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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 Dec 14 2020
Journal Name
Plos One
Healthy lifestyle behaviors are major predictors of mental wellbeing during COVID-19 pandemic confinement: A study on adult Arabs in higher educational institutions
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Background

In the past infectious diseases affected the quality of lifestyle during home confinement. The study conducted examines the influence of home confinement during the COVID-19 pandemic outbreak on lifestyle, mental wellbeing, nutritional status, and sleeping pattern.

Method

An online multicategorical questionnaire was distributed to collect demographic information combined with the following tools: Food Frequency Questionnaire (FFQ), International Physical Activity Questionnaire (IPAQ), WHO-5 wellbeing score, and Pittsburgh Sleep Quality Index (PSQI). A snowball non-discriminate sampling procedure was

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Publication Date
Tue Mar 30 2021
Journal Name
Iraqi Journal Of Science
Electrochemical Polymerization and Biological Activity of 4-(Nicotinamido)-4-Oxo-2-Butenoic Acid as An Anticorrosion Coating on A 316L Stainless Steel Surface
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In this study, poly4-(nicotinamido)-4-oxo-2-butenoic acid (PNOE) was prepared by the electro polymerization of 4-(nicotinamido)-4-oxo-2-butenoic acid (NOE) monomer on a 316 stainless steel (St.St) which acts as an anticorrosion coating.  Fourier transforms infrared (FTIR), atomic force microscopy (AFM), scanning electron microscopy (SEM), and cyclic voltammetry were used to diagnose the structure and the properties of the prepared polymer layer. The corrosion behavior of the uncoated and coated 316  St.St were evaluated by using an electro chemical polarization technique in 0.2 M hydrochloric acid  solution as a corrosive medium at a temperature range of 293 to 323 K. Nano materials, such as nano ZnO and graphene were added in di

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Publication Date
Sun Mar 04 2012
Journal Name
Baghdad Science Journal
Evaluation of cellular immune response in Golden Hamsters experimentally infected with Leishmania donovani comparing with cellular immune response against chicken Red Blood Cells.
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The Evaluation of the immune response in Golden Hamsters experimentally infected with Leishmania donovani was determined in this study, particularly, the cellular immune response. Follow up has maintained to determine the Delayed Type of Hypersensitivity using skin test both in infected and control lab animals. Chicken red blood cells were used as a parameter to evaluate the immune system; they are dull and have the ability of immunization. Two concentrations of chicken R.B.C were examined to determine which gives the higher titration in Hamsters and those were 1.5 X 109 cell/ml and 3 X 109 cell/ml , the second concentration gave the maximum titration where then used in this work. After sensitization with Chicken R.B.C for both infected a

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Publication Date
Sun Jan 17 2021
Journal Name
Academic Journal Of Interdisciplinary Studies
Employees Retention Strategy and its Impact on Organizational Memory: An Exploratory Research for the opinion of Faculty Members at Private Colleges on Baghdad
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The research aims to determine the impact of employees’ retention strategy on organizational memory. This research is historical, descriptive, and analytical. The sample consists of 158 faculty members in five private colleges in Baghdad. The technique used to analyze the data is SEM (Structural Equation Modeling), and SPSS (Statistical Package for the Social Sciences). The research concludes that the employees retaining strategy plays a vital role in retaining employees and hence maintains organizational memory. The findings and recommendations of this research assure the administrations of private colleges that employees retention strategy play a vital role in retaining its employee and hence maintains organizational memory. T

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Publication Date
Thu Oct 12 2017
Journal Name
Iraqi Journal Of Agricultural Sciences
THE BIOLOGICAL EFFECTIVENESS OF GIBBERELLIC ACID SEEDS SOAKING AND FOLIAR TO ABSCISIC ACID IN THE GROWTH , ANISE OIL YIELD AND ITS CHEMICAL CONTENT
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A field experiment was carried out during two winter season 2013, 2014 at the field of the Department of Field Crops, College of Agriculture, University of Baghdad, to study the effect of seeds soaking with Gibberellic acid and foliar with Abscisic Acid on the growth, yield, and content of Anise oil seeds using factorial experiment within RCBD design with three replicates. The seeds was treated within GA3 were soaked with two concentrations of  30, and 60 mg. litter-1 in addition to without soaking and the code has been B0 , B1 , B2 overlapped these transactions with two concentrations of Abscisic Acid  3, and 6 mg. litter-1 in addition to without foliar A0 , A1 , A2The seeds to be treated  with GA3 are soaked for 24 hours prior

