Preparation, Characterization and Evaluation of Coenzyme Q10 Binary Solid Dispersions for Enhanced Solubility and Dissolution
Phase solubility behavior of coenzyme Q10 (CoQ10) at 25 °C in various molar solutions of poloxamer 188 (P188) in water was observed and their binary solid dispersions (BSD) at different weight ratios were prepared by a simple, rapid, cost effective, uncomplicated and potentially scalable low tempera...
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| Veröffentlicht in: | Biological & Pharmaceutical Bulletin 2007, Vol.30(6), pp.1171-1176 |
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| container_title | Biological & Pharmaceutical Bulletin |
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| creator | Bhandari, Krishna Hari Newa, Madhuri Kim, Jung Ae Yoo, Bong Kyu Woo, Jong Soo Lyoo, Won Seok Lim, Hyun Tae Choi, Han Gon Yong, Chul Soon |
| description | Phase solubility behavior of coenzyme Q10 (CoQ10) at 25 °C in various molar solutions of poloxamer 188 (P188) in water was observed and their binary solid dispersions (BSD) at different weight ratios were prepared by a simple, rapid, cost effective, uncomplicated and potentially scalable low temperature melting method. BSDs were characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for improved solubility at 25 °C and 37 °C and in-vitro release of CoQ10 at 37 °C in distilled water. Solubility of CoQ10 increased with increasing concentrations of P188 in water. Gibbs free energy (ΔG°tr) values were all negative indicating the spontaneous nature of CoQ10 solubilization and decreased with increasing concentration of P188 demonstrating that the reaction conditions became more favorable as the concentration of P188 increased. DSC and SEM analysis indicated that the homogeneity of dispersion was not at the molecular level. However, BSDs exhibited a remarkably improved aqueous solubility and dissolution of CoQ10. |
| doi_str_mv | 10.1248/bpb.30.1171 |
| format | Article |
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BSDs were characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for improved solubility at 25 °C and 37 °C and in-vitro release of CoQ10 at 37 °C in distilled water. Solubility of CoQ10 increased with increasing concentrations of P188 in water. Gibbs free energy (ΔG°tr) values were all negative indicating the spontaneous nature of CoQ10 solubilization and decreased with increasing concentration of P188 demonstrating that the reaction conditions became more favorable as the concentration of P188 increased. DSC and SEM analysis indicated that the homogeneity of dispersion was not at the molecular level. However, BSDs exhibited a remarkably improved aqueous solubility and dissolution of CoQ10.</description><identifier>ISSN: 0918-6158</identifier><identifier>EISSN: 1347-5215</identifier><identifier>DOI: 10.1248/bpb.30.1171</identifier><identifier>PMID: 17541177</identifier><language>eng</language><publisher>Japan: The Pharmaceutical Society of Japan</publisher><subject>binary solid dispersion ; Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Chromatography, High Pressure Liquid ; coenzyme Q10 ; Coenzymes - analysis ; Coenzymes - chemistry ; Coenzymes - ultrastructure ; dissolution ; Drug Compounding ; Evaluation Studies as Topic ; Molecular Structure ; Poloxamer - chemistry ; poloxamer 188 ; Powders ; Solubility ; Solvents - chemistry ; Spectrophotometry, Ultraviolet ; Temperature ; Thermodynamics ; Ubiquinone - analogs & derivatives ; Ubiquinone - analysis ; Ubiquinone - chemistry ; Ubiquinone - ultrastructure ; Water - chemistry</subject><ispartof>Biological and Pharmaceutical Bulletin, 2007, Vol.30(6), pp.1171-1176</ispartof><rights>2007 The Pharmaceutical Society of Japan</rights><rights>Copyright Japan Science and Technology Agency 2007</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c664t-d303a5b5a6aaaf4e6af157d0a9be3af32381021d48018d85d61b5776c01909ad3</citedby><cites>FETCH-LOGICAL-c664t-d303a5b5a6aaaf4e6af157d0a9be3af32381021d48018d85d61b5776c01909ad3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,1877,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17541177$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bhandari, Krishna Hari</creatorcontrib><creatorcontrib>Newa, Madhuri</creatorcontrib><creatorcontrib>Kim, Jung Ae</creatorcontrib><creatorcontrib>Yoo, Bong Kyu</creatorcontrib><creatorcontrib>Woo, Jong