Population pharmacokinetics of maslinic acid, a triterpene from olives, after intravenous and oral administration in rats
SCOPE: Maslinic acid is a bioactive minor component of Olea europaea L. with health‐enhancing activities and no harmful effects. A pharmacokinetic (PK) study was conducted to determine its bioavailability for future studies of maslinic acid in humans. METHODS AND RESULTS: Intravenous (1 mg/kg) and o...
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| Veröffentlicht in: | Molecular nutrition & food research 2014-10, Vol.58 (10), p.1970-1979 |
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| container_title | Molecular nutrition & food research |
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| creator | Sánchez‐González, Marta Colom, Helena Lozano‐Mena, Glòria Juan, M. Emília Planas, Joana M |
| description | SCOPE: Maslinic acid is a bioactive minor component of Olea europaea L. with health‐enhancing activities and no harmful effects. A pharmacokinetic (PK) study was conducted to determine its bioavailability for future studies of maslinic acid in humans. METHODS AND RESULTS: Intravenous (1 mg/kg) and oral (50 mg/kg) administrations to Sprague‐Dawley rats were performed. Blood was obtained several times over 24 h and PKs were analyzed with NONMEM 7.2, applying a population approach. Body weight was included a priori in the model with fixed allometric exponents, based on allometric principles. Plasma concentrations versus time were best characterized by a two‐open compartment model with first‐order absorption and linear elimination. Maslinic acid had a relative rapid oral absorption with a peak concentration after administration at 0.51 h and a bioavailability of 5.13%. Once in bloodstream, it distributed extensively into tissues, since the central and peripheral distribution volumes were 8.41 L/70 kg and 63.6 L/70 kg, respectively. The clearance (8 L/h/70 kg) was related to unaltered renal excretion. The prediction‐corrected visual predictive check confirmed its stability and predictive ability. CONCLUSION: An allometric population PK model was performed for maslinic acid, which adequately described and predicted plasma concentrations. |
| doi_str_mv | 10.1002/mnfr.201400147 |
| format | Article |
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Emília ; Planas, Joana M</creator><creatorcontrib>Sánchez‐González, Marta ; Colom, Helena ; Lozano‐Mena, Glòria ; Juan, M. Emília ; Planas, Joana M</creatorcontrib><description>SCOPE: Maslinic acid is a bioactive minor component of Olea europaea L. with health‐enhancing activities and no harmful effects. A pharmacokinetic (PK) study was conducted to determine its bioavailability for future studies of maslinic acid in humans. METHODS AND RESULTS: Intravenous (1 mg/kg) and oral (50 mg/kg) administrations to Sprague‐Dawley rats were performed. Blood was obtained several times over 24 h and PKs were analyzed with NONMEM 7.2, applying a population approach. Body weight was included a priori in the model with fixed allometric exponents, based on allometric principles. Plasma concentrations versus time were best characterized by a two‐open compartment model with first‐order absorption and linear elimination. Maslinic acid had a relative rapid oral absorption with a peak concentration after administration at 0.51 h and a bioavailability of 5.13%. Once in bloodstream, it distributed extensively into tissues, since the central and peripheral distribution volumes were 8.41 L/70 kg and 63.6 L/70 kg, respectively. The clearance (8 L/h/70 kg) was related to unaltered renal excretion. The prediction‐corrected visual predictive check confirmed its stability and predictive ability. CONCLUSION: An allometric population PK model was performed for maslinic acid, which adequately described and predicted plasma concentrations.