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An eutomer/distomer ratio near unity does not justify non-enantiospecific assay methods in bioequivalence studies
The aim of the present investigation was to compare the pharmacokinetics of two tablet formulations of 600 mg of racemic ibuprofen obtained using enantiospecific and non‐enantiospecific assays, in order to explore if chiral assays should be employed in bioequivalence studies of chiral active substan...
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| Published in: | Chirality (New York, N.Y.) N.Y.), 2005, Vol.17 (8), p.470-475 |
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| cited_by | cdi_FETCH-LOGICAL-c3656-e724335edde6815532c23edf2ad55f0e84d2e76a0d7fda22c656d49dc04ea9393 |
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| cites | cdi_FETCH-LOGICAL-c3656-e724335edde6815532c23edf2ad55f0e84d2e76a0d7fda22c656d49dc04ea9393 |
| container_end_page | 475 |
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| container_title | Chirality (New York, N.Y.) |
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| creator | García-Arieta, Alfredo Abad-Santos, Francisco Rodríguez-Martínez, M. Angeles Varas-Polo, Yolanda Novalbos, Jesús Laparidis, Nikos Gallego-Sandín, Sonia Orfanidis, Kyriakos Torrado, Juan |
| description | The aim of the present investigation was to compare the pharmacokinetics of two tablet formulations of 600 mg of racemic ibuprofen obtained using enantiospecific and non‐enantiospecific assays, in order to explore if chiral assays should be employed in bioequivalence studies of chiral active substances. The stereoselective assay showed that, for both formulations, there was an initial phase where (R)‐ibuprofen was the predominant enantiomer followed by a final phase where (S)‐ibuprofen was the predominant one. Results from both analytical methods proved that the two formulations were bioequivalent. However, the chiral bioanalytical method detected a larger difference in the eutomer than that showed by the nonchiral bioanalytical method. In conclusion, although the exposure ratios of enantiomers are near unity, the measurement of unresolved ibuprofen alone is not an adequate measure of bioequivalence since it may mask the actual difference in the eutomer exposure among formulations. © 2005 Wiley‐Liss, Inc. Chirality 17:470–475, 2005. |
| doi_str_mv | 10.1002/chir.20186 |
| format | article |
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Angeles ; Varas-Polo, Yolanda ; Novalbos, Jesús ; Laparidis, Nikos ; Gallego-Sandín, Sonia ; Orfanidis, Kyriakos ; Torrado, Juan</creator><creatorcontrib>García-Arieta, Alfredo ; Abad-Santos, Francisco ; Rodríguez-Martínez, M. Angeles ; Varas-Polo, Yolanda ; Novalbos, Jesús ; Laparidis, Nikos ; Gallego-Sandín, Sonia ; Orfanidis, Kyriakos ; Torrado, Juan</creatorcontrib><description>The aim of the present investigation was to compare the pharmacokinetics of two tablet formulations of 600 mg of racemic ibuprofen obtained using enantiospecific and non‐enantiospecific assays, in order to explore if chiral assays should be employed in bioequivalence studies of chiral active substances. The stereoselective assay showed that, for both formulations, there was an initial phase where (R)‐ibuprofen was the predominant enantiomer followed by a final phase where (S)‐ibuprofen was the predominant one. Results from both analytical methods proved that the two formulations were bioequivalent. However, the chiral bioanalytical method detected a larger difference in the eutomer than that showed by the nonchiral bioanalytical method. In conclusion, although the exposure ratios of enantiomers are near unity, the measurement of unresolved ibuprofen alone is not an adequate measure of bioequivalence since it may mask the actual difference in the eutomer exposure among formulations. © 2005 Wiley‐Liss, Inc. Chirality 17:470–475, 2005.