The paper studies the adsorption of nine stobadin acylderivatives on active charcoal. Freundlich model of adsorption was employed to evaluate the course of adsorption in dependence on the concentration of substances. At the same time, the dependence of adsorption on lipophilicity and structural parameters of substances was evaluated. The dependence of the amount of the adsorbed substance on time served for the calculation of the rate constant of the 1st order of adsorption process. These values correlate with the parameters characterizing the size of the molecule.
- MeSH
- adsorpce MeSH
- dřevěné a živočišné uhlí chemie MeSH
- karboliny chemie MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- Názvy látek
- dicarbine MeSH Prohlížeč
- dřevěné a živočišné uhlí MeSH
- karboliny MeSH
The paper is concerned with the study of adsorption on active charcoal in a set of selected substances from the group of aryloxyaminopropanol derivatives with carbamate substitution on the benzene ring with beta-adrenolytic effect (Group A) and a set of substances, derivatives of [(arylcarbonyl)oxylaminopropanol with the identical, but assumed ultra-short effect (Group B), where the effect was produced by replacing the phenolether group with a metabolically unstable ester functional group. The course of adsorption in buffer solution with pH 7 in dependence on time and concentration is examined. Adsorptivity of substances is evaluated according to Freundlich and Langmuir models. Affinity of substances of Group A to adsorption material decreases with increasing hydrophilicity.
Active charcoal is one of important adsorbents capable of binding on their surface other substances in a relatively large amount. This property is often used in pharmacy as well as in the studies of the structure--biological activity relationships, where active charcoal serves as a model substance for the study of hyrophobic interactions. The present paper investigates the adsorptivity of eight potential local anaesthetics from the group of 1-methyl-2-piperidinoethylesters of 2-, 3- and 4-alkoxyphenylcarbamic acids to adjusted active charcoal, which complies with the requirements of Slovak Pharmacopoeia 1. Adsorptivity of substances is evaluated according to Freundlich model and according to the amount of the bound substance beta in per cents in dependence on time. The dependence of adsorptivity of substances beta on local anaesthetic activity in topical local anaesthesia, which increases with increasing lipophilicity, is evaluated.
- MeSH
- adsorpce MeSH
- anestetika lokální * MeSH
- chemie farmaceutická MeSH
- dřevěné a živočišné uhlí * MeSH
- fenylkarbamáty * MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- anestetika lokální * MeSH
- dřevěné a živočišné uhlí * MeSH
- fenylkarbamáty * MeSH
The paper presents the results of an analytical evaluation and a study of some physicochemical properties of a new potential drug of the prodrug type--the substance BL 443 pivalate with an assumed antidysrhythmic effect. The structure of the substance has been confirmed by elemental analysis, IR and UV spectroscopy. The following parameters were determined: melting point, solubility, dissociation constant, experimental partition coefficient in four different systems, and surface activity. The chromatographic behaviour of the drug on a thin layer (adsorption and partition chromatography) was also investigated. Acidimetric titration in non-aqueous medium and spectrophotometry in the ultraviolet region of the spectrum at the wavelength of the second absorption maximum of the drug was employed to determine the content of the drug in pure substance.
- MeSH
- antiarytmika chemie MeSH
- chemické jevy MeSH
- chemie fyzikální MeSH
- prekurzory léčiv chemie MeSH
- valeráty chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- ((2-pivaloyloxy-3-isopropylamine)propoxy)phenycarbamic acid, butyl ester MeSH Prohlížeč
- antiarytmika MeSH
- prekurzory léčiv MeSH
- valeráty MeSH
The pyridoindole derivative stobadin, [(-)-cis-2,8-dimetyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3b]-indole] is a perspective antiarrhythmic, antihistamine, anaesthetic, antiulcerous drug capable of extinguishing free oxygen radical. Its prodrug forms--N(5)- acyl-substituted stobadine--of the active substance--stobadine--have been prepared and it is assumed that the will be hydrolyzed in the organism and the active substance will be released in higher concentrations in different biological tissues. The present paper is concerned with the investigation of the kinetics of the hydrolysis of 13 acyl derivatives of stobadine in the medium of a buffer solution of pH 7 at temperatures of 70 degrees C and 75 degrees C spectrophotometrically in the UV region of the spectrum. The determined rate constants were correlated with the length of the side acyl chain and the pKa values of the drugs under study. The profile of log k--pH of substances was determined.
- MeSH
- hydrolýza MeSH
- karboliny chemie MeSH
- koncentrace vodíkových iontů MeSH
- prekurzory léčiv chemie MeSH
- scavengery volných radikálů chemie MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- dicarbine MeSH Prohlížeč
- karboliny MeSH
- prekurzory léčiv MeSH
- scavengery volných radikálů MeSH
Stobadin, (-)-cis-2,8-dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyridol[4,3b]- indol is a compound with a potential antiarrhythmic, antihistamine, anaesthetic, antiulcerous, and marked antioxidative effect. N5-acylsubstitution of stobadin yielded derivatives, which represent prodrug forms of the active principle--stobadin, and it is assumed that they will be hydrolysed in the organism and the active principle will be released in higher concentrations in various biological tissues. The present paper deals with the investigation of the kinetics of hydrolysis of 13 stobadin acylderivatives in a medium of 0.1 mol/l of sodium hydroxide at 70 degrees C, employing spectrophotometry in the UV region of the spectrum. The determined rate constants were correlated with the length of the side acyl chain and the pKa values of the compounds under study.
- MeSH
- hydrolýza MeSH
- karboliny chemie MeSH
- koncentrace vodíkových iontů MeSH
- prekurzory léčiv chemie MeSH
- scavengery volných radikálů chemie MeSH
- spektrofotometrie ultrafialová MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- dicarbine MeSH Prohlížeč
- karboliny MeSH
- prekurzory léčiv MeSH
- scavengery volných radikálů MeSH
The present paper has been focussed on the study of quantitative relations between structure, physico-chemical properties and biological activity in the series of substances with potential local anaesthetic and beta-adrenolytic effectiveness from the group of phenylcarbamic acid derivatives. The study of the above-mentioned relations and their interpretation could contribute to the optimization of new potential medicaments.
- MeSH
- anestetika lokální farmakologie MeSH
- chemické jevy MeSH
- chemie fyzikální MeSH
- karbamáty chemická syntéza farmakologie MeSH
- piperidiny chemická syntéza farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- anestetika lokální MeSH
- karbamáty MeSH
- phenylcarbamic acid MeSH Prohlížeč
- piperidiny MeSH
- MeSH
- anestetika lokální analýza chemická syntéza MeSH
- chemické jevy MeSH
- chemie fyzikální MeSH
- chromatografie na tenké vrstvě MeSH
- karbamáty chemická syntéza farmakologie MeSH
- piperidiny chemická syntéza farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- anestetika lokální MeSH
- karbamáty MeSH
- piperidiny MeSH
- MeSH
- anestetika lokální metabolismus MeSH
- karbamáty metabolismus MeSH
- piperidiny metabolismus MeSH
- trimekain metabolismus MeSH
- vazba proteinů MeSH
- vlna * MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- Názvy látek
- anestetika lokální MeSH
- heptacaine MeSH Prohlížeč
- karbamáty MeSH
- pentacaine MeSH Prohlížeč
- piperidiny MeSH
- trimekain MeSH
- MeSH
- anestetika lokální analýza MeSH
- chemické jevy MeSH
- chemie fyzikální MeSH
- estery analýza MeSH
- fenylmočovinové sloučeniny analýza MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- anestetika lokální MeSH
- estery MeSH
- fenylmočovinové sloučeniny MeSH
