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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
Fri Feb 17 2023
Journal Name
Biomass Conversion And Biorefinery
Effect of green synthesis of Fe3O4 nanomaterial on the removal of cefixime from aqueous solution
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In this paper, two types of iron oxide nanomaterial (Fe3O4) and nanocomposite (T-Fe3O4) were created from the bio-waste mass of tangerine peel. These two materials were utilized for adsorption tests to remove cefixime (CFX) from an aqueous solution. Before the adsorption application, both adsorbents have been characterized by various characterizations such as XRD, FTIR, VSM, TEM, and FESEM. The mesoporous nano-crystalline structure of Fe3O4 and T-Fe3O4 nanocomposite with less than 100-nm diameter is confirmed. The adsorption of the obtained adsorbents was evaluated for CFX removal by adjusting several operation parameters to optimize the removal. The optimal conditions for CFX removal were found to be an initial concentration of 40 and 50 m

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Publication Date
Thu Jul 01 2021
Journal Name
European Journal Of Dentistry
Effects of Long Durations of RF–Magnetron Sputtering Deposition of Hydroxyapatite on Titanium Dental Implants
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Objectives Dental implant is a revolution in dentistry; some shortages are still a focus of research. This study use long duration of radiofrequency (RF)–magnetron sputtering to coat titanium (Ti) implant with hydroxyapatite (HA) to obtain a uniform, strongly adhered in a few micrometers in thickness. Materials and Methods Two types of substrates, discs and root form cylinders were prepared using a grade 1 commercially pure (CP) Ti rod. A RF–magnetron sputtering device was used to coat specimens with HA. Magnetron sputtering was set at 150 W for 22 hours at 100°C under continuous argon gas flow and substrate rotation at 10 rpm. Coat properties were evaluated via field emission scanning electron microscopy (FESEM), scanning electro

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Thu Dec 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
The impact of financial reporting of earnings per share on the quality of financial reporting
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This research deals with the case of the Iraqi joint-stock companies listed on the Iraq Stock Exchange study in terms of compliance with the requirements of IAS 33 "Earnings per share" and the research problem Alrtash concentrated in a statement the commitment of those companies the requirements of the International Standard 33, which may adversely affect the quality of financial reporting where and in particular the quality of accounting information and content of the primary and secondary characteristics make them be of interest to the decisions of its users, so the aim of this research to the statement of financial reporting earnings per share on the quality of financial reporting in listed shareholding in Iraq Stock Exchange

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Publication Date
Thu Jun 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
The role of governance in the evaluation of the social performance of the economic units
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The aim of this investigation is to study and analysis the role of governance in the evaluation of the and social performance of the economic units to be addressed through the concept of corporate governance and then to the social performance and its relationship to corporate governance.

The most important obtained results from this research is that the corporate governance of extreme importance, and derive their importance from being an essential tool to contribute to the transparency and fair disclosure of the financial results of economic units in the fight against financial and administrative corruption in economic units, thus providing protection and confidence of all parties, and the evaluating soci

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Publication Date
Fri Jan 01 2021
Journal Name
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Evaluation of mechanical properties and cytotoxicity of maxillofacial silicone material after incorporation of zirconia nanopowder
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Resilient polymeric materials such as silicone elastomers are currently used for maxillofacial prostheses construction but the strength of these materials and their clinical performance need to be optimized with the addition of reinforcing fillers. This study investigates the effect of zirconia nanopowder addition on tear strength, tensile strength, elongation at break, Shore A hardness, surface roughness and cytotoxicity of VST-50 maxillofacial silicone. Silicone base was mixed with different amounts (1%, 2% and 3%) of zirconia nanopowder using a vacuum mixer. Silicone without filler was used as control for comparison. Scanning Electron Microscopy and Atomic Force Microscopy were utilized to assess the efficiency of high-shear vacuum mixin

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Publication Date
Mon Dec 02 2013
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Effect of Magnetized Water on Histological Structure of Heart, Lung and Spleen of Albino Rats
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The aim of the study was to investigate the effect of magnetized water on the histological structure of heart, lung and spleen. For this purpose, twenty five albino rats were divided into five equal groups, the first group was considered as control group. The other groups were given magnetized water with intensity of 250, 750, 1000, 1500 gause every day for 30 days. Then the animals were sacrificed and the histological change on heart, lung and spleen was studied. Histopathology of heart in rats treated with magnetic water with intensity of 250, 750, 1000, 1500 gause showed no clear pathological lesion. Lung section of rats treated with 250 gause of magnetic water showed no pathological lesion, while lung section belongs to rats group given

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Publication Date
Tue Jan 02 2018
Journal Name
Journal Of Educational And Psychological Researches
The effectiveness of educational design design according to the theory of Ozbal in the acquisition of geographical concepts among the pupils of the fourth primary in the geography and development of their habits of mind
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Summary The objective of the research is to learn the design of a learning educational learning according to the theory of Ausubel in the acquisition of geographical concepts among the students of the fourth primary in the field of geography and the development of their habits of mind. To achieve this, the researcher relied on the two hypotheses the researcher used the design of equal groups the first experimental group was studied according to the design educational educational learning according to the theory and the other is an officer according to the traditional method. The research community consists of fourth grade pupils in primary school day for girls in the Directorate of Education Baghdad, Al-Rusafa, the third academic year 20

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Publication Date
Sun Mar 06 2022
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The Use of Social Networking sites in the Marketing of Values Analytical : Study of the Official Pages of the Ministry of Culture, Tourism and Antiquities and the Ministry of Labor and Social Affairs on Facebook
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The social networking sites have brought about fundamental changes and a qualitative shift in the marketing industry and its strategies. The Iraqi ministries have used this site i.e. Facebook to spread and disseminate values in order to consolidate it in Iraqi society which has witnessed many changes in all aspects of life.

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     The researcher uses a survey method and content analysis for the publications of these two pages during the study period starting from January 1, 2

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Publication Date
Thu Mar 01 2012
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The role of Cost awareness of activation of strategic cost management techniques of industrial units: A prospective study at the General Company for the manufacture of medicines and medical supplies in the province of Mosul
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The last ten years observed a shift enormous scientific in the method and way that it deals professional with the cost accounting and reflected the result those shift enormous scientific of increase the competitive environmental that accompanied the emergence of a modern manufacturing environmental on surface the long roductive life and emergence advanced information technology that give a central focus of his important on client with growing global markets growth on a large scale.

        The research aim to define the concept of cost awareness, the concept and methods of  strategic cost management and the role of cost awareness for managers of industrial units in strategic of cost managem

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Publication Date
Sat Dec 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Developing strategic leadership practices in the light of transparency and organizational citizenship behavior - A field study of a sample of the staff of the Office of the Inspector General at the Iraqi Ministry of Culture
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Diversity the terms and practice the organizational filed with different concepts and environment, which Iraqi environment part from them. Some organizational in Iraqi environment leave its basic oriented to agreement with the leader desire, their fore this research focus tow basic variable (organizational citizenship behavior & transparence), we supposition which is dependent to explanation the response variable (strategic leadership). The results justification in part and not justification in another part. For example the organizational citizenship behavior effect on some parte of the strategic leadership. The transparence have faraway to fly from the relation with organizational citizenship behavior and strategic leadershi

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