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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
Sat Aug 01 2020
Journal Name
Surgical Neurology International
Unilateral absence of the internal carotid artery associated with anterior communicating artery aneurysms: Systematic review and a proposed management algorithm
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Background:

Absence or hypoplasia of the internal carotid artery (ICA) is a rare congenital anomaly that is mostly unilateral and highly associated with other intracranial vascular anomalies, of which saccular aneurysm is the most common. Blood flow to the circulation of the affected side is maintained by collateral pathways, some of which include the anterior communicating artery (Acom) as part of their anatomy. Therefore, temporary clipping during microsurgery on Acom aneurysms in patients with unilateral ICA anomalies could jeopardize these collaterals and place the patient at risk of ischemic damage. In this paper, we review the literature on cases with a unilaterally absent ICA associa

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Publication Date
Sun Dec 06 2015
Journal Name
Baghdad Science Journal
A Qualitative Study of Epiphytic Algae (Diatom) on Some Aquatic Plants in Al-Auda Marshes Within Maysan Province / Southern Iraq
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The study conducted on the compositions of epiphytic diatoms on three taxa of aquatic plants were selected (Phragmites australis Trin ex stand , Ceratophyllum demersum L. and Typha domengensis Pers) in three sites within Al-Auda Marsh, from autumn 2013 to summer 2014 . The study was measured physical and chemical factors of all the study sites, such as: air temperature, power of hydrogen (pH), electrical conductivity (EC), salinity (S‰), total hardness(TH), dissolved oxygen (DO), and plant nutrient. The results showed that water of marsh was oxygenated and it was very hard. A total of 111 taxa of phytoplankton were identified, which belonged to 13 families and 26 genus (one family and two genus of centric diatoms, 12 families and 26 ge

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Publication Date
Mon Nov 01 2021
Journal Name
Journal Of Physics: Conference Series
Neural Network Model for Synthesis of Thermally Sprayed (AI/AI<sub>2</sub>O<sub>3</sub>) Composite Protective Coatings
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Abstract<p>Al<sub>2</sub>O<sub>3</sub> and Al<sub>2</sub>O<sub>3</sub>–Al composite coatings were deposited on steel specimens using Oxy-acetylene gas thermal spray gun. Alumina was mixed with Aluminum in six groups of concentrations (0, 5, 10,12,15 and 20% ) Al2O3, Specimens were tested for corrosion using Potentiodynamic polarization technique. Further tests were conducted for the effect of temperature on polarization curve and the hardness tests for the coated specimens. At first, Modelling was carried out using MINITAB-19, least square method, as a 2nd degree nonlinear model, bad results were achieved because of the high nonlinearity. Better result w</p> ... Show More
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Publication Date
Mon Apr 03 2023
Journal Name
Journal Of Educational And Psychological Researches
Critical Thinking Skills of A’Sharqiah University Students According to California Critical Thinking Skills Test and Its Relationship to Some Variables
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Abstract

The research aims to measure the level of critical thinking skills among students of A’Sharqiah University in the Sultanate of Oman, as well as identify the level of their availability based on the variables: gender, academic level, school year, cumulative average, and general diploma / high school ratio. The researchers used the descriptive approach. To achieve the objectives of the study, they used The California Test for Critical Thinking Skills Picture (A) after evaluation (Farraj, 2006). It was applied to a sample of (487) students from A’sharqiah University. The results of the study found that the critical thinking skills of A’sharqiah University students are below the educationally acceptabl

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Publication Date
Sat Dec 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Causal relationship between sugar prices, imported sun flower oil, crude oil prices and the exchange rate of the Iraqi dinar
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Abstract

The increasing of some traded Agricultural crops prices coincide with the increasing of crude oil prices in global market since the beginning of 21st century which indicate the possibility of short run and long run causality relation between the imported economic variables. The study aims to analysis the causality effects between some of Agricultural crops prices imported by Iraq and the prices of crude oil and Iraq dinar exchange rate   in global markets for period (2004:1 -2016:4) theory for developing the adequate price and economic police for Iraqi economic sector. The results show the existence of short- run and long- run between the eco

