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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 Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
Measuring and analysis of the impact of public budget deficit on external debt in lraq with in the framework of joint integration of the period (1990 – 2016 )
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The concept of deficit in public budget becomes a chronic economic phenomenon in most of the world, whether the advanced countries or developing countries. Despite  the difference in the visions of the economic schools to accept or reject the deficit in public budget but the opinion that prevailed is the necessity of the state to reduce the public spending which led to a continuous deficits in the public budget which consequently increased the government borrowing ,increase income taxes and wealth, consequently this weakened the in motivation in private investment which contributed to the increase of in factionary stagnation , so that governments have to cover the lack of local funding sources which become difficult to be eq

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Mon Nov 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
Biological Effect of Different Concentrations of Bacillus Thurngensis Isolated From The Soils of Sawa Lake, Al Muthanna Governorate on The of Hypera postica at Different Time Periods
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Abstract<p>This study conduct in Al-Muthanna governorate to assess five concentrations of <italic>Bacillus</italic> thurngensisagonist <italic>Hyperapostica</italic>. The results showed the presence of <italic>Bacillus thurngensisin</italic> all the studied sites of Lake Sawa in Muthanna Governorate, and the rates of its presence were close to the same sites, and the rate of its presence in those sites was 35%, and its highest rate was recorded in the north and east of the lake, as it reached 40% and the lowest amounted to 30% in the two sites south and west site. The results of the study showed that five concentrations were taken from bacterial isolates of <it></it></p> ... Show More
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Fri Jul 01 2016
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A reflection of organizational citizenship behaviors in the performance of employees A prospective study of a sample of the teaching staff working in the Degla University College
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Abstract
        This research aims to identify the relationship and the impact of the behavior of organizational citizenship in the performance of employees, as practiced behaviors organizational citizenship substantial role in achieving the objectives of both the organization and its staff at the same time, so it affects a large extent on the characteristics and performance of individuals employees and thus influence the success of the organization as a whole, problem of the research has indicated that there is a clear failure in the study of the impact of the behavior of organizational citizenship in the performance of employees, was chosen

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Publication Date
Sat Feb 01 2020
Journal Name
Journal Of Economics And Administrative Sciences
The role of merger in creating differences in the profitability of companies Analytical research between a sample of subsidiaries to the Iraqi Ministry of Industry and Minerals
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The research aims to identify the impact of the merger of the companies affiliated to the Ministry of Industry and Minerals on their financial profitability since the companies before the merger suffered a rise in losses and the deficit reached very high levels that affected its overall performance and even on the morale of workers as losses are increasing and solutions Efficiency is absent. The problem stems from knowing the impact of the merger on the profitability ratios of the companies. The research field was represented by the companies affiliated to the Ministry of Industry and Minerals (21) companies, while the research sample reached (6) companies after the merger (14) companies before the merger, was based on data The f

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Publication Date
Sun Feb 15 2026
Journal Name
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The extent of Concern of the University Press in Students’ Issues (Journal of the University of Technology as a Model) for the Period from 2009 to 2012
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The university press is an essential pillar in building an academic community to achieve its objectives in the service of society. Since the university press is a means of university media, which is issued by the departments or units of media in Iraqi universities as academic governmental-institutions, so it highlights the activities of the university and link them to its internal society in the first place as the university press is a mirror of the university and its voice is sincerely expressed. This research comes to know the extent of interest of the university press in various student issues.

In order to identify the problem of the research, the method of content analysis was adopted within the survey method

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Publication Date
Mon Oct 01 2018
Journal Name
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Studying the effect of institutional pressures on the attitudes of the managers of small enterprises in Thi-Qar province toward intention continuance environmental disposal of e-waste
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       Currently, there is no established of e-waste treatment in Thi- Qar province, while their creating is increasing every year. It has been well- known that e-waste is a source of environmental degrading and their placement in landfills increases the irreversible climate change. A research model has been developed to link three components: coercive pressure, normative influence, and mimicry, then study their effect on e-waste adopt and continuance intentions. The model was validated using data collected from a field survey of 92 managers of small enterprises in Thi-Qar province.  A questionnaire was developed to collect data. It contains five major variables, exemplify by fourteen items. Als

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Publication Date
Mon Mar 07 2022
Journal Name
Journal Of Educational And Psychological Researches
The impact of the Roundtable and Self-Questioning strategies on achievement and self-efficacy For students of the Faculty of Education in the subject of research curricula
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The current research aims to identify "the impact of the round table strategies and the question of self-achievement and self-efficacy among students of the Faculty of Education in research methodology course.” The research sample consisted of (75) male and female-third stage students in the department of Life Sciences / College of Education for Pure Sciences / University of Dhi Qar for the academic year (2018-2019. The researcher adopted the experimental approach to achieving the study objectives. The researcher prepared two tools: the achievement test and the self-efficacy scale were applied to the collected sample to obtain the needed data. The result showed that there was a statistically significant difference at the level (0.05) b

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Mon Dec 01 2025
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المجلة العلمية لعلوم والتكنولوجية للنشاطات البدنية والرياضية
Attitudes of students of the College of Physical Education and Sports Sciences towards modern educational strategies used in scientific courses from the perspective of fourth-year students
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The aim of the research: To identify the trends of students of the College of Physical Education and Sports Sciences towards modern teaching methods. To determine the type of strategies used that students prefer in practical lessons. In light of the research results, the researcher adopted the descriptive method because it is appropriate for the study. The research community is represented by students of the College of Physical Education and Sports Sciences (fourth stage), amounting to (320) students. Conclusions: The research results indicate that students of the College of Physical Education and Sports Sciences have positive and strong attitudes towards using modern teaching methods, and they realize their reality in improving interaction

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Publication Date
Mon May 01 2023
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THE EFFECT OF ARRANGING WOMEN'S ISSUES IN THE IRAQI ELECTRONIC NEWSPAPERS' WEBSITES ON THE COGNITIVE LEVEL OF IRAQI UNIVERSITY FEMALE TEACHERS A FIELD STUDY OF A SAMPLE OF FEMALE TEACHERS AT THE UNIVERSITY OF BAGHDAD
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Women are considered the real power to build societies, as they are half of society, and it is their responsibility to raise generations، as human history testifies to the recording of great names with their giving and achievement in various scientific, social and humanitarian disciplines. Because of the importance of women in our lives, society must give them special care, whether at home or within the community structure to which they belong, so that they contribute to the image that brings about a transformation in the public scene, as well as providing them with support to take charge of bringing about change themselves, and this explains the interest of the press at all levels. Women's issues and topics through various journal

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Publication Date
Fri Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
The Role of Integration Between The Target Costing and Resource Consumption Accounting Techniques in Reducing Costs and Supporting Competitive Advantage - Analytical Study of The Opinions of a Sample of Employees of The Babylon Cement Factory.
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Abstract

The purpose of this research is to develop a proposed framework for achieving the Integration of the Target Cost and Resource Consumption Accounting Techniques and to show the role they play in reducing products costs and supporting the competitive advantage to cope with contemporary changes. To achieve this goal, the researchers followed the analytical method using the statistical questionnaire as a means of collecting data from the research sample include accounting, administrative, technical, engineering staffs and others. The research sample consists of (56) individuals and for the purpose of conducting statistical analysis of the data and testing hypotheses, the statistical program (SPSS) wa

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