Correlation of Plasma Ibuprofen Levels with Biological Activity
Investigations with ibuprofen [(±)-p-isobutylhydratropic acid], a well-tolerated, orally active, anti-inflammatory drug, were undertaken to: (a) determine the relationship among plasma drug concentrations, administered dose, and anti-inflammatory activity in developing and established polyarthritis...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 1974-05, Vol.63 (5), p.784-786 |
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| container_title | Journal of pharmaceutical sciences |
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| creator | Kaiser, David G. Myles Glenn, E. |
| description | Investigations with ibuprofen [(±)-p-isobutylhydratropic acid], a well-tolerated, orally active, anti-inflammatory drug, were undertaken to: (a) determine the relationship among plasma drug concentrations, administered dose, and anti-inflammatory activity in developing and established polyarthritis in rats; and (b) compare the plasma drug disappearance half-lives in normal and polyarthritic rats. The results indicated that plasma drug concentrations in normal and polyarthritic rats were dose related. The logarithm of biological activity expressed as [% IPA/(100 – % IPA)], where % IPA is the mean percent inhibition of developing or established polyarthritis as measured by plasma inflammation units, was related to the logarithms of: (a) administered dose (mg kg−1), (b) plasma drug concentrations (μg ml−1) at 2hr postadministration, and (c) average plasma drug concentrations (μg ml−1) in a dosage interval at the equilibrium state. Half-lives for elimination of ibuprofen from the plasma of normal rats (after single-dose oral drug administration) and polyarthritic rats (after 29 doses) were essentially identical. |
| doi_str_mv | 10.1002/jps.2600630530 |
| format | Article |
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The results indicated that plasma drug concentrations in normal and polyarthritic rats were dose related. The logarithm of biological activity expressed as [% IPA/(100 – % IPA)], where % IPA is the mean percent inhibition of developing or established polyarthritis as measured by plasma inflammation units, was related to the logarithms of: (a) administered dose (mg kg−1), (b) plasma drug concentrations (μg ml−1) at 2hr postadministration, and (c) average plasma drug concentrations (μg ml−1) in a dosage interval at the equilibrium state. Half-lives for elimination of ibuprofen from the plasma of normal rats (after single-dose oral drug administration) and polyarthritic rats (after 29 doses) were essentially identical.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.2600630530</identifier><identifier>PMID: 4830005</identifier><language>eng</language><publisher>Washington: Elsevier Inc</publisher><subject>Animals ; Anti-Inflammatory Agents - administration & dosage ; Anti-Inflammatory Agents - blood ; Anti-Inflammatory Agents - therapeutic use ; Anti-inflammatory agents-ibuprofen plasma levels correlated with biological activity ; Arthritis - drug therapy ; Biological activity-correlated with ibuprofen plasma levels ; Chromatography, Gas ; Dose-Response Relationship, Drug ; Half-Life ; Ibuprofen-plasma levels correlated with biological activity ; Male ; Phenylpropionates - administration & dosage ; Phenylpropionates - blood ; Rats ; Time Factors ; Tropanes - therapeutic use</subject><ispartof>Journal of pharmaceutical sciences, 1974-05, Vol.63 (5), p.784-786</ispartof><rights>1974 Wiley-Liss, Inc., A Wiley Company</rights><rights>Copyright © 1974 Wiley‐Liss, Inc., A Wiley Company</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4270-25febb074cf2e86246374f0bf9f1e46f778a3504186ee38b994cb12598f3e22e3</citedby><cites>FETCH-LOGICAL-c4270-25febb074cf2e86246374f0bf9f1e46f778a3504186ee38b994cb12598f3e22e3</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%2Fjps.2600630530$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.2600630530$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/4830005$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kaiser, David G.</creatorcontrib><creatorcontrib>Myles Glenn, E.</creatorcontrib><title>Correlation of Plasma Ibuprofen Levels with Biological Activity</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>Investigations with ibuprofen [(±)-p-isobutylhydratropic acid], a well-tolerated, orally active, anti-inflammatory drug, were undertaken to: (a) determine the relationship among plasma drug concentrations, administered dose, and anti-inflammatory activity in developing and established polyarthritis in rats; and (b) compare the plasma drug disappearance half-lives in normal and polyarthritic rats. The results indicated that plasma drug concentrations in normal and polyarthritic rats were dose related. The logarithm of biological activity expressed as [% IPA/(100 – % IPA)], where % IPA is the mean percent inhibition of developing or established polyarthritis as measured by plasma inflammation units, was related to the logarithms of: (a) administered dose (mg kg−1), (b) plasma drug concentrations (μg ml−1) at 2hr postadministration, and (c) average plasma drug concentrations (μg ml−1) in a dosage interval at the equilibrium state. Half-lives for elimination of ibuprofen from the plasma of normal rats (after single-dose oral drug administration) and polyarthritic rats (after 29 doses) were essentially identical.