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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 Jan 01 2024
Journal Name
Iraqi Journal Of Hematology
Evaluation of Vitamin D level in thalassemia patients: The experience of a single center
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Publication Date
Mon Sep 10 2018
Journal Name
Iraqi Journal Of Physics
Improvement of superconducting parameters of Bi1.6Pb0.4Sr 2Ca 2Cu 3O10+ δ added with Au nanoparticles
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Samples of Bi1.6Pb0.4Sr2Ca2Cu3O10+δ superconductor were prepared by solid-state reaction method to study the effects of gold nanoparticles addition to the superconducting system, Nano-Au was introduced by small weight percentages (0.25, 0.50, 0.75, 1.0, and 1.25 weight %). Phase identification and microstructural
characterization of the samples were investigated using XRD and SEM. Moreover, DC electrical resistivity as a function of the temperature, critical current density Jc, AC magnetic susceptibility, and DC magnetization measurements were carried to evaluate the relative performance of samples. x-ray diffraction analysis showed that both (Bi,Pb)-2223 and Bi-2212 phases coexist in the samples having an orthorhombic crystal struct

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Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
The role of Electronic human resources management practices in the sustainability of knowledge capital
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Abstract:

The aim of the research is to highlight the role of electronic human resources management practices in the sustainability of knowledge capital as one of its success factors, as well as the diagnosis and interpretation of the relationship between research variables and their dimensions. The research problem is that the University of Babil implements some electronic human resources management practices not in a complete way, The level of its application and the problems it faces, as well as the extent to which these practices reflect the knowledge capital and sustainability in the university, and highlights the importance of research as it is concerned with the electronic aspects and achieve the competitive advant

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Publication Date
Mon Jan 01 2024
Journal Name
Sustainable Construction Materials And Technologies (scmt)
TRIAXIAL TEST OF HYDRATED LIME ON THE MECHANICAL PROPERTIES OF HOT MIX ASPHALT CONCRETE
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This paper reports on the experimental study, which conducted a series of triaxial tests for the asphalt concrete using hydrated lime as a mineral additive. Three HMA mixes, prepared by the specification for wearing, levelling and base layers, were studied under three different temperatures. The test results have demonstrated that, compared with the control mixes excluding HL, the permanent deformation resistance of the HL modified mixes has significant improvement. The deformation has been reduced at the same load repetition number, meanwhile the flow number has been considerably increased. The degree of improvement in permanent deformation resistance using HL is more pronounced at high stress deviation states and high temperature.

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Publication Date
Sun Dec 04 2011
Journal Name
Baghdad Science Journal
Effect of Hyper and Hypothyroidism on Lipid Profile and Liver Function of Male Rats
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This study was designed to investigate the effect of thyroid hormone disturbance on lipids profiles and liver functions. Eighteen mature male rats Rattus norvegicus were divided into three groups. The first and the second groups were injected subcutaneously with thyroxine (T4) and carbimazol (both at 600 µg/kg BW) respectively on alternate days, to produce recurrent periods of hyper and hypothyroidism .The control group which is the third group was injected with physiological saline. The process continued 4 weeks, after that, injection, blood specimens were collected to estimate serum levels of T3 and T4, Total cholesterol (TC), Triglycerides (TG), High density lipoprotein cholesterol (HDL-C), Low density lipoprotein cholesterol (LDL-C) an

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Publication Date
Wed Jan 01 2025
Journal Name
E3s Web Of Conferences
The impact of military waste on Iraq’s waters: The case of the Jassim River
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This article aims to investigate how war contributes to the pollution of water bodies with harmful substances including heavy metals and toxic substances. The paper explains how these pollutants, carelessly dumped by military operations, have severely damaged the water quality of rivers and lakes all across Iraq. Based on the Jassim River as case study, the paper shows a close relationship between military operations and pollution. Shown is the effects of this pollution on local ecosystems like fish and wildlife, and human population, dependent on the river for drinking, irrigation, and other basic needs. The article reveals the problem of military waste in Iraq, focusing on the absence of satisfactory waste disposal techniques and

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Publication Date
Sun Sep 11 2022
Journal Name
Mathematics
Modeling and Analysis of the Influence of Fear on a Harvested Food Web System
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The food web is a crucial conceptual tool for understanding the dynamics of energy transfer in an ecosystem, as well as the feeding relationships among species within a community. It also reveals species interactions and community structure. As a result, an ecological food web system with two predators competing for prey while experiencing fear was developed and studied. The properties of the solution of the system were determined, and all potential equilibrium points were identified. The dynamic behavior in their immediate surroundings was examined both locally and globally. The system’s persistence demands were calculated, and all conceivable forms of local bifurcations were investigated. With the aid of MATLAB, a numerical simu

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Publication Date
Tue Oct 30 2018
Journal Name
Iraqi Journal Of Physics
Evaluation of radioactivity of cereals and legumes using a nuclear impact detector CN-85
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The research aims to evaluate the radioactivity in elected samples of cereals and legume which are wide human consumption in Iraq using Nuclear Track Detectors (NTDs) model CN-85.
The samples were prepared scientifically according to references in this field. After 150 days of exposure, the detector were collected and chemically treated according to scientific sources (etching chemical), nuclear effects have been calculated using the optical microscope.
Radon (222Rn) concentration and uranium (238U) were calculated in unit Bq/m3 and (ppm), the results indicate that the highest concentration of radon and uranium was in yellow corn where the concentration of radon was 137.17×102 Bq/m3 and uranium concentration 2.63 (ppm). The lowest

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Publication Date
Wed Aug 31 2022
Journal Name
Mathematical Modelling Of Engineering Problems
Evaluation of Al-Ishaqi Irrigation Project: A Case Study Eastern Canal of the Project
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An evaluation the performance of the irrigation system for the Al-Ishaqi irrigation project for the Eastern Canal was conducted to identify management strategies that can be used to improve the operation and performance of the irrigation system. The study area is located in Salah al-Din G.0overnorate, Iraq. The field work included determining the moisture content of the soil before and after irrigation, measuring the inflow of the field to find the depth of the applied water, field monitoring, and measuring the depth of the root zone for each irrigation process. Field measurements showed that the average efficiency of water application for the two fields (A, and B) are 59.81% and 38.6%, respectively. The results of the efficiency of

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Publication Date
Mon Jan 01 2018
Journal Name
International Journal Of Surgery Open
Effectiveness of conservative management of uncomplicated acute appendicitis: A single hospital based prospective study
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<bold>ABSTRACT</bold> <sec> <title>Background:

Acute appendicitis is one of the commonest causes of acute abdomen. There is a wide discussion and controversy on the surgical and nonsurgical treatment of acute uncomplicated appendicitis. The aim of this study was to evaluate the efficacy and outcomes of the conservative management of selected cases of acute appendicitis with an antibiotic first plan.

Patients and methods:

This was a single hospital-based prospective study with a durat

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