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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
Thu Dec 23 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Students Experience of Hybrid- Education Model at The University of Baghdad College of Pharmacy
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The impact of COVID-19 pandemic on education models was mainly through the expansion of technology use in the different educational programs. Earlier impact of COVID-19 was manifested in the complete and sudden transition to distance education regardless of institution preparedness status. Gradually, many institutions are moving back to on-campus face-to-face education. However, others including all higher education institutions in Iraq are adopting the hybrid education model. This report presents part of the end of semester evaluation survey conducted at the University of Baghdad College of Pharmacy for the Spring 2021 semester. The survey aims to address points of strength and weakness associated with the hybrid education model and spe

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Tue Feb 01 2022
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EFFICIENCY OF PERFORMANCE AND COLLECTION OF INCOME TAX -REALISTIC VIEW OF THE GENERAL TAX AUTHORITY
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The process of evaluating and measuring tax performance is critical to support the tax collection process. The comparison of the amount of revenue collection with what is expected and the process of measuring tax performance continuously by the tax administration leads to increase the collection of tax, determine the size of deviations and stand and know the reasons and take the necessary measures to address them to get a better result in the future. According to the different tasks assigned to them, criteria and indicators for measuring the tax performance vary from one organization to another. These are indicators or criteria that measure tax revenue (i.e., amounts). One of the research's main findings was to raise the tax collection leve

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Wed Jun 14 2023
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This study deals with the subject of art criticism by using Erwin Panofsky's theory to analyze a few Saudi artists' works. The study aims to identify Panofsky's theory and provide criticism of some Saudi artworks using it. The importance of the study is that it enriches the field of art criticism in the Kingdom of Saudi Arabia and helps critics and artists in using Panofsky’s theory to analyze artworks.
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Tue Dec 31 2019
Journal Name
Research On Crops
Influence of foliar application of ascorbic acid and atonik on growth and yield of potato
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Sun Jun 20 2021
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Comparison of Some of Estimation methods of Stress-Strength Model: R = P(Y < X < Z)
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Publication Date
Sun Dec 31 2017
Journal Name
College Of Islamic Sciences
The effect of the significance of the Qur'anic context in the allocation of the year
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Publication Date
Mon Oct 01 2012
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Al–bahith Al–a'alami
Skills of Media Marketing of the Public Relations Staff: (University of Baghdad as a Model)
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Departments and offices of public relations and media in any institution or company is the most important departments that reflect the results of their work negatively or positively on their reputation. This goes beyond the trust and credibility that its internal and external audiences will give it. Where such matter requires the staff, working in these departments and offices, to have communication skills that qualify them to do the role of marketing the communication message. Yet, the communication skills of public relations and media staff vary from person to person depending on the communication position. This skill has two criteria: Achieving the communication goal and the speed in achieving it as a number of skills

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Publication Date
Thu Aug 28 2025
Journal Name
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The Uses of Pedicled buccal Pad of Fat Flap in Reconstruction of Intra Oral Defects
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Introduction: Different surgical techniques used for closure of various oral defects. While each one of these techniques has its limitation; the buccal pad of fat used in last quarter of last century as pedicle or free graft in reconstruction of small to medium, congenital and acquired defects showed good potentials for success. The present study used the BPF as pedicled flap to reconstruct intra oral defects. The study aimed to evaluate of the success of buccal pad of fat pedicled flap in the reconstruction of intra oral defects. Outlining its indications, limitations and complications. Materials and Methods: The study included 19 patients (17 males and 2 females) with age range between (1- 70 years), all patients were treated with pedic

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Publication Date
Thu Oct 25 2018
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Competencies of the Curriculum of Digital Media Education from the Perspective of Iraqi University Professors:
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he research aims to determine the competencies that must be met in the digital media literacy curriculum, which contributes to a great extent in developing the skills of criticism and analysis of the media contents of the students. The study of the two researchers according to the methodology of the media survey. The research tools were: the questionnaire tool, which distributed on 86 . The main objectives of the research were:
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Tue Dec 16 2008
Journal Name
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City of Baghdad Analysis of the mechanisms of economic action in the development and development
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The economy of a city has an important role not only in its establishment but also in its development. This is quite clear in the city of Baghdad throughout its history since its building in 762 A.D. In addition, most of its problems that the city is suffering from are basically related to not giving enough importance to the economic factors in the master planning of Baghdad since 1950’s. This may explain the failiars of master plans in dealing with the actual population growth and the city's inability to absorb such increases and interrelated and diverse activities which are negatively reflected on the economic variables particularly the effect on the land values, and the strong competitions amongst the land uses without previ

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