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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
Tue Dec 01 2015
Journal Name
Journal Of Engineering
Importance of New Use of Concrete in Iraq Analysis of Development And Use of Concrete in Architecture
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Since its invention by the Ancient Romans and later developed during the mid-18th century, the concrete structure and finish, has been considered as the most powerful, practical, economic and constructional material that meets the building’s architectural and aesthetical requirements. By creating unique architectural forms, the pioneer architects used concrete widely to shape up their innovative designs and buildings.

The pre-mixed ultra-high performance concrete which manufactured by Lafarge.

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Publication Date
Fri Jan 23 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The Effect of LED Light on Depth of Cure and Microhardness of Three Types of Bulkfill Composite
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Background: To evaluate the ISO depth of cure of bulkfill composites and depth of cure which determined by Vickers microhardness test. Materials and Methods: Bulkfill resin composite specimens (n=150) were prepared of three bulkfill composite materials (TetricEvo Ceram, Quixfil and SDR) and light cured by Flash max p3 for 3, 10, 20 seconds and by wood pecker for 10, 20 seconds respectively, a mold was filled with one of the three bulkfill composites and light cured. The specimens removed from the mold and scraped by plastic spatula and the remaining length (absolute length) was measured which represent the ISO depth of cure. After that the specimens were returned into the mold and a microhardness indentation device applied on the specimen

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Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Educational And Psychological Researches
The Effect of PDEODE Strategy on the Acquisition of Historical Concepts of First Class of Intermediate Students
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The research aims to find out the effect of PEDODE Strategy on the acquisition of historical concepts of First Intermediate Grade. To achieve this goal, the researcher has put forward this zero hypothesis: There is no statistically significant difference at the level of (05,0) between the mean of the students' marks in the experimental group who study the history subject using PEDODE strategy and that of the students' marks in the control group who study the subject according to the traditional method in the post-testing on the acquisition of historical concepts. The sample of the study consists of (62 female-students) of First Intermediate Grade in the Directorate of Baghdad Education/ Karkh2nd for the academic year 2016-2017. The sampl

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Publication Date
Fri Jan 23 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Efficacy of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint
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Background: Temporomandibular joint disorders refer to a group of heterogeneous pain and dysfunction conditions involving the masticatory system, reducing life quality of the sufferers. Arthrocentesis is simple and less invasive surgical procedure for the treatment of internal derangement than arthroscopy and better than other conservative procedures such as drugs, occlusal appliances and physiotherapy. The aim of the study was to evaluate the effect of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint for the restoration of its function, reducing pain and preventing further deterioration of the temporomandibular joint dysfunction. Materials and methods: This study was perfo

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Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
The impact of managing employees' performance in building intellectual capital Analytical study of the views of a sample of heads of scientific departments At the University of Kirkuk
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The research aims to identify the impact of managing performance's employees in building intellectual capital, Because employing the practice of managing the performance of employees may acquire familiar skills to improve their performance and reflect on the construction of intellectual capital in the surveyed area, Especially that the independent dimension represented by the management of the performance of employees is one of the important topics that has received attention in the world of management in general and human resource management in particular.  While the adopted dimension was represented by Intellectual capital in the important practice of human resource management in the increasing of  their knowledge, to

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Publication Date
Mon Aug 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
The Role of Moral Intelligence of Internal Auditors in Support of the Performance of Internal Audit Process - Study for Opinions of a Sample of Internal Auditors in Iraq
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Abstract

      The  aim of  the research to define the concept of moral intelligence and its dimensions and its relationship to some personal characteristics with the internal auditors and identify the importance of the employment of moral intelligence dimensions of (empathy, conscience, self- control, respect, kindness, tolerance, fairness) in the internal audit and the extent of support for the performance of the internal audit process in light of these dimensions. And that by answering the following question : Is there a role for moral intelligence  of  internal auditors in support the performance of internal audit process ? How are employ these dimensions i

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Publication Date
Tue Apr 26 2016
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
Study of environmental pollution to soil of power station Dezlat alJadiriyah / University of Baghdad.: Study of environmental pollution to soil of power station Dezlat alJadiriyah / University of Baghdad.
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The study aimed to measure the concentration of some heavy metal elements and represented by (Pb, Cd,Cu) through the use of atomic absorption spectrometer Flame AAS-7000 type SHIMADZU underwent a process modeling to twelve samples from the soil of electricity Dezlat al Jadiriyah station in the Baghdad University compound at a depth of 30-60 cm from the surface and divided the samples into two groups first included six samples from inside the station while the second included six samples from outside the station. For the element of Pb was higher concentration reached by 29.32ppm and less concentration 17.56ppm. were elements Cd and Cu are growing and less and proportions of certain while the highest concentration of copper 9.69 ppm and le

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Publication Date
Wed Jun 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
The role of the cognitive peak and its implications for achieving outstanding performanceAnalytical study of the views of a sample of the staff of the University of Baghdad
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        Knowledge represents the foundation stone for the work of all organizations, are working who leads the thinking of individuals is the ability that leads to behavior based on rationality, it is the work that creates value to the organization and thus gain access to performance winning where that knowledge is a new type of capital based on the thought and experience and is the so-called intellectual capital, which is renewable and is constantly evolving. The study sought to explain the role of the climax  knowledge in achieving the highest levels of performance Organizational and then access to the performance winning in educational organizations the study sample, was found to be a co

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Publication Date
Fri Feb 01 2019
Journal Name
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The extent of the contribution of internal marketing in the management of human talent survey study of the views of some administrative leaders at the University of Mosul
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Investment in the human resource has become an important part of the strategies of educational organizations so that they can be competitive, so that the access of academics in universities to the international awards as a result of their research excellence indicates the effectiveness of this human talent so the interest has emerged in the implementation of a strategy to manage these human talent in organizations in general and educational ones In particular as one of the power sources  that can not be imitated. The focus of the organization on the interaction between the working people has increased attention to the human element in order to achieve the desired quality levels, which called for organi

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Publication Date
Tue Jan 01 2019
Journal Name
Plant Archives
Effect of the addition of guanidinoacetic acid to the dilute tris in some of the biochemical characteristics of the semen of the rams
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The study was planned to evaluate the effect of adding Guanidinoacetic acid in some characteristics of the sperm of the rams. This study was conducted in the animal field of the Animal Production Department / Faculty of Agricultural Engineering Sciences / University of Baghdad, for the period from 5/8/2018 to 28/2/2019. In this experiment, 3 rams were used at the age of 2-2.5 years and weighed 50-54 kg. The semen was collected early in the morning and once a week and the semen was pooled to remove the individual differences. The treatments were divided: GAA-free control group, treatment T1 (0.05 mg / 100 ml GAA), T2 treatment (0.1 mg / 100 ml GAA) and T3 treatment (0.2 mg / 100 ml GAA). The results of the study showed a significant decrease

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