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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
Thu Feb 12 2026
Journal Name
Al–bahith Al–a'alami
The contents of the opening article of electronic newspaper (Al-Nabaa): (Analytical study of duration 2015 for 2018)
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The study aimed to identify what (isis) (Daesh) have been touched in the opening article of Al-Nabaa newspaper

This objective is organized for asset of sub-targets it is the knowledge of media discourse and for those who are directed and methods of employing the strong content debt organization and we used the survay method to monitor and understand the content of opening anticale and the researcher took the numbers of the newspaper for years 2015-2018 consist of 157

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Publication Date
Fri Dec 01 2023
Journal Name
Iop Conference Series: Earth And Environmental Science
Effect of Vertical Boom Position of the Greenhouse Sprayer on the Penetration of Spray to the Eggplants Canopy
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Abstract<p>The research objective focuses on spraying the leaves of the plant from the top and bottom through a spraying machine designed and made of aluminum with a movable arm equipped with a nozzle holder divided into three parts and each piece contains a nozzle of the type (Flat Fan 120-C3) as the machine was tried in a greenhouse with a study of the effect of changing the positions of the upper and lower piece of the tube carrying the nozzles to four levels (A1, A2, A3, A4) and the effect of pressure change on two levels (2,4) bar and studying the effect of the previous factors on some of the characteristics of the study, Spray quality on adaxial of leaf, Spray quality on the abaxial surfac</p> ... Show More
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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Effect of Some Herbs on the Level of Some Biochemical Parameters in Blood of Diabetic Patients Type II
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This study included effect of polyherbs mixture treatment of diabetic patients type II for two months. The polyherbs mixture contains Nigella sativa seeds, Boswellia carterri gum, Citrus aurantifolia fruits, Elettaria cardamomum fruits. Also this study included estimation of some biochemical parameters in the serum Diabetes Mellitus (D.M.) patients-type II and knowing the relationship of these parameters with this disease. The parameters are glucose, cholesterol ,High density , Low density lipoproteins( HDL-C, LDL-C) respectively , Triglycerides TG, urea, total protein , albumin , Alkaline phosphatase ALP,Transaminase GOT, GPT enzymes . Take (77) samples of diabetic patients serum type II which included (47) samples for group one: herbs

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Publication Date
Thu Dec 14 2023
Journal Name
4th International Conference Of Modern Technologies In Agricultural Sciences
A study of the Effect of Diesel Oil Contamination with Glycol on the Performance of a Diesel Engine
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The performance of a diesel engine was tested with diesel oil contaminated with glycol at the engineering workshop/Department of Agricultural Machines and Equipment / College of the Agricultural Engineering Sciences at the University of Baghdad. To investigate the impact of different concentrations of glycol on the performance of a diesel engine, an experimental water-cooled four-stroke motor was utilized, with oil containing 0, 100, and 200 parts per million (ppm). Specific fuel consumption, thermal efficiency, friction power, and exhaust gas temperature were examined as performance indicators. To compare the significance of the treatments, the study employed a full randomization design (CRD), with three replicates for each treatment at th

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Publication Date
Fri Dec 01 2023
Journal Name
Case Studies In Construction Materials
Experimental and environmental investigations of the impacts of wood sawdust on the performance of reinforced concrete composite beams
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Publication Date
Mon Jun 01 2015
Journal Name
Journal Of Economics And Administrative Sciences
independence of the central banks with a focus on measuring the independence of the central bank of Jordan
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The main topic of this study is central around the independence of Jordanian central bank and the extent of the effectiveness at the bank in leading the monetary policy without interferences or pressures from side of the government.  the degree of independence of Jordanian central bank was  based on the following based hypothesis following ,there is relationship between the independence of the central bank and the legislative and economical indices. the most important recommendations are degree of independence of the Jordan central bank 43.5% is a good one, but it possible to reach a higher degree than this one by to making some modification on the Jordanian central bank law and by the central bank should be more rigid

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Publication Date
Thu Feb 16 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of Antileishmanial Activity of Osteospermum ecklonis Extract of Aerial Parts against Leishmania donovani: in vitro(Conference Paper) #
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Abstract

 

Lack of safe available non-resistant treatment for visceral leishmaniasis (Kala-azar) keeps limiting the complete cure of this disease ,drugs that have  toxic side effects or lack of effectiveness  have led to disease relapse ,all these factors have lightened  the way to the search for imperative drugs from natural resources that have been shown to have antileishmanial activity through literature survey

. In the present study, the comparative in vitro anti-leishmania activity of various fractions of Osteospermum ecklonis aerial parts fractions have been evaluated. Extracts were prepared through maceration and Soxhlet apparatus using 85% meth

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Publication Date
Thu Jul 23 2020
Journal Name
مجلة العلوم النفسية
Influence of Model of Active Thinking in Achievement of Eighth Grade Students and their Visual Thinking in Science
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The aim of this study is to recognize the influence of model of active thinking in achievement ofeighth grade students andtheir visual thinking in science.The finds of this research show the superiority students of the experimental group who studied the science material by using the active thinking model on the students of the control group who studied by usual method, in the achievement test. Also the finds show that the students of the experimental group are more successful than students of control group in the test of visual thinking, so the two null hypotheses have been rejected. In light of the results of the research, numbers of recommendations were made.

Publication Date
Thu Feb 12 2026
Journal Name
Revista Iberoamericana De Psicología Del Ejercicio Y El Deporte, Issn 1886-8576, Vol. 17, Nº. 6, 2022, Págs. 416-418
The Effect Of Katsu Exercises On Some Abilities Of Strength And Achievement Of Advanced Weight Lifters, Baghdad Clubs
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Autorías: Ghassan Adeeb Abdulhasan, Talib Faisal Shnawa, Yasir Wajih Qaddoori. Localización: Revista iberoamericana de psicología del ejercicio y el deporte. Nº. 6, 2022. Artículo de Revista en Dialnet.

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Scopus
Publication Date
Wed Sep 30 2015
Journal Name
Modern Sport
The administrative skills of the leaders of the faculties of sports education and their relations with administrative reform
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The research consists of five chapters and aims to explore the administrative skills of leaders in physical education colleges and their relationship with administrative reform. The study sample included (deans, vice deans, and heads of departments) from physical education colleges for the academic year 2012-2013, with a total of 61 individuals. They were selected using the purposive sampling method, and the researcher distributed questionnaires to them, collecting 60 valid responses and excluding one due to its invalidity. After defining the concepts of administrative skills and administrative reform and redownloading relevant literature and previous studies, as well as consulting with a group of experts in management and psychology, the r

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