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dc.contributor.authorEHRHARDT, CARSTENen
dc.date.accessioned2011-05-04T09:05:06Z
dc.date.available2011-05-04T09:05:06Z
dc.date.issued2010en
dc.date.submitted2010en
dc.identifier.citationP Stasiak, M Sznitowska, C Ehrhardt, M Juzwa, A Kowalczyk, P Grieb, In vivo assessment of parenteral formulations of oligo(3-hydroxybutyric acid) conjugates with the model compound ibuprofen, AAPS PharmSciTech, 11, 4, 2010, 1636-1641en
dc.identifier.otherYen
dc.identifier.urihttp://hdl.handle.net/2262/55312
dc.descriptionPUBLISHEDen
dc.description.abstractPolymer-drug conjugates have gained significant attention as pro-drugs releasing an active substance as a result of enzymatic hydrolysis in physiological environment. In this study, a conjugate of 3-hydroxybutyric acid oligomers with a carboxylic acid group-bearing model drug (ibuprofen) was evaluated in vivo as a potential pro-drug for parenteral administration. Two different formulations, an oily solution and an o/w emulsion were prepared and administered intramuscularly (IM) to rabbits in a dose corresponding to 40 mg of ibuprofen/kilogramme. The concentration of ibuprofen in blood plasma was analysed by HPLC, following solid-phase extraction and using indometacin as internal standard (detection limit, 0.05 mu g/ml). No significant differences in the pharmacokinetic parameters (C-max, T-max, AUC) were observed between the two tested formulations of the 3-hydroxybutyric acid conjugate. In comparison to the non-conjugated drug in oily solution, the relative bioavailability of ibuprofen conjugates from oily solution, and o/w emulsion was reduced to 17% and 10%, respectively. The 3-hydroxybutyric acid formulations released the active substance over a significantly extended period of time with ibuprofen still being detectable 24 h post-injection, whereas the free compound was almost completely eliminated as early as 6 h after administration. The conjugates remained in a muscle tissue for a prolonged time and can hence be considered as sustained release systems for carboxylic acid derivatives.en
dc.description.sponsorshipThis work was supported by a Galenos Fellowship in the Framework of the EU Project "Towards a European PhD in Advanced Drug Delivery", Marie Curie Contract MEST-CT-2004-4049922.en
dc.format.extent1636-1641en
dc.language.isoenen
dc.relation.ispartofseriesAAPS PharmSciTechen
dc.relation.ispartofseries11en
dc.relation.ispartofseries4en
dc.rightsYen
dc.subjectPharmacologyen
dc.subjectIbuprofenen
dc.titleIn vivo assessment of parenteral formulations of oligo(3-hydroxybutyric acid) conjugates with the model compound ibuprofenen
dc.typeJournal Articleen
dc.contributor.sponsorMarie Curieen
dc.type.supercollectionscholarly_publicationsen
dc.type.supercollectionrefereed_publicationsen
dc.identifier.peoplefinderurlhttp://people.tcd.ie/ehrhardcen
dc.identifier.rssinternalid69418en
dc.identifier.doi10.1208/s12249-010-9545-2en
dc.contributor.sponsorGrantNumberMEST-CT-2004-4049922en
dc.subject.TCDThemeImmunology, Inflammation & Infectionen
dc.subject.TCDThemeNanoscience & Materialsen
dc.identifier.rssurihttp://dx.doi.org/10.1208/s12249-010-9545-2en
dc.identifier.orcid_id0000-0003-0730-1829en


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