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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The market value between the two dilemmas of profit distribution and retention: an analytical study in the Iraqi stock market
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Abstract:

             The distribution or retention of profits is the third decision among financial management decisions in terms of priority, whether at the level of theory or practice, as the issue of distribution or retention is multi-party in terms of influence and impact, as determining the optimal percentage for each component is still the subject of intellectual debate because these decisions are linked to the future of the organization and several considerations, The research focus on the nature of the policies followed by the Iraqi banking sector As the sample chosen by the intentional sampling method was represented by the Commercial Bank of

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Theoretical Study of 4-(2-methyl-4-oxoquinazoline-3(4H)-yl) Benzoic acid with Some Transition Metal Ions
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New complexes of the type [ML2(H2O)2] ,[FeL2(H2O)Cl] and [VOL2] were M=Co(II),Ni(II) and Cu(II) ,L=4-(2-methyl-4-oxoquinazoline-3(4H)-yl) benzoic acid were synthesized and characterized by element analysis, magnetic susceptibility ,molar conductance ,FT-IR and UV-visible. The studies indicate that the L acts as doubly monodentate bridge for metal ions and form mononuclear complexes. The complexes are found to be octahedral except V(IV) complex is square pyrimde shape . The structural geometries of compounds were also suggested in gas phase by theoretical treatments, using Hyper chem-6 program for the molecular mechanics and semi-empirical calculations, addition heat of formation(?Hf ?) and binding energy (?Eb)for the free ligan

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Publication Date
Mon Mar 07 2022
Journal Name
Journal Of Educational And Psychological Researches
The Structural Model of the Relationship between Emotional Creativity and Self-Efficacy among Students at the Preparatory Year Tabuk University
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This research aimed to identify the structural model of the relationship between emotional creativity and self-efficacy among male and female students of the preparatory year at Tabuk University. The current study adopted the descriptive correlational approach, as it is appropriate to the nature of the study. The study tools contained (60) items that measure the relationship between emotional creativity and self-efficacy among the male and female students of the preparatory year at Tabuk University. The study sample was chosen by the stratified random method of the study community, where the study sample reached (183) male and female students of the preparatory year at the University of Tabuk. The results of the study showed that there a

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Publication Date
Tue Nov 01 2016
Journal Name
Journal Of Engineering
Ultrafiltration and Reverse Osmosis Membranes for Treating Wastewater Effluent from Gas Turbine Power Plants using the Statistical Method of Taguchi
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A study on the treatment and reuse of oily wastewater generated from the process of fuel oil treatment of gas turbine power plant was performed. The feasibility of using hollow fiber ultrafiltration (UF) membrane and reverse osmosis (RO) membrane type polyamide thin-film composite in a pilot plant was investigated. Three different variables: pressure (0.5, 1, 1.5 and 2 bars), oil content (10, 20, 30 and 40 ppm), and temperature (15, 20, 30 and 40 ᵒC) were employed in the UF process while TDS was kept constant at 150 ppm. Four different variables: pressure (5, 6, 7 and 8 bar), oil content (2.5, 5, 7.5 and 10 ppm), total dissolved solids (TDS) (100, 200,300 and 400 ppm), and temperature (15, 20, 30 and 40 ᵒC) were mani

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Publication Date
Thu Feb 01 2024
Journal Name
Baghdad Science Journal
Mangrove Landscaping As An Adaptation Pattern To Reduce The Impact of Climate Change in Segara Anakan Lagoon, Cilacap Regency Indonesia
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Mangrove landscaping in the Segara Anakan Lagoon (SAL) is an adaptation pattern of mangrove ecosystems to live and grow in unstable areas. This research aimed to develop a mangrove landscape to mitigate the impacts of ocean waves, currents, and inundation due to climate change. The study was conducted in SAL and Cilacap Coast (CC) using the environmental properties and climate change data. The data obtained were analyzed using mapping and trendline analyses. The results showed that mangrove landscaping in Segara Anakan had four zones with Nypa frutican, Rhizophora styllosa, Aegiceras corniculatum, Rhizophora apiculata, Avicennia marina, Sonneratia alba identified as the best adaptation of mangrove species. Climate change give a high impa

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