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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
Mon Mar 07 2022
Journal Name
Journal Of Educational And Psychological Researches
Math Word Problems in Mathematics Books for the First Three Grads of the Basic Stage in Palestine (An analytical and Evaluative Study)
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This study aimed at revealing the degree of availability of standards of word problems in mathematics books for the first three grades of the basic stage in Palestine. For this purpose, the researcher prepared an analysis tool and a list of criteria consisting of two areas: linguistic formulation and mathematical content. Every area had seven items. The results of the study showed that the third-grade mathematics book has the highest degree of availability of the standards with 85.75%, and then came the second-grade mathematics book with 83.12%. Finally, the first-grade mathematics book came with 80.13%. In the light of the previous results, the researcher recommended to develop the language of word problems, to take into account their i

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Publication Date
Sat Nov 30 2019
Journal Name
Journal Of Engineering And Applied Sciences
The use of Resource Consumption Accounting and Balanced Scorecard Methods as an Integrated Framework in Correcting the Economic Unit Performance: Applied Study
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Publication Date
Thu Aug 01 2019
Journal Name
International Journal Of Research - Granthaalayah
MULTIPLE MIXING RATIOS OF GAMMA RAY TRANSITIONS FROM 𝟔𝟎𝐍𝐝 𝟏𝟒𝟐− 𝟏𝟓𝟎 (𝐧, 𝐧 ˊ𝛄) 𝟔𝟎𝐍𝐝 𝟏𝟒𝟐− 𝟏𝟓𝟎 REACTION USING 𝒂𝟐- RATIO METHOD
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In the current work, the mixing ratios ( 𝛿 ) of gamma transitions were calculated from energy levels in the isotopes neodymium 60𝑁𝑎 142−150 populated in the 60Nd 142− 150 (n, n ˊγ) 60Nd 142− 150 using the 𝑎2 ratio method. We used the experimental coefficient (𝑎2 ) for two γ-transitions from the initial state itself, the statistical tensor 𝜌2(𝐽𝑖), associated with factor 𝑎2 , would be the same for the two transitions. The results obtained are in good agreement or within the experimental error with -those previously published. And existing contradictions resulting from inaccuracies in the empirical results of previous work. The current results confirm that the , 𝑎2 − method is used to calculate th

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Publication Date
Tue Sep 08 2020
Journal Name
Baghdad Science Journal
Improved throughput of Elliptic Curve Digital Signature Algorithm (ECDSA) processor implementation over Koblitz curve k-163 on Field Programmable Gate Array (FPGA)
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            The widespread use of the Internet of things (IoT) in different aspects of an individual’s life like banking, wireless intelligent devices and smartphones has led to new security and performance challenges under restricted resources. The Elliptic Curve Digital Signature Algorithm (ECDSA) is the most suitable choice for the environments due to the smaller size of the encryption key and changeable security related parameters. However, major performance metrics such as area, power, latency and throughput are still customisable and based on the design requirements of the device.

The present paper puts forward an enhancement for the throughput performance metric by p

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Publication Date
Sun Dec 28 2025
Journal Name
Journal Mustansiriyah Of Sports Science
The Impact of an Educational Curriculum according to the Five-year Learning Cycle on Some Offensive Skills in Basketball for Female Students
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Modern trends have appeared recently in educational thought that call for the achievement of the outcomes of the educational process. Some of these trends are the development of individual thinking skills, considering the individual differences, and learning basic skills. The five-year learning cycle is one of these models. It is called as five-year learning cycle because it passes through five stages. These five stages are: (operate - discover - clarify - expand – Evaluate), which make the learner as the main axis for activating thinking processes. This can be done by organizing study materials through research, investigation, and identifying concepts by himself, as in learning sports skills that depend on motor performance and teamwork,

