Valenta Pharmaceuticals JSC

Introduction.Excipients with sorption properties are used in pharmacy as carriers, glidants, stabilizers, thickeners.However, their use is limited by potentially incomplete desorption of active pharmaceutical ingredients (API), which can affect quantification of API.Accuracy of determining the content of polydimethylsiloxane (PDMS), which is main component of simethicone, is significantly depends on drug matrix.Objective: to investigate sorption of PDMS in tablets containing simethicone and magaldrate.Evaluate the contribution of individual components of tablet mixture (TM) to degree of sorption.Material and methods.TM of different composition were analyzed.The quant. content of PDMS in TM was determined by gel permeation chromatog. with refractometric detector.Results.The different grades of magaldrate, probably differing in the ratio of amorphous and crystalline phases, exhibit different sorption activity to PDMS.The granulation of magaldrate with hypromelose reduce sorption of PDMS on the antacid.The most significant sorption of PDMS was observed in presence of silicon dioxide (SD).While complete desorption of PDMS did not occur.Direct relationship has been established between the amount of SD and the amount of sorbed PDMS.Conclusion.We found that the main reason for decrease in degree of transition of PDMS into solution from simethicone and magaldrate TM is sorption of the polymer by antacid and SD.In case of magaldrate, we chose the conditions that allow complete desorption of polymer.While the similar structure of PDMS and SD, covalent and noncovalent interactions leads to partial chemisorption of PDMS and, consequently, its incomplete desorption.

A review.Acute respiratory viral infections (ARVI) are the most common illnesses worldwide.In some instances, mild cases of ARVI progress to hyperinflammatory responses, which are damaging to pulmonary tissue and requiring intensive care.Here we summarize available information on preclin. and clin. effects of XC221GI (1-[2-(1-Me imidazole-4-yl)-ethyl]perhydroazin-2,6-dione), an oral drug with a favorable safety profile that has been tested in animal models of influenza, respiratory syncytial virus, highly pathogenic coronavirus strains and other acute viral upper respiratory infections.XC221GI is capable of controlling IFN-gamma-driven inflammation as it is evident from the suppression of the production of soluble cytokines and chemokines, including IL-6, IL-8, CXCL10, CXCL9 and CXCL11 as well as a decrease in migration of neutrophils into the pulmonary tissue.An excellent safety profile of XC221GI, which is not metabolized by the liver, and its significant anti-inflammatory effects indicate utility of this compound in abating conversion of ambulatory cases of respiratory infections into the cases with aggravated presentation that require hospitalization.This drug is especially useful when rapid mol. assays determining viral species are impractical, or when direct antiviral drugs are not available.Moreover, XC221GI may be combined with direct antiviral drugs to enhance their therapeutic effects.