Vol 50, No 2 (2016)

Biological test results for a series of adamantane-containing pyrimidines, purines, and their derivatives that were synthesized and studied in 1999 – 2001 are reviewed.

Voriconazole is a triazole antifungal drug used to treat invasive fungal infections including candidiasis, aspergillosis, and certain emerging fungal infections. Voriconazole demonstrates low water solubility. Therefore, drug solubilization is necessary for effective topical delivery. Nano-strategy may overcome its poor aqueous solubility as well as controlled drug release at action site, reduction of total dose, avoidance of systemic absorption and dosage form retention on skin. In topical antifungal administration, drug should pass outermost layer of skin; stratum corneum to reach lower layers, particularly into follicular epithelium. Nano-formulations including colloidal systems, vesicular carriers, and nanoparticles may play a major role for enhancing antifungals permeation profile. Present review surveys key experiments with voriconazole nano-based formulations used in superficial fungal infections treatment.

A new approach to microbiological analysis of several pharmaceuticals, in particular, those that can be used in manufacturing sterile medical products, is presented. The proposed approach was verified using a series of 23 samples of various products, three of which were obtained by biotechnological methods. The scheme includes inoculation of samples with test strains followed by isolation and analysis of the contaminants. Validation results showed that the amount of products for microbiological analysis could be reduced to 3 g, which was sufficient for obtaining reliable results. Tryptic soy broth was used as the solvent (diluent) and enrichment broth for microbe growth.

A procedure for determining and separating a mixture of fat-soluble vitamins by gradient thin-layer chromatography was developed. It was shown that a theoretical approach could be used to select the optimum thin-layer chromatographic conditions for determining tocopherol acetate, retinol acetate, ergocalciferol, and β-carotene. The developed procedure was validated in terms of detection limit, specificity, efficiency, and precision. The procedure could be used for quality control of complex multivitamin preparations, medicinal plant raw material, and vegetable oils, oil extracts, and dietary supplements based on them.

Dimethylsulfoxide (DMSO) extracts of medicinal plants were studied by PMR spectroscopy in order to assess the possibility of using this method for the identification and quantitative determination of polyphenolic compounds (flavonoids, tannins, etc.). Dependences of polyphenol-hydroxyl proton chemical shifts on the nature and position of aromatic substituents were studied.

Results from research on formulation development and prolonged release of peroral 4-aminomethylbenzoic acid (amben) using hydrophobic lipid and polymer matrices are reported. It is shown that the amben release parameters considering its solubility at various pH values can be achieved by using the studied polymer hydrophobic matrices.

Qualitative and quantitative methods of analysis of carotenoids that are used to analyze drugs, dietary supplements, and food products are reviewed. UV and visible spectrophotometry and chromatographic methods, e.g., thin-layer (TLC), high-performance liquid (HPLC), and supercritical fluid (SFC) chromatography, are discussed. The importance of using hybrid chromatography methods with IR, NMR, and mass-spectroscopic detectors is demonstrated. The dependence of carotenoid chromatographic separation parameters on sorbate polarity (dipole moment) in TLC, HPLC, and SFC is demonstrated for the first time.