</description><subject>Animals</subject><subject>Anti-Inflammatory Agents - administration & dosage</subject><subject>Anti-Inflammatory Agents - blood</subject><subject>Anti-Inflammatory Agents - therapeutic use</subject><subject>Anti-inflammatory agents-ibuprofen plasma levels correlated with biological activity</subject><subject>Arthritis - drug therapy</subject><subject>Biological activity-correlated with ibuprofen plasma levels</subject><subject>Chromatography, Gas</subject><subject>Dose-Response Relationship, Drug</subject><subject>Half-Life</subject><subject>Ibuprofen-plasma levels correlated with biological activity</subject><subject>Male</subject><subject>Phenylpropionates - administration & dosage</subject><subject>Phenylpropionates - blood</subject><subject>Rats</subject><subject>Time Factors</subject><subject>Tropanes - therapeutic use</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1974</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1vEzEQhi0EKmnLlRvSnrhtmPXn7gmViH5A1FYCBDfL64xbFycO9iYl_75GGxVxQD2NrHneV-OHkNcNTBsA-u5unadUAkgGgsEzMmkEhVpCo56TSQFozQTvXpLDnO-gYCDEATngLSsPMSHvZzElDGbwcVVFV10Hk5emuug36xQdrqo5bjHk6t4Pt9UHH0O88daE6sQOfuuH3TF54UzI-Go_j8i3049fZ-f1_OrsYnYyry2nCmoqHPY9KG4dxVZSLpniDnrXuQa5dEq1hgngTSsRWdt3Hbd9Q0XXOoaUIjsib8fectavDeZBL322GIJZYdxk3VImFKWigNMRtCnmnNDpdfJLk3a6Af3HmC7G9F9jJfBm37zpl7h4xPeKyr4b9_c-4O6JNv3p-ss_3fWY9XnA349Zk35qqZgS-vvlmf6sKHTyR6dl4duRL8px6zHpbD2uLC58QjvoRfT_-8YD5ieXtw</recordid><startdate>197405</startdate><enddate>197405</enddate><creator>Kaiser, David G.</creator><creator>Myles Glenn, E.</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><scope>BSCLL</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>197405</creationdate><title>Correlation of Plasma Ibuprofen Levels with Biological Activity</title><author>Kaiser, David G. ; Myles Glenn, E.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4270-25febb074cf2e86246374f0bf9f1e46f778a3504186ee38b994cb12598f3e22e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1974</creationdate><topic>Animals</topic><topic>Anti-Inflammatory Agents - administration & dosage</topic><topic>Anti-Inflammatory Agents - blood</topic><topic>Anti-Inflammatory Agents - therapeutic use</topic><topic>Anti-inflammatory agents-ibuprofen plasma levels correlated with biological activity</topic><topic>Arthritis - drug therapy</topic><topic>Biological activity-correlated with ibuprofen plasma levels</topic><topic>Chromatography, Gas</topic><topic>Dose-Response Relationship, Drug</topic><topic>Half-Life</topic><topic>Ibuprofen-plasma levels correlated with biological activity</topic><topic>Male</topic><topic>Phenylpropionates - administration & dosage</topic><topic>Phenylpropionates - blood</topic><topic>Rats</topic><topic>Time Factors</topic><topic>Tropanes - therapeutic use</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kaiser, David G.</creatorcontrib><creatorcontrib>Myles Glenn, E.</creatorcontrib><collection>Istex</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>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kaiser, David G.</au><au>Myles Glenn, E.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Correlation of Plasma Ibuprofen Levels with Biological Activity</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>1974-05</date><risdate>1974</risdate><volume>63</volume><issue>5</issue><spage>784</spage><epage>786</epage><pages>784-786</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><abstract>Investigations with ibuprofen [(±)-p-isobutylhydratropic acid], a well-tolerated, orally active, anti-inflammatory drug, were undertaken to: (a) determine the relationship among plasma drug concentrations, administered dose, and anti-inflammatory activity in developing and established polyarthritis in rats; and (b) compare the plasma drug disappearance half-lives in normal and polyarthritic rats. The results indicated that plasma drug concentrations in normal and polyarthritic rats were dose related. The logarithm of biological activity expressed as [% IPA/(100 – % IPA)], where % IPA is the mean percent inhibition of developing or established polyarthritis as measured by plasma inflammation units, was related to the logarithms of: (a) administered dose (mg kg−1), (b) plasma drug concentrations (μg ml−1) at 2hr postadministration, and (c) average plasma drug concentrations (μg ml−1) in a dosage interval at the equilibrium state. Half-lives for elimination of ibuprofen from the plasma of normal rats (after single-dose oral drug administration) and polyarthritic rats (after 29 doses) were essentially identical.</abstract><cop>Washington</cop><pub>Elsevier Inc</pub><pmid>4830005</pmid><doi>10.1002/jps.2600630530</doi><tpages>3</tpages></addata></record> |
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| ispartof | Journal of pharmaceutical sciences, 1974-05, Vol.63 (5), p.784-786 |
| issn | 0022-3549 1520-6017 |
| language | eng |
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| source | Wiley Online Library - AutoHoldings Journals; MEDLINE; Alma/SFX Local Collection |
| subjects | Animals Anti-Inflammatory Agents - administration & dosage Anti-Inflammatory Agents - blood Anti-Inflammatory Agents - therapeutic use Anti-inflammatory agents-ibuprofen plasma levels correlated with biological activity Arthritis - drug therapy Biological activity-correlated with ibuprofen plasma levels Chromatography, Gas Dose-Response Relationship, Drug Half-Life Ibuprofen-plasma levels correlated with biological activity Male Phenylpropionates - administration & dosage Phenylpropionates - blood Rats Time Factors Tropanes - therapeutic use |
| title | Correlation of Plasma Ibuprofen Levels with Biological Activity |
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