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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
Tue Mar 30 2021
Journal Name
College Of Islamic Sciences
The authority of the ancient text in the poetry of Bashar bin Bard
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Abstract

Heritage represents the center around which poets revolve around and take advantage of its inexhaustible specific, and the connotations that this heritage holds of various values, values ​​and ideas, and the poet Bashar bin Bard from prominent poets who were inspired by that heritage and the culture of the first Abbasid era and whoever and others was worthy of studying and tracking his potentials and capabilities Creativity is based on the inspiration of the legacy of his predecessors, and the development of this legacy and renewal in it. The research methodology required its division into two topics, the first topic, a description of the beauty of women, a description of wine, while the second topic is a description

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Publication Date
Sun Apr 01 2018
Journal Name
Journal Of Educational And Psychological Researches
The reality of administrative creativity of secondary schools' managers in Al-zarqaa province
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The study focuses on identifying the reality of administrative creativity of secondary schools' managers in Al-zarqaa province. The descriptive approach was adopted to conduct this study. To achieve the study objective, the author designed a questionnaire composed of (24) items included (4) domains applied on (80) male and female school managers were selected randomly. The results showed that the administrative creativity level of secondary school's managers over all domains were too high which ranked as school management domain followed by public community domain then teacher domain and finally, school environment domain. Additionally, each of male, private sector, and experience over 10 years revealed significant differences.

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Publication Date
Fri Mar 15 2019
Journal Name
Journal Of Baghdad College Of Dentistry
Oral health knowledge and practices of women attending dental clinics of Baghdad University
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Background: Knowledge is considered to be essential for developing healthy practices and preventing the main oral diseases. In some developing countries, women were at higher risk to develop these diseases. This study was conducted to evaluate women’s dental knowledge and practices through a specific questionnaire and the relationship with patient’s educational level and the number of their children. Subjects and method: Women, aged from 25-35 years old, were selected to participate in the current study. They were attending dental clinics in the teaching hospital of Baghdad University. Each participant was instructed to answer questionnaire sheet which is previously prepared in Arabic language by the authors. The total numb

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Publication Date
Tue Jun 01 2021
Journal Name
Journal Of The College Of Languages (jcl)
A Multimodal Analysis of Hyperbolic Devices in Advertisements of Health and Beauty Products
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         This paper examines the use of one of the most common linguistic devices which is hyperbole. It shows how hyperbolic devices are used as an aspect of exaggeration or overstatement for an extra effect in which the speaker can use hyperbole to add something extra to a situation in order to exaggerate his idea or speech. It is, like other figures of speech, used to express a negative or positive attitude of a specific unit of language. Thus, this paper is set against a background of using hyperbole concerning two main fields (advertisements and propaganda). So, the use of hyperbole will be implied by analyzing them concerning their meaning) literal and non-literal).  Methodology of this

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Publication Date
Wed Oct 28 2015
Journal Name
Al-khwarizmi Engineering Journal
Interaction of Corrosion-Cumulative Fatigue and Shot Peening of 1100-H12 Aluminum Alloy
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Abstract

    Corrosion-fatigue occurs by the combined actions of cyclic loading and corrosive environment. The effect of shot peening on cumulative corrosion-fatigue life of 1100-H12 Al alloy was investigated. Before fatigue testing, specimens were submerged in 3.5%NaCl solution for 71 days. Constant fatigue tests were performed with and without corrosive environment. Cumulative corrosion-fatigue tests were also carried out in order to determine the fatigue life before and after shot peening. The constant fatigue life was significantly reduced due to corrosive environment and the endurance fatigue limit was reduced by 13% compared with dry fatigue. In case of shot peening the cumul

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Publication Date
Sun Jan 05 2014
Journal Name
Journal Of Educational And Psychological Researches
The role of educational curricula and teaching methods in the development of environmental
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Described the Arabic language being of genius sets by top models of eloquence , rhetoric and clarity of sounds and developments Moreover , it is an important element of our existence and our identity and our survival . That my methods and best in teaching Arabic language what has pursued the easiest ways to learning and teaching and helped learners to be aware of the function linguistic information , and they need it and its impact on their lives , and contributed to unleashing the potential of activism and led them to make the effort to apply them in the form of examples and uses of new life , as well as fits are the capabilities and tendencies of different learners , so the goal of current research into the importance of the curriculum

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Publication Date
Fri May 21 2021
Journal Name
Transportation Infrastructure Geotechnology
Behavior of Floating Stone Columns and Development of Porewater Pressure Under Cyclic Loading
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Publication Date
Thu Sep 01 2016
Journal Name
Journal Of Engineering
Effect of Lime Addition Methods on Performance Related Properties of Asphalt Concrete Mixture
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In the recent years, some of the newly constructed asphalt concrete pavements in Baghdad as well as other cities across Iraq showed premature failures with consequential negative impact on both roadway safety and economy. Frequently, load associated mode of failure (rutting and fatigue) as well as, occasionally, moisture damage in some poorly drained sections are the main failure types found in those newly constructed road.

In this research, hydrated lime was introduced into asphalt concrete mixtures of wearing course in two methods. The first one was the addition of dry lime on dry aggregate and the second one was the addition of dry lime on saturated surface dry aggregate moisturized by 2.0 to 3.0 percent of wa

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Publication Date
Tue Jan 02 2018
Journal Name
Journal Of Educational And Psychological Researches
The role of relaxation program for reducing anxiety of patients in dental clinic
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The role of relaxation program for reducing anxiety of patients in dental clinic  

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Publication Date
Fri Dec 15 2023
Journal Name
Bionatura
Evaluation of the quality of potable water in Al-Rusafa side, Baghdad, Iraq
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Safe drinking water is essential for the present and future generations' health. This study aims to assess drinking water quality in Baghdad's Al-Rusafa neighborhood. Water samples were taken from 32 neighborhoods on this side. The quality of the examined potable water samples differed depending on the water source. This investigation's pH, chlorine, EC, TDS, TSS, Cd, and Pb levels were below acceptable ranges. TDS levels in Al-Mada'in are more significant than acceptable (>600ppm) water levels. Bacteria have polluted six communities (Shigella, Salmonella, Escherichia coli, and Klebsiella). Bacterial quality of drinking water and gram-negative bacteria resistant to chlorine in Baghdad's municipal water supply. Regarding pH, the w

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