Improvement in the Physicochemical Properties of Ketoconazole through Complexation with Cyclodextrin Derivatives

Highly-soluble cyclodextrin derivatives, such as hydroxypropyl--cyclodextrin(HP--CD) and methyl--cyclodextrin (MEB), were tested as solubilizingagents for ketoconazole, with the aim of improving the physicochemical andbiopharmaceutical properties of this lipophilic imidazole antifungal agent. Productswere prepared in four molecular ratios by physical mixing, kneading and spray-dryingmethods. The kneaded products in a ratio of 1:2 and the spray-dried products exhibitedthe highest dissolution rates. The phase solubility diagrams of ketoconazole with thesecyclodextrins at 25 °C in water and in simulated intestinal medium wereconstructed. A solubility diagram of A_L type was obtained with HP--CD, and one of A_P type with MEB. The complexes were characterized by thermal methods(DSC, TG, DTG and DTA). Multicomponent systems were prepared with tartaric acid.The effects of water-soluble polymers, e.g., polyvinylpyrrolidone, on the aqueous solubility of ketoconazole were investigated. Particle size distribution, surface area, partition coefficient, heat of dissolution and wettability studies were also carried out. The formation of inclusion complexes was observed by means of thermoanalytical studies.     

Ureasulfonamide Polymeric Sorbent for Selective Mercury Extraction

Summary. A new polymeric resin with sulfonamide pendant functions has been prepared for the selective extraction of mercuric ions. This polystyrene sulfonamide urea resin with a 3.5 mmol/g total nitrogen content is able to selectively sorb mercury from aqueous solutions. The mercury sorption capacity of the resin is around 1.60 mmol/g under non-buffered conditions. The experiments performed under identical conditions with some metal ions reveal that Cd(II), Pb(II), Zn(II), and Fe(III) ions are also extractable in low quantity (0.05–0.1 mmol/g). The sorbed mercury can be eluted by repeated treatment with hot acetic acid without hydrolysis of the amide groups.     

Two new isoflavanoids from the rhizomes of Iris soforana

Two new isoflavones 1 and 2 along with eleven known compounds 3-13, have been isolated for the first time from the rhizomes of Iris soforana. The structures of these compounds were determined on the basis of spectroscopic methods and found to be 5,3'-dihydroxy-4'-methoxy-6,7-methylenedioxyisoflavone (1) (Soforanarin A), and 5,7,5'-trimethoxy-6,3',4'-trihydroxyisoflavone (2) (Soforanarin B).     

Diterpenoid Alkaloids of Delphinium buschianum Grossh.

From the aerial parts of Delphinium buschianum Grossh ., collected in Turkey, a new diterpenoid alkaloid 1 , named budelphine, was isolated along with the known diterpenoid alkaloids karakoline ( 2 ), 18‐hydroxy‐14‐O‐methylgadesine ( 3 ), delsoline ( 4 ), lapaconidine ( 5 ), columbianine ( 6 ), 14‐benzoylneoline ( 7 ), and hetisine ( 9 ). The structure of 1 was established on the basis of ¹H‐, ¹³C‐, DEPT, ¹H,¹H‐COSY, NOESY, HSQC, and HMBC NMR studies.     

Artificial intelligence–based models for the qualitative and quantitative prediction of a phytochemical compound using HPLC method

Isoquercitrin is a flavonoid chemical compound that can be extracted from different plant species such as Mangifera indica (mango), Rheum nobile , Annona squamosal , Camellia sinensis (tea), and coriander ( Coriandrum sativum L.). It possesses various biological activities such as the prevention of thromboembolism and has anticancer, antiinflammatory, and antifatigue activities. Therefore, there is a critical need to elucidate and predict the qualitative and quantitative properties of this phytochemical compound using the high performance liquid chromatography (HPLC) technique. In this paper, three different nonlinear models including artificial neural network (ANN), adaptive neuro-fuzzy inference system (ANFIS), and support vector machine (SVM),in addition to a classical linear model [multilinear regression analysis (MLR)], were used for the prediction of the retention time (tR) and peak area (PA) for isoquercitrin using HPLC. The simulation uses concentration of the standard, composition of the mobile phases (MP-A and MP-B), and pH as the corresponding input variables. The performance efficiency of the models was evaluated using relative mean square error (RMSE), mean square error (MSE), determination coefficient (DC), and correlation coefficient (CC). The obtained results demonstrated that all four models are capable of predicting the qualitative and quantitative properties of the bioactive compound. A predictive comparison of the models showed that M3 had the highest prediction accuracy among the three models. Further evaluation of the results showed that ANFIS–M3 outperformed the other models and serves as the best model for the prediction of PA. On the other hand, ANN–M3proved its merit and emerged as the best model for tR simulation. The overall predictive accuracy of the best models showed them to be reliable tools for both qualitative and quantitative determination.     

A practical analytical quality report on the effect of carotenemia on neonatal bilirubin levels

 The effect of haematocrit and β-carotene levels on the serum total bilirubin measurement in two analytical methods was studied as an example of the impact of practical analytical quality in medical decision making. The precision characteristics of the two methods were very similar. Based upon the significant difference in the correlation coefficient in a method comparison study before and after 20% trimming of the data, an interference effect study was performed. Haemoglobin (expressed as haematocrit) and β-carotene were the substances studied to explain the observed differences. The bilirubin test results from the Wako bilirubinometer were easily affected (n=19;X(S): 13.83±2.43;t=–6.17;P=0.000) and more elevated than in the Vitros dry chemistry systems (n=18;X(S): 12.72±2.21;t=–2.48;P=0.017), due to the presence of β-carotene (>200 μg/dl).     

Dicompleteness and real dicompactness of ditopological texture spaces

The authors consider interrelations between the completeness of certain initial di-uniformities and the real dicompactness of completely biregular bi-T₂ nearly plain ditopological spaces. Completions and real dicompactifications of almost plain spaces are also considered.     

Synthesis and characterization of nanomagnetite particles and their polymer coated forms

Superparamagnetic nanoparticles were prepared by coprecipitation of ferrous (Fe(2+)) and ferric (Fe(3+)) aqueous solution by a base. Nanomagnetite particles were coated with poly(St/PEG-EEM/DMAPM) and poly(St/PEG-MA/DMAPM) layer by emulsifier-free emulsion polymerization. Chemical structure of nanoparticles was characterized by both FTIR and (1)H NMR. Particle morphologies were determined by Zeta Sizer, DLS, XRD and SAXS. Structural analysis showed that after polymer coating nanomagnetite particles kept their superparamagnetic property. Besides the synthesized magnetites, polymer coated forms of these particles are more biocompatible, well dispersable and uniform. These properties make them a very strong candidate for bioengineering applications, such as bioseparation, gene transfer.     

The Molecular-Kinetic Approach to Hydrolysis of Boron Hydrides for Hydrogen Production

Kinetics and Catalysis - In this study, Langmuir–Hinshelwood and Michaelis–Menten kinetic models are applied to describe the kinetic behaviour of the Co–B catalyst in the...