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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
Wed Feb 01 2023
Journal Name
Journal Of Engineering
Effect of the Proposed Outlets on the Hydrodynamic Behavior and Water Quality of the South-West Part of the Al Hammar Marsh
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The current study aims to find a new plan to manage the water quality of the western part of the Hammar Marsh to reduce the salts that cause problems for the marshes and preserve their environmental life by isolating the southwestern part of the Hammar Marsh by closing the outlet under the railway embankment. The outlet is discharging saline water to the east-western part of Al Hammar Marsh. After isolating the southwestern part of the marsh, a new outlet is proposed. The impact of the flow hydrodynamics on improving the water quality was simulated using the SMS model. The hydrodynamics and water quality simulation models for the marsh are : a hydrodynamic model and average depth (SMS RMA2) and a two-dimensional water quality model (SMS

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Publication Date
Tue Dec 01 2009
Journal Name
Journal Of Economics And Administrative Sciences
The role of knowledge management in achieving outstanding university performance (Applied study in the Faculty of Management and Economics / University of Kufa)
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The research aims to determine the role of knowledge management to measure performance on a sample of faculties of Administration and Economics the University of Kufa, and to achieve this goal through a researcher from the theoretical literature and research and studies related to the construction of the scheme shows the hypothetical relationship between the variables, which was adopted by the independent variable knowledge management, distributed four variables are: (knowledge generation, knowledge storage, knowledge dissemination, the application of knowledge), as well as four variables representing the variables adopted for the performance of the university are:
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Publication Date
Sun Dec 18 2022
Journal Name
Journal Of The College Of Languages (jcl)
The Challenges of Translation from Persian to Arabic In Light of the Equivalence Theory of Mona Baker; Equivalence at the Word Level
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This dissertation studies the application of equivalence theory developed by Mona Baker in translating Persian to Arabic. Among various translation methodologies, Mona Baker’s bottom-up equivalency approach is unique in several ways. Baker’s translation approach is a multistep process. It starts with studying the smallest linguistic unit, “the word”, and then evolves above the level of words leading to the translation of the entire text. Equivalence at the word level, i.e., word for word method, is the core point of Baker’s approach.

This study evaluates the use of Baker’s approach in translation from Persian to Arabic, mainly because finding the correct equivalence is a major challenge in this translation. Additionall

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Publication Date
Sun Feb 10 2019
Journal Name
Journal Of The College Of Education For Women
Use of Remote Sensing in the assessment and classification of land degradation in the district of Mahmudiya for the period 1990-2007
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The study consisted in the development and use of a practical method to detect and
monitor, analyze and produce maps of changes in land use and land cover in the district of
Mahmudiya in Baghdad during the period 1990-2007 using the applications of remote sensing
techniques and with the assisstant of geographic information systems (GIS),as a valuable
contribution to land degradation studies.
This study is based maiuly on the processing on two subsets of landsat5 TM images picked up
in August 1990 and 2007 respectively in order to facilitate comparision and were thengeometrically and radiometrcally calibrated ,to used for digital classification purposes using
maximum liklihoods classification or six spectral bands of

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Publication Date
Wed Feb 25 2026
Journal Name
Journal Of Baghdad College Of Dentistry
A Comparative Study of Clinicopathological and Immunohistochemical Expression of CD1a, RANK and RANKL in Langerhans Cell Histiocytosis of Jaw and Skull Lesions
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Background: Langerhans' cell histiocytosis (LCH) is a group of conditions affecting the reticuloendothelial system. It includes Letterer-Siwe disease, Hand-Schuller-Christian disease and eosinophilic granuloma and most often presents in childhood. Materials and methods: Twenty-five cases of LCH were diagnosed histologically and confirmed by CD1a antibody and assessed immunohistochemically using anti-RANKL and anti-RANK antibodies to evaluate osteoclastogenic mechanism. Results: Regarding jaw cases, there was a significant correlation between CD1a and RANK (P=0.016). While in the skull, highly significant correlation existed between RANK and RANKL (p=0.001). Among the sites, there was no statistically significant difference found for each

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Publication Date
Fri Sep 30 2022
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The effect of technical indicators on the movement of bank stock prices : Applied research in a sample of Iraqi private commercial banks
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This study aimed at indicators of technical analysis and their impact on a group of trading stock indices related to it, by standing on the methods used in technical analysis and its various models, diagnosing the obstacles and difficulties that the participants face in predicting stock prices, and proposing solutions and recommendations to overcome and overcome them. From a scientific and practical perspective.

Where the research community consisted of (25) Iraqi private commercial banks, while the research sample consisted of (3) banks with a percentage of (12%) of the research community. The study used the analytical approach to the financial statements during the period between (1/2/ 2022-30/4/2022),

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Publication Date
Thu Jun 30 2016
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Determination of the Optimum Conditions for the Production of Gamma Alumina (ɤ-Al2O3) By the Precipitation Method of the Sodium Aluminate Solution
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Design of experiments (DOE) was made by Minitab software for the study of three factors used in the precipitation process of the Sodium Aluminate solution prepared from digestion of α-Al2O3  to determine the optimum conditions to a produce Boehmite which is used in production of ɤ-Al2O3 during drying and calcination processes, the factors are; the temperature of the sodium aluminate solution, concentration of HCl acid added for the precipitation and the pH of the solution at which the precipitation was ended. The design of the experiments leads to 18 experiments.

   The results show that the optimum conditions for the precipitation of the sodium aluminate solution which

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Publication Date
Fri Mar 29 2024
Journal Name
Molecular Biology Reports
Role of endoplasmic reticulum aminopeptidase-1 gene polymorphism (rs13167972) in occurrence susceptibility of ankylosing spondylitis in a sample of Iraqi male patients
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Publication Date
Wed Dec 13 2017
Journal Name
Al-khwarizmi Engineering Journal
Enhancing the Compressive Strength and Density of Cement Mortar by the Addition of Different Alignments of Glass Fibers and Styrene Butadiene Rubber
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Abstract

In the field of construction materials the glass reinforced mortar and Styrene Butadiene mortar are modern composite materials. This study experimentally investigated the effect of addition of randomly dispersed glass fibers and layered glass fibers on density and compressive strength of mortar with and without the presence of Styrene Butadiene Rubber (SBR). Mixtures of 1:2 cement/sand ratio and 0.5 water/cement ratio were prepared for making mortar. The glass fibers were added by two manners, layers and random with weight percentages of (0.54, 0.76, 1.1 and 1.42). The specimens were divided into two series: glass-fiber reinforced mortar without SBR and glass-fiber reinforced mortar with 7% SBR of mixture water. All s

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Publication Date
Thu Sep 15 2022
Journal Name
Alustath Journal For Human And Social Sciences
The Effectiveness of Counseling on Using the Technique of ‎Positive Self-talk to Develop the Habits of Mind Among Secondary ‎School Students
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This research aims to identify the effectiveness of counseling by using the technique of self-talkin developing the habits of mind among middle school students by testing important hypotheses, and choosing the experimental design for the two groups (experimental - control). The classification of "Costa & Kallick" was adopted to measure the habits of the mind, and the scale consisted of (64) items, and after confirming the psychometric properties of the scale, the researcher applied it to the research sample (487) students from middle school students. One of the students who got the lowest marks after answering the scale. purpose of applying the experiment. He divided them into two groups, one of them is experimental (10) students, as

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