ChloroquineV1, Main, Exploration, bibRecord, 002D77

Pharmacokinetic and Pharmacodynamic Aspects of Artelinic Acid in Rodents

Identifieur interne : 002D77 ( Main/Exploration ); précédent : 002D76; suivant : 002D78

Pharmacokinetic and Pharmacodynamic Aspects of Artelinic Acid in Rodents

Auteurs : H. A. C. Titulaer [Pays-Bas] ; W. M. C. Eling [Pays-Bas] ; J. Zuidema [Pays-Bas]

Source :

Journal of Pharmacy and Pharmacology [ 0022-3573 ] ; 1993-09.

RBID : ISTEX:D259521869C03137E6B71D44B330FCF6C6255FA1

English descriptors

Teeft :
- Absorption rate, Acidic environment, Antimalarial, Antimalarial action, Antimalarial drugs, Aqueous solution, Artelinate, Artelinic, Artelinic acid, Artelinic acid concentrations, Artemisinin, Bidistilled water, Bioavailability, Blood plasma, Cerebral malaria, Control group, Derivative, Elimination kinetics, Elimination rate, Gastric tube, Gastrointestinal tract, Histology study, Injection sites, Intramuscular, Intramuscular administration, Intramuscular injection, Intramuscular injections, Intravenous, Intravenous administration, Intravenous injection, Large variation, Linear elimination kinetics, Liquid chromatography, Microscopic examination, Mobile phase, Oral administration, Parent compound artemisinin, Pharm, Pharmacokinetic, Pharmacokinetic parameters, Pharmacokinetic study, Pharmacokinetics, Qinghaosu antimalarial research group, Rectal, Rectal administration, Regression analysis, Release rate, Sodium artelinate, Stability study, Statistical consultants, Titulaer, Uncomplicated malaria, Veterinary pharmacology, Zuidema.

Abstract

Abstract— The efficacy of artelinic acid and artemisinin, orally administered at 10 and 50 mg kg−1 day−1, was compared in Plasmodium berghei infected mice. Subsequently, the pharmacokinetics of artelinic acid after intravenous, intramuscular, oral and rectal administration of a 20 mg kg−1 aqueous solution to rabbits were studied in a four‐way randomized cross‐over experiment. After intravenous administration, artelinic acid concentrations in blood plasma were high (C0: 76 ± 15 mg L−1), and the drug was rapidly eliminated from the central compartment, showing linear elimination kinetics with an elimination half‐life of 15 ± 3 min. A large inter‐subject variation appeared in the absorption rate and the extent of absorption (2–92%) over the 120 min interval after intramuscular administration. Also, a large inter‐subject variation in individual rectal bioavailability (17–100%) was shown, which was dependent on the site of absorption in the rectum. The estimated oral bioavailability was low (4·6 ± 1·7%), probably due to a high first‐pass effect and possible decomposition in the acidic gastric environment.

Url:

https://api.istex.fr/ark:/67375/WNG-Z0ZVW29J-X/fulltext.pdf

DOI: 10.1111/j.2042-7158.1993.tb05695.x

Affiliations:

Pays-Bas

Links toward previous steps (curation, corpus...)

to stream Istex, to step Corpus: 001D84
to stream Istex, to step Curation: 001D84
to stream Istex, to step Checkpoint: 001B59
to stream Main, to step Merge: 002E42
to stream Main, to step Curation: 002D77

