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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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Sun Aug 01 2021
Journal Name
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BUILDING AND RATIONING SCALE MANAGEMENT CONSTRAINTS OF E-LEARNING FROM THE PERSPECTIVE OF TEACHING THE FACULTY OF PHYSICAL EDUCATION AND SPORTS SCIENCE UNIVERSITY OF BAGHDAD
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Evaluation of performance of the inspection teams in the appraisal of health situation in Dhi-Qar case research in the Health Department of Dhi-Qar
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Research aims : The aim of the research is to evaluate the reality of the inspection teams' work in the health institutions belonging to Dhi-Qar health office .

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The Reality of Alternative Assessment for Teachers of the First Cycle of the Basic Education in the Sultanate of Oman: Use, Self-Efficacy, and Attitude
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This study aims at identifying the reality of alternative assessment for teachers of the first cycle of the basic education in the Sultanate of Oman with respect to the degree of teachers' use of alternative assessment strategies, level of self-efficacy for alternative assessment strategies, and attitude towards alternative assessment, and their relationship with other variables. To achieve the aims of the study, a descriptive research approach was utilized. A 5-point self-rated questionnaire was developed. It consists of three sections: Actual use of alternative assessment strategies (21 items), self-efficacy for alternative assessment strategies (21 items), and attitude towards alternative assessment (27 items). The psychometric proper

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Thu Mar 30 2023
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The effect of readings on the multiplicity of explanatory significance of a single Qur’anic word, a study through the interpretation of Ibn Attia al-Andalusi
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The study aimed to clarify the meanings learned and inferred from reading books، letters and messages in Surat Al-Qur’an. The inductive method، the analytical method، and the deductive method، One of the most prominent results of the research: that the multiplicity of Qur’anic readings produces a variety and expansion in the meaning that has a clear impact on the interpretation by clarifying the meaning of the verse.

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Tue Jun 30 2020
Journal Name
Journal Of Economics And Administrative Sciences
The role of Techno strategy of Information management in achieving administrative innovation : A case study in the college of Management and Economics / University of Kirkuk
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The present research aims to identify and define the basic dimensions of the information management strategy and the administrative creativity in the Faculty of Management and Economics / the University of Kirkuk, as well as the role played by the dimensions of the information technology management strategy in achieving the administrative innovation in the college and the research problem was formulated in several questions. The research problem was formulated in several questions centered on the correlation between the research variables, and the research was based on a major hypothesis and five sub-hypotheses emerged from which it was subjected to several tests to ensure its validity. The researcher used the descriptive-analyti

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Publication Date
Thu Nov 01 2018
Journal Name
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Evaluation of the performance of private hospitals from the point of view of the beneficiaries (A field Study in the private Sector hospitals in Baghdad)
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Objectives: This Paper is an attempt to evaluate the services provided by the private hospitals
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and activate the role of private medical sector in society .
Methodology: A questionnaire has be designed for this purpose and distributed to ( 132 ) beneficiaries
mostly from Baghdad private hospitals .
Results: The paper has come out with many important results . Among These are the following :
* these who benefit from services provided by private hospitals believe that the good performance of
such hospital is not due to the medical services alone but also to scientific aspect

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Publication Date
Tue Oct 01 2019
Journal Name
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THE ROLE OF SOCIAL ENTREPRENEURSHIP IN IMPROVING THE QUALITY OF LIFE OF THE CUSTOMER Field research at the Iraqi Ministry of Labor and Social Affairs
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Sat Dec 01 2018
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The impact of electronic banking transactions to increase the net revenue of the Bank of paypal in United States of America for Period ( 2010-2016 )
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   It is clear to everyone how important it is to implement transactions electronically, as it facilitates the provision of services to beneficiaries, whether individuals or institutions, to achieve many benefits that are not exclusive to the beneficiary or the applicant, but extends to the governmental and international bodies. And the number of users has reached millions since its emergence in 1995, because the concepts of electronic transactions have great advantages for the economy in general and the banking sector in particular, so cooperation in various fields with the aim of becoming an information society has become paramount, It allows customers to pay money to any company they want t

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Publication Date
Thu Mar 01 2018
Journal Name
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The Effect of Addition of Combination of Plasma Treated Polyester and Polyamide Fibers on Surface Roughness and Some Mechanical Properties of Heat Cured Acrylic Resin
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Thu Mar 15 2018
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The Effect of Addition of Combination of Plasma Treated Polyester and Polyamide Fibers on Surface Roughness and Some Mechanical Properties of Heat Cured Acrylic Resin
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