About: Analytical evaluation of mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-isopropylamonium]fumarate     Goto   Sponge   NotDistinct   Permalink

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  • Predmetom prezentovanej práce je komplexné spektrálne a fyzikálno-chemické hodnotenie mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-izopropylamónium]fumarátu, potenciálneho ultrakrátko pôsobiaceho ß1-blokátora. Totožnosť študovanej substancie (pracovne označenej ako UPB-1) bola potvrdená 1H- a 13C-NMR spektrami ako aj IR spektrometriou. Medzi stanovené základné fyzikálno-chemické charakteristiky patrilo určenie teploty topenia, rozpustnosti v spektre rozpúšťadiel, overenie čistoty (adsorpčná chromatografia na tenkej vrstve), určenie povrchovej aktivity (Traubeho stalagmometrická metóda), acidobázické charakteristiky (hodnota pKa pomocou alkalimetrickej titrácie), určenie hodnôt log epsilon s využitím spektrofotometrie v UV/VIS oblasti, ako aj hodnotenie vplyvu kyslého a zásaditého prostredia na stabilitu študovanej látky. Ďalšími experimentálne stanovenými parametrami boli lipohydrofilné charakteristiky pomocou RP-HPLC (log k'), shake flask metódou stanovené hodnoty rozdeľovacích koeficientov Pexp (resp. log Pexp) v rôznych lipohydrofilných prostrediach. Na základe log Pexp-dát sa predikovala schopnosť látky prechádzať cez hematoencefalickú bariéru. Pre stanovenie obsahu UPB-1 sa použila RPHPLC (reversed-phase HPLC) metóda vnútorného štandardu a UV/VIS spektrofotometria pri vlnovej dĺžke 260 nm (vodné prostredie) a 258 nm (prostredie metanolu).
  • The present paper deals with a complex spectral and physicochemical evaluation of mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-isopropylammonium]fumarate, a potential ultrashort acting ß1-blocker. The identity of the substance under study (labelled as UPB-1) was confirmed by 1H- and 13C-NMR spectra as well as IR spectrometry. The determined fundamental physicochemical characteristics included the determination of the melting point, solubility in a spectrum of solvents, verification of purity (adsorption thin-layer chromatography), determination of surface activity (Traube's stalagmometric method), acidobasic characteristics (pKa value by means of alkalimetric titration), determination of log epsilon values using spectrophotometry in UV/VIS region, as well as the evaluation of the effect of acid and basic media on the stability of the substance under the study. Other experimentally determined parameters were lipohydrophilic characteristics essayed by means of RP-HPLC (log k'), and the shake-flask method was employed to determine the values of the partition coefficients Pexp (resp. log Pexp) in different lipohydrophilic media. On the basis of log Pexp-data, the ability of the substance to penetrate the hematoencephalic barrier was predicted. To determine the UPB-1 content, RP-HPLC (reversed-phase HPLC) method of the internal standard and UV/VIS spectrophotometry at the wavelength of 260 nm (aqueous medium) and 258 nm (methanol medium) were used. (en)
Title
  • Analytical evaluation of mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-isopropylamonium]fumarate (en)
  • Analytické hodnotenie mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-izopropylamónium]fumarátu
skos:prefLabel
  • Analytical evaluation of mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-isopropylamonium]fumarate (en)
  • Analytické hodnotenie mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-izopropylamónium]fumarátu
skos:notation
  • RIV/62157124:16370/11:43870770!RIV12-MSM-16370___
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  • 185878
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  • RIV/62157124:16370/11:43870770
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  • content determination; spectral and physicochemical characteristic; analytic evaluation; ß1-blockers (en)
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  • CZ - Česká republika
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  • [0A81E3A13425]
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  • 60
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  • Andriamainty, Fils
  • Csöllei, Jozef
  • Gališinová, Jana
  • Karlovská, Janka
  • Lukáč, Miloš
  • Malík, Ivan
  • Mokrý, Petr
  • Sedlárová, Eva
  • Čižmárik, Josef
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  • 1210-7816
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  • 16370
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