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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
Sun Aug 24 2025
Journal Name
Al–bahith Al–a'alami
The Impact of Means of Communication on Electoral Behavior and its Relationship to the Political Disparity of the Family (A Field Study of an Audience of the University of Baghdad’s Students)
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Iraq has seen many changes at the social, economic and political levels. This led to cause many shifts in the structure of its society and imposed great challenges reflected in the behavior and awareness of that society in general and youth in particular.

Those changes made the Iraqi society undergoing the transformation of value and culture aspects formed a political awareness that caused cultural and political diversity within the family and society. A greater openness to the outside world caused by the communication revolution, as the world has witnessed during the past two decades, has helped in making that change. Iraq had its share of media and political openness, which were included after the US occupation in 2003. As a re

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Thu Jul 07 2022
Journal Name
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COMPARISON BETEEEN THE CONSUMPTION OF RED MEAT AND WHITE MEAT FOR ASAMPLE OF CITIZENS OF THE CITY OF BAGHDAD/ AN EXPLORATORY STUDY : COMPARISON BETEEEN THE CONSUMPTION OF RED MEAT AND WHITE MEAT FOR ASAMPLE OF CITIZENS OF THE CITY OF BAGHDAD/ AN EXPLORATORY STUDY
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Three hundred Iraqi people participated in demographic and attitudes study about red and white meat consumption. The mean age of the participants was 50 SD ± 11 years (mean 30-72); 51% were females and 49% males, mostly in forties who lived ≥ 5 years in Baghdad. The results showed that 80% of individuals prefer red meat. A 90% of people prefer fresh meat compared to frozen and processed meat. A 60% of people buy meat from popular markets. Nearly 87% of respondents believe the improving of livestock sector is essential and 80% of people confirmed there are obstacles to development this sector. An 80% of participates thought the reasons of the high prices of local fresh meat is the lack of plann

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Publication Date
Mon Jul 01 2019
Journal Name
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The Impact of Strategy 3-2-1 in acquiring Concepts of Sociology of fourth grade students: The Impact of Strategy 3-2-1 in acquiring Concepts of Sociology of fourth grade students
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Abstract

The current research aims to identify the impact of triangular bridging strategy in the acquisition of sociology of fourth-stage students. To achieve the research objective, the following null hypotheses were adopted: there are no statistically significant differences at a significance level (0, 05) between the average grades of the experimental group students who studied the triangular bridging strategy in acquiring concepts of sociology and average grades of the control group. The researcher has selected the fourth-stage students from Alexandronah School for girls that s related to the Directorate General of Baghdad the sample consisted of (87) students at litera

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Publication Date
Thu Apr 25 2019
Journal Name
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HARNESSING DIGITIZATION TO ACHIEVE THE GOALS OF SUSTAINABLE DEVELOPMENT 2030\ EXPERIENCE OF THE EMIRATE OF DUBAI.: HARNESSING DIGITIZATION TO ACHIEVE THE GOALS OF SUSTAINABLE DEVELOPMENT 2030\ EXPERIENCE OF THE EMIRATE OF DUBAI.
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Experienced economic environmentRadical changes at the end of the last century and the beginning of the present century, resulting in new concepts and expectations in all aspects of economic, political, social and even behavioral.Each of these concepts is the result of rapid developments in the intangible space. Competition is no longer limited to the mere possession of tangible material resources, but because of its link to knowledge and technology content and to the comprehensive quality standards and efficient and effective policies of States. With the increasing pace of growth and interdependence among the global economies, this resulted in the birth of a new economic system led by technological development and financial liberalizati

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Publication Date
Sat Dec 31 2022
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EFFECT OF ADDING DIFFERENT LEVELS OF DILL SEEDS TO THE DIET ON PHYSIOLOGICAL TRAITS OF BROILERS : EFFECT OF ADDING DIFFERENT LEVELS OF DILL SEEDS TO THE DIET ON PHYSIOLOGICAL TRAITS OF BROILERS
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This study was conducted in the poultry field of the department of animal production, college of agricultural engineering sciences, university of Baghdad for the period from 10/15/2021 to 11/25/2021 with the aim of showing the effect of adding different levels of dill seeds to the diet on productive and carcass traits For broiler meat. In this study, 200 unsexed broiler chicks of breed (Ross 308) were used, one day age, with a starting weight of 41.46 g. The chicks were randomly distributed to 5 treatments, and each treatment included 4 replicates, 10 birds for each replicate. The birds were fed three diets: the starter diet, the growth diet and the final diet. The experiment treatments were T1,

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Publication Date
Wed Dec 01 2021
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The Mediating Role of Managing the High Involvement Management Between Organizational Power and Negotiation StrategiesAnalytical Research of the Views of a Sample of Leaders of the Iraqi Ministry of Industry and Minerals
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The research aims to test the relationship and impact of High Involvement Management as an independent variable in negotiation strategies as a response variable, at the headquarters of the Iraqi Ministry of Industry and Minerals in Baghdad Governorate, and then trying to come up with a set of recommendations that contribute to strengthening the negotiations carried out by the ministry’s leaders and based on the importance of the topic of research in public organizations and the importance of the surveyed organizations to the society. The descriptive-analytical approach was adopted in the completion of this research, and the research included a sample of (180) leaders of the Iraqi Ministry of Industry and Minerals, and data was

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Fri Jan 01 2021
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The effect of Daniel's model on the development of critical thinking in the subject of Arabic language among students of the College of Management and Economics
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Publication Date
Fri Mar 15 2019
Journal Name
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Assessing the Brief Book of the Modern and Contemporary History of Asia from the Perspective of the Students in the Department of History - University of Baghdad
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Wed Jan 01 2020
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Thu Dec 01 2016
Journal Name
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Abstract

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