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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
Tue Feb 01 2022
Journal Name
Baghdad Science Journal
Effect of the Concentration of Copper on the Properties of Copper Sulfide Nanostructure
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Nanoparticles of copper sulfide have been prepared by simple reaction between using copper nitrate with different concentrations ratio 0.1, 0.3, and 0.5 mM, thiourea by a simple chemical route. The prepared Nano powders have been deposited onto glass substrates by casting method at 60°C. The structure of the product Nano- films has been studied by x-ray diffraction, where the patterns showed that all the samples have a hexagonal structure of covellite copper sulfide with the average crystalline sizes 14.07- 16.51 nm. The morphology has been examined by atomic force microscopy, and field emission scan electron microscopy. The AFM images showed particles with almost spherical and rod shapes with average diameter sizes of 49.11- 90.64 nm.

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Publication Date
Fri Jan 01 2021
Journal Name
Prepodavatel Xxi Vek
The Structure of Russian Participles: Special Features of the Grammar Meaning of State
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Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
EFFECT OF SIX HATS IN THE DEVELOPMENT OF LANGUAGE SKILLS OF KINDERGARTEN CHILDREN
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Increasing need for day after day to find ways and innovative means of
helping to educate and give children the skills of different kind, has found a
researcher on the subject of hats, six room to give children language skills
through the experience of field reconnaissance conducted on the three
children found that language skills improved, he decided to make these study.
Objectives of the study:
Understand the differences between the experimental group first (the way the
debate) and second (six caps) depending on the test post administration.
to identify the language skills of the second group according to the pre and
post test
Differences between males and females in the second group (Six Hats)
Search T

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Publication Date
Fri Jan 17 2025
Journal Name
Opera Medica Et Physiologica
ASSESSMENT OF THE HARMFUL EFFECT OF DUPROST DRUG ON TESTES OF ALBINO MICE
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Publication Date
Sun Apr 02 2017
Journal Name
Journal Of Educational And Psychological Researches
Standraidization of Post traumatic Stress Disorder Scale on Students of University of Baghdad
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There are a lot of measures for Post Traumatic Stress Disorder (PTSD), but what distinguishes it from other measures is the number of short paragraphs and concise depending on the classification of American Psychiatric Association (APA), which can be applied by the researchers on a large number, Because the Iraqi society suffered from psychological trauma due to wars, conflicts and occupation and the resulting psychological disorders of the members of Iraqi society, especially post-traumatic stress disorder, as mentioned by many studies and researches.

Therefore, the aim of this study was to standardize the PTSD scale for students at Baghdad University. For the Psychologist Fua . E. which was applied in many foreign studies. 

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Publication Date
Sun Mar 04 2018
Journal Name
Baghdad Science Journal
Optical, Structural and Electrical Properties of Electrochemical Synthesis of Thin Film of Polyaniline
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Polyaniline membranes of aniline were produced using an electrochemical method in a cell consisting of two poles. The effect of the vaccination was observed on the color of membranes of polyaniline, where analysis as of blue to olive green paints. The sanction of PANI was done by FT-IR and Raman techniques. The crystallinity of the models was studied by X-ray diffraction technique. The different electronic transitions of the PANI were determined by UV-VIS spectroscopy. The electrical conductivity of the manufactured samples was measured by using the four-probe technique at room temperature. Morphological studies have been determined by Atomic force microscopy (AFM). The structural studies have been measured by (SEM).

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Publication Date
Sun Jun 05 2011
Journal Name
Baghdad Science Journal
The study of antibacterial activity of some plant extracts against causes of pneumonia
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Eighty five samples were taken from patients suffering from pneumonia. Seventy-eight isolates were diagnosed as following: Staphylococcus aureus (23), klebsiella pneumoniae (29), Streptococcus pneumoniae (15), Serratia sp. (4), Haemophilus influenzae (4) and Pseudomonas aeruginosa (3). The clinical isolates were tested for antibiotics sensitivity. They appeared highly resistance to penicillin G and Ampicillin at percentage 89.7 and 84.6% respectly while the results showed highly sensitivity to streptomycin at percentege of (12.8%). To study the antibacterial activity of Alium sativum, Eucalyptus microtheca leaves and Cydonia oblonga seeds extracts, five multi resistant strains were used by using agar well diffusion and disk methods at c

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Publication Date
Tue Jan 01 2013
Journal Name
Journal Of Genetic And Environmental Resources Conservation
The study of food preference of Callosobruchus maculatus to five types of fabaceae
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Publication Date
Tue Feb 01 2022
Journal Name
Baghdad Science Journal
Effect of the Concentration of Copper on the Properties of Copper Sulfide Nanostructure
...Show More Authors

Nanoparticles of copper sulfide have been prepared by simple reaction between using copper nitrate with different concentrations ratio 0.1, 0.3, and 0.5 mM, thiourea by a simple chemical route. The prepared Nano powders have been deposited onto glass substrates by casting method at 60°C. The structure of the product Nano- films has been studied by x-ray diffraction, where the patterns showed that all the samples have a hexagonal structure of covellite copper sulfide with the average crystalline sizes 14.07- 16.51 nm. The morphology has been examined by atomic force microscopy, and field emission scan electron microscopy. The AFM images showed particles with almost spherical and rod shapes with average diameter sizes of 49.11- 90.64

... Show More
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Crossref (2)
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Publication Date
Thu Jan 01 2015
Journal Name
International Journal Of Astronomy And Astrophysics
Determination of Velocity and Radius of Supernova Remnant after 1000 yrs of Explosion
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Supernova explosions are described as very violent events which transfer a significant amount of energy to interstellar media and are responsible for a large variety of physical processes. This study does not discuss the actual explosion mechanisms but follows the behavior of the dynamical evolution of some selected type I and type II supernova remnant and particularly after a thousand years from their explosion and shows how the density of the medium affects the evolution and the lifetime of each remnant. By studying such behaviors, a simplified model has been proposed here for the velocity and radius of the remnant after thousand years of explosion that depends only on the density of the medium and age of the remnant. It has been found th

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