Pharmaceutical Chemistry Journal (v.42, #8)

Synthesis and cytotoxic activity of 3-triarylmethylindoles. III. 3-[Diphenyl(pyridyl)methyl]indoles by D. F. Skurydina; V. N. Tolkachev; D. I. Zenkina; T. G. Nikolaeva; O. N. Tolkachev (443-445).
Aseries of isomeric heterosubstituted 3-triarylmethylindoles were synthesized and their properties were evaluated. The activity of the synthesized compounds was found to depend on the mass of the side-chain substituent and on the position of the nitrogen atom in the heteroaromatic ring.

A method for extracting ecdysteroids from Serratula coronata L. for the new phytopreparation Edcysterone-80 is proposed. Experiments on white rats established that this preparation has pronounced adaptogenic, antihypoxic, gastroprotective, and thermoprotective properties. Results of this study can be applied both in basic research and in the development of production technology for the new pharmaceutical preparation based on ecdysteroids of Serratula coronata.

Synthesis and antimicrobial activity of methyl esters of 2-(het)arylamino-4-oxo-Z-2-butenoic acids, their structural analogs, and conversion products by A. A. Boteva; O. P. Krasnykh; S. S. Dubrovina; M. I. Vakhrin; E. B. Babushkina; T. F. Odegova; I. V. Solova (452-455).
Synthesis of a small library of compounds containing an aminovinylketone fragment is described. Results of studying their antibacterial activity against S. aureus ATCC 6538-P and E. coli ATCC 25922 are reported.

Quantitative determination of total triterpenoid saponins in Polemonium caeruleum rhizomes and roots by Yu. A. Golyak; O. M. Khishova; N. V. Dubashinskaya; L. V. Kukhareva (456-459).
A spectrophotometric method of quantitative determination of total triterpenoid saponins in rhizomes and roots of Polemonium caeruleum is developed. The procedure does not require sandard samples. The standard relative error of determination does not exceed 4.88%. The proposed procedure is recommended for analysis of the raw material and ready-to-use medicinals based on Polemonium caeruleum.

Elemental composition of Euphrasia brevipila herbs and extracts by T. S. Shestakova; V. M. Petrichenko; T. V. Sukhinina (460-462).
The macro-and microelemental composition of Euphrasia brevipila Burn. et Gremli (Scrophulariaceae) herbs and extracts was studied. Eighteen elements found in the herbs are arranged in the order of decreasing content as P > Mn > Ba > Sr > Zn > Ti > Ni > Cu > Zr > Cr > Co > Nb > V > Pb = Mo > Ga > Be > Ag. The quantitative order of the content of these elements decreased similarly in the preparations but the amount of each element was considerably smaller than in the herbs. The maximum degree of extraction (60–100%) is typical of Nb, Zr, V, Ti, and Pb; a medium degree of extraction (20–60%), Ni, Co, Cr, Cu, Ag, Mo, Ba, and Sr; and the lowest degree of extraction (0–20%), Mn and Zn. All samples studied for heavy-metal content are in accordance with requirements of State Sanitary Rule 2.3.2.1078-01.

Extraction capacity of mono- and biphasic solvent systems for isolating flavonoids from Trifolium pratense herbs by V. V. Sorokin; V. A. Vainshtein; I. E. Kaukhova; T. Kh. Chibilyaev (463-465).
We have studied the extraction of Trifolium pratense L. herbs using aqueous ethanol solutions of various concentration and biphasic systems containing volatile solvents. Dependences of the yield of the active substances on the extractant composition and process factors have been studied. It is established that the maximum total yield of biologically active substances from Trifolium pratense herbs is obtained with the use of biphasic solvent systems.

Current state of IR spectroscopy applied to pharmaceutical analysis by A. P. Arzamastsev; N. P. Sadchikova; A. V. Titova (466-470).
Various techniques of IR spectroscopy are considered from the standpoint of their application in pharmaceutical analysis. It is demonstrated that attenuated total reflectance in the mid-IR range and near-IR spectroscopy are promising techniques for pharmaceutical analysis.

Determining tocopherols by thin-layer chromatography by O. V. Rybakova; E. F. Safonova; A. I. Slivkin (471-474).
A method for the identification and quantitative determination of α-tocopherol by means of thin-layer chromatography (TLC) is developed. The proposed technique has been tested on vegetable oils and oil extracts. Using this method the contribution of plant raw materials to the total content of tocopherols in oil extracts has been estimated.

