Optimization of application schedule of camphecene, a novel anti-influenza compound, based on its pharmacokinetic characteristics.

Due to high variability and rapid life cycle, influenza virus is able to develop drug resistance against direct-acting antivirals. Development of novel virus-in113039hibiting drugs is therefore important goal. Previously, we identified camphor derivative, camphecene, as an effective anti-influenza compound.

Quantitative determination of new anti-inflammatory drug indomenthyl and its metabolite in rabbit plasma by HPLC-MS/MS.

: Indomenthyl is an innovative anti-inflammatory drug with a high analgesic activity. Indomenthyl releases indomethacin under the influence of neutrophil esterases in the inflammation focus. /: This research is aimed at developing a highly sensitive method for the quantitative determination of indomenthyl and its active metabolite indomethacin in rabbit plasma by HPLC-MS/MS.

Dynamics of an externally driven cavitation bubble in an elastic microconfinement.

The subject of the present study is the dynamics of a single cavitation bubble in a spherical liquid cell surrounded by an infinite elastic solid. It is shown that volume confinement strongly affects the manifestation of the classical cavitation Blake threshold. In particular, at liquid cell sizes smaller than some critical size, the cavitation is completely suppressed by volumetric confinement.

Synthesis, Biological Evaluation, and Molecular Modeling of Aza-Crown Ethers.

Synthetic and natural ionophores have been developed to catalyze ion transport and have been shown to exhibit a variety of biological effects. We synthesized 24 aza- and diaza-crown ethers containing adamantyl, adamantylalkyl, aminomethylbenzoyl, and ε-aminocaproyl substituents and analyzed their biological effects in vitro. Ten of the compounds (, -, and ) increased intracellular calcium ([Ca]) in human neutrophils, with the most potent being compound (,'-[2-(1-adamantyl)acetyl]-4,10-diaza-15-crown-5), suggesting that these compounds could alter normal neutrophil [Ca] flux.

Development and validation of HPLC-UV method for quantitation of a new antithrombotic drug in rat plasma and its application to pharmacokinetic studies.

A selective and sensitive procedure for quantitation of a new antithrombotic drug (GRS) in rat plasma was developed and validated using an HPLC-UV. The method was validated according to recommendations of the FDA, EMA in terms of selectivity, linearity, accuracy, precision, recovery, matrix effect, stability, and carry-over. The preparation of the biological sample included liquid-liquid extraction with acetonitrile, separation of water-organic mixture with inorganic salts, organic phase clean-up with a sorbent (QuEChERS method), its evaporation to dryness and reconstitution of the residue with A:B eluents mixture (1:1).