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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 01 2024
Journal Name
Baghdad Science Journal
Molecular study of the relationship of gene expression of some genes with the temperature variation of bacterial growth
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Pseudomonas aeruginosa is an opportunistic pathogen responsible for serious infections. At least three different exopolysaccharides, alginate, polysaccharide synthesis locus (Psl), and pellicle exopolysaccharide (Pel) make up the biofilm matrix in P. aeruginosa . The effect of temperature on the biofilm formation and gene expression was examined by microtiter plate and real-time quantitative polymerase chain reaction (qRT-PCR). To be able to determine the effect of temperature on biofilm formation and gene expression of P. aeruginosa, 303 clinical and environmental samples were collected. Pseudomonas aeruginosa was isolated from 61 (20.1%) and 48 (15.8%) of the clinical and e

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Publication Date
Mon Mar 15 2021
Journal Name
Journal Of Baghdad College Of Dentistry
Efficacy of arthrocentesis with injection of hyaluronic acid in the treatment of inflammatory-degenerative disease of temporomandibular joint
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Background:Temporomandibular joint (TMJ) problems refer to a group of heterogeneous pain and dysfunction conditions involving the mastication, reducing life quality of the patients. Arthrocentesis is a simple and less invasive surgical method for the treatment of inflammatory-degenerative disease than other conservative procedures and better than arthroscope. This clinical study aimed at evaluating the benefit of arthrocentesis with injection of hyaluronic acid in the management of inflammatory-degenerative disease of the TMJ. Material and methods: Eighty consecutive patients were enrolled in this study with pain symptoms of TMJ, insufficient masticatory efficiency during function and limitation of mouth opening; they were assessed with

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Publication Date
Tue Jun 21 2022
Journal Name
Journal Of Planner And Development
Evaluation of some indicators of urbanization in the city of al-Qaim in the Iraqi province of Anbar
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Urban Balance is one of the important indicators that leads to an assessment of the urbanization process in a particular country  , province or even a city that is multi-centered. By examining  the data related to Anba  province, it was found that the value of this indicator is equal to 0.96, which is less than the absolute one, and therefore the urbanization in the province is distributed collectively  

The development of a mathematical or statistical model for estimating urban growth is a complex process due to the overlap between indicators or variables that can be adopted to calculate estimate growth rates Al-Qaim city has been considered as an example to develop a statistical method by which changes

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Publication Date
Mon Apr 04 2022
Journal Name
Journal Of Educational And Psychological Researches
The Degree of Availability of the Dimensions of Organizational Immunity Systems t the University of Tabuk in KSA from the Perspectives of Academic Leaders
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This study aims to investigate the academic leaders’ perceptions towards the degree of availability of the dimensions of organizational immunity systems at the University of Tabuk, as well as to reveal the statistically significant differences between the average responses of the study sample members about the degree of availability of these dimensions at their university due to the variables of (gender, leadership position, and college specialization). To achieve the objectives of the study, a descriptive survey method was used. The study population consisted of (200) male and female leaders who were academic leaders at the University of Tabuk. A questionnaire was used as a tool for collecting data, which its validity and reliability

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Publication Date
Mon Jan 02 2017
Journal Name
Journal Of Educational And Psychological Researches
Difficulties in the application of modern trends in physics in middle schools of the province of Baghdad, from the perspective of teachers of physics
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     The goal of current research is to identify the difficulties in the application of modern physics in the middle schools of the province of Baghdad schools from the perspective of teachers of physics trends, sample search of (127) teachers, Karkh Third Directorate, and use Researcher questionnaire data collection tool after applying it to teachers who have experience (5) years and more after confirmation of the validity and reliability of the scale (the tool) researcher has used the averages for the purpose of interpreting the results. the results showed that the difficulties have been in the order following: (difficulties related educational environment of modern trends of teaching, curriculum-related dif

