Vol 50, No 9 (2016)

Critical development needs for recombinant blood-coagulation factors (RBCFs) are reviewed. The production of less immunogenic drugs with suppressed induction of inhibitory antibodies and prolonged therapeutic effects resulting from an increased inactivation threshold is demonstrated to be a major need for designing new RBCF modifications differing in structure and composition from endogenous blood-coagulation factors while retaining their activity.

The pharmacokinetics of the promising antituberculosis drug dextrazide, the conjugate of polyaldehyde dextran with isonicotinic acid hydrazide, were studied using outbred ICR mice. The obtained results were indicative of two-phase dextrazide pharmacokinetics.

A simple new method for synthesizing N-aryl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxamides in high yields is proposed. A series of halo-substituted derivatives were synthesized. Their PMR and ¹³C NMR spectra and mass spectrometric characteristics were studied. Preliminary pharmacological screening showed that the investigated class of compounds was promising for designing potential analgesics and diuretics, thereby confirming the highly effective “flip-flop drug” methodology.

Results from studies of the local anesthetic activity of LAS-54 [4-(benzoyloxy)-3-butoxypiperidinium chloride] (synthesized at the Laboratory of the Chemistry of Synthetic and Natural Drugs, Bekturov Institute of Chemical Sciences) in combination with epinephrine are presented. It was found that joint application of the vasoconstrictor with LAS-54, especially at low concentrations, prolonged infiltration, conduction, and spinal anesthesia.

Amethod for determining anticomplementary activity of human immunoglobulin (Ig) preparations for i.v. administration by complement fixation test was validated for accuracy, precision (repeatability, intralaboratory precision), limit of quantitation (LOQ), linearity, and analytical domain. The method could be used for quality assessment using the “anticomplementary activity” as part of the pharmaceutical quality examination of human Ig preparations.

9-Aryl-12-imino-10,11-dioxatricyclo[5.3.2.0^1,6]dodecane-7,8,8-tricarbonitriles were synthesized via the reaction of 1-(2-oxocyclohexyl)ethane-1,1,2,2-tetracarbonitrile with aromatic aldehydes. The corresponding 3-aryl-1,1,2,2-tetracyanocyclopropanes were prepared from bromomalononitrile and aromatic aldehydes. The structures of the synthesized compounds were elucidated using IR, PMR, ¹³C NMR, and mass spectra. The analgesic activity of the synthesized compounds was investigated.

The antioxidant activity and total contents of phenolic compounds and flavonoids in extracts of several medicinal plants from southeastern Kazakhstan are studied. Antioxidant activity was evaluated in vitro using the cation-radical 2,2^′-azino-bis(3-ethylbenzothiazoline-6-sulfonate) (ABTS^•+), the radical 2,2-diphenyl-1-picrylhydrazyl (DPPH^•), and the FRAP method. The antioxidant and antiradical activities of the studied plants varied over wide ranges. Extracts of roots and the aerial part of Geranium collinum had the greatest antioxidant and antiradical activity; of Agrimonia asiatica, Alchemilla vulgaris, and Alhagi pseudalhagi, high activity. The antioxidant activities of H₂O–EtOH and H₂O–Me₂CO extracts of G. collinum and A. asiatica showed a reliable correlation with their contents of phenolic compounds.

The possibility of creating a new dosage form of the antituberculosis drug isoniazid using nanoparticles of the polymer poly(DL-lactic acid) was studied. It was shown that nanoprecipitation was promising for preparing nanoparticles and loading them with drugs.

The compositions of sea buckthorn oil (SBO) glycerides in concentrates from various manufacturers in Altai Krai were studied using high-temperature gas chromatography. The effects of the isolation method and raw material composition on the ratio of SBO triglycerides were studied. It was shown that the analysis provided direct differentiation of mono-, di-, and triglycerides and had demonstrable advantages over methods of fatty-acid analysis employing preliminary sample preparation. It was established that the ratio of individual types of SBO glycerides could be a characteristic of the oil production method and the composition of the used raw material.