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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 28 2025
Journal Name
Al–bahith Al–a'alami
The Semiology of Narrative Construction in Television Advertising to an Announce "God Will not Forget us" about the Covid-19 Pandemic for Zain Mobile Telecommunication Company
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This research paper tries to show the significance of the narrative structure in the television advertisement and its connotations. The researchers chose the annual advertisement of Zain Mobile Telecommunication Company for the year 2020, which shed light on the global Corona pandemic crisis. The idea of the advertisement won wide approval as it focused on the suffering that everyone is witnessing like medical and security personnel in particular, and family relationships consequences.
In addition to the positive global interaction with the message presented by the Company in these exceptional circumstances. The advertisement, which lasted for 2.35 minutes, exceeded 13 million views in a short period of time. This prompted us to choos

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Publication Date
Mon Apr 04 2022
Journal Name
Journal Of Research In Medical And Dental Science
Efficacy of Varnishes with: Bioactive Glass, Recaldent Technology and Silver Diamine Fluoride in Comparison with Sodium Fluoride on Tooth Surface Micro-hardness (an In Vitro Study)
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Efficacy of Varnishes with: Bioactive Glass, Recaldent Technology and Silver Diamine Fluoride in Comparison with Sodium Fluoride on Tooth Surface Micro-hardness (an In Vitro Study)

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Mon Mar 01 2010
Journal Name
Iraqi J Pharm Sci,
Synthesis, Characterization and Antibacterial Activities of Ligand Type N2O4 Schiff base and its Novel Complexes with Co(II), Ni(II), Cu(II) and Zn(II) ions
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The reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as magnetic susceptibility measurements. From the above data, the proposed molecular structu

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Publication Date
Sun Dec 28 2025
Journal Name
Journal Of Physical Education
The effect of dynamic lactic training according to the target time fo developing special endurance, lactic acid concentration, and achievement for 800m runners under20 years old
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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Physiological study to investigate the activity of an aqueous extract ofCinnamomum cassiabark on the blood glucose levels in healthy and diabetic rats induced by streptozotocin (stz)
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The present study was investigated the activity of aqueous extract from Cinnamomum cassia bark on the blood glucose levels in healthy and diabetic rats induced by Streptozotcin (STZ). In healthy rats the blood glucose levels were slightly decreased after six hoursof single oral administration with dose (25 mg/kg) of body wight, as well as four weeks after twice daily repeated oral administration of aqueous extract of Cinnamomum cassia bark. In streptozotocin induced diabetic rats we absorved high significant decreased (p<0.05) in blood glucose levels, after four weeks of oral administration of aqueous extract (25 mg /kg ).And blood glucose levels seems to be normal after the period of treatment .Glibenclamide used as standard drug to com

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Publication Date
Fri Mar 28 2014
Journal Name
Advances In Life Science And Technology
Synthesis and Characterization of Novel Schiff Bases, N-Acyl and Diazetines Derived from 3-((5-hydrazinyl-4-phenyl-4H-1,2,4- triazol-3-yl)methyl)-1H-indole
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This work involves synthesis of some new heterocyclic compounds including 1, 3-diazetine. The new Schiff bases [VI] ad derived from 3-((5-hydrazinyl-4-phenyl-4H-1, 2, 4-triazol-3-yl) methyl)-1H-indole [V] which was synthesized by refluxing 5-((1H-indol-3-yl) methyl)-4-phenyl-4H-1, 2, 4-triazole-3-thiol [IV] with hydrazine hydrate in absolute ethanol and this amino compound [V] condensation with different aromatic aldehydes in absolute ethanol to yielded a new Schiff bases [VI] ad. N-acyl compounds [VII] ad were synthesized by addition reaction of acetyl chloride to imine group of Schiff bases in dry benzene. The new diazetine derivatives [VIII] ad synthesized by the reaction of N-acyl compounds [VII] ad with sodium azide in dimethylformamid

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Fri May 15 2009
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Journal Of Planner And Development
Study of Change in Regional Land Use Using Remote Sensing Technology and Geographic Information Systems / Study Area (Hawr Al Huweiza) for the Years 1973-1990-2004
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his project try to explain the using ability of spatial techniques for land cover change detection on regional level with the time parameter and did select for explain these abilities study case (Hewaizah marsh ) . this area apply to many big changes with the time. These changes made action on characters and behaviors of this area as well as all activities in it . This Project concerting to recognize the Using importance of remote sensing and GIS Methodology in data collecting for the changes of land use and the methodology for the analyses and getting the results for the next using as a base data for development and drawing the plans as well as in regional planning .This project focus on practical

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Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
Flow injection analysis for the photometric determination of promethazine-HCl in pure and pharmaceutical preparation via oxidation by persulphate using Ayah 3SX3-3D solar micro photometer
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Publication Date
Tue Dec 29 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Management accounting techniques in product development and achievement customer requirements by adopting the technique of Quality Function Deployment: Applied Research in Baghdad Company for Soft Drinks
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The research aims to apply one of the techniques of management accounting, which is the Quality Function Deployment(QFD) on the Pepsi product in Baghdad Soft Drinks Company and to determine the technical requirements objectively that have been applied in practice in Baghdad Soft Drinks Company / a private shareholding company, as it focuses on meeting the quality requirements and achieving positive quality to provide a product It meets the requirements of current and future customers, hence the importance of research that indicates that the Quality Function Deployment(QFD) is a useful tool to develop the requirements of new products, being a design process driven by customers through their voices, and thus contribute to achieve a competi

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Activities of Ligand Type N2O4 Schiff base and its Novel Complexes with Co(II), Ni(II), Cu(II) and Zn(II) ions.
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The reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as m

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