</description><identifier>ISSN: 0899-0042</identifier><identifier>EISSN: 1520-636X</identifier><identifier>DOI: 10.1002/chir.20186</identifier><identifier>PMID: 16104026</identifier><language>eng</language><publisher>Hoboken: Wiley Subscription Services, Inc., A Wiley Company</publisher><subject>Administration, Oral ; Adult ; Analysis of Variance ; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal - blood ; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics ; Area Under Curve ; bioequivalence ; chirality ; Cross-Over Studies ; enantiomers ; Female ; Humans ; ibuprofen ; Ibuprofen - administration & dosage ; Ibuprofen - blood ; Ibuprofen - pharmacokinetics ; Intestinal Absorption ; Male ; pharmacokinetics ; Stereoisomerism ; Tablets ; Therapeutic Equivalency</subject><ispartof>Chirality (New York, N.Y.), 2005, Vol.17 (8), p.470-475</ispartof><rights>Copyright © 2005 Wiley‐Liss, Inc., A Wiley Company</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3656-e724335edde6815532c23edf2ad55f0e84d2e76a0d7fda22c656d49dc04ea9393</citedby><cites>FETCH-LOGICAL-c3656-e724335edde6815532c23edf2ad55f0e84d2e76a0d7fda22c656d49dc04ea9393</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%2Fchir.20186$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fchir.20186$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>315,786,790,4043,27956,27957,27958,50923,51032</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16104026$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>García-Arieta, Alfredo</creatorcontrib><creatorcontrib>Abad-Santos, Francisco</creatorcontrib><creatorcontrib>Rodríguez-Martínez, M. Angeles</creatorcontrib><creatorcontrib>Varas-Polo, Yolanda</creatorcontrib><creatorcontrib>Novalbos, Jesús</creatorcontrib><creatorcontrib>Laparidis, Nikos</creatorcontrib><creatorcontrib>Gallego-Sandín, Sonia</creatorcontrib><creatorcontrib>Orfanidis, Kyriakos</creatorcontrib><creatorcontrib>Torrado, Juan</creatorcontrib><title>An eutomer/distomer ratio near unity does not justify non-enantiospecific assay methods in bioequivalence studies</title><title>Chirality (New York, N.Y.)</title><addtitle>Chirality</addtitle><description>The aim of the present investigation was to compare the pharmacokinetics of two tablet formulations of 600 mg of racemic ibuprofen obtained using enantiospecific and non‐enantiospecific assays, in order to explore if chiral assays should be employed in bioequivalence studies of chiral active substances. The stereoselective assay showed that, for both formulations, there was an initial phase where (R)‐ibuprofen was the predominant enantiomer followed by a final phase where (S)‐ibuprofen was the predominant one. Results from both analytical methods proved that the two formulations were bioequivalent. However, the chiral bioanalytical method detected a larger difference in the eutomer than that showed by the nonchiral bioanalytical method. In conclusion, although the exposure ratios of enantiomers are near unity, the measurement of unresolved ibuprofen alone is not an adequate measure of bioequivalence since it may mask the actual difference in the eutomer exposure among formulations. © 2005 Wiley‐Liss, Inc. Chirality 17:470–475, 2005.</description><subject>Administration, Oral</subject><subject>Adult</subject><subject>Analysis of Variance</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - blood</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</subject><subject>Area Under Curve</subject><subject>bioequivalence</subject><subject>chirality</subject><subject>Cross-Over Studies</subject><subject>enantiomers</subject><subject>Female</subject><subject>Humans</subject><subject>ibuprofen</subject><subject>Ibuprofen - administration & dosage</subject><subject>Ibuprofen - blood</subject><subject>Ibuprofen - pharmacokinetics</subject><subject>Intestinal Absorption</subject><subject>Male</subject><subject>pharmacokinetics</subject><subject>Stereoisomerism</subject><subject>Tablets</subject><subject>Therapeutic Equivalency</subject><issn>0899-0042</issn><issn>1520-636X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><recordid>eNp9kUFv1DAQhS0Eokvhwg9APnFASju2Eyc5VivoVqpAQkARF8u1J6pLYu96EiD_nmx3gRuneYfvfYc3jL0UcCYA5Lm7C_lMgmj0I7YSlYRCK_31MVtB07YFQClP2DOiewBotSqfshOhBZQg9YrtLiLHaUwD5nMf6CHwbMeQeESb-RTDOHOfkHhMI7-faAzdvORYYLRx4WiLLnTBcUtkZz7geJc88RD5bUi4m8IP22N0yGmcfEB6zp50tid8cbyn7PO7t5_Wm-L6w-XV-uK6cEpXusBalkpV6D3qRlSVkk4q9J20vqo6wKb0Emttwdedt1K6peTL1jso0baqVafs9cG7zWk3IY1mCOSw723ENJHRzV6q6gV8cwBdTkQZO7PNYbB5NgLMfmCzH9g8DLzAr47W6XZA_w89LroA4gD8DD3O_1GZ9ebq4x9pcegsD8Bffzs2fze6VnVlbt5fmvab2nyBG2Fa9Rs3sJfQ</recordid><startdate>2005</startdate><enddate>2005</enddate><creator>García-Arieta, Alfredo</creator><creator>Abad-Santos, Francisco</creator><creator>Rodríguez-Martínez, M. 