Author/Editor | Kmetec, Vojko; Kozjek, Franc | |
Title | Correlation approaches for stability prediction of some 1,4-benzodiazepines in aqueous solution | |
Translated title | Korelacijski pristopi k napovedovanju stabilnosti nekaterih 1,4-benzodiazepinov v vodni raztopini | |
Type | članek | |
Source | Acta Pharm Zagreb | |
Vol. and No. | Letnik 50, št. 3 | |
Publication year | 2000 | |
Volume | str. 185-93 | |
Language | eng | |
Abstract | The stability of several 1,4-benzodiazepines in solution was compared using a correlation analysis approach. Substituent omega constants were used as quantitative descriptors of structure characteristics and were related to degradation kinetics of the drugs under study. Additionally, chromatographic retention factors of the drugs and their degradation products were applied in a similar way, correlating solvent effects with degradation rate constants. In an attempt to predict the relative stability of several 1,4-benzodiazepins in aqueous solution, it was found that relatively simple correlation models could be successfully applied using published substituent constants, as well as experimentally derived parameters. | |
Summary | Z uporabo korelacijske analize smo primerjali stabilnost nekaterih 1,4-benzodiazepinov v raztopini, pri čemer smo kinetiko razpada ovrednotili s tekočinsko kromatografijo visoke ločljivosti (HPLC). Kot deskriptorje strukturnih lastnosti proučevalnih spojin smo uporabili substituentne omega konstante, katerih skupni vpliv smo primerjali s kinetiko razgradnje. Na podoben način smo primerjali vpliv topila na hitrost razpada učinkovin. Pri tem smo vpliv topila opredelili s pomočjo retencijskih faktorjev učinkovin in ustreznih razpadnih produktov kot smo jih lahko izmerili s HPLC analizo vzorčnih raztopin. Ugotovili smo, da lahko na osnovi obeh parametrov in z uporabo relativno enostavnih modelov dovolj dobro napovedujemo stabilnost proučevanih 1,4-benzodiazepinov v vodni raztopini. | |
Descriptors | BENZODIAZEPINES DRUG STABILITY CHROMATOGRAPHY, LIQUID |