Biological activities of Sorbus aucuparia L. leaves extract

Biological activities of Sorbus aucuparia L. leaves extract was tested in our study. Antineurodegenerative activity was evaluated by acetylcholinesterase (AChE) and tyrosinase (TYR) inhibitory activity assays while antioxidant activity was by tested using four different assays. In all antioxidant test we noticed concentration dependent activity of tested extract and the highest applied concentration of 500 μg/ml was the most active. Extract applied in concentration of 200 μg/ml showed higher percent of inhibition in DPPH test compared to both applied concentrations of standard substances BHA and BHT (50 and 100 μg/ml). In ABTS test, activity of extract applied in 500 μg/ml was comparable or higher then BHA and BHT/Vitamin C, respectively. Moreover, all concentrations of tested extract were significantly more active in ß-carotene test than vitamin C. The lowest concentration of extract (100 μg/ml) was the most active in TYR assay reaching 42.57 % of the inhibition while in AChE assay there was not statistically significant differences among all applied concentrations

Development of gastroretentive floating granules with gentian root extract by hot-melt granulation

The roots of yellow gentian, Gentiana lutea L. (Gentianaceae) are used in traditional medicine for the treatment of gastrointestinal disorders, with the literature data indicate a local gastric effect of gentian root extract (GRE) and support the use of the solid pharmaceutical forms. Gentiopicroside, as a dominant secoiridoid in the GRE, has a short elimination half-life and low bioavailability and, consequently, its bioactivity is limited. The aim of the study was to develop gastroretentive floating delivery system with GRE, and to provide prolonged release of gentiopicroside. Floating granules with dry GRE (DGRE) were prepared by the hot-melt granulation technique, while formulations included effervescent components (citric acid and sodium bicarbonate), hydroxypropyl methylcellulose (HPMC) and meltable binders (Compritol® 888 ATO and Gelucire® 50/13). The flowability of the DGRE and prepared formulations was determined by calculating the Carr index and Hausner ratio. Floating properties and in vitro dissolution rate of gentiopicroside from investigated formulations were examined. Floating granules were characterized with improved flowability (Carr index 14-22 %; Hausner ratio 1.16-1.28) in comparison to the DGRE (Carr index 28.99 %; Hausner ratio of 1.41). Furthermore, the floating granules exhibited immediate and long-lasting buoyancy and prolonged-release of gentiopicroside (over 8 h). Compritol® 888 ATO has provided sustained release of gentiopicroside from floating granules, while HPMC has decreased release rate additionally. On the other hand, Gelucire® 50/13 has increased gentiopicroside release rate. The results have shown that hot-melt granulation technique, as a green granulation method was successfully employed for obtaining gastroretentive floating granules with DGRE