Ceskoslovenska farmacie最新文献

Dokloxytepin in the medium of the induced monooxygenase system of the microsomal fraction of the liver of the rat, rabbit and mice is metabolized into three metabolites: two identical, i.e., N-oxide and 5-sulfoxide, and a third different one. In the rat and rabbit it is the hitherto unknown metabolite M1, and in the mouse S,N-dioxide of dokloxytepin. The metabolites were identified by thin-layer chromatography by comparing with synthetic standards.

After the foundation of the course of pharmaceutical studies at Masaryk University in Brno in 1945, its Institute of Pharmaceutical Chemistry has been founded. In pharmaceutical chemistry, which was divided into the theoretical, synthetic and control-analytical parts, a system of classification was worked out based on classification of drugs according to the kind of effect for which it serves. This conception was incorporated into three editions of the book Chemická léciva (Chemical Drugs). The research programme of the Institute solved the development of novel local anaesthetic and antituberculous agents. After the disestablishment of the Faculty of Pharmacy in Brno, the development of pharmaceutical chemistry, continued at the Department of Pharmaceutical Chemistry, Comenius University, Bratislava, and beginning with 1969 at Charles University Faculty of Pharmacy in Hradec Králové.

The present paper describes an ultrafiltration method of determination of the concentration of free phenytoin (DPH) in serum and its use for the study of the binding equilibrium phenytoin--albumin. The procedure was employed to determine the binding affinity of serum albumin (a) in a group of healthy volunteers (n = 8) in in vitro conditions, (b) in a group of healthy volunteers (a mixed serum, n = 6) and (c) in a group of patients suffering from epilepsy with fits of the generalized type grand mal (n = 15) in in vivo conditions. The calculation of binding parameters was carried out by the method of nonlinear regression analysis with the use of the one-parameter Scatchard's model of the bond. Binding activity of serum albumin in the volunteers of group (a) was N.Ka = 17,500 l/mol, group (b) N.Ka = 18,700 l/mol, and in patients with epilepsy n.Ka = 19,200 l/mol. The results of covariational analysis demonstrated good agreement in the binding parameters of all three groups under study. The paper also discusses the suitability of the binding model used and the mathematical processing and possible use of the binding parameters measured in in vitro conditions for the estimation of the value of the free fraction of the drug in patients with epilepsy.

The Czech Association of Pharmacists was established as a state-constituted professional organization by the decree of the Czech Government dated 11 March 1784, the initiator of the decree being Josef Gottfried Mikan (1742-1818), the then Dean of the Faculty of Medicine and Professor of Botany and Chemistry at Charles University. His correspondence with the government between 10 February and 16 May 1784, preserved in the State Central Archives, Prague, clearly demonstrates Mikan's main contribution to the issue of the decree. In his letter of 10 February 1784, he asked the government to order the establishment of a compulsory nation-wide association of pharmacists. Their meetings were to be presided by dean of the faculty in order to prevent disorders which he did not specify and evaluate at all. The pharmacists of Prague were acquainted with the governmental decree of 23 February, 1784, at the Carolinum Hall on 6 March, 1784. The decree included Mikan's requirements and the introduction of tests for pharmacists' apprentices (tirones) prior to the journeyman's examination and compulsory registration of employed pharmacists (subjecti) at the Faculty of Medicine. These supplements to education were added by the government. The Prague pharmacist Ignác Broz, the owner of the Golden Bear pharmacy since 1763, was appointed chairman of the Association. The governmental decree of 11 March 1784, including the above-mentioned regulations, was sent to all districts of Bohemia. The emperor was informed about the decision of the government by a letter dated as late as 17 June 1784.(ABSTRACT TRUNCATED AT 250 WORDS)

The paper describes the preparation of 7 novel organic ammonium salts of N-[2-(10-undecenoyloxy)ethyl]-N,N,N-alkyl-dimethylammonium bromides, in which the alkyl chain was gradually lengthened from ethyl to tetradecyl, constantly keeping the other groups (10-undecenoyloxyethyl and methyl) bound to the ammonium nitrogen. In the paper the antimicrobial effect of the prepared ammonium salts and the aggregative properties of their aqueous solutions were studied. The aggregative properties are expressed by the values of the critical concentration of the micelles formation, which were determined tensiometrically and conductometrically. The antimicrobial activity expressed by the minimal inhibition concentration in dependence on the prolongation of the alkyl chain was determined by the dilution test on the strains Staphylococcus aureus, Escherichia coli and Candida albicans. As follows from the table, all ammonium salts prepared were active in this respect, the most effective ones possessing 6, 8 and 10 carbon atoms in the alkyl chain. They were more effective than the standard Ajatin to all strains of the microorganisms tested. The antimicrobial effect decreased with the increasing length of the alkyl chain. Also the structure--activity relationship was quantified by the QSAR analysis methods using two procedures: the dependence log ck vs. m was linear and the dependence log (1/MIC) vs. m and log (1/MIC) vs. log ck were nonlinear. The calculated coefficients of regression equations and statistical evaluation of dependences are shown in Table 4.(ABSTRACT TRUNCATED AT 250 WORDS)

Oxidation of 3-acetyl derivatives of 3-acetyl-1-ethyl-1,4-dihydro-6,7-methylenedioxyquinoline-4-one (VIc) and 3-acetyl-7-chloro-1-ethyl-6-fluoro-1,4-dihydroquinoline-4-one (VId) with selenium dioxide provided the corresponding acids, [1-ethyl-1,4-dihydro-6,7-methylenedioxy-4-oxoquinoline-3-yl]glyoxylic acid (VIe) and [7-chloro-1-ethyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-yl]glyoxylic acid (VIf), respectively. Reactions of compounds VIc--VIf with thiosemicarbazide yielded the respective thiosemicarbazones of 3-acetyl-1-ethyl-1,4-dihydro-6,7-methylenedioxyquinoline-4-one (VIIa), 3-acetyl-7-chloro-1-ethyl-6-fluoro-1,4-dihydroquinoline-4-one (VIIb), [1-ethyl-1,4-dihydro-6,7-methylenedioxy-4-oxoquinoline-3-yl]glyoxylic acids (VIId). The compounds showed no significant in vitro antibacterial activity.

On the basis of an analysis of time series of consumption of infusion solutions in the Czech Republic its prognosis was made till the year 2000 using the trend analysis method. The results have shown that a further increase in consumption of infusion solutions must be expected. The forecasted consumption in the year 2000 with 90% reliability will reach the volume of 5.2 to 5.6 million litres. The production capacity for infusion solutions in the individual branches of Czech pharmacy will have to be adjusted to this trend.

A method of the identification of tetracycline antibiotics in urine and gastric content, suitable for the routine toxicological analysis, was worked out. For the isolation, the extraction with ethyl acetate is recommended. The TLC method on Silufol layers impregnated with an aqueous solution of the disodium salt of ethylenediaminetetraacetic acid (Na2EDTA), in the concentration of 0.1 mol/l and pH value of 5 or 7.4 is used for the identification. The mobile phase chloroform--methanol--Na2EDTA 55:30:5 is suitable for the development of these layers; UV light of the wavelength 254 or 366 nm and Fast Blue B reagent are used for the detection. The conditions of the TLC (various modifications of the layer, mobile phase and detection) and the extraction solvents suitable for the isolation are discussed.