</description><identifier>ISSN: 1613-4125</identifier><identifier>EISSN: 1613-4133</identifier><identifier>DOI: 10.1002/mnfr.201400147</identifier><identifier>PMID: 25045029</identifier><language>eng</language><publisher>Weinheim: Wiley-VCH</publisher><subject>Administration, Oral ; Animals ; Antineoplastic Agents, Phytogenic - administration & dosage ; Antineoplastic Agents, Phytogenic - blood ; Antineoplastic Agents, Phytogenic - economics ; Antineoplastic Agents, Phytogenic - pharmacokinetics ; bioactive properties ; bioavailability ; Biological and medical sciences ; Biological Availability ; blood ; blood flow ; Body Weight ; Dietary Supplements ; Drug Stability ; excretion ; Feeding. Feeding behavior ; Food-Processing Industry - economics ; Fruit - chemistry ; Fundamental and applied biological sciences. Psychology ; HPLC-MS ; humans ; Industrial Waste - analysis ; Industrial Waste - economics ; Injections, Intravenous ; Intestinal Absorption ; intravenous injection ; Male ; Maslinic acid ; Metabolic Clearance Rate ; Models, Biological ; Olea - chemistry ; Olea europaea ; olives ; oral administration ; Oral bioavailability ; Pentacyclic triterpenes ; pharmacokinetics ; Rat plasma ; rats ; Rats, Sprague-Dawley ; Renal Elimination ; Tissue Distribution ; Triterpenes - administration & dosage ; Triterpenes - blood ; Triterpenes - economics ; Triterpenes - pharmacokinetics ; triterpenoids ; Vertebrates: anatomy and physiology, studies on body, several organs or systems</subject><ispartof>Molecular nutrition & food research, 2014-10, Vol.58 (10), p.1970-1979</ispartof><rights>2014 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim</rights><rights>2015 INIST-CNRS</rights><rights>2014 WILEY-VCH Verlag GmbH & Co. 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Emília</creatorcontrib><creatorcontrib>Planas, Joana M</creatorcontrib><title>Population pharmacokinetics of maslinic acid, a triterpene from olives, after intravenous and oral administration in rats</title><title>Molecular nutrition & food research</title><addtitle>Mol. Nutr. Food Res</addtitle><description>SCOPE: Maslinic acid is a bioactive minor component of Olea europaea L. with health‐enhancing activities and no harmful effects. A pharmacokinetic (PK) study was conducted to determine its bioavailability for future studies of maslinic acid in humans. METHODS AND RESULTS: Intravenous (1 mg/kg) and oral (50 mg/kg) administrations to Sprague‐Dawley rats were performed. Blood was obtained several times over 24 h and PKs were analyzed with NONMEM 7.2, applying a population approach. Body weight was included a priori in the model with fixed allometric exponents, based on allometric principles. Plasma concentrations versus time were best characterized by a two‐open compartment model with first‐order absorption and linear elimination. Maslinic acid had a relative rapid oral absorption with a peak concentration after administration at 0.51 h and a bioavailability of 5.13%. Once in bloodstream, it distributed extensively into tissues, since the central and peripheral distribution volumes were 8.41 L/70 kg and 63.6 L/70 kg, respectively. The clearance (8 L/h/70 kg) was related to unaltered renal excretion. The prediction‐corrected visual predictive check confirmed its stability and predictive ability. CONCLUSION: An allometric population PK model was performed for maslinic acid, which adequately described and predicted plasma concentrations.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antineoplastic Agents, Phytogenic - administration & dosage</subject><subject>Antineoplastic Agents, Phytogenic - blood</subject><subject>Antineoplastic Agents, Phytogenic - economics</subject><subject>Antineoplastic Agents, Phytogenic - pharmacokinetics</subject><subject>bioactive properties</subject><subject>bioavailability</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>blood</subject><subject>blood flow</subject><subject>Body Weight</subject><subject>Dietary Supplements</subject><subject>Drug Stability</subject><subject>excretion</subject><subject>Feeding. Feeding behavior</subject><subject>Food-Processing Industry - economics</subject><subject>Fruit - chemistry</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>HPLC-MS</subject><subject>humans</subject><subject>Industrial Waste - analysis</subject><subject>Industrial Waste - economics</subject><subject>Injections, Intravenous</subject><subject>Intestinal