Piroxicam was extracted from acid medium into chloroform and isolated on a thin layer of silica gel with the use of the system chloroform - absolute ethanol - benzene - aqueous ammonia (20:15:15:0.5). The intensity of fluorescence of stains was measured densitometrically (an Hg lamp, a filter FL - 39, 330 nm). The limit of detection of the stain is 0.020 microgram/ml of plasma.
{"title":"[Densitometric determination of piroxicam in plasma].","authors":"M Peterková, O Matousová, V Rejholec","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Piroxicam was extracted from acid medium into chloroform and isolated on a thin layer of silica gel with the use of the system chloroform - absolute ethanol - benzene - aqueous ammonia (20:15:15:0.5). The intensity of fluorescence of stains was measured densitometrically (an Hg lamp, a filter FL - 39, 330 nm). The limit of detection of the stain is 0.020 microgram/ml of plasma.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"40 1","pages":"40-1"},"PeriodicalIF":0.0,"publicationDate":"1991-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13038892","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
D Mlynarcík, J Bittererová, J Ciźmárik, L Masárová
The inhibitory effect of local anaesthetic agents of this type on the bacteria Escherichia coli were evaluated. The dependence between antimicrobial activity and structure (log 1/MIC = f/m) was studied with the use of a bilinear model. In the positional paraisomers a lower effect of spherical and electron effects than in the case of ortho- and meta-isomers is assumed. The efficacy of these agents depends on their lipophilicity. Membrane activity of these agents was confirmed. In subinhibitory concentrations they cause leakage of cytoplasmic material lysis of spheroplasts, they increase the permeability of the membrane for protons and inhibit dehydrogenase activity of cells. The mode of action of heptacainium chloride and its positional isomers on cells is identical and is similar as in organic ammonium salts and amine oxides.
{"title":"[The effect of piperidinoethylesters of n-alkoxyphenyl-carbamic acids on bacterial cells].","authors":"D Mlynarcík, J Bittererová, J Ciźmárik, L Masárová","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The inhibitory effect of local anaesthetic agents of this type on the bacteria Escherichia coli were evaluated. The dependence between antimicrobial activity and structure (log 1/MIC = f/m) was studied with the use of a bilinear model. In the positional paraisomers a lower effect of spherical and electron effects than in the case of ortho- and meta-isomers is assumed. The efficacy of these agents depends on their lipophilicity. Membrane activity of these agents was confirmed. In subinhibitory concentrations they cause leakage of cytoplasmic material lysis of spheroplasts, they increase the permeability of the membrane for protons and inhibit dehydrogenase activity of cells. The mode of action of heptacainium chloride and its positional isomers on cells is identical and is similar as in organic ammonium salts and amine oxides.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"40 1","pages":"25-8"},"PeriodicalIF":0.0,"publicationDate":"1991-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13039006","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"[Reform of pharmacy education in Hungary].","authors":"K Zalai","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 10","pages":"463-6"},"PeriodicalIF":0.0,"publicationDate":"1990-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13245854","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Oxyprothepine in the medium of the microsomal fraction of the rat liver is biotransformed to the corresponding metabolites originating by oxidation of both sulfur atoms. The formation of S-oxygenation products is bound to the presence of NADPH, with a marked synergism with NADH. Induction with phenobarbital increases the formation of the individual metabolites.
{"title":"[The effect of cofactors on microsomal S-oxygenation of oxyprothepine].","authors":"I Pauliková, O Helia","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Oxyprothepine in the medium of the microsomal fraction of the rat liver is biotransformed to the corresponding metabolites originating by oxidation of both sulfur atoms. The formation of S-oxygenation products is bound to the presence of NADPH, with a marked synergism with NADH. Induction with phenobarbital increases the formation of the individual metabolites.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 10","pages":"456-7"},"PeriodicalIF":0.0,"publicationDate":"1990-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13140407","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The present authors investigated the excretion, distribution and pharmacokinetics of the novel potential antirheumatic agent flobufen and its active metabolite after p.o. and i.v. doses of 2, 10 and 50 mg/kg administered to rats. The drug is resorbed well from the digestive tract and mostly it is metabolized to the principal metabolite M, which is only slowly excreted from the organism mainly by renal clearance. Within the whole dose range the kinetics of the drug is linear. Binding of flobufen and M to proteins is high (95-99%). The highest concentrations of radioactive metabolites (mostly M) were found in the plasma, liver, lungs, kidneys, connective tissue and inflammatory foci. The penetration of metabolites through the placenta and excretion in human milk are relatively important.
