Influence of alcohols on the critical micelle concentration of heptacainium chloride. Study of local anesthetics, part 171.

The critical micelle concentrations (CMC), of heptacainium chloride in various 0.5 M alcohols (methanol, ethanol and n-propanol) were determined using spectrophotometric measurements. CMC values were determined through the change in the slope when the absorbance versus surfactant concentration was plotted at 234 nm. The CMC values show that micelle formation occurred more easily in methanol than in other higher alcohols.

[Analytical profile of 1-(4-fluorophenyl)-4-[3-(3-propoxyphenylcarbamoyloxy)-2-hydroxypropyl]piperazinium chloride (6f)]. / Analytické hodnotenie 1-(4-fluorfenyl)-4-[3-(3-propoxy- fenylkarbamoyloxy)-2- hydroxypropyl]piperazíniumchloridu (látka 6f).

The paper presents the results of an analytical evaluation and a study of some physicochemical properties of a potential antiarrhythmic agent marked as 6f. The melting point, spectral properties, solubility and chromatographic behaviour of the drug on the thin layer were investigated. For the content determination, spectrophotometry in the ultraviolet region of the spectrum at the wavelength of the second absorption maximum of the substance and high-performance liquid chromatography were used.

[A study of physicochemical properties of 2-, 3-, 4-alkoxyphenylcarbamic acid derivatives with a substituted N-phenylpiperazine moiety in the basic part]. / Stúdium fyzikálno-chemických vlastností derivátov kyseliny 2-, 3-, 4-alkoxyfenylkarbámovej s bázickou castou tvorenou substituovaným N-fenylpiperazínom.

The paper presents the study of some physicochemical properties of 2-, 3-, 4-alkoxyphenylcarbamic acid derivatives with various substituted N-phenylpiperazin-1-yl moiety in the basic part of the molecule. Elemental analysis, melting point, solubility, surface activity, dissociation constant and some lipophilicity parameters i.e.--partition coefficient, capacity factor obtained from HPLC, and R(M) values from reversed-phase thin-layer chromatography were determined.

[Analytical evaluation of 1-(dipropalamino-3-piperidine-propane-1-yl)-3-pentyloxyphenylcarbamate (CK-3635)]. / Analytické hodnotenie 1-(dipropylamino-3-piperidino-propán-1-yl)-3-pentylox-yfenylkarbamátu (CK-3635).

The paper presents the results of analytical and pharmacological evaluation and study of some physicochemical properties of a potential drug marked as CK-3635 with high local anaesthetic activity. The structure of the substance has been confirmed by IR and UV spectroscopy. The melting point, solubility, partition coefficient, capacity factor, surface activity, and dissociation constant were determined. The chromatographic behaviour of the drug on a thin layer was also investigated. For the content determination, spectrophotometry in the ultraviolet region of the spectrum at the wavelenght of the second absorption maximum of the substance, the titration in the two-phases ambient, and high-performance liquid chromatography were used.

[Occurrence and use of anthracenones]. / Niektoré aspekty výskytu a vyuzitia antracenónov.

The present paper aims to inform the pharmaceutical public about anthracenons and their natural producers. The first available mention dates from 1888 and the present authors also describe their synthesis and use in clinical practice.

[Detection of secretion of beta-galactosidase by plant cells]. / Prezentácia sekrécie beta-galaktozidázy rastlinnými bunkami.

A simple, sensitive and reproducible method of detection of extracellular beta-galactosidase was worked out. beta-Galactosidase secreted by the callus culture, or the roots of sprouting plants, hydrolyzes the substrate (6-bromo-2-naphthyl-beta-D-galactopyranoside) to produce beta-D-galactose and 6-bromo-2-naphthol, which after simultaneous azocoupling with hexazotized p-rosaniline, or basic fuchsine, produce a reddish brown compound, nearly insoluble in water (a diazonium salt). The colouring under the callus culture and around it, as well as the colouring of the roots of the sprouting plants, is a manifestation of the activity of extracellular beta-galactosidase by the objects under study. The intensity of the colouring is a measure of their enzymatic activity. The share of intracellularly localized enzyme represents the majority and the share of extracellular beta-galactosidase the minority.

[Local anesthetics: part 153. Relation between the chemical structure, physico-chemical properties and biological activity in a series of piperidinopropylesters of alkoxy-substituted phenylcarbamic acids]. / Stúdium lokálnych anestetík: Cast 153. Vztah medzi chemickou struktúrou, fyzikálno-chemickými vlastnostami a biologickou aktivitou v sérii piperidinopropylesterov alkoxysubstituovaných kyselín fenylkarbámových.

Physical-chemical parameters (surface tension, dissociation constant, RF and RM values determined by means of TLC, logarithm of the capacity factor by means of HPLC) of 30 compounds from the group of piperidinopropylesters of o-, m-, p-alkoxyphenylcarbamic acids with local-anaesthetic activity were determined. The correlation chemical structure--physical-chemical properties--local-anaesthetic activity was studied by means of QSAR. The results of the study have demonstrated a linear dependence between log k, RM, and the number of C in the alkoxysubstituent.