Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique
The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug, itraconazole, by a solid dispersion technique. Solid dispersion particles of itraconazole were prepared with various pH-independent and -dependent hydrophilic polymers and were characteriz...
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| Veröffentlicht in: | International journal of pharmaceutics 1999-10, Vol.187 (2), p.209-218 |
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| container_title | International journal of pharmaceutics |
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| creator | Jung, Jae-Young Yoo, Sun Dong Lee, Sang-Heon Kim, Kye-Hyun Yoon, Doo-Sun Lee, Kyu-Hyun |
| description | The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug, itraconazole, by a solid dispersion technique. Solid dispersion particles of itraconazole were prepared with various pH-independent and -dependent hydrophilic polymers and were characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. Of the polymers tested, pH-dependent hydrophilic polymers, AEA® and Eudragit® E 100, resulted in highest increases in drug solubility (range, 141.4–146.9-fold increases). The shape of the solid dispersion particles was spherical, with their internal diameter ranging from 1–10 μm. The dissolution rate of itraconazole from the tablets prepared by spray drying (SD-T) was fast, with >90% released within 5 min. SD-T prepared with AEA® or Eudragit® E 100 at a 1:1 drug to hydrophilic polymer ratio (w/w) showed approximately 70-fold increases in the dissolution rate over a marketed product. |
| doi_str_mv | 10.1016/S0378-5173(99)00191-X |
| format | Article |
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Solid dispersion particles of itraconazole were prepared with various pH-independent and -dependent hydrophilic polymers and were characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. Of the polymers tested, pH-dependent hydrophilic polymers, AEA® and Eudragit® E 100, resulted in highest increases in drug solubility (range, 141.4–146.9-fold increases). The shape of the solid dispersion particles was spherical, with their internal diameter ranging from 1–10 μm. The dissolution rate of itraconazole from the tablets prepared by spray drying (SD-T) was fast, with >90% released within 5 min. SD-T prepared with AEA® or Eudragit® E 100 at a 1:1 drug to hydrophilic polymer ratio (w/w) showed approximately 70-fold increases in the dissolution rate over a marketed product.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/S0378-5173(99)00191-X</identifier><identifier>PMID: 10502627</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>AEA ; Antifungal Agents - chemistry ; Biological and medical sciences ; Calorimetry, Differential Scanning ; Dissolution ; Eudragit® E 100 ; General pharmacology ; Itraconazole ; Itraconazole - analysis ; Itraconazole - chemistry ; Medical sciences ; Microscopy, Electron, Scanning ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Solid dispersion ; Solubility ; Spray drying ; X-Ray Diffraction</subject><ispartof>International journal of pharmaceutics, 1999-10, Vol.187 (2), p.209-218</ispartof><rights>1999 Elsevier Science B.V.</rights><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c456t-2cfa15a088549785087911775100e5ed2ca59f79a7013298beba78ba6ad022233</citedby><cites>FETCH-LOGICAL-c456t-2cfa15a088549785087911775100e5ed2ca59f79a7013298beba78ba6ad022233</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0378-5173(99)00191-X$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1991879$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10502627$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Jung, Jae-Young</creatorcontrib><creatorcontrib>Yoo, Sun Dong</creatorcontrib><creatorcontrib>Lee, Sang-Heon</creatorcontrib><creatorcontrib>Kim, Kye-Hyun</creatorcontrib><creatorcontrib>Yoon, Doo-Sun</creatorcontrib><creatorcontrib>Lee, Kyu-Hyun</creatorcontrib><title>Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug, itraconazole, by a solid dispersion technique. Solid dispersion particles of itraconazole were prepared with various pH-independent and -dependent hydrophilic polymers and were characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. Of the polymers tested, pH-dependent hydrophilic polymers, AEA® and Eudragit® E 100, resulted in highest increases in drug solubility (range, 141.4–146.9-fold increases). The shape of the solid dispersion particles was spherical, with their internal diameter ranging from 1–10 μm. The dissolution rate of itraconazole from the tablets prepared by spray drying (SD-T) was fast, with >90% released within 5 min. SD-T prepared with AEA® or Eudragit® E 100 at a 1:1 drug to hydrophilic polymer ratio (w/w) showed approximately 70-fold increases in the dissolution rate over a marketed product.