Vol 52, No 12 (2019)

A series of R-benzylidenehydrazides of NH-furoyl-5-iodoanthranilic acid were synthesized by condensing NH-furoyl-5-iodoanthranilic acid hydrazide with aromatic aldehydes. Their structures were confirmed using IR and PMR spectroscopy. Their analgesic and antibacterial activities were studied.

A series of quaternary salts were obtained by reacting 3-(4-bromoacetylphenyl)-1-methylquinolin-2(1H)-one with Py, 4-methylpyridine, quinoline, benzo[f]quinoline, and triphenylphosphine. Derivatives of thiazole, imidazo[1,2-a]pyridine, and imidazo[1,2-a]pyrimidine were produced using dinucleophilic reagents. Several of the synthesized compounds possessed high antimicrobial activity, indicating that further research on this series of compounds was promising.

A microcolumn HPLC method with UV detection (MC-HPLC-UV) using ProntoSIL-120-5-C18 sorbent (1 × 60 mm, 1 μm) and gradient elution by LiClO₄(4.1 M)/HClO₄(0.1 M)–MeCN was developed for quantitative analysis of seven compounds (liquiritin-2″-O-glucoside, liquiritin, isoliquiritin-2″-O-apioside, isoliquiritin, licorice-saponin G2, yunganoside E2, glycyrrhizic acid) in Glycyrrhiza uralensis Fisch. roots. Validation of the procedure showed that the metrological parameters were satisfactory. The procedure was used for research on G. uralensis roots growing in Siberia and quantitative analysis of glycyrrhizic acid in 28 commercial licorice preparations.

The effect of solid dispersions (SDs) on the solubility of the nonsteroidal anti-inflammatory drug ketoprofen was determined. Ketoprofen and its SDs with poly(ethylene glycol) PEG-400, -1000, -1500, -2000, and -3000 were studied. Dissolution of ketoprofen from the SDs increased by 1.2 – 1.8 times; the dissolution rate, by 1.7 – 2.4 times. The improved release of ketoprofen from the SDs was proposed to be due to several factors such as solubilization and amorphization of the compound and formation of intermolecular H-bonds. The results could be used to develop rapidly dissolving ketoprofen solid dosage forms.

Drug elution profiles must be studied in vitro to optimize a polymer-drug formulation during development of drug-eluting stents (DESs). Results from HPLC assays of drug contents and elution kinetics from a biodegradable sirolimus coating and a stable zotarolimus coating on coronary DESs are presented. Drug contents were assessed for crimped stents on the delivery system and expanded stents. The drug coating morphology and elution kinetics were demonstrated to be associated. Significant coating morphological defects were shown to cause deviations in the drug elution profile.

Angionorm is an original Russian preparation based on the dried aqueous EtOH (25%) extract of a herbal mixture containing horse chestnuts (Aesculus hippocastanum L.), licorice roots (Glycyrrhiza glabra L.), hawthorn fruit (Crataegus), and dog-rose hips (Rosa canina). Areversed-phase HPLC-MS-MS procedure with gradient elution was developed to identify the main constituents in extracts of the mixture and each raw material type. Standards helped to identify 15 compounds of various classes (phenolic and hydroxycinnamic acids and their esters, flavonoids, flavonoid glycosides, triterpene saponins). Peaks of hyperoside, liquiritin, â-glycyrrhizic acid, and escin isomers were identified using MRM transitions, elution order, and literature data. Herbal sources of identified constituents were determined. Marker compounds characteristic of each raw-material type in the mixture extract were proposed.

Six compositions with various quantities of lipophilic and hydrophilic phases and different emulsifiers were developed. The suppository lipophilic component was type A solid fat; hydrophilic, poly (ethylene glycol) molecules with varying chain lengths and molecular masses. Comprehensive theoretical and experimental results led to formulation of the optimal composition with 35% marigold CO₂ extract. The processing parameters for producing such suppositories were optimized.

An HPLC-MS method for simultaneous quantitative determination of a novel gestagenic pharmaceutical and two of its metabolites in rat and rabbit blood sera was developed and validated. The method was selective and specific. The detection limit for all analytes was 5 ng/mL; lower limit of quantitation, 10 ng/mL. Calibration curves for all analytes had the form y = ax + b. The correlation coefficients were >0.99. Matrix effects, degree of extraction, and stability of analytes in standard solutions, analytical samples, and the biomatrix with multiple freeze—thaw cycles were studied.