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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
Thu Sep 30 2021
Journal Name
Journal Of Economics And Administrative Sciences
The Role of Product Innovation on an Improvement of the Organization's Reputation /A Field Study in State Organization for Marketing of Oil (SOMO)
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 This paper aims to verify the existence of relationships between product innovation and the reputation of the organization. The study problem is that the State Organization for Marketing of Oil (SOMO) system is inflexible in terms of marketing procedures and needs innovative, unconventional methods in innovating its products and improving performance. The reputation of the organization. The importance of the study lies in that it is an attempt to raise the interest of SOMO in its approach to the research variables in order to enhance its competitive position in the future and improve the marketing business environment, which contributes to enhancing the reputation of the organization by product innovation. The study sample

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Publication Date
Sun Jun 27 2021
Journal Name
Iraqi National Journal Of Nursing Specialties
Prevalence of Smoking among Health Workers and Effectiveness of Instructional Booklet concerning Risks of Smoking on Health Workers′ Knowledge in Baghdad Teaching Hospital
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Objective(s): The present study aims at assessing the prevalence of smoking among health workers in Baghdad Teaching Hospital and to find out the effectiveness of instructional booklet concerning risk of smoking on health workers′ knowledge in hospital.

Methodology: A pre-experimental design study was conducted from 1st of October 2019 to 17th of March 2020. A non-probability sample consists of (500) participant (343 non-smokers and 157 smokers) from (1500) health workers in Baghdad Teaching Hospital, they included the physicians, nurses, pharmacists, physiotherapists, Laboratory Technicians, Medical Assistants. A questionnaire is constructed to evaluate the effectiveness of instructional booklet on health workers’ knowledge

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Publication Date
Sun Jun 16 2019
Journal Name
Al–bahith Al–a'alami
Academic Trends of Paper Press in Comparison with Internet Press A Field Study on Professors o College of Media at University of Baghdad
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This search seeks to know the trends of academics in the field of Press and audio, video and read press about paper press compared with continued development and widespread deployment of web journalism. This research belongs to descriptive studies which depends on sample survey approach adopted by five-meter design measuring trends. It contains 28 items having applied honesty and reliability transaction and the scale form is distributed to the sample studied of about 110 professors and then the researcher collects them and then applying the appropriate statistical program to get the results. This search seeks to know the trends of academics in the field of Press and audio, video and read press about paper press compared with continu

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Publication Date
Mon Dec 03 2018
Journal Name
The Iraqi Postgraduate Medical Journal
Operative Treatment by Plate and Screws Versus Conservative Treatment of Closed Displaced Fracture of the Mid Third of Clavicle in Adults: Comparative Study
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BACKGROUND: Clavicle fractures are common injuries in young active individuals, the mid third of the clavicle is most commonly fractured part(80% of clavicle fracture) OBJECTIVE: To compare the outcomes of operative and non operative management of displaced and or comminuted closed fracture of the mid third of clavicle in young adults PATIENTS AND METHODS: This prospective observational study of 24 patients of fracture of the mid third of the clavicle was conducted in Alkindy teaching hospital from July 2015 to January 2017 and divided into two groups; one managed by operative treatment with plate and screws and the other by non operative sling immobilization after taking the consent and the patients were seen at 2, 4, 6 weeks,3, 6, and 9 m

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Publication Date
Tue Feb 19 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Federal Board of Supreme Audit and Role in the Assessment of Tax Performance: An Applied Research in The General Commission of Taxes
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The success of any institution must be based on means to protect its resources and assets from the waste, loss, misuse and the availability of accurate and reliable data by accounting reports to increase its operational efficiency, namely, that the internal control system is considered as a safety valve for top management in any economic unit. The problem is represented by the need for an efficient system, so to ensure its success, there must exist external parties which monitor and evaluate the performance because of its importance by following clear criteria. So, the research problem came to address performance evaluation indicators which are set by the Federal Board of Supreme Audit (FBSA) and identify the extent of its contribution t

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Publication Date
Sun Jan 01 2012
Journal Name
Baghdad Science Journal
Effect of Aquatic, Alcoholic and Oily Extracts of Cocos nucifera L.on the Growth of Certain Pathogenic Bacteria Isolated from Wounds and Burns Infections
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Publication Date
Mon Feb 25 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Impact of Using the Information Technology on The Audit Profession: A Study of the Sample of Auditor Viewpoints in Selected Arab Countries
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This study aims to clarify areas of using information technology in accounting and its impact on the profession of auditors by reviewing the concept, types, areas and the importance of information technology and its implications on the audit profession as well as to clarify the extent of contribution of information technology in  developing of procedures of the audit profession and what its requirement, also this study aims to enhance the theoretical side by identifying the views of a sample of auditors in  Arab countries selected (Iraq, Syria, Jordan), for the extent of using of information technology in their work and level of their perception for the importance of that

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Publication Date
Fri Jan 01 2021
Journal Name
Review Of International Geographical Education
Comparing environmental awareness under the Corona pandemic between students of the Faculty of Physical Education and Sports Sciences at the University of Kufa
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The purpose of this paper is to identify environmental awareness under the Corona pandemic among students of the Faculty of Physical Education and Sports Sciences at the University of Kufa. and comparison of environmental awareness under the Corona pandemic between students of the Faculty of Physical Education and Sports Sciences at the University of Kufa. The two researchers used the descriptive approach in the style of the survey and comparisons to identify the research community in the students of the College of Physical Education and Sports Sciences at the University of Kufa for the academic year 2020-2021, who numbered (210) students, then a sample of (80) students was chosen randomly, with a percentage of (38.09%) from the research co

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Publication Date
Tue Aug 01 2023
Journal Name
Iop Conference Series: Earth And Environmental Science
Sustainability of Agricultural Productivity of Potato Crop in Desert Soils and Evaluation of Water Productivity Under Drip Irrigation System with Future Climate Changes
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A field experiment was conducted during the spring season 2020 in Karbala proving/ Al-Sharia Distrit, located at latitude N 32° 42' 13.8" and longitude E 43° 54' 36.6" and at an altitude of 27 m above sea level. The experiment included a study of two factors: the first, Irrigation Interval, three treatments were used: irrigation treatment every 2 days, Irrigation treatment every 4 days, and Irrigation treatment every 6 days. The second factor is the addition of soil conditioners, in which four treatments were used: the control treatment without any addition, the treatment of adding bio-organic fertilizers, the treatment of adding water-conserving technology (polymer), and the treatment of adding water-conserving technology + fertilizers O

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Publication Date
Fri Aug 01 2014
Journal Name
Journal Of Economics And Administrative Sciences
Using Bayesian method to estimate the parameters of Exponential Growth Model with Autocorrelation problem and different values of parameter of correlation-using simulation
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We have studied Bayesian method in this paper by using the modified exponential growth model, where this model is more using to represent the growth phenomena. We focus on three of prior functions (Informative, Natural Conjugate, and the function that depends on previous experiments) to use it in the Bayesian method. Where almost of observations for the growth phenomena are depended on one another, which in turn leads to a correlation between those observations, which calls to treat such this problem, called Autocorrelation, and to verified this has been used Bayesian method.

The goal of this study is to knowledge the effect of Autocorrelation on the estimation by using Bayesian method. F

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