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Publication Date
Sun Apr 01 2018
Journal Name
Al–bahith Al–a'alami
The propaganda content of the elements of expression in the face of the promotion of terrorist thought: (Military information of the popular crowd model)
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The propaganda war is one of the most dangerous weapons used in various conditions of war and peace within any intellectual, political or military conflict to be targeted by multiple social groups and their effects on the intellectuals to change the viewpoints at the local and global level, including the use of technical treatment of the audio and visual medium, The impact of the psychological dimensions of the arms in the confrontation and spread terror in the ranks of the enemies and in the forefront of what Iraq faces in its battle against the And the use of it as a propaganda content contributes to the development of the spirit of tranquility and tranquility in the hearts of Iraqis and the return of the right to the owners “th

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Publication Date
Mon Dec 31 2018
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
ESTIMATION OF LEAD ELEMENT IN THE BLOOD OF TRAFFIC POLICE IN THE CITY OF BAGHDAD.: ESTIMATION OF LEAD ELEMENT IN THE BLOOD OF TRAFFIC POLICE IN THE CITY OF BAGHDAD.
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The current study aimed to determine the relation between the lead levels in the blood traffic men and the nature of their traffic work in Baghdad governorate. Blood samples were collected from 10 traffic men and the age about from 20-39 year from Directorate of Traffic Al Rusafa/ Baghdad and 10 samples another control from traffic men too with age 30-49 year and they livedrelatively in the clear cities or contained of Very few traffic areas. The levels of lead in blood estimated by used Atomic Absorption Spectrometry.
The result stated that there is no rising of the levels of lead in blood of traffic men Lead concentration was with more a range from 14 ppm in Traffic police are not healthy They are within the permissible limits, Ap

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Publication Date
Thu Jun 30 2022
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
STUDY OF YIELD AND ITS COMPONENTS OF INTRODUCED VARIETIES OF MAIZE UNDER DIFFERENT PLANTING DENSITIES: STUDY OF YIELD AND ITS COMPONENTS OF INTRODUCED VARIETIES OF MAIZE UNDER DIFFERENT PLANTING DENSITIES
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In order to evaluate the performance of introduced varieties of maize and test them under different levels of plant density, and to determine which of the introduced varieties give a high yield and at what plant density, a field experiment was carried out at Station A in the Department of Field Crops- College of Agricultural Engineering Sciences - University of Baghdad- Jadiriyah, for the fall season 2021, the RCBD design was used with four replications, in a split plot arrangement, the three plant densities (50.000, 70.000, and 90.000 Plant s ha-1) were the main plates, while the varieties represented the secondary factor, which is six varieties of maize, class 2 = 5783 DKC, Class 3 = 6315 DKC, Class 4= 6590 DKC, whic

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Publication Date
Wed Nov 12 2025
Journal Name
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The Role of Media Coverage of the Iraqi Satellite Channels in Shaping Public Attitudes towards Terrorism (a Field Study of a Sample of an Audience of the City of Baghdad)
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Violence is one of the most serious threats facing societies because it affects their internal structure and threatens the security and stability of society. It is classified as one of the types of security crises that are emerging in Arab and Islamic societies in particular, and in most countries of the world in general.

The threat of this crisis is increasing. Terrorism is considered as one of the most serious aspects of that all the countries of the world, currently, suffer from. The terrorism has begun to penetrate deep into society in one way or another starting from the Second World War, which led to the emergence of leftist movements in Western Europe, Japan, France, Italy and other countries as a result of emerging ideas

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Publication Date
Sat Sep 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Reflection of knowledge workers characteristics on knowledge acquision “Survey Study of the views of a sample of engineers and technicians in the Directorate of Electricity In the city of Sulaymaniyah
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Purpose: The research aims to diagnose the current availability of knowledge workers characteristics and the role of these characteristics in knowledge acquision in the city of Sulaimaniya Directorate of Electricity, and to identify the differences between personal and occupational characteristics of a sample of research and its impact on the availability of such properties.

Design/methodology/approach :to achieve the objectives of the research questionnaire was developed especially for it and then distributed to a sample of engineers and technicians working in the Directorate of Electricity city of Sulaimaniya, where the sample of the research (52) respondents.

Findings:  the most important conclusions reached

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