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bijps-706
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
Mon Feb 21 2022
Journal Name
Frontiers In Immunology
The Ability of Resveratrol to Attenuate Ovalbumin-Mediated Allergic Asthma Is Associated With Changes in Microbiota Involving the Gut-Lung Axis, Enhanced Barrier Function and Decreased Inflammation in the Lungs
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Asthma is a chronic respiratory disease highly prevalent worldwide. Recent studies have suggested a role for microbiome-associated gut–lung axis in asthma development. In the current study, we investigated if Resveratrol (RES), a plant-based polyphenol, can attenuate ovalbumin (OVA)-induced murine allergic asthma, and if so, the role of microbiome in the gut–lung axis in this process. We found that RES attenuated allergic asthma with significant improvements in pulmonary functions in OVA-exposed mice when tested using plethysmography for frequency (F), mean volume (MV), specific airway resistance (sRaw), and delay time(dT). RES treatment also suppressed inflammatory cytokines in the lungs. RES modulated lung microbiota and cause

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Publication Date
Thu Jan 06 2022
Journal Name
Iraqi National Journal Of Nursing Specialties
Effectiveness of an Educational Program on Mothers’ Attitudes toward Readiness for Discharge Care at Home for a Premature Baby in Intensive Care Unit at Teaching Hospitals in Medical City Complex
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Objectives:
To evaluate mothers’ attitudes toward readiness for discharge care at home for a premature baby in Intensive Care Unit at teaching hospitals in Medical City Complex and to find out the relationship between mothers’ attitudes and their socio-demographic characteristics.
Methodology: A quasi-experimental study design was carried out through the period of 6th January 2020 to 2021 to 11th March 2021, to evaluate mother’s attitude toward discharge care plan for premature babies. The study carried out in Welfare Teaching Hospital, Nursing Home Hospital and Baghdad Teaching Hospital at Medical City Complex in Baghdad City on 30 mother of premature babies in neonatal intensive care units using the nonprobability sampling

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Publication Date
Fri Jun 01 2018
Journal Name
Journal Of The College Of Languages (jcl)
L’imaginaire de l’épidémie dans La Peste d’Albert Camus et Le Choléra de Nazik al-Malaika The Imagination of Epidemic in Alber Kamo's Novel " Plague" and Nazik Al-Malaekah's poem "Cholera"
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The present study deals with the story of Epidemic in two literary works issued in the same year (1947). One of them is a novel titled "Plague" written by the French writer Alber Kamo, the second is a poem of the Iraqi poetess Nazik Al-Malaekah. The research reflects a contrastive study of the war vision in the two works as both writers used science to serve literature by using Epidemic as a metaphor to refer to the dangers that the societies faced.

The problem of the present research lies in answering the question about the reason that makes the two writers use metaphor while narrating the issues of the society instead of mentioning them directly and illuminate what implications do the narrative style of Epidemic story have and

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Publication Date
Sun Dec 27 2020
Journal Name
Journal Of The College Of Education For Women
Using the Image in Teaching Arabic Language Vocabulary to Non-Native Speakers: The Experience of the Arabic Language Institute - King Abdul-Aziz University - as a Model: آمال موسى عباس الإمام
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The study aims to demonstrate the importance of instructional methods in teaching Arabic language as a second language or teaching the Arabic language to non-native speakers. The study is in line with the tremendous development in the field of knowledge, especially in the field of technology and communication, and the emergence of many electronic media in education in general and language teaching in particular. It employs an image in teaching vocabulary and presenting the experience of the Arabic Language Institute for Non-Speakers-King Abdul-Aziz University. The study follows the descriptive approach to solve the problem represented by the lack of interest in the educational methods when teaching Arabic as a second language. Accordingl

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Publication Date
Wed Jun 07 2023
Journal Name
Journal Of Educational And Psychological Researches
The Feeling of Job Alienation and Its Relationship to Organizational Commitment among Free Lecturers in Secondary Schools: Imam Al-Kadhum College (peace be upon him ( Kindergarten and Special Education Department
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The current study aims to identify the feeling of job alienation and organizational commitment among free lecturers in secondary schools, as well as to identify the significance of the differences in the feeling of job alienation according to the gender and the significance of the differences in organizational commitment according to the gender. It also aims to identify the correlation between the feeling of job alienation and organizational commitment. To achieve the objectives of the research, the researcher developed two scales: one consisted of (24) items to measure the vacancy in job alienation and the other consisted of (24) items to measure the organizational commitment. The two tools were applied to a sample of (200) male and fem

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Publication Date
Wed May 10 2017
Journal Name
Journal Of The College Of Languages (jcl)
PROBLÉMATIQUE DE L’ENSEIGNEMENT DE LA TRADUCTION ET PROLÈMES DE SON APPRENTISSAGE DANS UNE CLASSE DE LANGUE The problem in teaching Translation and problems of its learning in a language lesson
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Le présent travail aborde la question de l’enseignement de traduction en tant que matière faisant partie du programme élaboré dans des Départements de Français au sein de certaines universités irakiennes, en particulier celle de Bagdad. La méthode d’enseigner suivie constitue une véritable problématique qu’on a bien diagnostiquée à partir de quelques années d’expériences, à la lumière des observations faites dans des cours de traduction professionnelle, et dans la perspective des citations et témoignages établies par des traductologues et pédagogues et principalement par Marianne LEDERER qui a établi la Théorie Interprétative de la traduction. Mais pourquoi l’enseignement lui-même poserait une telle probl

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Publication Date
Wed Jan 29 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Marketing mix and its role in promoting the status of insurance companies in the customers mind: Exploratory comparative research between the Iraq public insurance company and the private insurance company
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The ability of insurance companies to achieve goals depends on their ability to meet customers' requirements, and this requires them to identify target markets and respond to needs and wishes of the markets, the skill is to convince the company to operate what is in the interest of the customer if he is convinced the customer service provided to him, he would repeat to deal with, and where the cost of maintaining existing customers is less than the cost of attracting new customers, the insurance companies that is working hard to maintain their customers, the more customer satisfaction with the services provided has increased loyalty and weakened the ability of competitors lured.

       &nbs

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Publication Date
Wed Mar 12 2025
Journal Name
Al–bahith Al–a'alami
The Responsibility of the Iraqi Journalism in Promoting Political Culture in Society: (An Analytical Study in Newspapers: Al-Sabah, Al-Ittihad, Al-Aalam for 2/ 3/ 2013 - 31/ 3/ 2013)
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This study comes as: The responsibility of the Iraqi newspapers in promoting  the political culture inside society, an analytical study in newspapers: Al-Sabah, Al-Ittihad, Al-Aalam for 2/ 3/ 2013 to 31/ 3/ 2013 to spot light on the extent to which the three mentioned newspapers are compliance with the promotion  of the political culture inside society which is seen as one of the essential requirements for the success and promotion of the democratic process inside society.

The study aims to: finding out the extent to which these newspapers are compliance with their responsibility in the promoting the political culture inside society; knowing the nature of their role in pr

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Publication Date
Wed Aug 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Prepare a plan for the Total Productive Maintenance in the light of the concurrent engineering A Field Study in AL-Askandria General Company Machanical Industries and AL-Musaib Electric Power Station
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           Strives Total Productive Maintenance  to increase the overall effectiveness of the equipment through the early involvement in the design and manufacture of equipment productivity. It also operates in an environment of simultaneous engineering work on the synchronization of activities to take advantage of early information by maintenance engineers, design, operation, and that helps to reduce the faults and facilitate future maintenance tasks.

    Has adopted a search in the theoretical concept of the total maintenance productivity and concurrent engineering activities carried out during which the conjunction a

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Publication Date
Sun Jun 01 2008
Journal Name
Baghdad Science Journal
Synthesis and characterization of VO(II), Cr(III),Mn(II), Fe(II),Zn(II),Cd(II),Hg(II) and UO2(VI) complexes with ligands containing (ONO) and (ON) donor set atoms
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A new Schiff base o-hydroxybenzylidene-1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-on (HL) ,have been prepared and characterization.(HL) has been used as a chelating ligand to prepare a number of metal complexes VO(II) ,Cr(III) ,Mn(II),Fe(II),Hg(II) and UO2(II) .and mixed ligands complexes have been prepared between o-hydroxybenzylidene-1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-on and 8- hydroxy quinoline with VO(II),Zn(II),Cd(II), Hg(II) and UO2(II) the prepared complexes were isolated and characterized by (FT-IR)and (UV-Vis) spectroscopy. Elemental analysis (C.H.N) Chloride contents, Flame atomic absorption technique. in addition to magnetic susceptibility and conductivity measurement. Molar ratio measurement in solution gave comparabl

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