Houchi, Hitoshi Minakuchi, Kazuo |
| description | The aim of the present study was to improve the solubility and oral bioavailability of a poorly water‐soluble drug, 3‐bis(4‐methoxyphenyl) methylene‐2‐indolinone (TAS‐301), by its melt‐adsorption on a porous calcium silicate, Florite® RE (FLR), without any solvents. The melt‐adsorbed products were prepared by two methods: the small‐scale batch method and the twin screw extruder method. The drug was melted and adsorbed on FLR (i.e., “melt‐adsorption”), above its melting point. Crystallinity of the drug in the melt‐adsorbed product was estimated by differential scanning calorimetry (DSC) and powder X‐ray diffraction analysis. The dissolution test was conducted by the JP XIII paddle method. Oral absorption of the melt‐adsorbed product was studied in fasted and fed dogs. The melt‐adsorbed products prepared by the two methods were in powder forms. The drug existed in an amorphous state in the product and hardly recrystallized even after storing at a stressed condition (60°C/80% RH for 3 days). The TAS‐301 dissolution rate from the melt‐adsorbed product was markedly enhanced compared with drug crystals. The area under the plasma concentration‐time curve (AUC) and peak concentration (Cmax) values of the drug after dosing the melt‐adsorbed product were significantly greater than those after dosing the drug crystals. The solubility and bioavailability of TAS‐301 were improved by its melt‐adsorption on FLR. The present findings suggest melt‐adsorption is a useful technique for improving solubility and bioavailability of poorly water‐soluble drugs. |
| doi_str_mv | 10.1002/jps.10026 |
| format | Article |
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The melt‐adsorbed products were prepared by two methods: the small‐scale batch method and the twin screw extruder method. The drug was melted and adsorbed on FLR (i.e., “melt‐adsorption”), above its melting point. Crystallinity of the drug in the melt‐adsorbed product was estimated by differential scanning calorimetry (DSC) and powder X‐ray diffraction analysis. The dissolution test was conducted by the JP XIII paddle method. Oral absorption of the melt‐adsorbed product was studied in fasted and fed dogs. The melt‐adsorbed products prepared by the two methods were in powder forms. The drug existed in an amorphous state in the product and hardly recrystallized even after storing at a stressed condition (60°C/80% RH for 3 days). The TAS‐301 dissolution rate from the melt‐adsorbed product was markedly enhanced compared with drug crystals. The area under the plasma concentration‐time curve (AUC) and peak concentration (Cmax) values of the drug after dosing the melt‐adsorbed product were significantly greater than those after dosing the drug crystals. The solubility and bioavailability of TAS‐301 were improved by its melt‐adsorption on FLR. The present findings suggest melt‐adsorption is a useful technique for improving solubility and bioavailability of poorly water‐soluble drugs.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.10026</identifier><identifier>PMID: 11835196</identifier><identifier>CODEN: JPMSAE</identifier><language>eng</language><publisher>New York: Elsevier Inc</publisher><subject>Administration, Oral ; Adsorption ; amorphous ; Animals ; bioavailability ; Biological and medical sciences ; Biological Availability ; Calcium Compounds - pharmacokinetics ; Capsules ; dissolution ; Dogs ; General pharmacology ; Hot Temperature ; Indoles - blood ; Indoles - chemistry ; Indoles - pharmacokinetics ; Male ; Medical sciences ; melt adsorption ; Pharmacology. Drug treatments ; Physicochemical properties. Structure-activity relationships ; porous calcium silicate ; Powders ; Silicates - pharmacokinetics ; Solubility ; twin screw extruder</subject><ispartof>Journal of pharmaceutical sciences, 2002-02, Vol.91 (2), p.362-370</ispartof><rights>2002 Wiley-Liss, Inc., and the American Pharmaceutical Association</rights><rights>Copyright © 2002 Wiley‐Liss, Inc. and the American Pharmaceutical Association</rights><rights>2002 INIST-CNRS</rights><rights>Copyright 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:362-370, 2002</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4996-ad1ab4940a34f06ba4e9531447036f20fe639459cb9a6a45f35b9d3137b2bf9d3</citedby><cites>FETCH-LOGICAL-c4996-ad1ab4940a34f06ba4e9531447036f20fe639459cb9a6a45f35b9d3137b2bf9d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.10026$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.10026$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=13477877$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11835196$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kinoshita, Masahiro</creatorcontrib><creatorcontrib>Baba, Kazuhiko</creatorcontrib><creatorcontrib>Nagayasu, Atushi</creatorcontrib><creatorcontrib>Yamabe, Kanoo</creatorcontrib><creatorcontrib>Shimooka, Takashi</creatorcontrib><creatorcontrib>Takeichi, Yoh'ichiro</creatorcontrib><creatorcontrib>Azuma, Mami</creatorcontrib><creatorcontrib>Houchi, Hitoshi</creatorcontrib><creatorcontrib>Minakuchi, Kazuo</creatorcontrib><title>Improvement