Le document en format XML

<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title xml:lang="en">Pharmacokinetic and Pharmacodynamic Aspects of Artelinic Acid in Rodents</title>
<author><name sortKey="Titulaer, H A C" sort="Titulaer, H A C" uniqKey="Titulaer H" first="H. A. C." last="Titulaer">H. A. C. Titulaer</name>
</author>
<author><name sortKey="Eling, W M C" sort="Eling, W M C" uniqKey="Eling W" first="W. M. C." last="Eling">W. M. C. Eling</name>
</author>
<author><name sortKey="Zuidema, J" sort="Zuidema, J" uniqKey="Zuidema J" first="J." last="Zuidema">J. Zuidema</name>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">ISTEX</idno>
<idno type="RBID">ISTEX:D259521869C03137E6B71D44B330FCF6C6255FA1</idno>
<date when="1993" year="1993">1993</date>
<idno type="doi">10.1111/j.2042-7158.1993.tb05695.x</idno>
<idno type="url">https://api.istex.fr/ark:/67375/WNG-Z0ZVW29J-X/fulltext.pdf</idno>
<idno type="wicri:Area/Istex/Corpus">001D84</idno>
<idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">001D84</idno>
<idno type="wicri:Area/Istex/Curation">001D84</idno>
<idno type="wicri:Area/Istex/Checkpoint">001B59</idno>
<idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Checkpoint">001B59</idno>
<idno type="wicri:doubleKey">0022-3573:1993:Titulaer H:pharmacokinetic:and:pharmacodynamic</idno>
<idno type="wicri:Area/Main/Merge">002E42</idno>
<idno type="wicri:Area/Main/Curation">002D77</idno>
<idno type="wicri:Area/Main/Exploration">002D77</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title level="a" type="main">Pharmacokinetic and Pharmacodynamic Aspects of Artelinic Acid in Rodents</title>
<author><name sortKey="Titulaer, H A C" sort="Titulaer, H A C" uniqKey="Titulaer H" first="H. A. C." last="Titulaer">H. A. C. Titulaer</name>
<affiliation wicri:level="1"><country xml:lang="fr">Pays-Bas</country>
<wicri:regionArea>Department of Pharmaceutics, Faculty of Pharmacy, University of Utrecht</wicri:regionArea>
<wicri:noRegion>University of Utrecht</wicri:noRegion>
</affiliation>
<affiliation wicri:level="1"><country xml:lang="fr">Pays-Bas</country>
<wicri:regionArea>Correspondence address: Department of Pharmaceutics, Faculty of Pharmacy, University of Utrecht, PO Box 80082, 3508 TB Utrecht</wicri:regionArea>
<wicri:noRegion>3508 TB Utrecht</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Eling, W M C" sort="Eling, W M C" uniqKey="Eling W" first="W. M. C." last="Eling">W. M. C. Eling</name>
<affiliation wicri:level="1"><country xml:lang="fr">Pays-Bas</country>
<wicri:regionArea>Department of Medical Parasitology, University of Nijmegen</wicri:regionArea>
<wicri:noRegion>University of Nijmegen</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Zuidema, J" sort="Zuidema, J" uniqKey="Zuidema J" first="J." last="Zuidema">J. Zuidema</name>
<affiliation wicri:level="1"><country xml:lang="fr">Pays-Bas</country>
<wicri:regionArea>Department of Pharmaceutics, Faculty of Pharmacy, University of Utrecht</wicri:regionArea>
<wicri:noRegion>University of Utrecht</wicri:noRegion>
</affiliation>
</author>
</analytic>
<monogr></monogr>
<series><title level="j" type="main">Journal of Pharmacy and Pharmacology</title>
<title level="j" type="alt">JOURNAL OF PHARMACY AND PHARMACOLOGY</title>
<idno type="ISSN">0022-3573</idno>
<idno type="eISSN">2042-7158</idno>
<imprint><biblScope unit="vol">45</biblScope>
<biblScope unit="issue">9</biblScope>
<biblScope unit="page" from="830">830</biblScope>
<biblScope unit="page" to="835">835</biblScope>
<biblScope unit="page-count">6</biblScope>
<publisher>Blackwell Publishing Ltd</publisher>
<pubPlace>Oxford, UK</pubPlace>
<date type="published" when="1993-09">1993-09</date>
</imprint>
<idno type="ISSN">0022-3573</idno>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><idno type="ISSN">0022-3573</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Absorption rate</term>
<term>Acidic environment</term>
<term>Antimalarial</term>
<term>Antimalarial action</term>
<term>Antimalarial drugs</term>
<term>Aqueous solution</term>
<term>Artelinate</term>
<term>Artelinic</term>
<term>Artelinic acid</term>
<term>Artelinic acid concentrations</term>
<term>Artemisinin</term>
<term>Bidistilled water</term>
<term>Bioavailability</term>
<term>Blood plasma</term>
<term>Cerebral malaria</term>
