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The limited availability of pharmaceutical formulations tailored for cardiovascular diseases in both pediatric and geriatric populations generates the need for compounded dosage forms to guarantee precise dosing and medication adherence. This study aimed to analyze the physicochemical properties and stability of formulations of atenolol and enalapril maleate prepared with a proprietary oral vehicle, SuspendIt®. To this end, palatability, injectability, pH, rheological behavior, and physical, microbiological, and chemical stability over a 180-day storage period at 25 °C and 5 °C were evaluated. Injectability tests confirmed the suitable use of both formulations for administration through enteral feeding tubes. By using a potentiometric electronic tongue, it was confirmed that the SuspendIt® vehicle effectively served as a bitter-blocking strategy for atenolol and enalapril maleate. Adequate stability throughout the storage period was confirmed in terms of the mechanical properties, pH, and effectiveness of the preservative system. The atenolol concentration remained above 90% of the initial amount, while the concentration of enalapril maleate decreased to 88% after 90 days of storage at 25 °C. In summary, the atenolol formulation maintained suitable chemical, physical, and microbiological stability after 180 days at both storage temperatures, while the enalapril maleate formulation remained stable up to 60 days at 25 °C and for 180 days at 5 °C. [ABSTRACT FROM AUTHOR]

Patient acceptance of pediatric formulations is critical to compliance and consequently therapeutic outcomes; thus, having an in vitro method to evaluate sensory perception of pharmaceutical products would be beneficial. The objective of this research is to develop a sensitive and reproducible tribological method to characterize pharmaceutical suspensions at low force and sliding speeds. The discriminating potential of the method was examined using tribology profiles (coefficient of friction (COF) vs. sliding speed) for commercially available products and products made for this study with widely varying sweetness, thickness, and grittiness; these formulations were used to judge the sensitivity of the method. Samples were measured using 3M Transpore™ surgical tape to simulate the tongue surface, steel half ring geometry, constant gap setting, target axial force of 2 N in a 600 s exponential ramp for rotation speed. The COF ranged from 0.1 to 0.6. For the speeds studied, the high viscosity commercial suspension ibuprofen drops and acetaminophen suspension show a classic Stribeck curve with an increasing COF at the higher rotation speeds, which indicates these formulations entered the hydrodynamic lubrication phase, while the lower viscosity suspensions only reached the mixed lubrication phase. The contribution of particles affects the COF in a dynamic tribologic pattern compared to products that are categorized as either low gritty or high viscosity. These results are important as they provide a potentially rapid in vitro method for screening pediatric medications and help to identify the factors that affect the palatability of pediatric formulations. [ABSTRACT FROM AUTHOR]

The effect of the sodium salt of succinyl chitosan (SCTS) and the presence of modifying additives (ethanol and glycerin) on the kinetics of the release of a medicinal substance (MS) of dioxidine (DO) from the liquid dosage form is studied. It is found that the addition of ethanol to a liquid dosage form based on succinyl of chitosan is accompanied by a change in the viscosity characteristics of the polymer, which leads to a decrease in the amount of the MS retained by the polymer chain and an increase in the rate of DO released. The introduction of glycerol, on the contrary, leads to a decrease in the MS release rate and the diffusion coefficient, which is accompanied by an increase in the prolonging effect of the polymer on the release of the MS from the liquid dosage form due to the increase in the total viscosity of the system. [ABSTRACT FROM AUTHOR]

The article describes the approaches to classification and separation of groups of excipients in oral suspensions of both domestic and foreign authors. A number of existing classifications of excipients for oral suspensions are presented. The analysis of formulations of oral suspensions that are registered on the pharmaceutical market of Russia to assess the range of excipients the most relevant at the present time. Evaluations of the frequency of use of specific excipients are carried out and, if possible, the concentrations used.

Nowadays, the safety of parabens as pharmaceutical preservatives is debated. Recent studies investigated their interference with the oestrogen receptors, nevertheless their carcinogenic activity was also proved. That was the reason why the re-evaluation of the biocompatibility and antimicrobial activity of parabens is required using modern investigation methods. We aimed to test the cytotoxic, antifungal and antibacterial effect of parabens on Caco-2 cells, C. albicans, C. parapsilosis, C. glabrata, E. coli, P. aeruginosa and S. aureus. Two complex systems (glycerol—Polysorbate 20; ethanol—Capryol PGMC™) were formulated to study—with the MTT-assay and microdilution method, respectively—how other excipients may modify the biocompatibility and antimicrobial effect of parabens. In the case of cytotoxicity, the toxicity of these two systems was highly influenced by co-solvents and surfactants. The fungi and bacteria had significantly different resistance in the formulations and in some cases the excipients could highly modify the effectiveness of parabens both in an agonistic and in a counteractive way. These results indicate that with appropriate selection, non-preservative excipients can contribute to the antimicrobial safety of the products, thus they may decrease the required preservative concentration.

Nowadays, the safety of parabens as pharmaceutical preservatives is debated. Recent studies investigated their interference with the oestrogen receptors, nevertheless their carcinogenic activity was also proved. That was the reason why the re-evaluation of the biocompatibility and antimicrobial activity of parabens is required using modern investigation methods. We aimed to test the cytotoxic, antifungal and antibacterial effect of parabens on Caco-2 cells, C. albicans, C. parapsilosis, C. glabrata, E. coli, P. aeruginosa and S. aureus. Two complex systems (glycerol—Polysorbate 20; ethanol—Capryol PGMC™) were formulated to study—with the MTT-assay and microdilution method, respectively—how other excipients may modify the biocompatibility and antimicrobial effect of parabens. In the case of cytotoxicity, the toxicity of these two systems was highly influenced by co-solvents and surfactants. The fungi and bacteria had significantly different resistance in the formulations and in some cases the excipients could highly modify the effectiveness of parabens both in an agonistic and in a counteractive way. These results indicate that with appropriate selection, non-preservative excipients can contribute to the antimicrobial safety of the products, thus they may decrease the required preservative concentration. [ABSTRACT FROM AUTHOR]