{"title":"[Disposition of [3H]flobufen and its active metabolite in rats].","authors":"R Lapka, A Brejcha, S Smolík, Z Franc","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The present authors investigated the excretion, distribution and pharmacokinetics of the novel potential antirheumatic agent flobufen and its active metabolite after p.o. and i.v. doses of 2, 10 and 50 mg/kg administered to rats. The drug is resorbed well from the digestive tract and mostly it is metabolized to the principal metabolite M, which is only slowly excreted from the organism mainly by renal clearance. Within the whole dose range the kinetics of the drug is linear. Binding of flobufen and M to proteins is high (95-99%). The highest concentrations of radioactive metabolites (mostly M) were found in the plasma, liver, lungs, kidneys, connective tissue and inflammatory foci. The penetration of metabolites through the placenta and excretion in human milk are relatively important.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 10","pages":"443-7"},"PeriodicalIF":0.0,"publicationDate":"1990-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13245792","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
On the model of the Soviet monoclonal anti-A and anti-B antibody--erythrocytes of the groups A1, A2, A1B and A2B the conditions for the elaboration of the branch standard for anti-A and anti-B monoclonal antibodies were worked out. In comparison with the standard for human sera determining the ABO groups, the requirement for avidity can be increased, furthermore it seems necessary to determine the percentage of non-A blood cells in the A2B group, which should not exceed 30%, and the percentage of non-B blood cells in A1B erythrocytes, which should not exceed 10%.
{"title":"[Requirements for standards for monoclonal anti-A and anti-B antibodies].","authors":"A Májský","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>On the model of the Soviet monoclonal anti-A and anti-B antibody--erythrocytes of the groups A1, A2, A1B and A2B the conditions for the elaboration of the branch standard for anti-A and anti-B monoclonal antibodies were worked out. In comparison with the standard for human sera determining the ABO groups, the requirement for avidity can be increased, furthermore it seems necessary to determine the percentage of non-A blood cells in the A2B group, which should not exceed 30%, and the percentage of non-B blood cells in A1B erythrocytes, which should not exceed 10%.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 9","pages":"409-11"},"PeriodicalIF":0.0,"publicationDate":"1990-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13251207","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
R Cizmáriková, A Dingová, J Kozlovský, O Greksáková
Within the framework of the study of the structure-effect relationship, a series of novel potential beta-adrenolytic agents derived from p-hydroxyacetophenone and p-hydroxypropiophenone with an alyloxymethyl and a cycloalkyloxymethyl group in the lipophilic part of the molecule and an isopropyl and a tert-butyl group in the hydrophilic part on the basic nitrogen were prepared by means of a well-tried method. The structure of the prepared drugs was confirmed on the basis of interpretation of the IR, UV, 1H-NMR and mass spectra. The results of pharmacological evaluation of selected drugs show that the agents poses beta-adrenolytic and antiarrhythmic activity. From the viewpoint of comparison of the individual drugs subjected to testing the presence of an alyl seems more advantageous than that of a cyclohexyl. The characteristic of the prepared drugs was supplemented by the determination of their partition coefficients, surface tension and acute toxicity.
{"title":"[Derivatives of para-hydroxyacetophenone and para-hydroxypropiophenone as a potential new beta-adrenolytic agent].","authors":"R Cizmáriková, A Dingová, J Kozlovský, O Greksáková","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Within the framework of the study of the structure-effect relationship, a series of novel potential beta-adrenolytic agents derived from p-hydroxyacetophenone and p-hydroxypropiophenone with an alyloxymethyl and a cycloalkyloxymethyl group in the lipophilic part of the molecule and an isopropyl and a tert-butyl group in the hydrophilic part on the basic nitrogen were prepared by means of a well-tried method. The structure of the prepared drugs was confirmed on the basis of interpretation of the IR, UV, 1H-NMR and mass spectra. The results of pharmacological evaluation of selected drugs show that the agents poses beta-adrenolytic and antiarrhythmic activity. From the viewpoint of comparison of the individual drugs subjected to testing the presence of an alyl seems more advantageous than that of a cyclohexyl. The characteristic of the prepared drugs was supplemented by the determination of their partition coefficients, surface tension and acute toxicity.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 9","pages":"403-8"},"PeriodicalIF":0.0,"publicationDate":"1990-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13141668","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The drugs which are foreign to the organism can increase the production of free oxygen radicals either spontaneously or by means of metabolic activation, or they can act as inhibitors of protective enzymic systems. They can thus activate the process of peroxidation of lipids (LPO) causing gradual structural degradation of biomembranes, thus negatively affecting the course of both pathological and physiological processes in the organism. Investigation of the inductive or inhibitory effect of newly developed drugs on LPO should become a part of their preclinical and clinical testing. The present paper proposes and recommends on the basis of the present authors' results the methodical approaches to the investigation of LPO processes.
