Determination of minor quantities of linezolid polymorphs in a drug substance and tablet formulation by powder X-ray diffraction technique
Linezolid (LZD) is one of the first commercially available synthetic oxazolidinone antibiotics and is widely used for the treatment of multidrug-resistant Gram-positive bacterial infection. LZD was found to have five polymorphic forms. The most stable and commercialized polymorphs are known as forms...
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| Veröffentlicht in: | Powder diffraction 2017-06, Vol.32 (2), p.78-85 |
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| creator | Sun, Mengying Hu, Xiurong Zhou, Xinbo Gu, Jianming |
| description | Linezolid (LZD) is one of the first commercially available synthetic oxazolidinone antibiotics and is widely used for the treatment of multidrug-resistant Gram-positive bacterial infection. LZD was found to have five polymorphic forms. The most stable and commercialized polymorphs are known as forms II and IV. Trace content of form II in LZD form IV will cause to transition LZD form IV to II rapidly. Powder X-ray diffraction (PXRD) methods were evaluated for the determination of the polymorphic content of the drug substance and drug product. The estimated limit of detection values of the single peak method for LZD polymorph form II in drug substance and tablet formulation were 0.4 and 0.6%, respectively, while the limit of detection value of Rietveld Refinement (full-profile fitting) evaluated LZD polymorph form II in drug substance was 0.2%. The results clearly show that levels |
| doi_str_mv | 10.1017/S0885715617000069 |
| format | Article |
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LZD was found to have five polymorphic forms. The most stable and commercialized polymorphs are known as forms II and IV. Trace content of form II in LZD form IV will cause to transition LZD form IV to II rapidly. Powder X-ray diffraction (PXRD) methods were evaluated for the determination of the polymorphic content of the drug substance and drug product. The estimated limit of detection values of the single peak method for LZD polymorph form II in drug substance and tablet formulation were 0.4 and 0.6%, respectively, while the limit of detection value of Rietveld Refinement (full-profile fitting) evaluated LZD polymorph form II in drug substance was 0.2%. The results clearly show that levels <1 wt.% (in active pharmaceutical ingredients) and 2 wt.% (in tablets) LZD form II in form IV can be detected and quantified by PXRD. Validation of the analytical method proved that the method is repeatable, sensitive, and accurate.</description><identifier>ISSN: 0885-7156</identifier><identifier>EISSN: 1945-7413</identifier><identifier>DOI: 10.1017/S0885715617000069</identifier><language>eng</language><publisher>New York, USA: Cambridge University Press</publisher><subject>Antibiotics ; Bacteria ; Bioavailability ; Commercialization ; Crystals ; Gram-positive bacteria ; Mathematical analysis ; Methods ; Pharmaceuticals ; Polymorphism ; Product development ; Quantitative analysis ; Solids ; Staphylococcus infections ; Technical Articles ; X-ray diffraction</subject><ispartof>Powder diffraction, 2017-06, Vol.32 (2), p.78-85</ispartof><rights>Copyright © International Centre for Diffraction Data 2017</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c317t-5c6d687af4bf5b2ec27f9331a6d30e5e27dbc5aaeb2227526a4b1342bb8dec33</citedby><cites>FETCH-LOGICAL-c317t-5c6d687af4bf5b2ec27f9331a6d30e5e27dbc5aaeb2227526a4b1342bb8dec33</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.cambridge.org/core/product/identifier/S0885715617000069/type/journal_article$$EHTML$$P50$$Gcambridge$$H</linktohtml><link.rule.ids>164,314,778,782,27907,27908,55611</link.rule.ids></links><search><creatorcontrib>Sun, Mengying</creatorcontrib><creatorcontrib>Hu, Xiurong</creatorcontrib><creatorcontrib>Zhou, Xinbo</creatorcontrib><creatorcontrib>Gu, Jianming</creatorcontrib><title>Determination of minor quantities of linezolid polymorphs in a drug substance and tablet formulation by powder X-ray diffraction technique</title><title>Powder diffraction</title><addtitle>Powder Diffr</addtitle><description>Linezolid (LZD) is one of the first commercially available synthetic oxazolidinone antibiotics and is widely used for the treatment of multidrug-resistant Gram-positive bacterial infection. LZD was found to have five polymorphic forms. The most stable and commercialized polymorphs are known as forms II and IV. Trace content of form II in LZD form IV will cause to transition LZD form IV to II rapidly. Powder X-ray diffraction (PXRD) methods were evaluated for the determination of the polymorphic content of the drug substance and drug product. The estimated limit of detection values of the single peak method for LZD polymorph form II in drug substance and tablet formulation were 0.4 and 0.6%, respectively, while the limit of detection value of Rietveld Refinement (full-profile fitting) evaluated LZD polymorph form II in drug substance was 0.2%. The results clearly show that levels <1 wt.