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Publication Date
Sun Nov 23 2025
Journal Name
Yarsi Medical And Dental Science - Yasmine Journal
Oral Biopsy: Evaluating Awareness and Knowledge Among Dental Students at University of Baghdad: Oral Biopsy: Evaluating Awareness and Knowledge Among Dental Students
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Introduction Oral biopsy is a fundamental diagnostic procedure in dentistry, essential for the early detection of oral cancer and other pathologies. While theoretical knowledge is a core component of dental education, the translation of this knowledge into clinical confidence and practical ability is critical for patient care. Objective: : evaluate the awareness, knowledge, and self-perceived ability to perform oral biopsies Material and Methods: A cross-sectional study was conducted among dental students. Participants (n=110) comprising 14 multiple-choice questions assessing key variables: knowledge of biopsy principles, techniques, lesion identification, specimen preservation, and ability to perform the procedure Results: While theoretica

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Publication Date
Sun May 10 2020
Journal Name
Baghdad Science Journal
Prevalence of Quinolones Resistance Proteins Encoding Genes (qnr genes) and Co-Resistance with β-lactams among Klebsiella pneumoniae Isolates from Iraqi Patients
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This study investigated the prevalence of quinolones resistance proteins encoding genes (qnr genes) and co-resistance for fluoroquinolones and β-lactams among clinical isolates of Klebsiella pneumoniae.  Out of 150 clinical samples, 50 isolates of K. pneumoniae were identified according to morphological and biochemical properties. These isolates were collected from different clinical samples, including 15 (30%) urine, 12 (24%) blood, 9 (18%) sputum, 9 (18%) wound, and 5 (10%) burn. The minimum inhibitory concentrations (MICs) assay revealed that 15 (30%) of isolates were resistant to ciprofloxacin (≥4µg/ml), 11 (22%) of isolates were resistant to levofloxacin (≥8 µg/ml), 21 (42%) of isolates were re

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Publication Date
Sat Nov 13 2021
Journal Name
International Journal Of Pharmacy Practice
A comprehensive review of drivers influencing flu vaccine acceptance in the Middle East over the last six years: using Health Belief Model
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Abstract<sec> <title>Objectives

The objectives of this study were to review the literature covering the perceptions about influenza vaccines in the Middle East and to determine factors influencing the acceptance of vaccination using Health Belief Model (HBM).

Methods

A comprehensive literature search was performed utilizing PubMed and Google Scholar databases. Three keywords were used: Influenza vaccine, perceptions and Middle East. Empirical studies that dealt with people/healthcare worker (HCW) perceptio

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Publication Date
Thu Aug 31 2017
Journal Name
Journal Of Engineering
The Effect of Cyclic Bending Loads on Crack Growth in Pipes for Inclined and Transverse Cracks with or Without Internal Pulsing Pressure
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In the present research a new test rig has been proposed to be suitable for different cyclic loads such as cyclic bending, cyclic torsion, proportional and non proportional loads. In this work the efforts were concentrated on the cyclic bending loads concerning cracked pipes with or without internal pulsing pressure to study crack propagation in small bore pipes (up to 1'') for transverse or inclined cracks. The rig simulates the real service conditions under different stresses by means the least dangerous case will be suggested, so the experiments were considered for copper pipe, and the results have been tabulated and drawn to demonstrate the crack growth behavior as well as to justify the outcomes practically, consequently the durabil

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Publication Date
Sun Jan 02 2022
Journal Name
Journal Of The College Of Languages (jcl)
The Argumentative Elements Of Discours In The Plague For Albert Camus: Les éléments argumentatifs dans le discours de La Peste d’Albert Camus
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Argumentation is not a contemporary, yet a deep rooted intellectual phenomenon dates back to Romans and Greeks times. The argumentative elements ,the author is trying to convey to the reader, are  linguistic procedures aim at persuading and being persuaded of what is true. The present study traces, through Camus’ novel The plague, the best method to construct argumentative techniques used to express the author’s deep philosophies.

Résumé        

          L’argumentation n’est pas un phénomène intellectuel nouveau, ses origines reviennent aux savants grecs et romains. Elle est une act

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