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Investigation of Solubility Enhancement Approaches of Ticagrelor
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ABSTRACT

                   Ticagrelor is an orally administered antiplatelet medicine, direct-acting P2Y12-receptor antagonist. Ticagrelor binds reversibly and noncompetitively to the P2Y12 receptor at a site distinct from that of the endogenous agonist adenosine diphosphate (ADP). Inhibition of platelet aggregation stimulated by ADP is a commonly used pharmacodynamic parameter for P2Y12-receptor antagonists.

                  Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10?g/mL at room temperature. Ticagrelor exhibits no pKa value within the physiological range. Ticagrelor does not exhibit pH-dependent solubility and is defined as ‘low solubility low permeability’ under the Biopharmaceutics Classification System (Class IV). The mean absolute bioavailability of ticagrelor in healthy volunteers is 36 %

                   Nanoparticles preparation and complexation is one of the recently used approaches to enhance the solubility of drugs. The aim of the present work was to improve the solubility and dissolution of ticagrelor by preparing nanoparticles and cyclodextrin inclusion complex of ticagrelor and then incorporated in to tablet dosage form. Fifteen formulas of nanoparticles were prepared by antisolvent precipitation method (solvent displacement method) utilizing one of the three polymers (PVP, Poloxamer, and HPMC) at three different drugs: polymer and solvent: anti-solvent ratios and nine formulas of cyclodextrin inclusion complex with HP?CD  by three preparation methods, physical trituration, kneading and solvent evaporation, which increase the solubility and dissolution rate of ticagrelor via formation of inclusion complex with HP?CD.

              The prepared formulas were characterized regarding the saturated solubility, polydispersity index, particle size by nano laser particle size analyzer, % yield, entrapment efficiency, and flowability, FTIR, DSC, and SEM. The selected formulas were prepared as tablets.

             The prepared tablets were evaluated for drug content, weight variation, hardness, and friability. In vitro dissolution data of the prepared tablets were analyzed using similarity factor (f2) and dissolution efficiency (DE).  

           Among all the prepared nanoparticles formulas, formula (F12) which contain HPMC as a polymer at polymer: drug ratio of (1:1) and solvent: antisolvent ratio of (1:1) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 9 times than that of the pure drug. The nanoparticle of the selected formula (F12) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 88 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the selected formula is a promising formula for the preparation of ticagrelor nanoparticles the incorporation in a tablet dosage form.

          Regarding ticagrelor inclusion complex with HP?CD Solvent evaporation method was the most effective method regarding ticagrelor solubilization and optimum formula of inclusion complex (F23) show increment in saturated solubility about ten times that of pure drug.

          The ticagrelor inclusion complex of the selected formula (F23) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 90 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  

 

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Publication Date
Fri Nov 10 2023
Journal Name
Chalcogenide Letters
Enhancement efficiency of cadmium selenium solar cell by doping within silver
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We studied at the morphology, structural setup, and optical characteristics of thin cadmium (CdSe) films a thickness of 250 nm that were created by thermal evaporation over glass, The films exhibited a hexagonal shape were crystalline, and tended to form grains in the (111) crystallographic direction, according to the X-ray diffraction examinations. These characteristics were established using the investigation's findings. Through the use of thin films of CdSe doped with Ag at a concentration of 1.5%, the crystal structure orientations for pure CdSe (25.32, 41.84) and CdSe:Ag (25.39, 41.01) that were both pure as well as those that were doped with silver were both determined. The band gap of the optical spectrum decreased by 1.93–

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Sat Apr 01 2017
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Enhancement of LBP-based face identification system by adopting preprocessing techniques
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Face Identification system is an active research area in these years. However, the accuracy and its dependency in real life systems are still questionable. Earlier research in face identification systems demonstrated that LBP based face recognition systems are preferred than others and give adequate accuracy. It is robust against illumination changes and considered as a high-speed algorithm. Performance metrics for such systems are calculated from time delay and accuracy. This paper introduces an improved face recognition system that is build using C++ programming language with the help of OpenCV library. Accuracy can be increased if a filter or combinations of filters are applied to the images. The accuracy increases from 95.5% (without ap

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Wed Jan 01 2020
Journal Name
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Enhancement of lsb audio steganography based on carrier and message characteristics
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Data steganography is a technique used to hide data, secret message, within another data, cover carrier. It is considered as a part of information security. Audio steganography is a type of data steganography, where the secret message is hidden in audio carrier. This paper proposes an efficient audio steganography method that uses LSB technique. The proposed method enhances steganography performance by exploiting all carrier samples and balancing between hiding capacity and distortion ratio. It suggests an adaptive number of hiding bits for each audio sample depending on the secret message size, the cover carrier size, and the signal to noise ratio (SNR). Comparison results show that the proposed method outperforms state of the art methods

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Wed Jan 01 2020
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Enhancement of lsb audio steganography based on carrier and message characteristics
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Tue Jan 08 2019
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Enhancement of vanadium oxide doped Eu+3 for gas sensor application
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Thin films of vanadium oxide nanoparticles doped with different concentrations of europium oxide (2, 4, 6, and 8) wt % are deposited on glass and Si substrates with orientation (111) utilizing by pulsed laser deposition technique using Nd:YAG laser that has a wavelength of 1064 nm, average frequency of 6 Hz and pulse duration of 10 ns. The films were annealed in air at 300 °C for two hours, then the structural, morphological and optical properties are characterized using x-ray diffraction (XRD), Field emission scanning electron microscopy (FESEM) and UV-Vis spectroscopy respectively. The X-ray diffraction results of V2O5:Eu2O3 exhibit that the film has apolycrystalline monoclinic V2O5 and triclinic V4O7 phases. The FESEM image shows a h

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Publication Date
Sun Dec 27 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Phytochemical Investigation of Aerial Parts of Iraqi Cardaria draba
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Sat Mar 01 2008
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An Investigation of Photoconductivity in Indium Antimonide Crystal
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Various Hall Effects have been successfully observed in samples of n-type indium antimonide with values for conductivity, energy gap, Hall mobility and Hall coefficient all agreeing with theory. A particular interest in developing a method for obtaining accurate values of carrier concentrations in semiconductor samples has been fulfilled with an experimental result of (1.6×1016 cm-3 ±10.7%) giving a percentage difference of (6.7%) to a quoted value of (1.5×1016cm-3) at (77K) using an (80mW C.W. CO2) laser beam at (10.6μm) to illuminate a similar sample of n-type indium antimonide, an "Optical" Hall effect has been observed. Although some doubt has been raised as to the validity of effect i.e. "thermal" rather than "Optical", values o

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Publication Date
Sun Dec 01 2019
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Investigation of Effecting Parameters in a Turning Operation
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Publication Date
Fri Sep 01 2023
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Investigation of Numerical Simulation for Adaptive Optics System
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