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Angeles ; Varas-Polo, Yolanda ; Novalbos, Jesús ; Laparidis, Nikos ; Gallego-Sandín, Sonia ; Orfanidis, Kyriakos ; Torrado, Juan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3656-e724335edde6815532c23edf2ad55f0e84d2e76a0d7fda22c656d49dc04ea9393</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Administration, Oral</topic><topic>Adult</topic><topic>Analysis of Variance</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - blood</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</topic><topic>Area Under Curve</topic><topic>bioequivalence</topic><topic>chirality</topic><topic>Cross-Over Studies</topic><topic>enantiomers</topic><topic>Female</topic><topic>Humans</topic><topic>ibuprofen</topic><topic>Ibuprofen - administration & dosage</topic><topic>Ibuprofen - blood</topic><topic>Ibuprofen - pharmacokinetics</topic><topic>Intestinal Absorption</topic><topic>Male</topic><topic>pharmacokinetics</topic><topic>Stereoisomerism</topic><topic>Tablets</topic><topic>Therapeutic Equivalency</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>García-Arieta, Alfredo</creatorcontrib><creatorcontrib>Abad-Santos, Francisco</creatorcontrib><creatorcontrib>Rodríguez-Martínez, M. 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Angeles</au><au>Varas-Polo, Yolanda</au><au>Novalbos, Jesús</au><au>Laparidis, Nikos</au><au>Gallego-Sandín, Sonia</au><au>Orfanidis, Kyriakos</au><au>Torrado, Juan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>An eutomer/distomer ratio near unity does not justify non-enantiospecific assay methods in bioequivalence studies</atitle><jtitle>Chirality (New York, N.Y.)</jtitle><addtitle>Chirality</addtitle><date>2005</date><risdate>2005</risdate><volume>17</volume><issue>8</issue><spage>470</spage><epage>475</epage><pages>470-475</pages><issn>0899-0042</issn><eissn>1520-636X</eissn><notes>istex:9A901C66D82FD92FAEFFB8172C0E9DCCB9EF9FC6</notes><notes>This manuscript represents the personal opinion of the author and does not necessarily represent the views or policy of the Spanish Agency for Medicines and Health Care Products</notes><notes>ark:/67375/WNG-9Z3HV0W1-9</notes><notes>ArticleID:CHIR20186</notes><notes>ObjectType-Article-2</notes><notes>SourceType-Scholarly Journals-1</notes><notes>ObjectType-Feature-1</notes><notes>ObjectType-News-3</notes><notes>content type line 23</notes><abstract>The aim of the present investigation was to compare the pharmacokinetics of two tablet formulations of 600 mg of racemic ibuprofen obtained using enantiospecific and non‐enantiospecific assays, in order to explore if chiral assays should be employed in bioequivalence studies of chiral active substances. The stereoselective assay showed that, for both formulations, there was an initial phase where (R)‐ibuprofen was the predominant enantiomer followed by a final phase where (S)‐ibuprofen was the predominant one. Results from both analytical methods proved that the two formulations were bioequivalent. However, the chiral bioanalytical method detected a larger difference in the eutomer than that showed by the nonchiral bioanalytical method. In conclusion, although the exposure ratios of enantiomers are near unity, the measurement of unresolved ibuprofen alone is not an adequate measure of bioequivalence since it may mask the actual difference in the eutomer exposure among formulations. © 2005 Wiley‐Liss, Inc. Chirality 17:470–475, 2005.</abstract><cop>Hoboken</cop><pub>Wiley Subscription Services, Inc., A Wiley Company</pub><pmid>16104026</pmid><doi>10.1002/chir.20186</doi><tpages>6</tpages></addata></record> |
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| identifier | ISSN: 0899-0042 |
| ispartof | Chirality (New York, N.Y.), 2005, Vol.17 (8), p.470-475 |
| issn | 0899-0042 1520-636X |
| language | eng |
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| source | Wiley-Blackwell Journals |
| subjects | Administration, Oral Adult Analysis of Variance Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - blood Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Area Under Curve bioequivalence chirality Cross-Over Studies enantiomers Female Humans ibuprofen Ibuprofen - administration & dosage Ibuprofen - blood Ibuprofen - pharmacokinetics Intestinal Absorption Male pharmacokinetics Stereoisomerism Tablets Therapeutic Equivalency |
| title | An eutomer/distomer ratio near unity does not justify non-enantiospecific assay methods in bioequivalence studies |
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