Soo</creatorcontrib><creatorcontrib>Lyoo, Won Seok</creatorcontrib><creatorcontrib>Lim, Hyun Tae</creatorcontrib><creatorcontrib>Choi, Han Gon</creatorcontrib><creatorcontrib>Yong, Chul Soon</creatorcontrib><creatorcontrib>aCollege of Pharmacy</creatorcontrib><creatorcontrib>Yeungnam University</creatorcontrib><creatorcontrib>bSchool of Textiles</creatorcontrib><title>Preparation, Characterization and Evaluation of Coenzyme Q10 Binary Solid Dispersions for Enhanced Solubility and Dissolution</title><title>Biological & Pharmaceutical Bulletin</title><addtitle>Biol Pharm Bull</addtitle><description>Phase solubility behavior of coenzyme Q10 (CoQ10) at 25 °C in various molar solutions of poloxamer 188 (P188) in water was observed and their binary solid dispersions (BSD) at different weight ratios were prepared by a simple, rapid, cost effective, uncomplicated and potentially scalable low temperature melting method. BSDs were characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for improved solubility at 25 °C and 37 °C and in-vitro release of CoQ10 at 37 °C in distilled water. Solubility of CoQ10 increased with increasing concentrations of P188 in water. Gibbs free energy (ΔG°tr) values were all negative indicating the spontaneous nature of CoQ10 solubilization and decreased with increasing concentration of P188 demonstrating that the reaction conditions became more favorable as the concentration of P188 increased. DSC and SEM analysis indicated that the homogeneity of dispersion was not at the molecular level. However, BSDs exhibited a remarkably improved aqueous solubility and dissolution of CoQ10.</description><subject>binary solid dispersion</subject><subject>Calorimetry, Differential Scanning</subject><subject>Chemistry, Pharmaceutical</subject><subject>Chromatography, High Pressure Liquid</subject><subject>coenzyme Q10</subject><subject>Coenzymes - analysis</subject><subject>Coenzymes - chemistry</subject><subject>Coenzymes - ultrastructure</subject><subject>dissolution</subject><subject>Drug Compounding</subject><subject>Evaluation Studies as Topic</subject><subject>Molecular Structure</subject><subject>Poloxamer - chemistry</subject><subject>poloxamer 188</subject><subject>Powders</subject><subject>Solubility</subject><subject>Solvents - chemistry</subject><subject>Spectrophotometry, Ultraviolet</subject><subject>Temperature</subject><subject>Thermodynamics</subject><subject>Ubiquinone - analogs & derivatives</subject><subject>Ubiquinone - analysis</subject><subject>Ubiquinone - chemistry</subject><subject>Ubiquinone - ultrastructure</subject><subject>Water - chemistry</subject><issn>0918-6158</issn><issn>1347-5215</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkdGL1DAQxoMo3t7qk-9SEHw5eyZNk7Rv6rqnwoGK-hzSJPWyZJOatMIe-L873e554Mtkkvnlm2E-hJ4RfEmqunndDd0lhZwI8gCtCK1FySrCHqIVbklTcsKaM3Se8w5jLHBFH6MzIlgNvFihP1-SHVRSo4vhVbG5gVSPNrnb40uhgim2v5Wflmvsi0204fawt8VXgot3Lqh0KL5F70zx3uXBpgxcLvqYim24UUFbM5enznk3Ho56wGV4mQWfoEe98tk-PZ1r9ONq-33zsbz-_OHT5u11qTmvx9JQTBXrmOJKqb62XPWECYNV21mqelrRhuCKmLrBpDENM5x0TAiuMWlxqwxdo5eL7pDir8nmUe5d1tZ7FWycshSYwUJAZ41e_Afu4pQCzCZJXbeUU9gmUBcLpVPMOdleDsntYROSYDl7IsETSSEHT4B-ftKcur019-zJBACuFgCqTisfg3fB3nfWWXQu-igrMFBiTDHmElftUX4OHEYTdO70ZhHa5VH9tP86qTQ67e3dVHwJx993JQ3OSxvoXy8OtRs</recordid><startdate>20070601</startdate><enddate>20070601</enddate><creator>Bhandari, Krishna Hari</creator><creator>Newa, Madhuri</creator><creator>Kim, Jung Ae</creator><creator>Yoo, Bong Kyu</creator><creator>Woo, Jong Soo</creator><creator>Lyoo, Won Seok</creator><creator>Lim, Hyun Tae</creator><creator>Choi, Han Gon</creator><creator>Yong, Chul Soon</creator><general>The Pharmaceutical Society of Japan</general><general>Pharmaceutical Society of Japan</general><general>Japan Science and Technology Agency</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>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U9</scope><scope>8FD</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20070601</creationdate><title>Preparation, Characterization and Evaluation of Coenzyme Q10 Binary Solid Dispersions for Enhanced Solubility and Dissolution</title><author>Bhandari, Krishna Hari ; Newa, Madhuri ; Kim, Jung Ae ; Yoo, Bong Kyu ; Woo, Jong Soo ; Lyoo, Won Seok ; Lim, Hyun Tae ; Choi, Han Gon ; Yong, Chul