% (in active pharmaceutical ingredients) and 2 wt.% (in tablets) LZD form II in form IV can be detected and quantified by PXRD. Validation of the analytical method proved that the method is repeatable, sensitive, and accurate.</description><subject>Antibiotics</subject><subject>Bacteria</subject><subject>Bioavailability</subject><subject>Commercialization</subject><subject>Crystals</subject><subject>Gram-positive bacteria</subject><subject>Mathematical analysis</subject><subject>Methods</subject><subject>Pharmaceuticals</subject><subject>Polymorphism</subject><subject>Product development</subject><subject>Quantitative analysis</subject><subject>Solids</subject><subject>Staphylococcus infections</subject><subject>Technical Articles</subject><subject>X-ray diffraction</subject><issn>0885-7156</issn><issn>1945-7413</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><recordid>eNp1UMlKBDEQDaLguHyAt4Dn1iydTs9R3EHwoAdvTZbKTKQ7GZM0Mn6CX22P40EQ61JFvQ0eQieUnFFC5fkTaVshqWioJNM08x00o_NaVLKmfBfNNnC1wffRQc6vhFDaCjZDn1dQIA0-qOJjwNHh6Y4Jv40qFF885M2v9wE-Yu8tXsV-PcS0WmbsA1bYpnGB86hzUcEAVsHionQPBbuYhrHf2ur1JHy3kPBLldQaW-9cUuYbK2CWwb-NcIT2nOozHP_sQ_R8c_18eVc9PN7eX148VIZTWSphGtu0UrlaO6EZGCbdnHOqGssJCGDSaiOUAs0Yk4I1qtaU10zr1oLh_BCdbm1XKU6puXSvcUxhSuzonE5DGtZMLLplmRRzTuC6VfKDSuuOkm7TePen8UnDfzRq0MnbBfyy_lf1BX7JhnA</recordid><startdate>201706</startdate><enddate>201706</enddate><creator>Sun, Mengying</creator><creator>Hu, Xiurong</creator><creator>Zhou, Xinbo</creator><creator>Gu, Jianming</creator><general>Cambridge University Press</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7SR</scope><scope>8BQ</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>ABJCF</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>CCPQU</scope><scope>D1I</scope><scope>DWQXO</scope><scope>HCIFZ</scope><scope>JG9</scope><scope>KB.</scope><scope>PDBOC</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>S0W</scope></search><sort><creationdate>201706</creationdate><title>Determination of minor quantities of linezolid polymorphs in a drug substance and tablet formulation by powder X-ray diffraction technique</title><author>Sun, Mengying ; 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LZD was found to have five polymorphic forms. The most stable and commercialized polymorphs are known as forms II and IV. Trace content of form II in LZD form IV will cause to transition LZD form IV to II rapidly. Powder X-ray diffraction (PXRD) methods were evaluated for the determination of the polymorphic content of the drug substance and drug product. The estimated limit of detection values of the single peak method for LZD polymorph form II in drug substance and tablet formulation were 0.4 and 0.6%, respectively, while the limit of detection value of Rietveld Refinement (full-profile fitting) evaluated LZD polymorph form II in drug substance was 0.2%. The results clearly show that levels <1 wt.% (in active pharmaceutical ingredients) and 2 wt.% (in tablets) LZD form II in form IV can be detected and quantified by PXRD. Validation of the analytical method proved that the method is repeatable, sensitive, and accurate.</abstract><cop>New York, USA</cop><pub>Cambridge University Press</pub><doi>10.1017/S0885715617000069</doi><tpages>8</tpages></addata></record> |
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| source | Cambridge University Press Journals Complete |
| subjects | Antibiotics Bacteria Bioavailability Commercialization Crystals Gram-positive bacteria Mathematical analysis Methods Pharmaceuticals Polymorphism Product development Quantitative analysis Solids Staphylococcus infections Technical Articles X-ray diffraction |
| title | Determination of minor quantities of linezolid polymorphs in a drug substance and tablet formulation by powder X-ray diffraction technique |
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