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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
Sun Jul 01 2018
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
ANNOTATED CHECKLIST OF REPTILIAN FAUNA OF BASRAH, SOUTH OF IRAQ
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    Basrah province is situated at the extreme south of Iraq,  it has an interesting reptile fauna (Squamata and Serpentes) and represents a land bridge between three different zoogeographical regions ( Oriental, Palaearctic and  Ethiopian).

     This situation gave Basrah province a topographic specific opportunity for raising its own faunal diversity including reptiles; in this study Basrah province was divided into four main zones: the cities and orchards, marshes and wetlands (sabkha), the true dessert, the seashore and Shat Al-Arab.

Forty nine reptile species were recorded including snakes, sea and fresh water turtles, and Lizards; brief notes and descriptions for the rare

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Publication Date
Sat Oct 01 2022
Journal Name
Al–bahith Al–a'alami
THE CHALLENGES OF GLOBALIZATION OF MEDIA AND WAYS OF CONFRONTATION
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The successive international changes in the economic, political, cultural and other fields resulted in many phenomena that occupied different levels of interest, and have been followed up, studied and analysed by specialists and researchers especially under the development of the media in the global communication.

Even though these phenomena had reflections in the communication domain like development and changes in the mechanism of behaviours between the international communities, they created in the meantime a phenomenon that caused an imbalance in the production, spread and the use of the informations that were supposed to be for fewer than 5 countries whereas it actually it is for more than 180 countries.

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Publication Date
Wed Jun 20 2018
Journal Name
Bulletin Of Iraq Natural History Museum
ANNOTATED CHECKLIST OF REPTILIAN FAUNA OF BASRAH, SOUTH OF IRAQ
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Publication Date
Wed Dec 12 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Assessment of Quality of Life for Parents of Autistic Child
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Objectives: The study aims to assess the QOL for parents of a child with autism Methodology: A descriptive study was conducted on parents of autistic child in Baghdad city. A purposive (non-probability) sample of (156) parents, (78) mothers and (78) fathers of (78) autistic children who are clients and receive care in the private specialization centers for autism were selected to participated in the current study. The study used a self- administrative questionnaire for data collection. Results: The findings indicated that both parents (mothers and fathers) were participated in this study, and they comprised

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Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
THE EFFECT OF AGE ON DEVEOPMENT OF CONCEPT OF MIND
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Educational of the mind is a weapon to a different knowledges which
benefit in ife and developed the mind in many field and practice him in a
regular form in a right thinking and practice sense on exactly recognizing and
conception things which is senses and regulating the memory and providing
with benefit information which fit to minded of person,the present research
aimed at answering the following two questions:
1-Does the concept of mind differ with age?
2-Does the recognition on function of mind developed with development of
age?
The research population consisted of the children in the primary schools
of Baghdad/center,and the students of the Education for woman
college/Baghdad university for the age

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Publication Date
Thu Jun 27 2019
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
CHECKLISTS OF PARASITES OF FISHES OF AL-DIWANIYAH PROVINCE, IRAQ
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    Literature reviews of reports concerning the parasitic fauna of fishes of Al-Diwaniyah province, Iraq till the end of December 2018 showed that a total of 43 parasite species are so far known from 13 valid fish species investigated for parasitic infections. The parasitic fauna included one euglenozoan, two myzozoans, six ciliophorans, three myxozoans, three trematodes, nine monogeneans, four cestodes, six nematodes, three acanthocephalans and six crustaceans. The infection with the trematodes, one monogenean, two cestodes and one nematode occurred with larval stages, while the remaining infections were either with trophozoites or adult parasites. Among the inspected fishes, Carasobarbus luteus was infected wit

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Publication Date
Sun Dec 16 2018
Journal Name
Al-academy
The Impact of the Use of Piano on the Development of Musical Possibilities of Violinists
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This research is to take advantage of the performance capabilities which the piano has become famous with and transfer the impact of that advantage to the possibilities of playing the violin. The research aims to introduce the effect of using the piano on the development of the violinists' musical potential. The research, in its literature, focuses on the interpretation of the impact on the possibility of both instruments (piano and violin) in two main sections: the piano (its origin, potential and role in music) and the violin (its origin, potential and role in music). The procedures of the research consisted of presenting a special analysis of a questionnaire consisting of a number of questions presented by the researcher to her resear

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Publication Date
Fri Feb 01 2019
Journal Name
Journal Of The College Of Education For Women
The Necessity of College of Education for Woman from the Point of view of Students
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The Necessity of College of Education for Woman from the Point of view of Students

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Publication Date
Tue Dec 16 2008
Journal Name
Journal Of Planner And Development
Evaluation of the efficiency of the regional transport network of the district center of Mahmudiya
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The Study aims at evaluating the efficiency of the regional transportation net in Al-mahmoodiya Qadaa center. The bus station of the Qadaa center is suffering from heavy traffic jam, which is due to the ongoing movement of the adjacent provinces, particularly the small cities. They vary in the degree of their link by the regional transportation net that links the province with the centers of big cities. That affects the traffic flow of the civilians of these cities and their daily activities in hierarchical way To achieve the purpose of the study, a questionnaire has been constructed to collect data through selecting a random sample including the passengers who are coming to the bus station in Al-Mahmoodiya center to know the flo

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Publication Date
Wed Jan 01 2014
Journal Name
Journal Of Physical Education
The use of physical exercises of mind (knowledge) to develop the level of performance of the rulers of women's football
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Football from popular task the referees the most important elements this game through this study shows the importance of physical training mental and its effects the level of performance for referees and especially woman referees which entered the game in the newly in our country was used physical exercise mind through films and means to assist through visualization some of the cases do the articles of law and also exercises the evolution of the level of performance of the rulers of woman the research sample 12 of referees certified by the Iraqi central football and referees committee achtbarien was chosen for this study including mental cognitive test approved by the referees committee the second test questionnaire to assess the level of p

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