0000000000904925

AUTHOR

Aki T. Heikkinen

0000-0002-1923-8153

showing 3 related works from this author

Dissolution behavior of co-amorphous amino acid-indomethacin mixtures: The ability of amino acids to stabilize the supersaturated state of indomethac…

2017

Article

Magnetic Resonance SpectroscopyArgininesupersaturationIndomethacinCo-amorphousbiorelevantPharmaceutical ScienceExcipientPhenylalanine02 engineering and technologyPrecipitationprecipitation030226 pharmacology & pharmacy03 medical and health sciences0302 clinical medicineco-amorphousSpectroscopy Fourier Transform InfraredmedicineAmino AcidsSolubilityDissolutionta116Chromatography High Pressure LiquidSupersaturationChromatographyAqueous solutionCalorimetry Differential ScanningChemistryAnti-Inflammatory Agents Non-SteroidalTryptophanGeneral Medicine021001 nanoscience & nanotechnologyAmino acidSupersaturationSolubilityBiorelevant0210 nano-technologyPowder Diffractionamino acidBiotechnologymedicine.drug
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In vitro sulfonation of 7-hydroxycoumarin derivatives in liver cytosol of human and six animal species

2020

Sulfonation is an important high affinity elimination pathway for phenolic compounds.In this study sulfonation of 7-hydroxycoumarin and 13 its derivatives were evaluated in liver cytosols of human and six animal species. 7-hydroxycoumarin and its derivatives are strongly fluorescent, and their sulfate conjugates are nonfluorescent at excitation 405 nm and emission 460 nm. A convenient fluorescence based kinetic assay of sulfonation was established.The sulfonation rate of most of the 7-hydroxycoumarin derivatives was low in liver cytosol of human and pig, whereas it was high with most compounds in dog and intermediate in rat, mouse, rabbit, and sheep. Sulfonation of the 7-hydroxycoumarin der…

Health Toxicology and MutagenesisLiver cytosolToxicologyliver030226 pharmacology & pharmacyBiochemistryArticle03 medical and health sciences0302 clinical medicineanimalhumanAnimal specieskumariinitsulfonationPharmacologyChemistrymaksaGeneral MedicinelääkeaineetIn vitroBiochemistry7-hydroxycoumarinfarmakokinetiikka030220 oncology & carcinogenesiseläimetihmiset
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In vitro glucuronidation of 7-hydroxycoumarin derivatives in intestine and liver microsomes of Beagle dogs

2019

Beagle dog is a standard animal model for evaluating nonclinical pharmacokinetics of new drug candidates. Glucuronidation in intestine and liver is an important first-pass drug metabolic pathway, especially for phenolic compounds. This study evaluated the glucuronidation characteristics of several 7-hydroxycoumarin derivatives in beagle dog's intestine and liver in vitro. To this end, glucuronidation rates of 7-hydroxycoumarin (compound 1), 7-hydroxy-4-trifluoromethylcoumarin (2), 6-methoxy-7-hydroxycoumarin (3), 7-hydroxy-3-(4-tolyl)coumarin (4), 3-(4-fluorophenyl)coumarin (5), 7-hydroxy-3-(4-hydroxyphenyl)coumarin (6), 7-hydroxy-3-(4-methoxyphenyl)coumarin (7), and 7-hydroxy-3-(1H-1,2,4-t…

entsyymitColonGlucuronidationPharmaceutical Science02 engineering and technologyliver030226 pharmacology & pharmacyBeaglekoira7-hydroxycoumarin derivative03 medical and health scienceschemistry.chemical_compound0302 clinical medicineDogsGlucuronidesPharmacokineticsMicrosomesenzyme kineticsIntestine SmallmedicineAnimalsHumansUmbelliferonesGlucuronosyltransferasekumariinitaineenvaihduntachemistry.chemical_classificationChemistryglucuronidationdog intestinemaksaMetabolismlääkeaineet021001 nanoscience & nanotechnologyCoumarinSmall intestineEnzymemedicine.anatomical_structureBiochemistryLiverfarmakokinetiikkasuolistoMicrosomekoe-eläinmallit0210 nano-technology
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