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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 Dec 16 2018
Journal Name
Al-academy
The Effect of 3DS Max in Developing the Skill of Designing Theatrical Decoration among the Students of the Department of Art Education
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The research aims at benefiting from the technological development and the technical progress. This development necessitated that the educational process take advantage of this progress, and the development of special computer software, especially the design programs, made the two researchers think about how to benefit from these design programs in teaching students the skills of theatrical design.

The current search aims at:

Identifying the effect of 3Ds Max in developing the skill of theatrical decoration design among the students of the Department of Art Education "Third stage / Department of Art Education / Faculty of Fine Arts / University of Diyala for the academic year 2014-2015.

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Tue Nov 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Analysis of The Effect of The Administration of Communications Towers in The Selling Prices of Residential Real estate )New University Village Model(
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Tue Dec 06 2011
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Journal Of Planner And Development
The Development of the planning and architectural thought of the holy city of Kadhimia in line with the spirit of the time
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The evolution of thought, planning for Urban Communities in the second half of the twentieth century, through several successive stages. He was thought of planning urban communities depends on identifying the general plan for land uses of the project area as a basis for drawing charts the physical, social, economic, and put the general plan for land uses based on the terms of reference set by the number of experts in the ministries and agencies. I have lived cities in the Arab-Muslim region, during the transition period the natural and historic environment, urban, sophisticated balanced ways mentioned in the cultural, social, inspired by the teachings of Islam and the customs and traditions of the Arab social, put forth a set of

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Sat Dec 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
The Impact of the Dominions of Mindfulness on the Organizational Innovation “Descriptive analytical study in some faculties of the University of Baghdad”
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Research seeks to test the impact of the dimensions of mindfulness on  organizational Innovation, proposed in the light of the review literature on two variables of the research, which referred in General to the dynamic relationship between them, as result of weakness of mindfulness as one important factor driving the diversity of innovation and time, ways to sustain and preserve and then support innovations made by creators, weakness in the overall level of organizational Innovation, this represents the problem research, data collection over designing   identification, distributed to sample Formed from (30) head Department at a number of colleges of the University of Baghdad, results confirms the validity of resea

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Wed Oct 17 2018
Journal Name
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Effect Of Using Quantitative Methods Of Demand Forecasting In Improving Of Supply Chain Performance:" Case Study In One Of An Industerial Organization"
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Objecte The study aims to test the effect of using the appropriate quantitative method of demand forecasting in improving the performance of supply chain of the aviation fuel product ( The study sample), One of the products of the Doura refinery (The study site), By testing a set of quantitative methods of demand forecasting using forecasting error measurements, and choosing the least faulty, most accurate and reliable method and adept it in the building  chain.

Is the study of problem through a starting with the fol

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Publication Date
Wed Oct 24 2018
Journal Name
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The impact of social capital dimensions on the structural empowerment of workers Applied research in the Directorate of the Municipality of Samawa
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The purpose of the research is to identify the social capital of the Municipality of Samawah Municipality by defining the level of its three dimensions (the structural dimension, the relational dimension and the cognitive dimension) and identifying the appropriate means that contribute to increasing the structural empowerment of the workers in the Municipality of Samawah. Between the social capital and the structural empowerment of the workers. From the perspective of social capital, the researchers examined the correlation and the effect of dimensions (structural, relational, cognitive) on the structural empowerment of the workers and with data collected from a sample of (168) Samawah, which is part of the Ministry of Constructi

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Publication Date
Tue Jan 20 2026
Journal Name
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The impact of the use of mirrors in the level of performance of some skills epeeEmpirical researchStudents on the third stage in the Faculty of Physical Education for Girls
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Sun Oct 25 2020
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EFFECT OF EXERCISES USING DIFFERENT RESISTORS IN THE DEVELOPMENT OF THE SPECIAL STRENGTH OF THE ARMS AND THE COMPLETION OF JAVELIN FOR THE ATHLETES OF THE SCHOOL SPECIALIZED ATHLETICS
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Athletics are different from other games as a competition between individuals to show their competence and physical ability to achieve new record numbers in the various activities and various between the boards, jumping and throwing and each type of these activities in particular performance so found the researcher to find the method of training resistors in the development of special power and achievement In the effectiveness of javelin, where the researchers chose the sample of the athletes from the specialized school of athletics to effectively throw the spear at the ages of 15-17 years and carried out the tests of the research, which includes the strength of the speed of the arms and explosive power and The various resistance exercise

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Publication Date
Sun Jun 03 2012
Journal Name
Baghdad Science Journal
Study the effect of the mixture aquatic extract of Peganum harmala seeds and Pericarp of Punica granutum on viability of protoscolices of Echinococcus granulosus in vitro and in vivo
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This study included the preparation of the mixture aquatic extracts of Peganum harmala seeds and Pericarp of Punica granutum at concentration (10+50) ?(15+55)? (20+60) mgml .To study the influence of the mixture on the percentage of vitality of the protoscolices of E. granulosus In vitro, as the vitality of protoscolices had caused complete death when the using concentration at time 120,90,60 minute respectively. Also study the effect of mixture in white mice with infectious protoscolices In vivo and study the change occurred in the averages of the weights of the liver and spleen and the averages of its distension In vivo in processed group with mixture at concentration (15+55) , (10+50)mgml ,as which was approach to the negative gro

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Publication Date
Thu Dec 01 2016
Journal Name
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The role of my style (CPM / PERT) in enhancing the performance of construction projectsAn Empirical Study in the Department of projects in the office of the province of Baghdad
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This study was to demonstrate the role-use planning scientific methods is disabled and little used in the planning and follow-up construction of vital projects in the province of Baghdad, including network planning methods, in order to find the optimal time to finish the project in light of the resources available and the budget set for it, in the current research has been used the most prominent network planning methods and two stylistic (CPM / PERT), was the application of the critical path method on standard-design school project (traditional) to draw Action Network according to confirmed times for the activities of the project and account his Crashing time , It was Pert technique applied to the project hemato

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