</description><subject>AEA</subject><subject>Antifungal Agents - chemistry</subject><subject>Biological and medical sciences</subject><subject>Calorimetry, Differential Scanning</subject><subject>Dissolution</subject><subject>Eudragit® E 100</subject><subject>General pharmacology</subject><subject>Itraconazole</subject><subject>Itraconazole - analysis</subject><subject>Itraconazole - chemistry</subject><subject>Medical sciences</subject><subject>Microscopy, Electron, Scanning</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Solid dispersion</subject><subject>Solubility</subject><subject>Spray drying</subject><subject>X-Ray Diffraction</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0UFrFDEUwPEgFrtWP4JlDlL0MPUl2UySk0ipVij0UIW9hTeZNzQyO9kms0L99M3sLra3ngLh95LwD2MfOJxz4M2XW5Da1Ipr-cnazwDc8nr1ii240bKWS928Zov_5Ji9zfkPADSCyzfsmIMC0Qi9YKvL8Q5HT12V47BtwxCmhwrHrupCnnemEMcq4URV7KswJfRxxH9xoKotbh4KO7uhlGc6kb8bw_2W3rGjHodM7w_rCfv9_fLXxVV9ffPj58W369ovVTPVwvfIFYIxamm1UWC05VxrxQFIUSc8Kttrixq4FNa01KI2LTbYgRBCyhN2tj93k2K5Nk9uHbKnYcCR4jY7DdrIRi8LVHvoU8w5Ue82KawxPTgObk7qdknd3MtZ63ZJ3arMnR4u2LZr6p5N7RsW8PEAMHsc-lR6hvzkrC1_Ygv7umdUavwNlFz2geb0IZGfXBfDCy95BIJ7kys</recordid><startdate>19991005</startdate><enddate>19991005</enddate><creator>Jung, Jae-Young</creator><creator>Yoo, Sun Dong</creator><creator>Lee, Sang-Heon</creator><creator>Kim, Kye-Hyun</creator><creator>Yoon, Doo-Sun</creator><creator>Lee, Kyu-Hyun</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>19991005</creationdate><title>Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique</title><author>Jung, Jae-Young ; Yoo, Sun Dong ; Lee, Sang-Heon ; Kim, Kye-Hyun ; Yoon, Doo-Sun ; Lee, Kyu-Hyun</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c456t-2cfa15a088549785087911775100e5ed2ca59f79a7013298beba78ba6ad022233</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>AEA</topic><topic>Antifungal Agents - chemistry</topic><topic>Biological and medical sciences</topic><topic>Calorimetry, Differential Scanning</topic><topic>Dissolution</topic><topic>Eudragit® E 100</topic><topic>General pharmacology</topic><topic>Itraconazole</topic><topic>Itraconazole - analysis</topic><topic>Itraconazole - chemistry</topic><topic>Medical sciences</topic><topic>Microscopy, Electron, Scanning</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Solid dispersion</topic><topic>Solubility</topic><topic>Spray drying</topic><topic>X-Ray Diffraction</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jung, Jae-Young</creatorcontrib><creatorcontrib>Yoo, Sun Dong</creatorcontrib><creatorcontrib>Lee, Sang-Heon</creatorcontrib><creatorcontrib>Kim, Kye-Hyun</creatorcontrib><creatorcontrib>Yoon, Doo-Sun</creatorcontrib><creatorcontrib>Lee, Kyu-Hyun</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>Jung, Jae-Young</au><au>Yoo, Sun Dong</au><au>Lee, Sang-Heon</au><au>Kim, Kye-Hyun</au><au>Yoon, Doo-Sun</au><au>Lee, Kyu-Hyun</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>1999-10-05</date><risdate>1999</risdate><volume>187</volume><issue>2</issue><spage>209</spage><epage>218</epage><pages>209-218</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug, itraconazole, by a solid dispersion technique. Solid dispersion particles of itraconazole were prepared with various pH-independent and -dependent hydrophilic polymers and were characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. Of the polymers tested, pH-dependent hydrophilic polymers, AEA® and Eudragit® E 100, resulted in highest increases in drug solubility (range, 141.4–146.9-fold increases). The shape of the solid dispersion particles was spherical, with their internal diameter ranging from 1–10 μm. The dissolution rate of itraconazole from the tablets prepared by spray drying (SD-T) was fast, with >90% released within 5 min. SD-T prepared with AEA® or Eudragit® E 100 at a 1:1 drug to hydrophilic polymer ratio (w/w) showed approximately 70-fold increases in the dissolution rate over a marketed product.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>10502627</pmid><doi>10.1016/S0378-5173(99)00191-X</doi><tpages>10</tpages></addata></record> |
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| ispartof | International journal of pharmaceutics, 1999-10, Vol.187 (2), p.209-218 |
| issn | 0378-5173 1873-3476 |
| language | eng |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | AEA Antifungal Agents - chemistry Biological and medical sciences Calorimetry, Differential Scanning Dissolution Eudragit® E 100 General pharmacology Itraconazole Itraconazole - analysis Itraconazole - chemistry Medical sciences Microscopy, Electron, Scanning Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Solid dispersion Solubility Spray drying X-Ray Diffraction |
| title | Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique |
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