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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
Sat Oct 01 2016
Journal Name
World Journal Of Pharmaceutical Research
EFFECT OF LEVETIRACETAM ON THE CEREBRAL CORTEX OF NEWBORN RAT
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Background: Levetiracetam is a member of the new antiepileptic drugs and has a broad spectrum effect, used as an adjunctive therapy in addition to monotherapy in the treatment of partial onset-seizures. The effect of levetiracetam on the development of embryo nervous system after maternal exposure during pregnancy has not been identified. Objective: to evaluate the effect of antiepileptic drug, levetiracetam (LEV) within its therapeutic dose 350mg/Kg body weight on albino female rat to clarify its effect on the developing cerebral cortex histologically. Material And Methods: Ten pregnant female rats were separated into two groups, control group and experimental group. They were obtained from the animal house of the high institute of inferti

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Publication Date
Mon Feb 09 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Immunohistochemical study of PDGF, IGF of radiated tooth rat embryo
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Background: Oral health is important to the quality of life of all individuals. Oral lesions can cause discomfort or pain that interferes with mastication, swallowing, and speech. Oral disease is a health problem that is not only a matter of oral hygiene and local condition, but can also be a precursor to other dangerous and potentially life threatening illnesses. The present study was designed to analyze the main clinicopathological aspects of most common oral lesions in patients who visit the Oral Diagnosis Clinic of the College of Dentistry, University of Sulaimani, Kurdistan region, Iraq. Patients and methods: This prospective study was performed on 3144 patients from July 2009-July 2010. In this study a total of 3144 patients were e

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
study Of Optical Properties Of Copper-Doped Cds Thin Films
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Thin films of CdS:Cu were deposited onto glass substrate temperature 400 °c. The optieal properties have been studied for Cds doped with (1,3, 8) wt% of Cu before and after Gamma irradiation. It was found that the irradiation caused an ( Frenkel defects) where the atom is displaced from its original site leaving vacancy and forming on interstitial atom. It was found the irradiation caused an absorption edge shifting towards long wavelength as a result of the increasing of Cu concentration.

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Publication Date
Wed Feb 29 2012
Journal Name
Al-khwarizmi Engineering Journal
Effect of Construction Joints on Performance of Reinforced Concrete Beams
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Construction joints are stopping places in the process of placing concrete, and they are required because in many structures it is impractical to place concrete in one continuous operation. The amount of concrete that can be placed at one time is governed by the batching and mixing capacity and by the strength of the formwork. A good construction joint should provide adequate flexural and shear continuity through the interface.

In this study, the effect of location of construction joints on the performance of reinforced concrete structural elements is experimentally investigated.

Nineteen beam specimens with dimensions of 200×200×950 mm were tested. The variables investigated are the location of the construction joints

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Publication Date
Mon Feb 09 2026
Journal Name
Al–bahith Al–a'alami
Radio Republic of Iraq and Awareness Promoting of Minorities’ Rights
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Proposals to raise awareness of the rights of minorities and secure their freedoms have begun to receive attention Internationally. It is escalated, especially after the increasing impact of wars and conflicts on these situations Minorities, and UNESCO stresses the need to take over information and communication policies Greater attention to protect minority rights.

Hence the importance of our research, the problem of which lies in the main question: (What is the role Radio Republic of Iraq has played in promoting awareness of minority rights at the level : Public and  Social?) . As one of the Iraqi media networks , laws oblige them to pay attention to the rights of minorities and to spread a culture of pluralism , diversity

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Publication Date
Sun Dec 30 2012
Journal Name
College Of Islamic Sciences
The importance of logic in the study of Islamic sciences
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Logic is one of the sciences that have receded and regressed in the field of Islamic sciences. This regression is the result of several factors, the most important of which are:

1- The Aristotelian logic, concerned with the seemingly essential shape and the underlying truth in the text, which has been translated into Arabic, is no longer able to keep pace with scientific revelations and epistemological spaces of our time.
2- The existence of logic in the curricula of Islamic studies was not subject to a study linking logic and Islamic sciences. Therefore, we find that the student studies logic as if it were a strange subject that has nothing to do with the subjects of Islamic studies and even Islamic philosophy.
3- Logic is

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Publication Date
Sun Jan 08 2023
Journal Name
Journal Of Planner And Development
Analysis of Walking Accessibility of Community Park in Duhok City
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Research studies show that urban green spaces promote physical activity, the health of urban residents, and psychological well-being. Taking the community park in Duhok city as the research object, the spatial service area in terms of accessibility of to the Community Park under the mode of pedestrian transportation is analyzed by using the network analysis service area function of the geographic information system (GIS). The results show that under the walking mode in the research area, Parks are concentrated in the north and south of the city, but community parks are few in disadvantaged neighborhoods. In addition, there is a significant disparity between the number of community parks and the number of communities. Only 11 communities

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Publication Date
Mon Jun 30 2003
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Study of the Drying of Ethanol using Zeolite Molecular Sieves
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Publication Date
Wed Sep 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
Influence of Temperature on Mechanical Properties of Asphalt Concrete Mixture
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Asphalt binder is a thermoplastic material that conducts as an elastic solid at lower service temperatures or throughout fast loading rate. At a high temperature or slow rate of loading, asphalt binder conducts as a different liquid. The classical duplication generates a required to assess the mechanical properties of asphalt concrete at the anticipated service temperature to reduce the stress cracking, which happens at lower temperatures, fatigue, and the plastic deformation at higher temperatures (rutting). In this study, an achievement was made to assess the effect of temperature on the mechanical characteristics of asphalt concrete mixes. A total of 132 asphalt concrete samples were attended utilizing two asphalt cement grades (40-50) a

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Publication Date
Sat Dec 11 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Study of Microbial Contamination of Some Commercial Contact Lens Solutions
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Sixty samples of commercially available contact lens solutions were collected from students at the Pharmacy College/Baghdad University. The types of lenses used varied from medical to cosmetic. They were cultured to diagnose any microbial contamination within the solutions. Both used and unused solutions were subject for culturing. Thirty six (60%) used samples showed bacterial growth, fungal growth was absent. Pseudomonas aeruginosa accounts for the highest number of isolates (25%) followed by E. coli (21%), Staphylococcus epidermidis (6.6%), Pseudomonas fluorescence (5%) and Proteus mirabilis (1.6%) respectively. Only one (1) unused (sealed) sample showed growth of P. fluorescence.

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