of solubility and oral bioavailability of a poorly water‐soluble drug, TAS‐301, by its melt‐adsorption on a porous calcium silicate</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>The aim of the present study was to improve the solubility and oral bioavailability of a poorly water‐soluble drug, 3‐bis(4‐methoxyphenyl) methylene‐2‐indolinone (TAS‐301), by its melt‐adsorption on a porous calcium silicate, Florite® RE (FLR), without any solvents. The melt‐adsorbed products were prepared by two methods: the small‐scale batch method and the twin screw extruder method. The drug was melted and adsorbed on FLR (i.e., “melt‐adsorption”), above its melting point. Crystallinity of the drug in the melt‐adsorbed product was estimated by differential scanning calorimetry (DSC) and powder X‐ray diffraction analysis. The dissolution test was conducted by the JP XIII paddle method. Oral absorption of the melt‐adsorbed product was studied in fasted and fed dogs. The melt‐adsorbed products prepared by the two methods were in powder forms. The drug existed in an amorphous state in the product and hardly recrystallized even after storing at a stressed condition (60°C/80% RH for 3 days). The TAS‐301 dissolution rate from the melt‐adsorbed product was markedly enhanced compared with drug crystals. The area under the plasma concentration‐time curve (AUC) and peak concentration (Cmax) values of the drug after dosing the melt‐adsorbed product were significantly greater than those after dosing the drug crystals. The solubility and bioavailability of TAS‐301 were improved by its melt‐adsorption on FLR. The present findings suggest melt‐adsorption is a useful technique for improving solubility and bioavailability of poorly water‐soluble drugs.</description><subject>Administration, Oral</subject><subject>Adsorption</subject><subject>amorphous</subject><subject>Animals</subject><subject>bioavailability</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Calcium Compounds - pharmacokinetics</subject><subject>Capsules</subject><subject>dissolution</subject><subject>Dogs</subject><subject>General pharmacology</subject><subject>Hot Temperature</subject><subject>Indoles - blood</subject><subject>Indoles - chemistry</subject><subject>Indoles - pharmacokinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>melt adsorption</subject><subject>Pharmacology. Drug treatments</subject><subject>Physicochemical properties. Structure-activity relationships</subject><subject>porous calcium silicate</subject><subject>Powders</subject><subject>Silicates - pharmacokinetics</subject><subject>Solubility</subject><subject>twin screw extruder</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kc1u1DAQxyMEotvCgRdAvoBUqaH2-iP1sarYUrR8SF20Ehdr4jjIxYm3drIlNx6BCy_Ik-DdBHoByZJH49_8Z-bvLHtG8CuC8fz0ZhP3gXiQzQif41xgUjzMZik1zyln8iA7jPEGYyww54-zA0LOKCdSzLKfV80m-K1pTNshX6PoXV9aZ7sBQVshH8Ch0nrYgnUwPSQM0Mb74AZ0B50Jv77_2Nc5g6rQfzlBq_PrlKOYnKByQLaLqDGuSymoog-bzvoWpbNTCb6PSIPTtm9QTA10UnySParBRfN0uo-yT4vXq4s3-fLD5dXF-TLXTEqRQ0WgZJJhoKzGogRmJKeEsQJTUc9xbQSVjEtdShDAeE15KStKaFHOyzpFR9nLUTd5cNub2KnGRm2cg9akuVSRtCQXIoHHI6iDjzGYWm2CbSAMimC1s16lP9gHO_b5JNqXjanuycn0BLyYAIhp8zpAq2285ygrirOiSNzpyN1ZZ4b_d1RvP17_aZ2PFTZ25tvfCghflShowdX6_aVafX63WK8XC7VMPB15k0zeWhNU1Na02lQ2GN2pytt_LPgbb_XDEQ</recordid><startdate>200202</startdate><enddate>200202</enddate><creator>Kinoshita, Masahiro</creator><creator>Baba, Kazuhiko</creator><creator>Nagayasu, Atushi</creator><creator>Yamabe, Kanoo</creator><creator>Shimooka, Takashi</creator><creator>Takeichi, Yoh'ichiro</creator><creator>Azuma, Mami</creator><creator>Houchi, Hitoshi</creator><creator>Minakuchi, Kazuo</creator><general>Elsevier Inc</general><general>John Wiley & Sons, Inc</general><general>Wiley</general><general>American Pharmaceutical Association</general><scope>BSCLL</scope><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>200202</creationdate><title>Improvement of solubility and oral bioavailability of a poorly water‐soluble drug, TAS‐301, by its melt‐adsorption on a porous calcium silicate</title><author>Kinoshita, Masahiro ; Baba, Kazuhiko ; Nagayasu, Atushi ; Yamabe, Kanoo ; Shimooka, Takashi ; Takeichi, Yoh'ichiro ; Azuma, Mami ; Houchi, Hitoshi ; Minakuchi, Kazuo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4996-ad1ab4940a34f06ba4e9531447036f20fe639459cb9a6a45f35b9d3137b2bf9d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Administration, Oral</topic><topic>Adsorption</topic><topic>amorphous</topic><topic>Animals</topic><topic>bioavailability</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Calcium Compounds - pharmacokinetics</topic><topic>Capsules</topic><topic>dissolution</topic><topic>Dogs</topic><topic>General pharmacology</topic><topic>Hot Temperature</topic><topic>Indoles - blood</topic><topic>Indoles - chemistry</topic><topic>Indoles - pharmacokinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>melt adsorption</topic><topic>Pharmacology. Drug treatments</topic><topic>Physicochemical properties. Structure-activity relationships</topic><topic>porous calcium silicate</topic><topic>Powders</topic><topic>Silicates - pharmacokinetics</topic><topic>Solubility</topic><topic>twin screw extruder</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kinoshita, Masahiro</creatorcontrib><creatorcontrib>Baba, Kazuhiko</creatorcontrib><creatorcontrib>Nagayasu, Atushi</creatorcontrib><creatorcontrib>Yamabe, Kanoo</creatorcontrib><creatorcontrib>Shimooka, Takashi</creatorcontrib><creatorcontrib>Takeichi, Yoh'ichiro</creatorcontrib><creatorcontrib>Azuma, Mami</creatorcontrib><creatorcontrib>Houchi, Hitoshi</creatorcontrib><creatorcontrib>Minakuchi, Kazuo</creatorcontrib><collection>Istex</collection><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>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kinoshita, Masahiro</au><au>Baba, Kazuhiko</au><au>Nagayasu, Atushi</au><au>Yamabe, Kanoo</au><au>Shimooka, Takashi</au><au>Takeichi, Yoh'ichiro</au><au>Azuma, Mami</au><au>Houchi, Hitoshi</au><au>Minakuchi, Kazuo</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Improvement of solubility and oral bioavailability of a poorly water‐soluble drug, TAS‐301, by its melt‐adsorption on a porous calcium silicate</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>2002-02</date><risdate>2002</risdate><volume>91</volume><issue>2</issue><spage>362</spage><epage>370</epage><pages>362-370</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><coden>JPMSAE</coden><abstract>The aim of the present study was to improve the solubility and oral bioavailability of a poorly water‐soluble drug, 3‐bis(4‐methoxyphenyl) methylene‐2‐indolinone (TAS‐301), by its melt‐adsorption on a porous calcium silicate, Florite® RE (FLR), without any solvents. The melt‐adsorbed products were prepared by two methods: the small‐scale batch method and the twin screw extruder method. The drug was melted and adsorbed on FLR (i.e., “melt‐adsorption”), above its melting point. Crystallinity of the drug in the melt‐adsorbed product was estimated by differential scanning calorimetry (DSC) and powder X‐ray diffraction analysis. The dissolution test was conducted by the JP XIII paddle method. Oral absorption of the melt‐adsorbed product was studied in fasted and fed dogs. The melt‐adsorbed products prepared by the two methods were in powder forms. The drug existed in an amorphous state in the product and hardly recrystallized even after storing at a stressed condition (60°C/80% RH for 3 days). The TAS‐301 dissolution rate from the melt‐adsorbed product was markedly enhanced compared with drug crystals. The area under the plasma concentration‐time curve (AUC) and peak concentration (Cmax) values of the drug after dosing the melt‐adsorbed product were significantly greater than those after dosing the drug crystals. The solubility and bioavailability of TAS‐301 were improved by its melt‐adsorption on FLR. The present findings suggest melt‐adsorption is a useful technique for improving solubility and bioavailability of poorly water‐soluble drugs.</abstract><cop>New York</cop><pub>Elsevier Inc</pub><pmid>11835196</pmid><doi>10.1002/jps.10026</doi><tpages>9</tpages></addata></record> |
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| subjects | Administration, Oral Adsorption amorphous Animals bioavailability Biological and medical sciences Biological Availability Calcium Compounds - pharmacokinetics Capsules dissolution Dogs General pharmacology Hot Temperature Indoles - blood Indoles - chemistry Indoles - pharmacokinetics Male Medical sciences melt adsorption Pharmacology. Drug treatments Physicochemical properties. Structure-activity relationships porous calcium silicate Powders Silicates - pharmacokinetics Solubility twin screw extruder |
| title | Improvement of solubility and oral bioavailability of a poorly water‐soluble drug, TAS‐301, by its melt‐adsorption on a porous calcium silicate |
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