Evaluation of Stability of Potential Betaadrenolytics in Various Solutions by thin Layer Chromatography and by Kinetics of Hydrolysis

Abstract

The aim of this work is the study of stability and kinetics of hydrolysis of the chosen compounds, derivatives of 2-hydroxy-3-[2-(4-methoxyphenyl)ethylamino]propyl-4-[(alkoxycarbonyl)amino]benzoates and 2-hydroxy-3-[2-(2-methoxyphenyl)ethylamino] propyl-4-[(alkoxycarbonyl)amino]benzoates with potential ultra-short beta-adrenolytic activity. The studied compounds are different in the position of the substituent on the benzene ring in the side chain as well as in the aromatic ring in position 4 with alkyl-(methyl-to butyl-) carbamate. Thin layer chromatography and UV-area spectrophotometry are used in order to establish the stability of these potential pharmaceuticals. The stability studies of the compounds were examined in acidic and alkaline media, in buffers and due oxidation at room and at elevated temperature chromatographically, and R f values of incipient products and degradation products were detected. Kinetics of acid and base hydrolysis in various solutions at temperatures 80 °C and 100 °C were examined through UV-area spectrophotometry. Kinetic parameters such as rate constant k, half-life period t 1/2 and usable life t 90 were determined.

Study of physico-chemical properties of potential beta-adrenolytics

“…Kinetics of acid and base hydrolysis in various solutions at temperature 80°C and 100°C was examined through ultraviolet-area spectrophotometry. Kinetic parameters such as rate constant k, half-life period t 1/2 and usable life t 90 were determined (Stankovičová et al, 2012). For clarification of relationships between structure and biological activity of potential drugs, it is necessary to state their physicochemical parameters that are related to biological effect such lipophilicity, surface activity, capability of binding on phase boundary, and acidobasic properties.…”