The place of combined mucoactive drugs in the treatment of acute respiratory infections in children

The problem of respiratory diseases and their therapy options still retains much of its urgency. Respiratory diseases in children are still super common. According to the data on infectious morbidity among children in the Russian Federation for the period 2018–2020, current trends have not changed, and the acute respiratory infections (ARI) are still ranked number one in terms of the frequency of registered diseases. According to the official records, the frequency of ARI in children among infectious diseases is 71,850.02 per 100,000 population, or 71%. Such well-known symptom as cough is one of the most frequent manifestations of respiratory diseases. It causes the greatest discomfort for both the little patients and their parents, the quality of life of the children and those around them worsens, many domestic and foreign authors mention this symptom in their works. And it is this problem that doctors of various specialties most often face. The cough is currently treated with drugs with different effects depending on the characteristics and manifestations of the disease. Systematic reviews and multicenter studies show that prescription of mucoactive drugs to treat cough in children with underlying ARI is substantiated and feasible. The authors substantiated the necessity of using combinations of various drugs aimed to reduce inflammation of the airways, improve mucociliary clearance, thin out and promote sputum discharge and, accordingly, reduce cough. The article briefly discusses the mechanisms of the development of cough in ARI, the action of drug substances included in the combination drugs used to treat cough in children, the possibility of using the combination of muco- and bronchoactive drugs of synthetic and plant origin.

ROSUVASTATIN CALCIUM NANOSPONGES IN THE FORMULATION OF EXTENDED RELEASE TABLETS

Cyclodextrin has been recognized as a linker molecule that can link with the various drug substances to produce a nano-porous structure called nanosponges (NS) and increase the dissolution rate of poorly soluble drug substances. This work aimed to load rosuvastatin calcium (RSC) with solubility enhancer’s β-cyclodextrin (β-CD) or polyvinyl alcohol (PVA). β-CD based RSC-NS were fabricated by the emulsion solvent diffusion technique; with solubilizer dichloromethane and different ratios of ethyl cellulose as a co-polymer. Characterization of the prepared nanosponges was done by various testing procedures that confirm its nanosize and particle size and drug release. RSC loading in NS was assessed by DSC, FTIR and SEM. Among all the formulations F5 has 78.23 % entrapment efficiency. 2-3 folds of increased solubility were obtained with RSC-NS. F1-F6 formulations released 76.35 % - 98.69 % of the drug at the end of 30 min. In the preparation of extended-release tablets, NS prepared from F5 formulation was used and the best tablet formulation was selected based on various evaluation tests. All the formulations except S3, S8 followed first-order release kinetics. S1 & S2 drug release mechanism is Higuchi while other formulations are Korsemeyer-Peppas, so the release mechanism for most of the formulations is erosion than diffusion.

Accelerating pre-formulation investigations in early drug product lifecycle using predictive methodologies and computational algorithms

Precisely developed computational methodologies can allow the drug product lifecycle process to be time-efficient, cost-effective and reliable through a thorough fundamental understanding at the molecular level. Computational methodologies include computational simulations, virtual screening, mathematical modeling and predictive tools. In light of current trends and increased expectations of product discovery in early pharmaceutical development, we have discussed different case studies. These case studies clearly demonstrate the successful application of predictive tools alone or in combination with analytical techniques to predict the physicochemical properties of drug substances and drug products, thereby shortening research and development timelines. The overall goal of this report is to summarize unique predictive methodologies, which can assist pharmaceutical scientists in achieving time-sensitive research goals and avoiding associated risks that can potentially affect the drug product quality.

Assessment of Drug Interactions with Online Electronic Checkers in Multi-Pathological Patients

<b><i>Introduction:</i></b> Multi-pathological patients are at high risk of drug interactions and side effects. We aimed to assess the usefulness of 3 online drug interaction checkers. <b><i>Methods:</i></b> In a cross-sectional study, carried out in the Medicine Department of Hospital General of Castellon, Spain, in February 2020, we assessed drug interaction detection with 3 online electronic checkers, Drugs.com, Lexicomp®, and Medscape, and compared results obtained with the 3 tools. From every hospitalized patient, we obtained the list of drugs he or she had been taking until admission. Bivariable tests were used for analysis. <i>p</i> values &#x3c;0.05 were considered significant. <b><i>Results:</i></b> We included data from 134 patients; 68 (51%) were male; median (and interquartile range) of their age was 82 (76–88) years. A total of 1,082 substance drugs were entered in the checkers. The number of highest grade interactions found with every program was Drugs.com 85, Lexicomp® 33, and Medscape 67. Positive correlations were found between age and number of drug substances prescribed (<i>p</i> = 0.009) and between number of drug substances prescribed and interactions found with any of the 3 checkers (<i>p</i> &#x3c; 0.001 in all 3 cases). Regarding highest grade interactions, agreement among all 3 checkers was poor. <b><i>Conclusions:</i></b> The 3 online checkers we assessed found a large number of interactions. The 3 programs gave very discrepant results. <b><i>Impact on Practice Statements:</i></b> The analyzed programs, Drugs.com, Lexicomp®, and Medscape Interactions, found a large number of drug interactions in the studied patients. The 3 programs gave very discrepant results among them.