Absorption</subject><subject>intravenous injection</subject><subject>Male</subject><subject>Maslinic acid</subject><subject>Metabolic Clearance Rate</subject><subject>Models, Biological</subject><subject>Olea - chemistry</subject><subject>Olea europaea</subject><subject>olives</subject><subject>oral administration</subject><subject>Oral bioavailability</subject><subject>Pentacyclic triterpenes</subject><subject>pharmacokinetics</subject><subject>Rat plasma</subject><subject>rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Renal Elimination</subject><subject>Tissue Distribution</subject><subject>Triterpenes - administration & dosage</subject><subject>Triterpenes - blood</subject><subject>Triterpenes - economics</subject><subject>Triterpenes - pharmacokinetics</subject><subject>triterpenoids</subject><subject>Vertebrates: anatomy and physiology, studies on body, several organs or systems</subject><issn>1613-4125</issn><issn>1613-4133</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM1v1DAQxS0EomXhyhF8QeJAFn_GybGsaEEqBUErKi7WrGODaWIHO1vY_x4vWZYjB8ujmd97M3oIPaZkSQlhL4fg0pIRKkh56g46pjXllaCc3z3UTB6hBzl_J4RTJvh9dMQkEZKw9hhtP8Rx08PkY8DjN0gDmHjjg528yTg6PEDuffAGg_HdCwx4Sn6yabTBYpfigGPvb20uE1fa2Icpwa0NcZMxhA7HBD2GbigWuUz-rPEBlyo_RPcc9Nk-2v8LdHX6-nL1pjp_f_Z2dXJeGcGZqNZry4wE2cq6k6xWTtWqAcNb24oOlBSik3XruKHNmkhDbFu3kja8bbkSQki-QM9n3zHFHxubJz34bGzfQ7DlTE1lU5coS2IFXc6oSTHnZJ0ekx8gbTUlehe33sWtD3EXwZO992Y92O6A_823AM_2AGQDvUsQjM__uKaRdHfqAomZ--l7u_3PWv3u4vQjY0IUWTXLSrr210EG6UbXiiupP1-cabIS6sv15St9XfinM-8gaviayilXn4qvJIQ0hDLFfwPdObFd</recordid><startdate>201410</startdate><enddate>201410</enddate><creator>Sánchez‐González, Marta</creator><creator>Colom, Helena</creator><creator>Lozano‐Mena, Glòria</creator><creator>Juan, M. Emília</creator><creator>Planas, Joana M</creator><general>Wiley-VCH</general><general>Blackwell Publishing Ltd</general><general>Wiley</general><scope>FBQ</scope><scope>BSCLL</scope><scope>IQODW</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>201410</creationdate><title>Population pharmacokinetics of maslinic acid, a triterpene from olives, after intravenous and oral administration in rats</title><author>Sánchez‐González, Marta ; Colom, Helena ; Lozano‐Mena, Glòria ; Juan, M. Emília ; Planas, Joana M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4324-bbe2c5a5956d5267f7678ac39e94da7544d569f3c18b05c0e9695183993744453</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antineoplastic Agents, Phytogenic - administration & dosage</topic><topic>Antineoplastic Agents, Phytogenic - blood</topic><topic>Antineoplastic Agents, Phytogenic - economics</topic><topic>Antineoplastic Agents, Phytogenic - pharmacokinetics</topic><topic>bioactive properties</topic><topic>bioavailability</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>blood</topic><topic>blood flow</topic><topic>Body Weight</topic><topic>Dietary Supplements</topic><topic>Drug Stability</topic><topic>excretion</topic><topic>Feeding. Feeding behavior</topic><topic>Food-Processing Industry - economics</topic><topic>Fruit - chemistry</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>HPLC-MS</topic><topic>humans</topic><topic>Industrial Waste - analysis</topic><topic>Industrial Waste - economics</topic><topic>Injections, Intravenous</topic><topic>Intestinal Absorption</topic><topic>intravenous injection</topic><topic>Male</topic><topic>Maslinic acid</topic><topic>Metabolic Clearance Rate</topic><topic>Models, Biological</topic><topic>Olea - chemistry</topic><topic>Olea europaea</topic><topic>olives</topic><topic>oral administration</topic><topic>Oral bioavailability</topic><topic>Pentacyclic triterpenes</topic><topic>pharmacokinetics</topic><topic>Rat plasma</topic><topic>rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Renal Elimination</topic><topic>Tissue Distribution</topic><topic>Triterpenes - administration & dosage</topic><topic>Triterpenes - blood</topic><topic>Triterpenes - economics</topic><topic>Triterpenes - pharmacokinetics</topic><topic>triterpenoids</topic><topic>Vertebrates: anatomy and physiology, studies on body, several organs or