The aim of the study was to investigate the modified release of a model substance, of tablets containing different types of Kollidon and particular additives. Additionally, the release kinetics and mechanism of prolonged release of certain tablet preparations were investigated. In this work, tablets containing different types of povidone (Kollidon CL, Kollidon 30, Kollidon SR and other excipients) were prepared by the direct compression technique. The results showed that tablets with fast disintegration and release should contain in their composition, Kollidon CL, lactose and Avicel, however, the use of β-CD instead of lactose or Avicel brings about a slight prolongation in the disintegration time of tablets and the release of an active substance. Furthermore, while other tablet compositions generated within this study must be considered as being prolonged release types, only two of these showed the best fitted mathematical models. The in vitro dissolution data reveal that the dissolution profiles of the two formulations, one containing Kollidon SR with the addition of Kollidon 30, and the second with HPMC K15M, Kollidon 30, Kollidon CL and lactose, best fitted the Higuchi model. Moreover, the release mechanism of these two formulations plotted well into Korsmeyer-Peppas, indicating a coupling of drug diffusion in the hydrated matrix, as well as polymer relaxation – the so-called anomalous transport (non-Fickian).
Flu cona zole, as the syn thetic an ti fun gal de riva tive of the tria zole, is used in treat ment of the sur face my co ses of the skin such as: tinea cor po ris, tinea cru ris, tinea fa ciei, tinea man num and tinea pe dis [2,15]. The fun gi cidal activ ity is the in hib it ing of 14-de meth y lase that is re spon si ble for the syn the sis of er gos terole-the compound re quired for the syn the sis of cell wall [4]. Men thol, a mono cyc lic monot er pene, is the main component of mint and pep per mint of Labi ate plants and has a long ap pli ca tion his tory in tra di tional medi cine. Com pared with other syn thet ics, men thol has lower toxic side ef fects and higher safety [11]. Men thol is also approved as a pene tra tion en han cer in the trans der mal trans port of sev eral drugs [12]. Sali cylic acid is phar ma ceu ti cal ac tive sub stance for topi cal use. It in hib its the se cre tion of se ba ceous and sweat glands. At low con cen tra tion it has kera to plas tic and in high doses kera to lytic ef fect. Sali cylic acid has a weak an ti mi cro bial ac tiv ity.
The aim of the study was obtaining the cosmetic cream containing walnut oil, defatted walnut seeds and gelling agents like beeswax and witepsol. The walnut oil and defatted walnut seeds were received by extraction method using chloroform: methanol (1: 1), (v/v). Then the physical and chemical properties of the cream were investigated. The consistency, drop point and flow temperature, the spreadability and rheological properties in the temperature range 22°C -50°C were estimated. The release of the model substance, 4-aminobenzoic acid, in the same range of temperatures, was defined as well. Previously, no studies had been conducted, in which the physicochemical properties of semisolid preparations with walnut oil and defatted walnut seeds would be estimated.
Caffeine is a methylxanthine typically found in the Coffee Arabica L plant. Generally, caffeine is well-known as a orally administered mild stimulant of the central nervous system. However, for cosmetic purpose, caffeine is an active compound ingredient, at 7% concentration, in several anticellulite products. The efficiency of this mode of delivery is not fully understood. Hence, the aim of the study was to ascertain the effectiveness of particular carriers to release this ingredient. In so doing, we prepared six creams based upon different oils (Sesame oil, Rice oil, Walnut oil, Coconut oil, Sweet almond oil and Jojoba oil), containing 5% of caffeine, and compared the release of the substance from the obtained preparations. Initially, all of the creams were subjected to a variety of physical tests, among these being for slippage and spreadability. Furthermore, their rheological properties were evaluated. Subsequently, the creams were tested for caffeine release. In the slippage and spreadability tests, the coconut oil-based cream was revealed as having the best parameters. However, the rheological tests showed that all of the preparations had the pseudoplastic character of flowing according to the Ostwald de Waele power law model. The power low index (n) for all the preparations was from 0.2467-0.3179 at 20°C and 0.2821-0.3754 at 32°C. At 20°C, the Sesame oil-, Walnut oil-, Sweet almond oil- and Jojoba oil-based creams were thixotropic, but at 32°C, thixotropy appeared only in the Walnut oil-based creams. The release studies, conducted by way of an extracting chamber (according to Polish Pharmacoeia IX) in the Paddle Apparatus (according to Polish Pharamcopoeia IX), showed that the amount of released caffeine is the largest in the case of Jojoba oil-based cream, at 85.23% ± 0.8% (SD), and the least in the case of Coconut oil-based cream, at 62,78%± 0.87% (SD).
A series of new derivatives of 9-(2-pyridyl)-3-aryl(arylalkyl)-2,4,5(9H)trioxo-7,8- dihydroimidazo [1,2-a][1,3,5] triazepine was obtained by condensation of 1-[1-(2-pyridyl) imidazolidine-2-ylidene]-3-aryl(arylalkyl)ureas) with diethyl oxalic acid ester. Considering the structure of the obtained compounds, it can be expected that these compounds can reveal pharmacological activity.
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