{"title":"[The importance of studying lipid peroxidation in testing new drugs].","authors":"B Binková, R J Srám","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The drugs which are foreign to the organism can increase the production of free oxygen radicals either spontaneously or by means of metabolic activation, or they can act as inhibitors of protective enzymic systems. They can thus activate the process of peroxidation of lipids (LPO) causing gradual structural degradation of biomembranes, thus negatively affecting the course of both pathological and physiological processes in the organism. Investigation of the inductive or inhibitory effect of newly developed drugs on LPO should become a part of their preclinical and clinical testing. The present paper proposes and recommends on the basis of the present authors' results the methodical approaches to the investigation of LPO processes.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 9","pages":"415-7"},"PeriodicalIF":0.0,"publicationDate":"1990-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13251069","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Unplanned DNA synthesis (UDS) represents one of the methods for the evaluation of genetic risk due to the action of xenobiotics in the organism. UDS is a parameter enabling quantification of the process of excisional repair of DNA, which results in the regeneration of the integrity of the genetic information (i. e,. correct sequence of nucleotides in DNA) after interaction with a mutagen. If the activity of the repair enzymic systems is not sufficient, the gene expression is affected, disorders in the functions of the damaged cells and tissues occur, or the cells die. The most important result is, however, the initiation of the process of carcinogenesis. A study of UDS within the framework of testing of novel drugs would markedly contribute to reveal possible negative as well as positive effects of the drugs tested both in vitro and in vivo tests. The present paper thus discusses possible uses of UDS study within preclinical and clinical testing of novel drugs.
非计划DNA合成(Unplanned DNA synthesis, UDS)是评估生物体内由外源生物作用引起的遗传风险的方法之一。UDS是一个能够量化DNA切除修复过程的参数,该过程导致遗传信息完整性的再生(即DNA的完整性)。与诱变原相互作用后,DNA中核苷酸的正确序列)。如果修复酶系统的活性不足,基因表达就会受到影响,受损细胞和组织的功能就会紊乱,或者细胞就会死亡。然而,最重要的结果是致癌过程的开始。在新药物测试框架内对UDS进行研究将显著有助于揭示在体外和体内测试中测试的药物可能产生的消极和积极影响。因此,本文讨论了UDS研究在新药临床前和临床试验中的可能用途。
{"title":"[Unscheduled DNA synthesis and evaluation of the effects of drugs].","authors":"J Topinka, R J Srám","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Unplanned DNA synthesis (UDS) represents one of the methods for the evaluation of genetic risk due to the action of xenobiotics in the organism. UDS is a parameter enabling quantification of the process of excisional repair of DNA, which results in the regeneration of the integrity of the genetic information (i. e,. correct sequence of nucleotides in DNA) after interaction with a mutagen. If the activity of the repair enzymic systems is not sufficient, the gene expression is affected, disorders in the functions of the damaged cells and tissues occur, or the cells die. The most important result is, however, the initiation of the process of carcinogenesis. A study of UDS within the framework of testing of novel drugs would markedly contribute to reveal possible negative as well as positive effects of the drugs tested both in vitro and in vivo tests. The present paper thus discusses possible uses of UDS study within preclinical and clinical testing of novel drugs.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 9","pages":"412-4"},"PeriodicalIF":0.0,"publicationDate":"1990-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13251068","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
An analytical method was developed for the determination of naphthidrofuryl and its principle metabolite--naphthidrofurylic acid in human plasma by the RP-HPLC method with fluorimetric detection. The analytical method is based on a single extraction with a 5 ml mixture ether: hexane (1:1 by volume), with salting out by means of potassium chloride after which the organic phase after centrifugation, evaporation and reconstitution is sprayed on the reverse phase of HPLC and the separated substances are determined fluorimetrically (excitation 271 nm, emission 240 nm). Lonazolac served as the internal standard. The mobile phase consisted of 72% methanol, 1% triethylamine, 0.6% phosphoric acid. Optimization of the composition of the mobile phase from the aspect of the amino base, dependence of the percent content of methanol in the mobile phase and dependence of the recovery of substances on the composition of the extracting reagent are presented. The limit of detection was 4 ng/ml of plasma for naphthidrofuryl. The stability of compounds (a minimum of 2 months) and interference of some other drugs are shown.
{"title":"[Determination of naphthidrofuryl and naphthidrofurylic acid in human plasma using RP-HPLC and fluorimetric detection].","authors":"P Stehlík, H Houbová","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>An analytical method was developed for the determination of naphthidrofuryl and its principle metabolite--naphthidrofurylic acid in human plasma by the RP-HPLC method with fluorimetric detection. The analytical method is based on a single extraction with a 5 ml mixture ether: hexane (1:1 by volume), with salting out by means of potassium chloride after which the organic phase after centrifugation, evaporation and reconstitution is sprayed on the reverse phase of HPLC and the separated substances are determined fluorimetrically (excitation 271 nm, emission 240 nm). Lonazolac served as the internal standard. The mobile phase consisted of 72% methanol, 1% triethylamine, 0.6% phosphoric acid. Optimization of the composition of the mobile phase from the aspect of the amino base, dependence of the percent content of methanol in the mobile phase and dependence of the recovery of substances on the composition of the extracting reagent are presented. The limit of detection was 4 ng/ml of plasma for naphthidrofuryl. The stability of compounds (a minimum of 2 months) and interference of some other drugs are shown.</p>","PeriodicalId":9871,"journal":{"name":"Ceskoslovenska farmacie","volume":"39 9","pages":"394-9"},"PeriodicalIF":0.0,"publicationDate":"1990-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13251206","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}