systems</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sánchez‐González, Marta</creatorcontrib><creatorcontrib>Colom, Helena</creatorcontrib><creatorcontrib>Lozano‐Mena, Glòria</creatorcontrib><creatorcontrib>Juan, M. Emília</creatorcontrib><creatorcontrib>Planas, Joana M</creatorcontrib><collection>AGRIS</collection><collection>Istex</collection><collection>Pascal-Francis</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>Molecular nutrition & food research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sánchez‐González, Marta</au><au>Colom, Helena</au><au>Lozano‐Mena, Glòria</au><au>Juan, M. Emília</au><au>Planas, Joana M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Population pharmacokinetics of maslinic acid, a triterpene from olives, after intravenous and oral administration in rats</atitle><jtitle>Molecular nutrition & food research</jtitle><addtitle>Mol. Nutr. Food Res</addtitle><date>2014-10</date><risdate>2014</risdate><volume>58</volume><issue>10</issue><spage>1970</spage><epage>1979</epage><pages>1970-1979</pages><issn>1613-4125</issn><eissn>1613-4133</eissn><abstract>SCOPE: Maslinic acid is a bioactive minor component of Olea europaea L. with health‐enhancing activities and no harmful effects. A pharmacokinetic (PK) study was conducted to determine its bioavailability for future studies of maslinic acid in humans. METHODS AND RESULTS: Intravenous (1 mg/kg) and oral (50 mg/kg) administrations to Sprague‐Dawley rats were performed. Blood was obtained several times over 24 h and PKs were analyzed with NONMEM 7.2, applying a population approach. Body weight was included a priori in the model with fixed allometric exponents, based on allometric principles. Plasma concentrations versus time were best characterized by a two‐open compartment model with first‐order absorption and linear elimination. Maslinic acid had a relative rapid oral absorption with a peak concentration after administration at 0.51 h and a bioavailability of 5.13%. Once in bloodstream, it distributed extensively into tissues, since the central and peripheral distribution volumes were 8.41 L/70 kg and 63.6 L/70 kg, respectively. The clearance (8 L/h/70 kg) was related to unaltered renal excretion. The prediction‐corrected visual predictive check confirmed its stability and predictive ability. CONCLUSION: An allometric population PK model was performed for maslinic acid, which adequately described and predicted plasma concentrations.</abstract><cop>Weinheim</cop><pub>Wiley-VCH</pub><pmid>25045029</pmid><doi>10.1002/mnfr.201400147</doi><tpages>10</tpages></addata></record> |
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| ispartof | Molecular nutrition & food research, 2014-10, Vol.58 (10), p.1970-1979 |
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| subjects | Administration, Oral Animals Antineoplastic Agents, Phytogenic - administration & dosage Antineoplastic Agents, Phytogenic - blood Antineoplastic Agents, Phytogenic - economics Antineoplastic Agents, Phytogenic - pharmacokinetics bioactive properties bioavailability Biological and medical sciences Biological Availability blood blood flow Body Weight Dietary Supplements Drug Stability excretion Feeding. Feeding behavior Food-Processing Industry - economics Fruit - chemistry Fundamental and applied biological sciences. Psychology HPLC-MS humans Industrial Waste - analysis Industrial Waste - economics Injections, Intravenous Intestinal Absorption intravenous injection Male Maslinic acid Metabolic Clearance Rate Models, Biological Olea - chemistry Olea europaea olives oral administration Oral bioavailability Pentacyclic triterpenes pharmacokinetics Rat plasma rats Rats, Sprague-Dawley Renal Elimination Tissue Distribution Triterpenes - administration & dosage Triterpenes - blood Triterpenes - economics Triterpenes - pharmacokinetics triterpenoids Vertebrates: anatomy and physiology, studies on body, several organs or systems |
| title | Population pharmacokinetics of maslinic acid, a triterpene from olives, after intravenous and oral administration in rats |
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