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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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Sun Mar 19 2023
Journal Name
Journal Of Educational And Psychological Researches
The Effect of Using the Generative Learning Model on the Achievement of First-Grade Intermediate Students of Chemical Concepts in Science
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The current research aims to identify the effect of using a model of generative learning in the achievement of first-middle students of chemical concepts in science. The researcher adopted the null hypothesis, which is there is no statistically significant difference at the level (0.05) between the mean scores of the experimental group who study using the generative learning model and the average scores of the control group who study using the traditional method in the chemical concepts achievement test. The research consisted of (200) students of the first intermediate at Al-Farqadin Intermediate School for Boys affiliated with the Directorate of General Education in Baghdad Governorate / Al-Karkh 3 wit

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Sat Dec 01 2018
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Journal Of Accounting And Financial Studies ( Jafs )
Survey theopinions professional and academics on building the strategy of internal audit function and the possibility of keeping abreast of developments
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The research problem is clearly deficient suffered by the internal audit function in all institutions of Iraq, as a result of the lack of sponsor organizations for this profession and there is no law or local legislation determine its powers and its responsibilities and scope of work As well as the lack of interest of senior management in economic units that function, as it focuses its work on the scope of financial and accounting matters only So required to rebuild this function in line with the current developments as well as the lack of a framework that defines the strategy of this function, and it came the idea of research to find out how to create a regulatory method for re-strategic construction of the internal audit function depen

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Thu Sep 01 2022
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Patterns of thinking about chemical identity among students of the College of Education for Pure Sciences - Ibn Al-Haytham in Iraq
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Thu Jan 04 2024
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Journal Of Accounting And Financial Studies ( Jafs )
The impact of recent trends of the Central Bank of Iraq in activating bank credit for the private commercial banking sector
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                 Central banks seek to control and supervise credit and follow it up effectively due to the high credit risks surrounding it that may lead to damage to banks, and may even lead to damage to the reputation and confidence of the banking system as a whole.

The main role of supervisory control is to control credit by controlling it from excessive expansion during periods of economic inflation or its revitalization and improvement and expansion of credit transactions in cases of economic recession, or when central banks desire to support the national economy or support a sector of various

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Fri Feb 09 2024
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Eximia
The reality of the moral climate and its relationship to the decision-making of boxing referees from the standpoint of coaches
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The purpose of this paper is to identifying the relationship between the moral climate and the decision-making of boxing referees from the standpoint of the coaches, and the research problem lies through the work of the researchers in training and managing the teams. It was noted that the role of the referees is one of the most important roles played by the workers to achieve the objectives of the federation, and that the moral climate that prevails among the administrative body the union and the referees on the one hand and between the referees and coaches on the other hand are among the factors of the success of everyone’s work and the survival and strengthening of confidence in their work and thus the continuity of success and

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Achieve of Marketing Superiority under the adoption of the concept of internal marketing: Applied Research at National Company for Insurance Company.
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The insurance Sector of important vessels saving that work on the accumulation of capitals which contribute to the financing of economic and social development plans of countries, in order to achieve of marketing superiority in presenting the insurance services it would require insurance companies focus their marketing efforts and increased interest in internal customer to recruitment new customers and keep of current customers, so the research aims to release the impact of the dimensions of the internal marketing of (the company's vision, training and development, incentive and, motivation, internal communication) in the dimensions of the marketing superiority (to keep the customer, service quality, customer satisfaction, customer, valu

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Publication Date
Thu Oct 25 2018
Journal Name
Journal Of Economics And Administrative Sciences
Find the fuzzy maximum flow of Imam Kadhimen visitors using fuzzy dynamic programming University of Baghdad - Faculty of Administration and Economics
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    Baghdad and the other Iraqis provinces have witnessed many   of celebrations which have the significant effect on the souls of Arabic and Islamic people in general , and Iraqi people, especially the birthday and death of two al-kadhimen Imams(peace upon them) and others .From here the researcher begin to study the visiting of imam kadhimen (peace upon him) on 25 Rajab the commemoration of his sacrifice, simply because have implications of religious, ideological and cultural sectors which represents in finding the greatest flow of visitors .the problem of research appeared due to the clear difference in number of visitors during one day, beside the significant increase in number of visitors  throu

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Mon Dec 30 2024
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French Language in Iraq: Study of the Relationship between University Education and Social Activities (The Case of the University of Baghdad)
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Cumhuriyet Üniversitesi Fen-Edebiyat Fakültesi Sosyal Bilimler Dergisi | Volume: 48 Issue: 2

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Publication Date
Tue Oct 07 2025
Journal Name
Journal Of Baghdad College Of Dentistry
The effect of the addition of silanated poly propylene fiber to polymethylmethacrylate denture base material on some of its mechanical properties
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Background: Poly propylene fibers with and without silane treatment have been used to reinforce heat cure denture base acrylic but, some mechanical properties like transverse strength, impact strength, tensile strength, hardness, wear resistance and wettability. Which are related to the clinical use of the prosthesis are not evaluated yet. The aim of the study is to identify the influence of incorporation of treated and untreated fibers on these properties Materials and methods: Eighty four heat cure acrylic specimens were constructed by conventional flasking technique. They were divided into six groups according to the tests and each group was subdivided into two subgroups control and experimental groups (seven samples for each subgroup

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Tue Jan 01 2019
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Effect of welding heat input on corrosion rate of sprinkler irrigation piping joints by tig welding used in South of Iraq
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