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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 Feb 24 2019
Journal Name
Iraqi Journal Of Physics
Synthesis of polyynes by laser ablation of graphite in ethanol
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In this work  Polyynes was synthesized by pulse laser ablation of graphite target in ethanol solution. UV-Visible Spectrophotometer, Fourier Transform Infrared Spectroscopy (FTIR) and Transmission electron microscopy (TEM) were used to study the optical absorption, chemical bonding, particle size and the morphology.  UV absorption peaks coincide with the electronic transitions corresponding to linear hydrogen – capped polyyne (Cn+1H2), the absorption peaks intensity increased when the polyynes were produced at different laser energies and the formation rats of polyynes increased with the increasing of laser pulse number. The FTIR absorption peak at 2368.4 cm-1, 1640.0 cm-1 and 1276.

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Publication Date
Mon Dec 20 2021
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
A SURVEY OF RUNNING CRAB SPIDERS PHILODROMIDAE (ARANEAE) OF ARMENIA
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Twelve species of philodromid crab or running crab spiders (Philodromidae) have been recorded in Armenia. Nine species are new to the spider fauna of this country: Philodromus cespitum (Walckenaer, 1802); Philodromus emarginatus (Schrank, 1803), Philodromus rufus Walckenaer, 1826; Rhysodromus histrio (Latreille, 1819), Thanatus atratus Simon, 1875; Thanatus formicinus (Clerck, 1757); Thanatus imbecillus L. Koch, 1878; Thanatus vulgaris Simon, 1870 and Thanatus pictus L. Koch, 1881.

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Publication Date
Tue Feb 10 2026
Journal Name
Journal Of Al-turath University College
Implications of the political responsibility of the government (Comparative study)
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Publication Date
Tue Feb 10 2026
Journal Name
Imam Ja'afar Al-sadiq University Journal Of Legal Studies
Weaponization of outer space from the perspective of international law
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Publication Date
Fri Apr 01 2016
Journal Name
Journal Of Engineering
Preparation and Study of morphological properties of ZnO nano Powder
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In this work, ZnO nanostructures for powder ZnO were synthesized by Hydrothermal Method. Size and shape of ZnO nanostructureas can be controlled by change ammonia concentration. In the preparation of ZnO nanostructure, zinc nitrate hexahydrate [Zn(NO3)2·6H2O] was used as a precursor. The structure and morphology of ZnO nanostructure have been characterized by scanning electron microscopy (SEM), atomic force microscopy (AFM), X-ray diffraction (XRD). The synthesized ZnO nanostructures have a hexagonal wurtzite structure. Also using Zeta potential and Particle Size Analyzers and size distribution of the ZnO powder

 

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Publication Date
Tue May 23 2023
Journal Name
Journal Of Namibian Studies : History Politics Culture
The Ability of Cities to Withstand the Disasters of Pandemic
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This study examines the opportunity presented by the COVID-19 pandemic for city planners and leaders to learn from the crisis and build resilient cities with long-term societal, economic, and environmental resilience against future disasters. The research focuses on the relationship between urban planning and policies and the extent of their resilience, particularly in response to pandemic-related disasters. The study evaluates the ability of the city of Baghdad to respond to the pandemic and identifies gaps in its resilience. The study uses the scorecard measurement instrument to examine the disaster resilience of cities, with a focus on governance and financial capability, disaster planning and preparedness, and disaster response

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Publication Date
Fri Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
Role of ERP In Enhancing the Accuracy of Financial Reporting
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Abstract

Nowadays, the adoption of economic unity on the accuracy of financial reporting is very important. Economic units need accurate financial reporting to be more competitive and to improve the performance. Management can also achieve financial information in real time through the application of ERP systems. This system will facilitate management to access the most up-to-date information such as planning, monitoring and evaluating the business processes of the organization to be more effective.

On the practical side, the Enterprise Resource Planning (ERP) system was applied to the General Company for Vegetable Oils to demonstrate a course in enhancing the accuracy of financial reporting.

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Publication Date
Sun Jul 01 1990
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
DESCRIPTION OF NEW SPECIES OF TERMITES (INSECTA, ISOPTERA) FROM IRAQ
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Two specie's of terrnitls are described as new to science from Iraq Amitermes corpnlentus sp. n. and Anacanthotermes savvensis sp. n., with two figures.

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Publication Date
Thu Jul 01 2004
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
MICROFACIE STUDY OF SUBSURFACE SECTION OF BEKHME FORMATION (NORTH IRAQ)
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Bekhme formation, Dernir Dagh well -1 has been divided into two facies units using core
sample slides and depending on sedimentary structures and diagenetic processes .The facies
reflect the environment of the foreslope.This work proves the absence of Bekhme formation
in Dernir Dagh
Well- 1 as a tongue as reported by the Oil Exploration Company. Some species and genera of
bentonic foraminifera were identified. The age of Bekhme formation was estimated
depending on the recognized index fossils to be lower Maastrichtian.

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Publication Date
Wed Feb 19 2020
Journal Name
International Journal Of Development In Social Sciences And Humanities
The Effect of Context on the Comprehension of English Idioms
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DBN Rashid, International Journal of Development in Social Sciences and Humanities, 2020

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