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Publication Date
Thu Jun 30 2016
Journal Name
Al-kindy College Medical Journal
Adenoidectomy with Myringotomy and Tympanostomy Tube Versus Adenoidectomy with Myringotomy in Treatment of Otitis Media with Effusion in 5-7 Years Old Children
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Background: Adenoiditis is a common cause of otitis media with effusion (OME) in children & perhaps OME is one of the most common diseases leads to hearing impairment in children with subsequent impairment of speech development & learning difficulties , however, treatment remains controversial. Objectives: To evaluate if there is a significant advantage of tympanostomy tube insertion in association with adenoidectomy over adenoidectomy in association with myringotomy alone in treatment of children with OMEType of the study: This is a prospective study. Patients & methods: The study consisted from 63 children diagnosed as cases of bilateral OME & variable degrees of adenoid hypertrophy. The patients were divided randomly i

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Publication Date
Thu Mar 19 2015
Journal Name
Al-academy
The Significance of the Folk Symbols and Their Influence on The National Identity (Chosen samples from the Contemporary Iraqi Pottery): زينب كاظم صالح
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The contemporary art culture is considered a resultant of preceding human civilizations from the early days. At the same time, it got closer to the local privacy, because the contemporary Iraqi potter worked hard to create new art, refusing to base his art on the early works, creating art pieces that contains properties to inherited art and their form significance, in order to create a new identity of his own, bringing an empowerment to his deepened civilization, with the goal to create national identity ideas from one hand, and entity and locality from another. Europeans also followed the direction of our civilization, such as (Picasso, Henry Moore, Barbra Hurth, Brankouzi, Hans Arp,..etc). From this point of view comes the importance o

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Publication Date
Thu Nov 06 2025
Journal Name
Al–bahith Al–a'alami
ACADEMIC TRAINING IN MEDIA AND COMMUNICATION SCIENCES AND ITS RELATIONSHIP TO MEDIA PRACTICE:: (Reading In The Nature Of The Relationship: Integration Or Separation)
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The aim of this scientific study is to diagnose the nature of the relationship between academic education in the field of media, communication and media practice. The university offers theoretical and practical lessons to students on the concepts of communication sciences, theories, models, legislations, ethics, and techniques over three years or more. And the diploma in the field of communication and Media Sciences gives students the opportunity to work in the field of journalism and media in the future, this is what many academics and media thinkers in Algeria believe, while another trend sees the exact opposite: The study of information and communication sciences within the university in the form of theoretical lessons cannot contribu

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Publication Date
Tue Sep 11 2018
Journal Name
Iraqi Journal Of Physics
Synthesis and characterization of ligands derived 2-hydroxy-1- naphthaldehyde and their complexes with divalent metal ions (Mn+2, Fe+2, Ni +2)
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In this work, Schiff base ligands L1: N, N-bis (2-hydroxy-1-naphthaldehyde) hydrazine, L2: N, N-bis (salicylidene) hydrazine, and L3:N –salicylidene- hydrazine were synthesized by condensation reaction. The prepared ligands were reacted with specific divalent metal ions such as (Mn2+, Fe2+, Ni2+) to prepare their complexes. The ligands and complexes were characterized by C.H.N, FT-IR, UV-Vis, solubility, melting point and magnetic susceptibility measurements. The results show that the ligands of complexes (Mn2+, Fe2+) have octahedral geometry while the ligands of complexes (Ni2+) have tetrahedral geometry.

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Publication Date
Fri Sep 15 2023
Journal Name
Al-academy
The plastic dimension of the balcony scene in the movie (Romeo and Juliet) and its relationship to the movie and theatrical original text
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This research deals with one scene from the movie Romeo and Juliet, which is the balcony scene, due to the importance of this scene in the formation of the construction of the subsequent events of the movie.

The first chapter contained the methodological framework of the research, where the research problem was identified in how Zeffirelli dealt with the balcony scene in the play Romeo and Juliet and enriched it in the cinematic language with a comparison with the original text of the scene. In the balcony scene with comparative parts between the film and the text and the limits of the research that was limited to the film Zeffirelli and the translated text by Munis Taha Hussein.

The second chapter contained the theoretic

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