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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 Jun 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Development of a Simple Colorimetric Determination of Dexamethasone
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A simple, environmentally benign, cost-effective, and sensitive colorimetric determination for the pharmaceutical drug dexamethasone sodium phosphate (DXP) has been developed by the formation of a colored complex with fluoranil. The process was sensitive and linear over the range 1 to 40 μg/mL, excellent correlation coefficient 0.9989, recovery% 99.80 ± 1.3, limit of detection (LOD) and limit of quantification (LOQ) were 0.23 and 0.9 μg/mL, respectively, and good RSD ~1.63%. The experimental conditions were optimized after an intensive study. The approach was validated statistically for the quantification of the analyte in its pure and/or pharmaceutical form. Despite the proposed approach is selective, it still can be applied for

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Publication Date
Tue Jun 01 2021
Journal Name
Int. J. Nonlinear Anal. Appl.
Study of the dual ideal of ku-algebra
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In this work, we apply the notion of a filter of a KU-Algebra and investigate several properties. The paper defined some filters such as strong filter, n-fold filter and P-filter and discussed a few theorems and examples.

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Publication Date
Sun Dec 01 2019
Journal Name
Acoustical Society Of America
Effect of ultrasonic pretreatment on pyrolysis of microalgae
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Publication Date
Sun Sep 01 2019
Journal Name
Journal Of Physics: Conference Series
Synthesis, Characterization Of Organic Nanoparticles of Oxadiazole Derivative
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Abstract<p>The synthesis oxadiazole derivative 2,5-disubstituted-1,3,4oxadiazole (3a,3b,3c) was prepared from reaction of N-(4-amino benzene sulphonyl)Morpholipebut-2-enehydrazide with (4-hydroxybenzaldehyde,4-methoxy benzaldehyde,4-ethoxybenzaldehyde) in the presence of lone as catalyst. The structure of (3a,3b,3c) was characterized by using FT-IR, H-NMR and spectroscopy. Nanoparticles of the prepared compounds have been fabricated in aqueous media using re-precipitation method.Characterization of the nano particles (ONPs) have been performed by using UV-VIS spectrophotometer and scanning electron micro scope ( SEM). The size of the nanoparticales were around 150-200 nm as indicated by (SEM). T</p> ... Show More
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Publication Date
Sat Apr 01 2023
Journal Name
Baghdad Science Journal
Detour Polynomials of Generalized Vertex Identified of Graphs
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The Detour distance is one of the most common distance types used in chemistry and computer networks today. Therefore, in this paper, the detour polynomials and detour indices of vertices identified of n-graphs which are connected to themselves and separated from each other with respect to the vertices for n≥3 will be obtained. Also, polynomials detour and detour indices will be found for another graphs which have important applications in Chemistry.

 

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Publication Date
Wed Sep 28 2022
Journal Name
Journal Of The College Of Education For Women
The Degree of Application of Digital Leadership and its Relationship to the Development of Administrative Work at the University of Tabuk
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This study aims to explore the relationship between the degree of application of digital leadership and the development of administrative work at the University of Tabuk. It further aims to examine the presence of statistically significant differences between the average responses of faculty members and employees at the University of Tabuk regarding the study axes that are attributed to the following variables: (scientific rank, gender, and job), the study used the descriptive approach in its correlative style, and the questionnaire was used as a tool for data collection, as it was applied to a simple random of (310) members of the faculty and staff. University of Tabuk. The results showed that the degree of digital leadership applicatio

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Publication Date
Tue May 26 2026
Journal Name
Journal Of The College Of Basic Education
Objective trends of university theses and dissertations of the College of Political Science at the University of Baghdad: an analytical study
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The research sought to identify the objective trends of postgraduate students at the College of Political Science - University of Baghdad for the period from 2000-2012 through the objective trends of university theses and dissertations and what are the most and least studied topics, with a re-adjustment of previously studied topics towards topics that serve issues of concern to society and avoiding topics that have been studied a lot to avoid repetition. The research came out with the following results, the most prominent of which are: The total number of what was accomplished in this college is 401 theses and dissertations, and the dissertations had the largest share of them, as their percentage reached 69%, with 275 theses compared to 126

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Publication Date
Tue Jan 29 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Impact of Tax Laws and Decisions in Determining the Tax Base of the Results of the Financial Statements of Companies
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This research aims to measure the discrepancy between the accounting income which is prepared according to generally accepted accounting principles and the tax income that is being prepared according to the rules and tax laws, and find out the most important differences that arise between incomes.The research found the most important to the following conclusions:1.Faces determining the tax base for companies subject to income challenges related to the weakness of the efficiency and the possibility of technical angel tax and its ability to examine the financial statements submitted to the tax administration tax.2.That the tax system in Iraq does not comply with accepted accounting principles generally accepted.The research recommends the

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Publication Date
Wed Dec 30 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The effect of salary Domiciliation in the rate of return on assets (ROA): Applied research of a sample of Iraqi banks
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Abstract

The research attempted to find an explanation and solution to a problem related to the fluctuation and decrease In the rate of return on assets for the research sample banks during the duration of the research, The search started from the hypothesis that, The effect of salary Domiciliation on the banking profitability of a sample of Iraqi banks participating in the salary settlement system for the period (2016-2019),The research used the descriptive historical approach, the quantitative analytical approach and the statistical approach. The research reached a set of conclusions, the most important of which is The effect of salary Domiciliation on banking profitability was achieved in three banks

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Publication Date
Fri Jan 01 2021
Journal Name
Prepodavatel Xxi Vek
Enrichment of Vocabulary and the Formation of Grammatically Correct Speech of Foreign Students When Studying the Text of a Literary Work
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