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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 Dec 01 2017
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The impact of multiple sources of funding on the disclosure of cash flow and the activation of control procedures
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The principle of an interview requires revenues to expenditures by linking the efforts and achievements and disclosure sufficient to result activity, in the case generate future benefits of a particular asset, this asset appears in the balance sheet to reflect with the rest of the accounting unit's assets on the strength of financial position In the absence of future benefits from the effort are so loaded effort on the result accounts that reflect the outcome of activity during a specific period if the month or be separated or fiscal year. 

The researcher reached the following conclusions:

 1- difficult to control the cash inflows and outflows as a result of the multiplicity of sources of funding.

2- wea

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Publication Date
Wed Oct 01 2014
Journal Name
Journal Of Economics And Administrative Sciences
The Sources and Effects of Risks of Forms of Islamic Financing in the Islamic Branches of the Commercial Bank
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Proved Islamic banks in many countries where they are present, whether Muslim or non-Muslim in the wake of the global financial crisis, it is more efficient, profitable, and stable compared with the conventional banks, so went many of the worlds towards providing Islamic banking through Islamic windows to Besides financial services and products offered by the traditional, or the initiative to enter formulas Islamic finance is fully compliant with the principles and rules of Islamic law and is Brokerage basic function of conventional banks and Islamic alike ) and that means working on the mobilization of savings from surplus units and directed towards the financial units of the fiscal deficit) , which operates commercial banks

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Publication Date
Sun Apr 01 2018
Journal Name
Journal Of Educational And Psychological Researches
Problems and needs of Baghdad university students from perspective of college of political sciences and college of engineering’s students
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The current research aims to identify the problems and needs for both college of political science and college of engineering’s students. The sample was (100) male and female student. The results showed bunch of problems which could be organized descendingly, the scientific domain ranged between (2 - 2.42), the mean of the psychological domain was (2.85), the moral domain ranged between (2.2 – 2.28)m the problems of study earned (2.30), the material domain got (1.95), the medical and social domain obtained (1.925), and finally, the family domain received (1.887).

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Publication Date
Sun Mar 04 2018
Journal Name
Iraqi Journal Of Science
Effect of maternal exposure of silver nanoparticles on the histogenesis of cerebellum in post-implantation of albino rats embryos
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The central nervous system is the most important system and is very sensitive to any accidental infection during ontogenesis; it includes brain and spinal cord. The cerebellum is the second largest part of the brain after cerebrum and it’s very sensitive to the abnormal changes during the embryological development. This study was designed to investigate the effect of the maternal exposure of selected concentrations of suspension of nanoparticles on the ontogenesis of the rat cerebellum after embryos implanted in uterus. A total of 60 female pregnant rats were divided in to three groups, each contains 20 females. Group1 (G1) was treated orally with 2mg/kg /body weight (b. wt) of suspension of silver nanoparticles (Ag NPs). While group 2 (G

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Publication Date
Sun Mar 04 2018
Journal Name
Iraqi Journal Of Science
Effect of maternal exposure of silver nanoparticles on the histogenesis of cerebellum in post-implantation of albino rats embryos
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Publication Date
Wed Jun 07 2023
Journal Name
Journal Of Educational And Psychological Researches
The Extent of Academic Knowledge in the Colleges of Applied Sciences of the Areas of the National Learning Strategy 2040 in the Sultanate of Oman
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The study aims to identify the extent the academics in colleges of applied sciences are familiar with the themes of the national strategy of education 2040 in the Sultanate of Oman. The researchers used the descriptive approach, as well as they adopted a questionnaire with five dimensions as a tool for data collection, which was applied to (120) academics. The results showed that the academics of the applied colleges' familiarity with the National Strategy for Education 2040 in the Sultanate of Oman is average. The study also found that there were no statistically significant differences in the academics estimates of the extent of the Colleges of Applied Sciences academics’ familiarity with the themes of the National Education 2040 Str

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Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
The Role of Culture Consumption in an Increase of Deception Marketing , a Sample Survey of Cosmetic Users Employees College of Administration & Economics / University of Mosul
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Economics / University of Mosul

 

Abstract

The spread of the phenomenon of excessive buying in our society, especially for cosmetics, and at the same time increase the marketing deception by the organizations to take quick profit 'and accordingly was identified the problem of research in several questions, including:

Is there a significant effect of consumption culture on marketing deception?                                                &n

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Publication Date
Wed Jun 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
The role of knowledge management strategies in building core competenciesAn exploratory study of the views of a sample of managersOffice of Financial Supervision in Iraq
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The strategies of knowledge management have became the basis in the promotion of core competencies. Therefore gained an increasing prominence. This led the administrations of organizations to work to effectiveness of there strategies, which results to build there core competences through teamwork, empowerment and personal effectiveness of employees. From this arises research problem about the  organizations leaders recognize extent of knowledge management strategies which that lead to core competence. In addition the research tray definition the relation and nature of affect between its variables. The research was carried on sample (72) managers from board of supreme audit in Iraq and used statistical tools and methods.

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Publication Date
Thu Sep 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
Leadership ethics and transformational leadership to develop perceptions of organizational work supportA survey of a sample of the staff of the Ministry of Water Resources
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The aim of organizational contemporary is development man power active, in spit-of there are littlie resources. But in the Iraqi environment there are too much resources with performance inhabiting. specially in the ministry of water resources (sample of this research), about dryness and lower levels of rivers. There for this study have some important variable, it is ethical leadership & transformational leadership as (independent variable), and Perceived organizational support(dependent variable). Over here to invest with authority on the problem of research, is weakness harmony between employed perception and the pattern of leadership. We find decline in of reaction of organ compound between the variable to weaken high perf

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Publication Date
Wed Sep 08 2021
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Obstacles facing the application of electronic banking An exploratory: study of the opinions of a sample of bank employees operating in the city of Nasiriyah
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Electronic banking plays a prominent role in providing the best banking services and upgrading the banking sector for the better, so this study aimed to shed light on the most prominent obstacles that prevent the application of electronic banking in banks operating in the city of Nasiriyah, and in order to achieve this goal the researcher used the descriptive analytical approach And through a questionnaire form that was distributed to a group of employees, numbering (60) employees in the upper, middle and operational departments in a number of branches of private banks operating in the city of Nasiriyah, namely (the Iraqi Trade Bank, the Gulf Commercial Bank, the Bank of Baghdad, the Union Bank of Iraq), which represented The stu

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