<term>Control group</term>
<term>Derivative</term>
<term>Elimination kinetics</term>
<term>Elimination rate</term>
<term>Gastric tube</term>
<term>Gastrointestinal tract</term>
<term>Histology study</term>
<term>Injection sites</term>
<term>Intramuscular</term>
<term>Intramuscular administration</term>
<term>Intramuscular injection</term>
<term>Intramuscular injections</term>
<term>Intravenous</term>
<term>Intravenous administration</term>
<term>Intravenous injection</term>
<term>Large variation</term>
<term>Linear elimination kinetics</term>
<term>Liquid chromatography</term>
<term>Microscopic examination</term>
<term>Mobile phase</term>
<term>Oral administration</term>
<term>Parent compound artemisinin</term>
<term>Pharm</term>
<term>Pharmacokinetic</term>
<term>Pharmacokinetic parameters</term>
<term>Pharmacokinetic study</term>
<term>Pharmacokinetics</term>
<term>Qinghaosu antimalarial research group</term>
<term>Rectal</term>
<term>Rectal administration</term>
<term>Regression analysis</term>
<term>Release rate</term>
<term>Sodium artelinate</term>
<term>Stability study</term>
<term>Statistical consultants</term>
<term>Titulaer</term>
<term>Uncomplicated malaria</term>
<term>Veterinary pharmacology</term>
<term>Zuidema</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">Abstract— The efficacy of artelinic acid and artemisinin, orally administered at 10 and 50 mg kg−1 day−1, was compared in Plasmodium berghei infected mice. Subsequently, the pharmacokinetics of artelinic acid after intravenous, intramuscular, oral and rectal administration of a 20 mg kg−1 aqueous solution to rabbits were studied in a four‐way randomized cross‐over experiment. After intravenous administration, artelinic acid concentrations in blood plasma were high (C0: 76 ± 15 mg L−1), and the drug was rapidly eliminated from the central compartment, showing linear elimination kinetics with an elimination half‐life of 15 ± 3 min. A large inter‐subject variation appeared in the absorption rate and the extent of absorption (2–92%) over the 120 min interval after intramuscular administration. Also, a large inter‐subject variation in individual rectal bioavailability (17–100%) was shown, which was dependent on the site of absorption in the rectum. The estimated oral bioavailability was low (4·6 ± 1·7%), probably due to a high first‐pass effect and possible decomposition in the acidic gastric environment.</div>
</front>
</TEI>
<affiliations><list><country><li>Pays-Bas</li>
</country>
</list>
<tree><country name="Pays-Bas"><noRegion><name sortKey="Titulaer, H A C" sort="Titulaer, H A C" uniqKey="Titulaer H" first="H. A. C." last="Titulaer">H. A. C. Titulaer</name>
</noRegion>
<name sortKey="Eling, W M C" sort="Eling, W M C" uniqKey="Eling W" first="W. M. C." last="Eling">W. M. C. Eling</name>
<name sortKey="Titulaer, H A C" sort="Titulaer, H A C" uniqKey="Titulaer H" first="H. A. C." last="Titulaer">H. A. C. Titulaer</name>
<name sortKey="Zuidema, J" sort="Zuidema, J" uniqKey="Zuidema J" first="J." last="Zuidema">J. Zuidema</name>
</country>
</tree>
</affiliations>
</record>

Pour manipuler ce document sous Unix (Dilib)

EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Main/Exploration

HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 002D77 | SxmlIndent | more

HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 002D77 | SxmlIndent | more

Pour mettre un lien sur cette page dans le réseau Wicri

{{Explor lien
   |wiki=    Sante
   |area=    ChloroquineV1
   |flux=    Main
   |étape=   Exploration
   |type=    RBID
   |clé=     ISTEX:D259521869C03137E6B71D44B330FCF6C6255FA1
   |texte=   Pharmacokinetic and Pharmacodynamic Aspects of Artelinic Acid in Rodents
}}

This area was generated with Dilib version V0.6.33.
Data generation: Wed Mar 25 22:43:59 2020. Site generation: Sun Jan 31 12:44:45 2021

	Serveur d'exploration Chloroquine
	Attention, ce site est en cours de développement ! Attention, site généré par des moyens informatiques à partir de corpus bruts. Les informations ne sont donc pas validées.

Serveur d'exploration Chloroquine

Pharmacokinetic and Pharmacodynamic Aspects of Artelinic Acid in Rodents

Pharmacokinetic and Pharmacodynamic Aspects of Artelinic Acid in Rodents

Source :

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri