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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
Mon Jul 01 2019
Journal Name
Journal Of Educational And Psychological Researches
The Impact of Strategy 3-2-1 in acquiring Concepts of Sociology of fourth grade students: The Impact of Strategy 3-2-1 in acquiring Concepts of Sociology of fourth grade students
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Abstract

The current research aims to identify the impact of triangular bridging strategy in the acquisition of sociology of fourth-stage students. To achieve the research objective, the following null hypotheses were adopted: there are no statistically significant differences at a significance level (0, 05) between the average grades of the experimental group students who studied the triangular bridging strategy in acquiring concepts of sociology and average grades of the control group. The researcher has selected the fourth-stage students from Alexandronah School for girls that s related to the Directorate General of Baghdad the sample consisted of (87) students at litera

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Publication Date
Sat Dec 31 2022
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EFFECT OF ADDING DIFFERENT LEVELS OF DILL SEEDS TO THE DIET ON PHYSIOLOGICAL TRAITS OF BROILERS : EFFECT OF ADDING DIFFERENT LEVELS OF DILL SEEDS TO THE DIET ON PHYSIOLOGICAL TRAITS OF BROILERS
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This study was conducted in the poultry field of the department of animal production, college of agricultural engineering sciences, university of Baghdad for the period from 10/15/2021 to 11/25/2021 with the aim of showing the effect of adding different levels of dill seeds to the diet on productive and carcass traits For broiler meat. In this study, 200 unsexed broiler chicks of breed (Ross 308) were used, one day age, with a starting weight of 41.46 g. The chicks were randomly distributed to 5 treatments, and each treatment included 4 replicates, 10 birds for each replicate. The birds were fed three diets: the starter diet, the growth diet and the final diet. The experiment treatments were T1,

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Publication Date
Wed Sep 18 2019
Journal Name
مجلة الدراسات الدولية
The media message of ISIS: The content of the discourse and the mechanisms of media confrontation. The media message of ISIS: The content of the discourse and the mechanisms of media confrontation.
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يهدف البحث الى صياغة استراتيجية اعلامية لمواجهة اعلام التنظيمات الارهابية

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Publication Date
Tue Feb 01 2022
Journal Name
International Journal Of Special Education
Cultural Perspective of Male Outfit in the Text of the Play of Hamlet by William Shakespeare and the Application of (the Status of Apparels) Textual Analysis
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Publication Date
Sun Jan 01 2023
Journal Name
International Journal Of Research In Social Sciences & Humanities
The Impact of Strategic Improvisation on Organizational Health: An Analytical Study of the Opinions of a Sample of the Leaders of the Dhi Qar Health Department
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The current research aims to identify the level of impact of strategic improvisation as an independent variable on organizational health. The dependent variable in the Department of Health of Dhi Qar to reach appropriate mechanisms in order to reach appropriate mechanisms and recommendations proposed to contribute to the achievement of organizational health in the Department of Health of Dhi Qar (the research department) and based on the importance of the subject of research in government institutions and the important and service role of the Department of Health of Dhi Qar in the Iraqi society. The descriptive analytical approach was adopted in the completion of the research based on the opinions of the leaders in the surveyed depa

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Publication Date
Fri Mar 15 2019
Journal Name
Journal Of The College Of Education For Women
Assessing the Brief Book of the Modern and Contemporary History of Asia from the Perspective of the Students in the Department of History - University of Baghdad
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The current research aims to assess the Brief Book of the Modern and Contemporary History of Asia from the perspective of the students in the Department of History, University of Baghdad. The study is carried out in Iraq and the research group has included students of the Department of History in the College of Education--Ibn Rushd and the College of Education for Women- University of Baghdad. The chosen sample of the assigned research consisted of (72) students from third stage in the Department of History, which equals (0.38%) of the total group members amounted (188) female and male students representing (40) students from the College of Education--Ibn Rushd, and 32 students from

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Publication Date
Sat Dec 01 2018
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Rationalization the costs of agricultural Activities under the use of genetic engineering: An applied research in ministry of agriculture - The directorate of inspection & certification of seeds
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The importance of this research has been to rationalize the cost of producing maize seeds through the followers of modern techniques and methods in agricultural activities such as genetic engineering for increasing production efficiency of maize seeds as well as the importance of calculating seed cost rationalization through the ABC system and thus rationalizing government spending. The research is based on one hypothesis in two ways that the use of genetic engineering on maize seeds works to: one - increase production efficiency of seeds and savings in agricultural inputs. 2. Rationalize the costs of examining and planting maize seeds. In order to calculate the costs will be based on the cost system based on activities ABC. The research

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Publication Date
Sat Sep 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Effect of strategic thinking in human resource management strategies “Analytical field study of the views of a sample of managers in the Iraqi Ministry of Health”
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The researcher attempts to diagnose the level of the effect  of strategic thinking skills (intuition, meditation, creativity) of the managers in the Ministry of Health in Iraq and some of its institutions in the formulation of human resources management: (selection, training, incentivence , performance appraisal (Recognizing the importance of the subjects studied, and because of the importance of the expected results of th

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Publication Date
Fri Jan 01 2021
Journal Name
Psychology And Education
The effect of Daniel's model on the development of critical thinking in the subject of Arabic language among students of the College of Management and Economics
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This research aims to identify the impact of Daniel's model on the development of critical thinking. In order to achieve this objective, the following hypotheses are formulated: 1. There is no statistically significant difference at the significance level (0.05) between the average differences in the posttest scores of the experimental group taught according to Daniel's model and the control group taught according to the traditional method in the measure of critical thinking. 2. There is no statistically significant difference at the significance level (0.05) between the average differences in the preand post-tests scores of the experimental group taught according to Daniel's model in the measure of critical thinking. The current research i

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Publication Date
Wed Jan 01 2020
Journal Name
Annals Of Tropical Medicine And Public Health
STUDY OF SOME BIOLOGICAL ASPECTS OF MICE INFECTED WITH HYDATID CYST OF Echinococcus granulosus PARASITE AND THE THERAPEUTIC CAPACITY OF ETHANOLIC EXTRACT OF Cladophora glomerate ALGAE
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