36 research outputs found
Enhanced pharmacological efficacy of sumatriptan due to modification of its physicochemical properties by inclusion in selected cyclodextrins
The study focused on the pharmacological action of sumatriptan, in particular its antiallodynic and antihyperalgesic properties, as an effect of cyclodextrinic inclusion of sumatriptan, resulting in changes of its physicochemical qualities such as dissolution and permeability through artificial biological membranes, which had previously been examined in vitro in a gastro-intestinal model. The inclusion of sumatriptan into 尾-cyclodextrin and 2-hydroxylpropylo-尾-cyclodextrin by kneading was confirmed with the use of spectral (fourier-transform infrared spectroscopy (FT-IR); solid state nuclear magnetic resonance spectroscopy with magic angle spinning condition, 1H and 13C MAS NMR) and thermal (differential scanning calorimetry (DSC)) methods. A precise indication of the domains of sumatriptan responsible for its interaction with cyclodextrin cavities was possible due to a theoretical approach to the analysis of experimental spectra. A high-performance liquid chromatography with a diode-array detector method (HPLC-DAD) was employed to determine changes in the concentration of sumatriptan during dissolution and permeability experiments. The inclusion of sumatriptan in complex with cyclodextrins was found to significantly modify its dissolution profiles by increasing the concentration of sumatriptan in complexed form in an acceptor solution compared to in its free form. Following complexation, sumatriptan manifested an enhanced ability to permeate through artificial biological membranes in a gastro-intestinal model for both cyclodextrins at all pH values. As a consequence of the greater permeability of sumatriptan and its increased dissolution from the complexes, an improved pharmacological response was observed when cyclodextrin complexes were applied
Evaluation of antinociceptive and antioxidant properties of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one in mice
Passiflora incarnata attenuation of neuropathic allodynia and vulvodynia apropos GABA-ergic and opioidergic antinociceptive and behavioural mechanisms
Background: Passiflora incarnata is widely used as an anxiolytic and sedative due to its putative GABAergic
properties. Passiflora incarnata L. methanolic extract (PI-ME) was evaluated in an animal model of streptozotocininduced
diabetic neuropathic allodynia and vulvodynia in rats along with antinociceptive, anxiolytic and sedative
activities in mice in order to examine possible underlying mechanisms.
Methods: PI-ME was tested preliminary for qualitative phytochemical analysis and then quantitatively by proximate
and GC-MS analysis. The antinociceptive property was evaluated using the abdominal constriction assay and hot
plate test. The anxiolytic activity was performed in a stair case model and sedative activity in an open field test. The
antagonistic activities were evaluated using naloxone and/or pentylenetetrazole (PTZ). PI-ME was evaluated for
prospective anti-allodynic and anti-vulvodynic properties in a rat model of streptozotocin induced neuropathic pain
using the static and dynamic testing paradigms of mechanical allodynia and vulvodynia.
Results: GC-MS analysis revealed that PI-ME contained predominant quantities of oleamide (9-octadecenamide),
palmitic acid (hexadecanoic acid) and 3-hydroxy-dodecanoic acid, among other active constituents. In the
abdominal constriction assay and hot plate test, PI-ME produced dose dependant, naloxone and pentylenetetrazole
reversible antinociception suggesting an involvement of opioidergic and GABAergic mechanisms. In the stair case
test, PI-ME at 200 mg/kg increased the number of steps climbed while at 600 mg/kg a significant decrease was
observed. The rearing incidence was diminished by PI-ME at all tested doses and in the open field test, PI-ME
decreased locomotor activity to an extent that was analagous to diazepam. The effects of PI-ME were antagonized
by PTZ in both the staircase and open field tests implicating GABAergic mechanisms in its anxiolytic and sedative
activities. In the streptozotocin-induced neuropathic nociceptive model, PI-ME (200 and 300 mg/kg) exhibited static
and dynamic anti-allodynic effects exemplified by an increase in paw withdrawal threshold and paw withdrawal
latency. PI-ME relieved only the dynamic component of vulvodynia by increasing flinching response latency.
Conclusions: These findings suggest that Passiflora incarnata might be useful for treating neuropathic pain. The
antinociceptive and behavioural findings inferring that its activity may stem from underlying opioidergic and
GABAergic mechanisms though a potential oleamide-sourced cannabimimetic involvement is also discussed
Aryl-1,3,5-triazine ligands of histamine H4 receptor attenuate inflammatory and nociceptive response to carrageen, zymosan and lipopolysaccharide
The PLC controls in learning of agricultural engineering
W pracy zaprezentowano informacje o nowej pracowni dydaktyczno-badawczej sterownik贸w programowalnych w SGGW a szczeg贸lno艣ci om贸wiono rodzaje sterownik贸w i modeli. Om贸wiono opracowany program wyk艂ad贸w i 膰wicze艅, kt贸ry zosta艂 pozytywnie sprawdzony w czasie realizacji przedmiotu. Przedstawiono planowany rozw贸j i unowocze艣nianie laboratorium sterownik贸w PLC oraz poszerzenie programu nauczania.The following paper presents information about new laboratory of teaching and research of PLC controls in SGGW. Particularly different types of PLC controls and models are described below. The syllabus of lectures and practices, which has been successfully carried out is also presented here. The planned development and modernization of the PLC control laboratory as well as the widening of the syllabus are shown in this paper
Comparative studies of the chemical composition of goldsmith objects from the collection of regional museum in Torun
Przedstawiono charakterystyk臋 toru艅skich wyrob贸w z艂otniczych z kolekcji Muzeum Okr臋gowego w Toruniu. Przytoczono wyniki bada艅 sk艂adu chemicznego metod膮 XRF wykonane urz膮dzeniem NITON kilkuset obiekt贸w zabytkowych oraz zestawiono je w tabeli. Podj臋to pr贸b臋 interpretacji wynik贸w pomiaru z zastosowaniem sieci neuronowej "Odwzorowanie Sammona". Wskazano, jak istotne s膮 dla kustoszy muze贸w takie badania, rozszerzaj膮c w ten spos贸b zas贸b informacji o obiektach muzealnych.The characteristics of goldsmith objects included in the collection of Regional Museum in Torun were presented. The results of the chemical composition measurements taken by XRF method on a Niton device on hundreds of historic objects were given and the concluding findings were summarised in a table. An attempt was made to interpret the results of measurements using a "Sammon Mapping" neural network. It was indicated how important these investigations are for museum keepers, extending the range of information about museum objects