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Solid inclusion complexes of TolperisoneHCl with five various cyclodextrins were prepared by kneading and spray drying. The complex formation between the drug and the cyclodextrins were proven using thermoanalytical methods, X-ray diffraction, IR spectroscopy. The results of the solid state investigations were supported by the liquid phase investigations, such solubility and parition constant measurements and stability constant determination. Among all cyclodextrins used the β- and γ-CD-s were found to be the best complexing agents.

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Abstract  

Solid formulas obtained between furosemide and two β-cyclodextrin derivatives (HP-β-CD and RAMEB) were prepared by different methods and in various ratios (1:1 and 1:2). The inclusion complex formation between the drug and the β-CDs of 1:1 ratio was evaluated by mean of thermal analysis (DSC, TG and EGD). Supplementary techniques, such as X-ray diffraction, were also applied to interpret the results of the thermal study of physically mixed and kneaded products. Both studies demonstrated the formation of inclusion complexes in all samples except the physical mix samples; formation of true inclusion complexes was then possible only when the components were in melted form. The complexation increased the solubility and the rate of dissolution of the drug. RAMEB was found to be a better complexing agent than HP-β-CD; in both ratios it can be selected as a vehicle in furosemide tablet preparations.

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Abstract  

γ-Cyclodextrin and dimethyl-β-cyclodextrin were used as solubilizing agents for a very poorly water-soluble drug, an imidazole derivative antifungal agent, clotrimazole; with the aim of improving the physicochemical properties of the drug. Solid products were prepared by physical mixing, kneading, precipitation and spray-drying methods in 1:1 and 1:2 drug:cyclodextrin molar ratios. Drug interactions were studied by thermoanalytical methods such as DSC, DTA, TG and DTG, X-ray diffractometry and Fourier transformation-infrared spectroscopy. The results demonstrated the formation of inclusion complexes in some products.

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Abstract  

Inclusion complexation between cyclodextrin derivatives (hydroxypropyl-β-cyclodextrin and methyl-β-cyclodextrin) and a very poorly water-soluble antifungal agent, ketoconazole, was studied. Solid products were prepared by physical mixing, kneading and spray-drying methods in four molecular ratios: 2:1, 1:1, 1:2 and 1:3. The possibility of complex formation between the drug and the cyclodextrins was studied by thermal analysis. Supplementary techniques, such as X-ray diffractometry and Fourier transformation-infrared spectroscopy, were also applied to interpret the results of the thermal study of the products.

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Summary Inclusion complexation between dimethyl-β-cyclodextrin and a very poorly water-soluble serum lipid-regulating agent, gemfibrozil, was studied. Products were prepared by several methods (physical mixing, kneading, spray-drying and ultrasonic treatment) in four different molecular ratios (2:1, 1:1, 1:2 and 1:3). The possibility of complex formation between the drug and the host molecule was studied by thermal analysis. Supplementary techniques, such as Fourier transformation-infrared spectroscopy and X-ray diffractometry, were also applied to interpret the results of thermal study of the products.

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In pharmaceutical practice it is important and useful to know the crystallinity of materials and to monitor it during formulation development, production processes and storage. The purpose of this study was to assess the quantitative capability of DSC for determining crystallinity in crystalline/amorphous powder mixtures and to compare the accuracy of the DSC method with that of conventional powder X-ray diffraction. Alpha-lactose monohydrate was chosen as the model material. On the basis of this study it can be concluded, that DSC method can be applied safely for semiquantitative evaluation of the crystallinity of lactose samples consisting of an amorphous content higher than 20%.

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Acta Biologica Hungarica
Authors: T. Kucserka, Kata Karádi-Kovács, M. Vass, G. Selmeczy, Katalin Hubai, Viktória Üveges, I. Kacsala, N. Törő and Judit Padisák

The aim of the study was to estimate the breakdown of the allochthonous litter in an artificial stream running in an agricultural area and compare it with the same values following a toxic mud spill into the same stream. Litter bags were filled with three types of leaves (Quercus robur, Populus tremula and Salix alba) and placed to the bottom of the river. Ergosterol was used to detect fungal biomass. We supposed the absence of fungi and the retardation of leaf litter decomposition. Only pH and conductivity increased significantly. Leaf mass loss after the catastrophe was much slower than in 2009 and the decay curves did not follow the exponential decay model. Prior to the catastrophe, leaf mass loss was fast in Torna, compared to other streams in the area. The reason is that the stream is modified, the bed is trapezoid and covered with concrete stones. Fungal biomass was lower, than in the pre-disaster experiment, because fungi did not have enough leaves to sporulate. Leaf mass loss followed the exponential decay curve before the disaster, but after that it was possible only after a non-change period.

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