6533b855fe1ef96bd12b007e

RESEARCH PRODUCT

In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats

Benno IngelseRené HolmRené HolmPeter LangguthErik MannaertSandy Van HemelryckJonatan DewulfMarjolein Van HeerdenHarm Niekus

subject

In situPO Propylene oxideIV IntravenousP338 Poloxamer 338lcsh:RS1-441Pharmaceutical Sciencechemistry.chemical_compoundn Sample sizeSD Standard deviationIM Intramuscularchemistry.chemical_classificationC0 Analyte plasma concentration at time zeroDoE Design of experimentsUV UltravioletPharmacology. TherapyK2.EDTA Potassium ethylenediaminetetraacetic acidLC–MS/MS Liquid chromatography-tandem mass spectrometryH&E Hematoxylin and eosintmax Sampling time to reach the maximum observed analyte plasma concentrationIn situ forming gelsCMC Critical micellar concentrationCmax Maximum observed analyte plasma concentrationIntramuscular injectionDN Dose normalizedGPT Gel point temperaturePLGA Poly-(DL-lactic-co-glycolic acid)TFA Trifluoroacetic acidCAN AcetonitrileATP Adenosine 5′ triphosphateSalt (chemistry)Polyethylene glycolPoloxamerArticlelcsh:Pharmacy and materia medicaPharmacokineticsIn vivoUHPLC Ultra-high performance liquid chromatographyPharmacokineticsAUClast Area under the analyte concentration versus time curve from time zero to the time of the last measurable (non-below quantification level) concentrationEO Ethylene oxideNMP N-methyl-2-pyrrolidoneComputingMethodologies_COMPUTERGRAPHICSAUC∞ Area under the analyte concentration vs time curve from time zero to infinite timeP407 Poloxamer 407In vitro releasePoloxamerCMT Critical micellar temperatureGel erosionIn vitrot1/2 Apparent terminal elimination half-lifechemistryMDR-TB Multi-drug resistant tuberculosisAUC80h Area under the analyte concentration versus time curve from time zero to 80 htlast Sampling time until the last measurable (non-below quantification level) analyte plasma concentrationMRM Multiple reaction monitoringNuclear chemistrySustained release

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Graphical abstract

10.1016/j.ijpx.2019.100016http://europepmc.org/articles/PMC6733418