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[Densitometric determination of piroxicam in plasma]. 血浆中吡罗昔康的密度测定。
Pub Date : 1991-03-01
M Peterková, O Matousová, V Rejholec

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.

用氯仿-无水乙醇-苯-水氨(20:15:15:5 .5)体系从酸性介质中提取吡罗昔康,在硅胶薄层上进行分离。采用密度法(Hg灯,滤光片FL - 39, 330 nm)测定染色液的荧光强度。本法的检出限为0.020微克/毫升血浆。
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引用次数: 0
[The effect of piperidinoethylesters of n-alkoxyphenyl-carbamic acids on bacterial cells]. [正烷氧基苯基氨基甲酸酯对细菌细胞的影响]。
Pub Date : 1991-03-01
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.

评价了该类局部麻醉药对大肠杆菌的抑制作用。采用双线性模型研究了抗菌活性与结构(log 1/MIC = f/m)之间的关系。在位置异构体中,假设球效应和电子效应比邻位异构体和间位异构体低。这些药物的功效取决于它们的亲脂性。证实了这些制剂的膜活性。在亚抑制浓度下,它们引起细胞质物质渗漏,球质体裂解,它们增加质子膜的通透性,抑制细胞的脱氢酶活性。七氯铵及其位置异构体在细胞上的作用方式与有机铵盐和胺氧化物中的作用方式相同。
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引用次数: 0
[Reform of pharmacy education in Hungary]. [匈牙利药学教育改革]
Pub Date : 1990-12-01
K Zalai
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引用次数: 0
[The effect of cofactors on microsomal S-oxygenation of oxyprothepine]. [辅助因子对氧原素微粒体s -氧合的影响]。
Pub Date : 1990-12-01
I Pauliková, O Helia

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.

大鼠肝脏微粒体部分培养基中的氧原肽被生物转化为由两种硫原子氧化产生的相应代谢物。s -氧合产物的形成与NADPH的存在相结合,与NADH有明显的协同作用。苯巴比妥诱导增加了个体代谢物的形成。
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引用次数: 0
[Disposition of [3H]flobufen and its active metabolite in rats]. [3H]氟布芬及其活性代谢物在大鼠体内的分布]。
Pub Date : 1990-12-01
R Lapka, A Brejcha, S Smolík, Z Franc

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.

本文研究了新型潜在抗风湿药氟布芬及其活性代谢物在大鼠腹腔注射2、10和50 mg/kg后的排泄、分布和药代动力学。药物从消化道吸收良好,大部分被代谢为主要代谢物M,主要通过肾脏清除缓慢排出体外。在整个剂量范围内,药物的动力学是线性的。氟布芬和M与蛋白质的结合率很高(95-99%)。血浆、肝、肺、肾、结缔组织和炎症灶中放射性代谢物(主要为M)浓度最高。代谢物通过胎盘的渗透和在母乳中的排泄是相对重要的。
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引用次数: 0
[Requirements for standards for monoclonal anti-A and anti-B antibodies]. 【单克隆抗a、抗b抗体标准品要求】。
Pub Date : 1990-11-01
A Májský

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%.

以苏联单克隆抗a和抗b抗体——A1、A2、A1B和A2B组红细胞为模型,制定了抗a和抗b单克隆抗体分支标准的条件。与测定ABO血型的人血清标准相比,对血清学的要求可以提高,而且似乎有必要测定A2B组中非a血细胞的百分比,不应超过30%;测定A1B红细胞中非b血细胞的百分比,不应超过10%。
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引用次数: 0
[Derivatives of para-hydroxyacetophenone and para-hydroxypropiophenone as a potential new beta-adrenolytic agent]. [对羟基苯乙酮和对羟基丙烯酮的衍生物作为一种潜在的新型β -肾上腺溶解剂]。
Pub Date : 1990-11-01
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.

在结构-效应关系研究的框架内,以对羟基苯乙酮和对羟基丙烯酮为原料,在分子亲脂部分有alyloxy甲基和cycloalkyloxy甲基,在碱性氮上亲水部分有异丙基和叔丁基,通过一种经过验证的方法制备了一系列新型的β -肾上腺素潜在解药。通过IR、UV、1H-NMR和质谱分析,确定了药物的结构。所选药物的药理学评价结果表明,这些药物具有β -肾上腺素溶解和抗心律失常活性。从被测试的单个药物的比较的观点来看,芳烯的存在似乎比环己基的存在更有利。通过分配系数、表面张力和急性毒性的测定来补充所制备药物的特性。
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引用次数: 0
[The importance of studying lipid peroxidation in testing new drugs]. [研究脂质过氧化在新药测试中的重要性]。
Pub Date : 1990-11-01
B Binková, R J Srám

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.

外来药物可以自发地或通过代谢激活的方式增加自由基的产生,或者它们可以作为保护性酶系统的抑制剂。因此,它们可以激活脂质过氧化(LPO)过程,导致生物膜的逐渐结构降解,从而对生物体的病理和生理过程产生负面影响。研究新开发药物对LPO的诱导或抑制作用应成为其临床前和临床试验的一部分。本论文提出并建议在本作者的结果的基础上,有条理的方法来调查LPO过程。
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引用次数: 0
[Unscheduled DNA synthesis and evaluation of the effects of drugs]. [计划外的DNA合成和药物作用的评价]。
Pub Date : 1990-11-01
J Topinka, R J Srám

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。
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引用次数: 0
[Determination of naphthidrofuryl and naphthidrofurylic acid in human plasma using RP-HPLC and fluorimetric detection]. [RP-HPLC和荧光法测定人血浆中萘酰和萘酰呋喃]。
Pub Date : 1990-11-01
P Stehlík, H Houbová

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.

建立了RP-HPLC荧光检测法测定人血浆中萘甲呋喃及其主要代谢物萘甲呋喃酸的方法。分析方法为:用5 ml乙醚:己烷(体积比为1:1)混合物进行单次萃取,用氯化钾盐析,将离心、蒸发、重构后的有机相喷洒在HPLC反相上,用荧光法测定分离物质(激发271 nm,发射240 nm)。内标为Lonazolac。流动相为72%甲醇、1%三乙胺、0.6%磷酸。从氨基基的角度对流动相的组成进行了优化,并对流动相中甲醇的百分含量和萃取剂的组成对物质回收率的影响进行了研究。萘甲呋喃的检出限为4 ng/ml。化合物的稳定性(至少2个月)和一些其他药物的干扰显示。
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Ceskoslovenska farmacie
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