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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 29 2019
Journal Name
Iraqi Journal Of Physics
Enhancement In Ballistic Performance Of Composite Armor Through Nano Ceramic
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In this study, industrial fiber and polymer mixtures were used for high-speed impact (ballistic) applications where the effects of polymer (epoxy), polymeric
mixture (epoxy + unsaturated polyester), synthetic rubber (polyurethane), Kevlar fiber, polyethylene fiber (ultra High molecular weight) and carbon fiber.
Four successive systems of samples were prepared. the first system component made of (epoxy and 2% graphene and 20 layer of fiber), then ballistic test was
applied, the sample was successful in the test from a distance of 7 m. or more than, by using a pistol personally Glock, Caliber of 9 * 19 mm. The second
system was consisting of (epoxy, 2% graphene, 36 layers of fiber and one layer of hard rubber), it was succeeded

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Publication Date
Sat Mar 19 2022
Journal Name
Al-khwarizmi Engineering Journal
Enhancement of System Security by Using LSB and RSA Algorithms
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A steganography hides information within other information, such as file, message, picture, or video. A cryptography is the science of converting the information from a readable form to an unreadable form for unauthorized person. The main problem in the stenographic system is embedding in cover-data without providing information that would facilitate its removal. In this research, a method for embedding data into images is suggested which employs least significant bit Steganography (LSB) and ciphering (RSA algorithm) to protect the data. System security will be enhanced by this collaboration between steganography and cryptography.

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Publication Date
Tue Jun 03 2025
Journal Name
Journal Of Umm Al-qura University For Applied Sciences
Application of Benesi–Hildebrand and Tauc approaches of new synthesized Schiff bases interacted with two types of electron acceptors modules
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This study has three parts, the first one is the synthesis of a novel Schiff bases by the condensation of guanine or 9-[{2-hydroxyethoxy}methyl]-9H-guanine with variety aldehydes to yield four different bases as follows: (E)-2-((4-nitrobenzylidene)amino)-1,9-dihydro-6H-purin-6-one (S1), (E)-2-((4-methoxybenzylidene)amino)-1,9-dihydro-6H-purin-6-one (S2), (E)-2-((2-hydroxybenzylidene) amino)-9-((2-hydroxy ethoxy)methyl)-1,9-dihydro-6H-purin-6-one (S3), and (E)-2-(((9-((2-hydroxy ethoxy)methyl)-6-oxo-6,9-dihydro-1H-purin-2-yl)imino)methyl)benzoic acid (S4). Then, spectroscopic analyses such as Elemental Analysis, UV/VIS, Mass spectra, FTIR, 1H,13C-NMR were made to recognize these bases. In the second part, the ability of synthesized bases to

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Publication Date
Fri Jun 20 2025
Journal Name
Bulletin Of The Iraq Natural History Museum
INVESTIGATION OF MACROFUNGI IN THE MIDDLE OF IRAQ
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The study aimed to survey mushroom species from fields among herbs, palm trunks, and trees in central Iraq and to identify them on the basis of morphological and molecular characteristics. As a molecular identification result with polymerase chain reaction six species were recorded (with eight isolates): Agaricus bitorquis (Quéllt) Saccardo. 1887 (SHA14); Candolleomyces candolleanus (Fr.) D. Wächter & Melzer, 2020 (SHA15); Cyclocybe cylindracea (D.C.) Vizzini & Angelini, 2014 (SHA13); Leucoagaricus hesperius Vellinga, 2010 (SHA16); Volvariella sp. (SHA17), and Volvopluteus gloiocephalus (D. C.) Vizzini, Contu & Justo, 2011 (SHA10, SHA101 and SHA12), belonging to four families of Basidiomycetes: Agaricaceae, Pluteaceae,

