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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 Dec 21 2021
Journal Name
International Journal Of Design & Nature And Ecodynamics
Environmental Influences on the Settlements Patterns of Communities in the Marshes of Iraq
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In the field of residential community planning, one of the appropriate places to study the mutual influences between man and the environment, away from the influences, concepts and mechanisms of contemporary planning theories are isolated environments in rural areas, and the marshlands in Iraq represent one of these models. These areas still retain the planning patterns of residential communities for thousands of years. This research attempts to conduct a descriptive study of traditional settlement patterns, which relied on the capabilities of the surrounding areas to provide planning and architectural solutions based on the environmental factor. Establishing such a clear framework for these impacts can help in any future interventi

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Publication Date
Thu Sep 01 2016
Journal Name
Journal Of Engineering | University Of Baghdad
Correction Factor for Methods of Installation of Piles Group in Sandy Iraqi Soils
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Many problems are facing the installation of piles group in laboratory testing and the errors in results of load and settlement are measured experimentally may be happened due to select inadequate method of installation of piles group. There are three main methods of installation in-flight, pre-jacking and hammering methods. In order to find the correction factor between these methods the laboratory model tests were conducted on small-scale models. The parameters studied were the methods of installation (in-flight, pre-jacking and hammering method), the number of piles and in sandy soil in loose state. The results of experimental work show that the increase in the number of piles value led to increase in load carrying capacity of piled raft

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Publication Date
Tue Mar 15 2022
Journal Name
Journal Of Baghdad College Of Dentistry
The effect of age on the clinicopathological features of oral squamous cell carcinoma
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Background: Squamous cell carcinoma is a disease of elderly peopleand it is uncommon in people with less than 40 years old; however many literatures revealed that tumor developing in patients younger than forty years appears more aggressive at the time of diagnosis. The purpose of the present study was to focus on the clincopathological features of the oral SCC in different age groups. Material and methods: In this study thirty five cases of paraffin embedded tissue blocks of oral squamous cell carcinoma were studied. The age range was from 16 to 80 years. The clinicopathological data were recorded for evaluating the tumor characters according to age of patients. Results : The age was not significantly correlated to the clinicopathological

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Publication Date
Tue Feb 17 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Soft tissue facial profile analysis of adult Iraqis with different classes of malocclusion
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Background: Complete analysis of facial profile should also include an evaluation of soft tissue morphology. Materials and Method:The sample consisted of 90 Iraqi adults (45 males and 45 females) aged 18-25 years from Baghdad city divided into 3 groups according to the ANB angle with 30 subjects in each group (15 males and 15 females) for class I, II and III. Lateral cephalometric radiograph was taken for each subject and 8 angular and 5 linear measurements were identified and determined, t-test, ANOVA and LSD test were used to compare between both genders and between different classes. Results:Showed that females had greater angular measurements and smaller linear measurements with more lip prominence than males in all classes, there was m

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Publication Date
Tue Jul 23 2013
Journal Name
Arabian Journal Of Geosciences
Morphodynamics, landform development and origin of the Ga’ara depression, Western Desert of Iraq
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This work deals with the study of the morphodynamics, history of development of landforms and the origin of the Ga’ara depression. The depression is a suboval erosional topographic feature extending in E-Wdirection and located about 50 km north of Rutba Town, at the Western Desert of Iraq. The area is characterized by fresh and clean surfaces, scarcity of vegetation, abundance of rills, intense drainage and immature soil. These clues indicate that the erosion in the study area is effective. Four types of erosion features are recognized in this area namely sheet, rill, badland and wind erosion. The extent of the wind erosion depends on its position in relation to the prevailing wind direction. Water, wind and gravity are the main agents of

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Publication Date
Sun Jun 25 2017
Journal Name
Biomedical And Pharmacology Journal
The Impact of Toxoplasma gondii on Mitochondrial DNA of Sub-fertile Men Sperms
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Toxoplasmosis is the most common, widespread disease in the world which is caused by Toxoplasma gondii.The objective of the current study is to determine the effect of the Toxoplasma gondii infection on male sperm, especially on the mitochondria of sperm for men who suffer infertility and the possibility of a hereditary mutation. Sixty seminal fluid and serum samples were taken from sub- fertile patients who attended Teba center for in vitro fertilization / Babylon and similarly samples were also obtained from healthy individuals as a control group, their ages ranged from 20 to 60 years old during the period from 1st may /2016 till 25th January/2017. All samples subjected to the tests included Macroscopic and microscopic examination, molecu

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Publication Date
Wed Jan 01 2020
Journal Name
Plant Archives
Study of bacterial contamination of defected eggshells and egg contents in Baghdad city
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The main aim of the current research is to focus the light on some bacterial contamination on cracked eggshell and egg content plus studying the sensitivity of these bacterial isolates to antibiotics. For this purpose, a total of 50 eggs were collected from the markets in Baghdad city (Iraq) and examined for bacterial isolation from cracked eggshells and from the egg contents. The bacterial isolates were cultured and purified then transferred to a specific media to study its sensitivity against antibiotics. The results revealed that bacteria isolated from both cracked eggshells (46%) and egg contents (44%). The bacteria isolated include E. coli, Staphylococcus, Enterococcus faecalis, Enterobacter and Pseudomonas. The results of antibiotic s

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Preparation and Characterization of Bimetallic Catalyst (NiO – CoO) for Desulfurization of Gas Oil
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In this study NiO - CoO bimetallic catalysts are prepared with two Ni/Co ratios (70:30 and 80: 20) using the precipitation method of nitrate salts. The effects of Ni /Co ratio and preparation methods on the catalyst are analyzed by using different characterization techniques, i.e. atomic absorption (AA) , XRD, surface area and pore volume measurements according to the BET method . The results indicate that the best catalyst is the one containing the percentage of Ni :Co ( 70 : 30 ). Experiments indicate that the optimal conditions to prepare catalyst are stirring for three hours at a temperature of 60oC of the preparation , pH= (8-9) , calcination temperature at 400oC for two hours

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Publication Date
Sun Mar 20 2016
Journal Name
Al-academy
Aesthetical Utilization of Sound in film of Alfred Hitchcock: حكمت مطشر مجيد البيضاني
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This research deals with the nature of the aesthetic employment of wool in the Alfred Hitchcock films, as this director is characterized by rich his experience that dealt with the photo film days of silent film and managed efficiently in the construction of his films, as well as when the audio input The Hitchhiker employ sound aesthetic ways still emulated so far. So I rely researcher this subject and the division of research into four chapters, such as the first quarter included the methodological framework which dealt with the problem of research and the importance of research, and the goals of the research, as well as the limits of research and finally determine the terms.The second chapter includes theoretical framework and previous

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Publication Date
Sat Sep 01 2018
Journal Name
Water Resources
Carcinogenic Risk Assessment of Trihalomethanes in Major Drinking Water Sources of Baghdad City
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