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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
Mon Jul 03 2017
Journal Name
Iraqi New Medical Journal
Coarctation of aorta in pediatric age group: mode of presentation, early and intermediate outcomes of interventional treatment
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Although rare, coarctation of aorta is a treatable cause of hypertension, transcatheter dilatation by balloon with or without stent are a well-known treatment strategy

Publication Date
Sun Dec 01 2019
Journal Name
Baghdad Science Journal
Diversity, Abundance, and Distribution of Cladocera at the end of the Tigris River North of Basrah – IRAQ
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Seasonal variations of the species composition and abundance of Cladocera were studied in two stations at the end of the Tigris River and one station at the confluence of the Tigris with Euphrates area, at the beginning of the Shatt Al-Arab River in Al-Qurnah North of Basrah Province, from October 2015 to August 2016. Samples of zooplankton were collected by plankton net 100-µm. mesh size. The population density of Cladocera ranged between 1 Ind /m³ during summer and 211 Ind./m³ during winter at station 1 (Al-Jewaber Bridge). A total of 16 species of Cladocera belonging to 12 genera were recorded in the study. The average density of Cladocera ranged from 23.2 ind./m3 at Station 2 (Hamayon Bridge) to 53.7 Ind./m3

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Publication Date
Thu Sep 11 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of Andrews' six keys of normal occlusion in a sample of Iraqi adults in Baghdad city
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Background: The Andrews’ six keys of normal occlusion contribute individually and collectively to the total scheme of occlusion and, therefore, are viewed as essential to successful orthodontic treatment. The present research aims to evaluate the presence of the parameters of the Andrews’ Six Keys of normal occlusion in a sample of 100 Iraqi adults with complete permanent dentition and clinically acceptable normal occlusion (Angle’s Class I) in Baghdad city. Their age range 18-25 years (60 males and 40 females). Materials and methods: Each patient was subjected to clinical examination and then study cast models were made, with their occlusal records. The measuring tools that have been used involved: Three-dimensional goniometer to me

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Publication Date
Thu Dec 01 2016
Journal Name
Journal Of Engineering
Numerical and Experimental Investigations of the Effect of PVD and Vacuum Pressure on the Degree of Saturation
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    Soft clays are generally characterized by low shear strength, low permeability and high compressibility. An effective method to accelerate consolidation of such soils is to use vertical drains along with vacuum preloading to encourage radial flow of water.  In this research numerical modeling of prefabricated vertical drains with vacuum pressure was done to investigate the effect of using vertical drains together with vacuum pressure on the degree of saturation of fully and saturated-unsaturated soft soils.  Laboratory experiments were conducted by using a specially-designed large consolidometer cell where a central drain was installed and vacuum pressure was applied. All tests were conducted

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Publication Date
Fri Apr 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Foreign Trade of Iraq Between the imperatives of economic diversification And the challenges of joining the (WTO)
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         Interested in this research shed light on the reality of foreign trade to Iraq Who suffers from a marked deterioration due to poor economic diversification of the country And increase the degree of economic exposure   , Which creates a state of extreme caution towards the question of accession to the (WTO)   , As controls Iraq's foreign trade commodity  , a president of one oil As well as the contribution of this item  , and by a large formation in GDP   , And that such a large and dangerous decline in the degree of economic diversification will create negative effects On overall economic activity components&

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Publication Date
Sat Feb 09 2019
Journal Name
Journal Of The College Of Education For Women
The Impact of Polia Strategy in the Achievement and Retention of the Grammar of the Arabic Language
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ABSTRACT
Threw this research to the following:
1 - Know the impact of strategy Puglia in the collection of the rules of the Arabic language
students at the Institute of preparation parameters .
2 - Know the impact of the retention strategy in Puglia collection rules Arabic language
students at the Institute of preparation parameters .
To verify the status Mmermaa Find researcher Elsafreeten following two hypotheses :
1 - There is no statistically significant difference between the average score for the collection
of the fourth grade students at the Institute for the preparation of material parameters who
were studying grammar strategy Puglia and average grades collectible fourth grade
students at the Institu

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Publication Date
Thu Jun 15 2023
Journal Name
Jornal Of Al-muthanna For Agricultural Sciences
Effect of different levels of Adrenocorticotropic hormone (ACTH) on physiological performance of broiler under heat stress conditions.
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This experiment was holdup in A-Faris poultry farms from 1st March to 11 of Aprile 2019. (ACTH) hormone infusion was tested in this experiment on acid-base regulation in broiler chickens. For 7 days, osmotic pumps dispensed 8 IU of ACTH in saline/kg of BW/d, or the same volume of saline as in ACTH at 1 l/h. On days 0 and 14, after the beginning of the infusions, blood samples were obtained to establish a baseline. The plasma concentrations of Na+, K+, and Cl- were decreased, whereas the partial pressure of CO2, anion gap, corticosterone, mean corpuscular hemoglobin concentration, and blood concentrations of hemoglobin and HCO - were all elevated due to the ACTH administration. When given ACTH, neither blood pH nor plasma Ca2+ levels changed

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Publication Date
Wed Mar 30 2022
Journal Name
Journal Of Educational And Psychological Researches
The extent of including logical intelligence in the Book of chemistry for the fifth Grade of science
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The aim of the current research to determine the extent of logical intelligence in the book of chemistry for the fifth grade of science and to achieve the goal the researcher has prepared a special criterion in the areas of logical intelligence main and sub-to be included in the book after reviewing the previous literature and studies in this regard may be the final form after presentation to experts and arbitrators in the field of Educational and psychological sciences, curricula and teaching methods from (3) main areas and (21) sub-fields, then the researcher analyzed the book Bibih and applied branches and adopted the idea of ​​both explicit and implicit as a unit of registration and repet

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Publication Date
Tue Jun 15 2021
Journal Name
Al-academy
Forms of post-modernism in performance of Iraqi theatre "dream of Baghdad exam": عمار عبد سلمان محمد
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  The effects of postmodernism on theatrical form was managed by the director (Anas Abdul Samad) to be employed in the Iraqi play (Dream in Baghdad) and the researcher sought to study this problem and divided it into four chapters dealt with in the first chapter the problem of research and its need, the importance of research, As well as the definition of terminology, either Chapter II theoretical framework divided by the researcher to the first two is the postmodernism in the theater is the most prominent reference references and the second most important postmodern applications in the world play and then the researcher concluded the second chapter of the most important indicators. In the third chapter, the researcher identified th

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Publication Date
Sun Mar 01 2009
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Importance of the Corporate of Governances to the Activate the Quality and Integrity of Financial Reports
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The study aims at showing the Importance of the Corporate of Governances to the Activate the quality and integrity of financial reports prepared inside the companies through explaining what they should be obliged to in writing the reports and financial and nonfinancial statements according to the international standards of accounting to be transparent and integral. It also aims at giving the independence that the auditors should enjoy through connecting them to an Auditing Commissions to submit additional services in addition to assessing the instrument of control to evaluate risks, give consultations and the services related to the governance and independence of Supervising Council.         &

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