Eutectic crystal of regorafenib and pimelic acid and preparation method thereof
The invention discloses a eutectic crystal of regorafenib and pimelic acid and a preparation method thereof. The molar ratio of regorafenib to pimelic acid in the eutectic crystal is 1: 1, and an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks when 2[theta] values a...
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| creator | DAI XIALIN CHEN JIAMEI JIA JUNLONG CHE HAOJIE |
| description | The invention discloses a eutectic crystal of regorafenib and pimelic acid and a preparation method thereof. The molar ratio of regorafenib to pimelic acid in the eutectic crystal is 1: 1, and an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks when 2[theta] values are 7.9 +/-0.2 degrees, 11.2 +/-0.2 degrees, 16.7 +/-0.2 degrees, 19.7 +/-0.2 degrees and 24.1 +/-0.2degrees. The preparation method is simple in process, easily controls the crystallization process, is good in reproducibility and is suitable for industrial production. Compared with regorafenib monohydrate, the eutectic crystal has lower hygroscopicity and higher apparent solubility, and is beneficial to improving the stability and oral absorption efficiency of regorafenib.
本发明公开了一种瑞戈非尼与庚二酸共晶及其制备方法。该共晶中瑞戈非尼与庚二酸的摩尔比为1∶1，该共晶X射线粉末衍射图在2theta值为7.9±0.2°、11.2±0.2°、16.7±0.2°、19.7±0.2°、24.1±0.2°处具有特征峰。本发明提供的共晶制备方法工艺简单，结晶过程易于控制，重现性好，适用于工业化生产。这种共晶较瑞戈非尼一水合物具有较低的吸湿性，较高的表观溶解度，有利于提高瑞戈非尼的稳定性和口服吸收效率。 |
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本发明公开了一种瑞戈非尼与庚二酸共晶及其制备方法。该共晶中瑞戈非尼与庚二酸的摩尔比为1∶1，该共晶X射线粉末衍射图在2theta值为7.9±0.2°、11.2±0.2°、16.7±0.2°、19.7±0.2°、24.1±0.2°处具有特征峰。本发明提供的共晶制备方法工艺简单，结晶过程易于控制，重现性好，适用于工业化生产。这种共晶较瑞戈非尼一水合物具有较低的吸湿性，较高的表观溶解度，有利于提高瑞戈非尼的稳定性和口服吸收效率。</description><language>chi ; eng</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2020</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20201016&DB=EPODOC&CC=CN&NR=111777552A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20201016&DB=EPODOC&CC=CN&NR=111777552A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>DAI XIALIN</creatorcontrib><creatorcontrib>CHEN JIAMEI</creatorcontrib><creatorcontrib>JIA JUNLONG</creatorcontrib><creatorcontrib>CHE HAOJIE</creatorcontrib><title>Eutectic crystal of regorafenib and pimelic acid and preparation method thereof</title><description>The invention discloses a eutectic crystal of regorafenib and pimelic acid and a preparation method thereof. The molar ratio of regorafenib to pimelic acid in the eutectic crystal is 1: 1, and an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks when 2[theta] values are 7.9 +/-0.2 degrees, 11.2 +/-0.2 degrees, 16.7 +/-0.2 degrees, 19.7 +/-0.2 degrees and 24.1 +/-0.2degrees. The preparation method is simple in process, easily controls the crystallization process, is good in reproducibility and is suitable for industrial production. Compared with regorafenib monohydrate, the eutectic crystal has lower hygroscopicity and higher apparent solubility, and is beneficial to improving the stability and oral absorption efficiency of regorafenib.
本发明公开了一种瑞戈非尼与庚二酸共晶及其制备方法。该共晶中瑞戈非尼与庚二酸的摩尔比为1∶1，该共晶X射线粉末衍射图在2theta值为7.9±0.2°、11.2±0.2°、16.7±0.2°、19.7±0.2°、24.1±0.2°处具有特征峰。本发明提供的共晶制备方法工艺简单，结晶过程易于控制，重现性好，适用于工业化生产。这种共晶较瑞戈非尼一水合物具有较低的吸湿性，较高的表观溶解度，有利于提高瑞戈非尼的稳定性和口服吸收效率。</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2020</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNyjEKAjEQRuE0FqLeYTyARZQltSwrVtrYL2Pyxw1kk5CMhbdX0ANYPXh8S3UdngIrwZKtryYcKXuqeOTKHinciZOjEmbED2Eb3HdUFK4sISeaIVN2JBMqsl-rhefYsPl1pban4dafdyh5RCtskSBjf9FaG2O6bn88_GPeWhA2_A</recordid><startdate>20201016</startdate><enddate>20201016</enddate><creator>DAI XIALIN</creator><creator>CHEN JIAMEI</creator><creator>JIA JUNLONG</creator><creator>CHE HAOJIE</creator><scope>EVB</scope></search><sort><creationdate>20201016</creationdate><title>Eutectic crystal of regorafenib and pimelic acid and preparation method thereof</title><author>DAI XIALIN ; CHEN JIAMEI ; JIA JUNLONG ; CHE HAOJIE</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN111777552A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>chi ; eng</language><creationdate>2020</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>DAI XIALIN</creatorcontrib><creatorcontrib>CHEN JIAMEI</creatorcontrib><creatorcontrib>JIA JUNLONG</creatorcontrib><creatorcontrib>CHE HAOJIE</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>DAI XIALIN</au><au>CHEN JIAMEI</au><au>JIA JUNLONG</au><au>CHE HAOJIE</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Eutectic crystal of regorafenib and pimelic acid and preparation method thereof</title><date>2020-10-16</date><risdate>2020</risdate><abstract>The invention discloses a eutectic crystal of regorafenib and pimelic acid and a preparation method thereof. The molar ratio of regorafenib to pimelic acid in the eutectic crystal is 1: 1, and an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks when 2[theta] values are 7.9 +/-0.2 degrees, 11.2 +/-0.2 degrees, 16.7 +/-0.2 degrees, 19.7 +/-0.2 degrees and 24.1 +/-0.2degrees. The preparation method is simple in process, easily controls the crystallization process, is good in reproducibility and is suitable for industrial production. Compared with regorafenib monohydrate, the eutectic crystal has lower hygroscopicity and higher apparent solubility, and is beneficial to improving the stability and oral absorption efficiency of regorafenib.
本发明公开了一种瑞戈非尼与庚二酸共晶及其制备方法。该共晶中瑞戈非尼与庚二酸的摩尔比为1∶1，该共晶X射线粉末衍射图在2theta值为7.9±0.2°、11.2±0.2°、16.7±0.2°、19.7±0.2°、24.1±0.2°处具有特征峰。本发明提供的共晶制备方法工艺简单，结晶过程易于控制，重现性好，适用于工业化生产。这种共晶较瑞戈非尼一水合物具有较低的吸湿性，较高的表观溶解度，有利于提高瑞戈非尼的稳定性和口服吸收效率。</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
| title | Eutectic crystal of regorafenib and pimelic acid and preparation method thereof |
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