Bacteriostatic activity and decomposition products of rifampicin in aqueous solution and liposomal composition by G. M. Sorokoumova; V. V. Vostrikov; A. A. Selishcheva; E. A. Rogozhkina; T. Yu. Kalashnikova; V. I. Shvets; V. I. Golyshevskaya; L. P. Martynova; V. V. Erokhin (475-478).
Products of the decomposition and oxidation of rifampicin were obtained; characterized by spectrophotometry, TLC, and HPLC; and identified by mass spectrometry. The stability of the drug in aqueous solutions and in liposomal compositions at 4 and 25°C was evaluated. The main product of rifampicin decomposition on storage is 3-formylrifampicin SV. The antimicrobial activity of the antibiotic in liposomal compositions is the same as that in aqueous solutions and is well retained on storage.

Gas-chromatographic determination of methylmethanesulfonate in anti-arthrosis tablets by D. V. Kompantsev; L. S. Ushakova; I. V. Grigoryan; L. I. Shcherbakova; E. V. Kompantseva (479-480).
New tablets possessing anti-arthrosis properties have been created. The basic active agents in this preparation are glucosamine sulfate and methylmethanesulfonate (mesylmethane, MM). It is established that glucosamine in combination with willow-bark extract exhibits more pronounced specific activity. It is suggested to determine the quantitative content of MM by a gas chromatographic (GC) method with the use of a working reference sample. The validation has been carried out. The metrological performance of the proposed method is characterized. The calculated validation parameters confirmed the applicability of GC to the quantification of MM in the anti-arthrosis tablets.

Ion-selective electrodes for determining cephazolin in biological media by O. I. Kulapina; V. V. Baraguzina; N. V. Skoblikova (481-484).
An ion-selective electrode with plasticized polyvinylchloride membrane that is based on a cephazolin—tetradecylammonium ionic associate has been developed. The ratio of components and the solubility product of the ionic associates [(2.2 ± 0.1) × 10− 8] were determined. The compound is thermally stable up to 70°C. The EMF is linearly dependent on the cephazolin concentration in the range from 1 × 10 − 5 to 1 × 10− 1 M. The slope of the electrode function is 56 ± 2 mV/pC. The selectivity to inorganic ions allows the proposed system to be used for cephazolin determination in biological media. In particular, a method for rapid determination of cephazolin in complex saliva is developed.

Voltammetric study of the antioxidant properties of catalase and superoxide dismutase by E. I. Korotkova; O. I. Lipskikh; M. A. Kiseleva; V. V. Ivanov (485-487).
The antioxidant properties of catalase and superoxide dismutase (SOD) have been studied by voltammetry. The effect of pH on the antioxidant properties of catalase and SOD has been evaluated. It is established that the antioxidant activity of both enzymes is maximum at pH 6.86. Mechanisms of the interaction of enzymes with reactive oxygen species are considered. Antioxidant activity criterion (IC50) for SOD and some copper complexes have been estimated by voltammetry and spectrophotometry.

Optimum conditions for the analytical determination of isonicotinic acid hydrazide in urine using ammonium metavanadate are established. Anoninvasive method for the indirect determination of N-acetyltransferase activity in human hepatocytes that is based on measurement of the isoniazide fraction excreted with urine for 6 h is proposed.

Determining amlodipine in blood plasma by liquid chromatography coupled to tandem mass spectrometry by I. I. Miroshnichenko; A. A. Lelishentsev; Yu. M. Kalmykov; Yu. A. Fedotov; A. A. Ivashchenko (493-495).
Asimple and rapid high-performance liquid chromatography (HPLC) method with tandem mass spectrometry (TMS) detectoin has been developed for the determination of amlodipine in blood plasma. The HPLC system is coupled to a TMS detector via an electrospray ionization (ESI) interface in the positive-ion mode. The plasma samples were extracted either with a diethylether:hexane (8:2, v/v) mixture of by means of solid-phase extraction with Oasis HLB 1-cc cartridges (Waters, USA). The analytes were chromatographed under reversed-phase conditions on a Zorbax 300 SB-C18 column. The proposed HPLC/TMS procedure was successfully used for the study of the clinical pharmacokinetics of amlodipine and other calcium-channel blockers.