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Publication Date
Fri Aug 10 2018
Journal Name
In Book: Challenges In Mechanics Of Time-dependent Materials, Volume 2edition: 1stchapter: 12
Experimental Investigation of Segmental Post-tensioned Girders
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Publication Date
Wed Sep 23 2020
Journal Name
Artificial Intelligence Research
Hybrid approaches to feature subset selection for data classification in high-dimensional feature space
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This paper proposes two hybrid feature subset selection approaches based on the combination (union or intersection) of both supervised and unsupervised filter approaches before using a wrapper, aiming to obtain low-dimensional features with high accuracy and interpretability and low time consumption. Experiments with the proposed hybrid approaches have been conducted on seven high-dimensional feature datasets. The classifiers adopted are support vector machine (SVM), linear discriminant analysis (LDA), and K-nearest neighbour (KNN). Experimental results have demonstrated the advantages and usefulness of the proposed methods in feature subset selection in high-dimensional space in terms of the number of selected features and time spe

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Publication Date
Wed Jan 01 2020
Journal Name
Journal Of Southwest Jiaotong University
The Arithmetic Coding and Hybrid Discrete Wavelet and Cosine Transform Approaches in Image Compression
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Image compression is one of the data compression types applied to digital images in order to reduce their high cost for storage and/or transmission. Image compression algorithms may take the benefit of visual sensitivity and statistical properties of image data to deliver superior results in comparison with generic data compression schemes, which are used for other digital data. In the first approach, the input image is divided into blocks, each of which is 16 x 16, 32 x 32, or 64 x 64 pixels. The blocks are converted first into a string; then, encoded by using a lossless and dictionary-based algorithm known as arithmetic coding. The more occurrence of the pixels values is codded in few bits compare with pixel values of less occurre

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Publication Date
Wed Feb 15 2023
Journal Name
Remote Sensing
Combining Remote Sensing Approaches for Detecting Marks of Archaeological and Demolished Constructions in Cahokia’s Grand Plaza, Southwestern Illinois
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Remote sensing data are increasingly being used in digital archaeology for the potential non-invasive detection of archaeological remains. The purpose of this research is to evaluate the capability of standalone (LiDAR and aerial photogrammetry) and integration/fusion remote sensing approaches in improving the prospecting and interpretation of archaeological remains in Cahokia’s Grand Plaza. Cahokia Mounds is an ancient area; it was the largest settlement of the Mississippian culture located in southwestern Illinois, USA. There are a limited number of studies combining LiDAR and aerial photogrammetry to extract archaeological features. This article, therefore, combines LiDAR with photogrammetric data to create new datasets and inv

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Publication Date
Mon Dec 05 2022
Journal Name
F1000research
Enhancement of surface properties of polyetheretherketone implant material by fractional laser texturing
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Background: Polyetheretherketone (PEEK) is a promising implant material due to its superior biomechanical strength. However, due to its hydrophobic nature and lack of cellular adhesion properties, it has poor integration with bone tissue. Methods: A fractional CO2 laser was used with various parameters for surface texturing of PEEK substrate to enhance its surface properties. An optical microscope and field-emission scanning electron microscope (FESEM) were used to examine the surface morphology of untextured and laser-textured samples. Energy dispersive X-ray spectroscopy (EDX) was performed to determine the effect of the laser on the microstructure of PEEK. Surface microroughness, atomic force microscopy (AFM), and wettability were invest

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Publication Date
Wed Sep 30 2015
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Enhancement of Uniformity of Solid Particles in Spouted Bed Using Stochastic Optimization
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Performance of gas-solid spouted bed benefit from solids uniformity structure (UI).Therefore, the focus of this work is to maximize UI across the bed based on process variables. Hence, UI is to be considered as the objective of the optimization process .Three selected process variables are affecting the objective function. These decision variables are: gas velocity, particle density and particle diameter. Steady-state solids concentration measurements were carried out in a narrow 3-inch cylindrical spouted bed made of Plexiglas that used 60° conical shape base. Radial concentration of particles (glass and steel beads) at various bed heights and different flow patterns were measured using sophisticated optical probes. Stochastic Genetic

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