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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
Wed Aug 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Adoption of multi – model Assignment Fuzzy to find Optimizing for the use of internet line in the Ministry of Science and Technlogy
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We have provided in this research model multi assignment  with  fuzzy function goal has been to build programming model is correct Integer Programming fogging  after removing the case from the objective function data and convert it to real data .Pascal triangular graded mean using Pascal way to the center of the triangular.

The data processing to get rid of the case fogging which is surrounded by using an Excel 2007 either model multi assignment  has been used program LNDO to reach the optimal solution, which represents less than what can be from time to accomplish a number of tasks by the number of employees on the specific amount of the Internet, also included a search on some of the

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Publication Date
Mon Apr 03 2023
Journal Name
Journal Of Educational And Psychological Researches
The Effectiveness of Concept Maps in Academic Achievement among Family Education Students in the Subject of the Art of Elegance and Fashion
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Abstract

The current research aims to identify the effectiveness of concept maps in the academic achievement of the art of elegance and fashion for third vocational students. The current research is a quasi-experimental one. The research sample consisted of (74) female students in Al-Saydiyah secondary school for girls, they were divided into two groups: the experimental group and the control group. The following hypothesis was developed: There are no statistically significant differences at the level (0.05) between the average scores of the students who studied the subject using concept maps and the average scores of the students who studied the subject in the traditional method in the post-achievement test. The

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Publication Date
Wed Oct 17 2018
Journal Name
Journal Of Economics And Administrative Sciences
The impact of the "Senge" Model of Organizational Learning in the adoption of Total Quality Management principles) Exploratory study in an organization)
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      This study is concerned with organizational learning and its impact on total quality management in the education sector. Organizational learning is a process that provides the educational sector with the ability to adapt and respond rapidly to developments and changes in a better way according to its main dimensions (Mental Models, Personal Mastery, Team Learning, Shared Vision, System Thinking) by adopting the philosophy of Total Quality Management (TQM) in accordance with its basic dimensions (leadership, customer satisfaction, participation of workers, continuous improvement, training and education). The main purpose of this study is to know (the impact of the Senge model of organizational learni

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Publication Date
Sun Jan 04 2015
Journal Name
Journal Of Educational And Psychological Researches
Effectiveness of the self-questioning strategy in the achievement of the third stage Institutes of teacher preparation and decision - making in Chemistry
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This research aims to find out "the effectiveness of the self-questioning strategy in the achievement of students Phase III institutes of teacher preparation and decision-making in chemistry." The researcher follows approach quasi-experimental with a post-test, and the sample consisted of (27) from " Teachers Training Institute-AL-Byaa "in Directorate of Education Baghdad Karkh / 2 students divided into two unequal groups: experimental its number (14) students studied using reciprocal teaching strategy and control its number (13) students have studied in the usual way.The two groups were equivalent extraneous variables.

The researcher was prepare achievement test consist of 40 items was the adoption of a measure of decision-makin

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Publication Date
Wed Jun 29 2022
Journal Name
College Of Islamic Sciences
Explanation of the correct jurisprudence for calculating the value of the selling price, not the purchase, in the zakat of trade offers
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 After completing the research, with the help and success of God  Almighty , I will summarize what has been mentioned in a concise and understandable form, without boring prolongation or abbreviation .

    The subject, in general, was clarified, clarified and corrected, as I mentioned, for an incorrect concept, about paying zakat on trade goods.

    It has known trade offers parts and combination of language and idiomatic .

   The rule of zakat on trade goods, and evidence from the Qur'an, Sunnah and consensus .

    As well as the conditions of its zakat according to the jurists and their differences in it .

    It

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Publication Date
Wed Jan 01 2020
Journal Name
Annals Of Tropical Medicine And Public Health
Isolation and identification of fungi from fish feedstuff of cyprinus carpio and detection of aflatoxin b1 and ochratoxin a using ELISA technique
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This study was conducted at the College of Education for Pure Sciences (Ibn Al-Haitham), University of Baghdad. The aim of this study was to isolate and diagnose fungi from fish feedstuff samples, and also detection of aflatoxin B1 and ochratoxin A in fish muscles and feedstuffs. Randomly, the samples were collected from some fish farms from Baghdad, Babil, Wasit, Anbar, and Salah al-Din provinces. This study included the collection of 35 feedstuff samples and 70 fish muscle samples, and each of the two fish samples fed on one sample of the feedstuff. The results showed the presence of several genera of different fungi including Aspergillus spp, Mucor spp., Penicillium spp., Yeast spp., Fusarium spp., Rhizopus spp., Scopiolariopsis spp., Ep

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Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Estimation of parameters of two-dimensional sinusoidal signal model by employing Deferential Evaluation algorithm and the use of Sequential approach in estimation
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Estimation the unknown parameters of a two-dimensional sinusoidal signal model is an important and a difficult problem , The importance of this model  in modeling Symmetric gray- scale texture image . In this paper, we propose employment Deferential Evaluation algorithm and the use of Sequential approach to estimate the unknown frequencies and amplitudes of the 2-D sinusoidal components when the signal is affected by noise. Numerical simulation are performed for different sample size, and various level of standard deviation to observe the performance of this method in estimate the parameters of 2-D sinusoidal signal model , This model was used for modeling  the Symmetric gray scale texture image and estimating by using

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Publication Date
Thu Dec 13 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Women's Knowledge about Risk Factors and Early Detection of Breast Cancer at Ibn Rushd College of Education in Baghdad University
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Objective: Evaluation of women's knowledge about risk factors and early detection of breast cancer at
Ibn Rushd college of education in Baghdad University.
Methodology: The study sample included (184) women in the Ibn Rushd College / University of
Baghdad, whose age ranged between (17-58) years. Data were collected through a structured
questionnaire prepared by the National Cancer Research Center which were answered during a scientific
symposium about breast cancer. The score was calculated by correcting the results of the answer, giving
one score for each correct answer and then estimating the level of knowledge and inputting all data in a
statistical program.
Results: The results showed limited level of women's

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Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Analysis of the sustainability of the public debt in light of the volatile oil revenues in Iraq for the period (2005-2015)
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Abstract

This study deals with the fluctuations of oil revenues and its effect on the public debt. This can be studied through the indicators of debt sustainability, the financial, and economic indicators which express the risk of debt. The study focuses on clarification of the public debt path and its management both domestic and foreign. The sustainability of debt takes an important role according the macroeconomic variables. This study stresses the relationship between the rental economy in Iraq and the risk of the public debt, it is very important to work high oil prices, and on investigating during high work to establish a fund to support the budget deficit. This will reduce future risks arising from the use of publi

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Publication Date
Sat Jan 04 2020
Journal Name
زانكو - الإنسانيات
The Effect of Linguistic Propositions on the Collection of Arabic Language Norms and the Development of Critical Thinking among Middle-Grade Students.
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The reality of teaching the Arabic language rules is not satisfactory, as the pedagogical methods used do not help students develop their mental skills, especially critical thinking skills. They are often traditional in terms of teaching students, who are passive, passive, often passive, active, and often active, their listening task, and the teacher's task of narrating facts and judgments. It is a blind simulation student, a dependency on others, and a weak spirit of creativity, innovation, and opinion. The opinions of educators and teachers almost agree on the reasons for students' weakness in learning the rules of Arabic, and that the reason lies in the way of teaching. The difficulty or the ease of the rules of Arabic does not lie in th

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