Soon</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c664t-d303a5b5a6aaaf4e6af157d0a9be3af32381021d48018d85d61b5776c01909ad3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>binary solid dispersion</topic><topic>Calorimetry, Differential Scanning</topic><topic>Chemistry, Pharmaceutical</topic><topic>Chromatography, High Pressure Liquid</topic><topic>coenzyme Q10</topic><topic>Coenzymes - analysis</topic><topic>Coenzymes - chemistry</topic><topic>Coenzymes - ultrastructure</topic><topic>dissolution</topic><topic>Drug Compounding</topic><topic>Evaluation Studies as Topic</topic><topic>Molecular Structure</topic><topic>Poloxamer - chemistry</topic><topic>poloxamer 188</topic><topic>Powders</topic><topic>Solubility</topic><topic>Solvents - chemistry</topic><topic>Spectrophotometry, Ultraviolet</topic><topic>Temperature</topic><topic>Thermodynamics</topic><topic>Ubiquinone - analogs & derivatives</topic><topic>Ubiquinone - analysis</topic><topic>Ubiquinone - chemistry</topic><topic>Ubiquinone - ultrastructure</topic><topic>Water - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bhandari, Krishna Hari</creatorcontrib><creatorcontrib>Newa, Madhuri</creatorcontrib><creatorcontrib>Kim, Jung Ae</creatorcontrib><creatorcontrib>Yoo, Bong Kyu</creatorcontrib><creatorcontrib>Woo, Jong Soo</creatorcontrib><creatorcontrib>Lyoo, Won Seok</creatorcontrib><creatorcontrib>Lim, Hyun Tae</creatorcontrib><creatorcontrib>Choi, Han Gon</creatorcontrib><creatorcontrib>Yong, Chul Soon</creatorcontrib><creatorcontrib>aCollege of Pharmacy</creatorcontrib><creatorcontrib>Yeungnam University</creatorcontrib><creatorcontrib>bSchool of Textiles</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Biological & Pharmaceutical Bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bhandari, Krishna Hari</au><au>Newa, Madhuri</au><au>Kim, Jung Ae</au><au>Yoo, Bong Kyu</au><au>Woo, Jong Soo</au><au>Lyoo, Won Seok</au><au>Lim, Hyun Tae</au><au>Choi, Han Gon</au><au>Yong, Chul Soon</au><aucorp>aCollege of Pharmacy</aucorp><aucorp>Yeungnam University</aucorp><aucorp>bSchool of Textiles</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation, Characterization and Evaluation of Coenzyme Q10 Binary Solid Dispersions for Enhanced Solubility and Dissolution</atitle><jtitle>Biological & Pharmaceutical Bulletin</jtitle><addtitle>Biol Pharm Bull</addtitle><date>2007-06-01</date><risdate>2007</risdate><volume>30</volume><issue>6</issue><spage>1171</spage><epage>1176</epage><pages>1171-1176</pages><issn>0918-6158</issn><eissn>1347-5215</eissn><abstract>Phase solubility behavior of coenzyme Q10 (CoQ10) at 25 °C in various molar solutions of poloxamer 188 (P188) in water was observed and their binary solid dispersions (BSD) at different weight ratios were prepared by a simple, rapid, cost effective, uncomplicated and potentially scalable low temperature melting method. BSDs were characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for improved solubility at 25 °C and 37 °C and in-vitro release of CoQ10 at 37 °C in distilled water. Solubility of CoQ10 increased with increasing concentrations of P188 in water. Gibbs free energy (ΔG°tr) values were all negative indicating the spontaneous nature of CoQ10 solubilization and decreased with increasing concentration of P188 demonstrating that the reaction conditions became more favorable as the concentration of P188 increased. DSC and SEM analysis indicated that the homogeneity of dispersion was not at the molecular level. However, BSDs exhibited a remarkably improved aqueous solubility and dissolution of CoQ10.</abstract><cop>Japan</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>17541177</pmid><doi>10.1248/bpb.30.1171</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | binary solid dispersion Calorimetry, Differential Scanning Chemistry, Pharmaceutical Chromatography, High Pressure Liquid coenzyme Q10 Coenzymes - analysis Coenzymes - chemistry Coenzymes - ultrastructure dissolution Drug Compounding Evaluation Studies as Topic Molecular Structure Poloxamer - chemistry poloxamer 188 Powders Solubility Solvents - chemistry Spectrophotometry, Ultraviolet Temperature Thermodynamics Ubiquinone - analogs & derivatives Ubiquinone - analysis Ubiquinone - chemistry Ubiquinone - ultrastructure Water - chemistry |
| title | Preparation, Characterization and Evaluation of Coenzyme Q10 Binary Solid Dispersions for Enhanced Solubility and Dissolution |
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