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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
Tue Nov 08 2022
Journal Name
Aip Conference Proceedings
Prevalence of common skin diseases among outpatients clinic of Baghdad hospital
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Abstract. Healthy skin is an important layer that gives appearance and self-confidence. The skin is affected by internal and external factors that surrounding the body. The problem of skin diseases is considered as one of the widespread diseases. The occurrence of these diseases varies from place to place depending on the nature of climate, the culture of the people, and their economic condition. A cross-sectional study of skin diseases was conducted at the dermatology centre for outpatient clinic of Baghdad hospital. The study is based on 7555 patients of all ages who are attended to this hospital in order to determine the prevalence of skin diseases. The study shows that the most prevalence skin diseases were infectious diseases with

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Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Educational And Psychological Researches
Measuring Gratitude of the Sample of Displaced people in Baghdad city
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Displacement is a problem that worries the human conscience and has received the attention of the international community. Furthermore, it has become one of the most urgent issues nowadays, especially when the number of displaced people in different countries are increased because of the causes of displacement and their political, economic, environmental, social and psychological effects. Iraq is one of the countries where displacement has taken place in several governorates, according to United Nations and International Organization for Migration (IOM), Iraq is considered the second largest country in the world after Syria in terms of the number of displaced people in 2015. Gratitude, a positive emotional response to benevolence, is a m

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Publication Date
Thu Jun 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Evaluation of the Mishrif Formation Using an Advanced Method of Interpretation
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The Mishrif Formation is one of the most important geological formations in Iraq consisting of limestone, marl, and shale layers since it is one of the main oil producing reservoirs in the country, which contain a significant portion of Iraq's oil reserves. The formation has been extensively explored and developed by the Iraqi government and international oil companies, with many oil fields being developed within it. The accurate evaluation of the Mishrif formation is key to the successful exploitation of this field. However, its geological complexity poses significant challenges for oil production, requiring advanced techniques to accurately evaluate its petrophysical properties.

   This study used advanced well-logging analysi

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Publication Date
Sun Dec 01 2019
Journal Name
2019 Ieee Asia-pacific Conference On Computer Science And Data Engineering (csde)
Effect of Clay Content on Performance of a Crushed Rock Mix
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Publication Date
Thu Mar 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Practices of managers and their impact on the contributions of personnel
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This research was based on two pillars. The first is a comparison between of research done and the result of a particular  variable of research  indebendently in the united state, and second, knowledge and determine the effect of managers  practices on the contributions of personnel. The manager and staff are considered to be the most important elements in the organization and all of them  have a duty towards the others which governed by the relationship rules of procedure of the ministry researched, on the one  hand  and the interests of the organization and hence employees , whether executives  or employees within management formations that the availability of an acceptable level of good pract

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Publication Date
Mon Oct 01 2012
Journal Name
Journal Of Engineering
Prediction of Smear Effect on the Bearing Capacity of Driven Piles
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This paper deals with prediction the effect of soil re-moulding (smear) on the ultimate bearing capacity of driven piles. The proposed method based on detecting the decrease in ultimate bearing capacity of the pile shaft (excluding the share of pile tip) after sliding downward. This was done via conducting an experimental study on three installed R.C piles in a sandy clayey silt soil. The piles were installed so that a gap space is left between its tip and the base of borehole. The piles were tested for ultimate bearing capacity according to ASTM D1143 in three stages. Between each two stages the pile was jacked inside the borehole until a sliding of about 200mm is achieved to simulate the soil re-moulding due to actual pile driving. The re

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Publication Date
Fri Oct 01 2010
Journal Name
Iraqi Journal Of Physics
The axial profile of plasma characteristics of cylindrical magnetron sputtering device
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In the present work, a d.c. magnetron sputtering system was designed and fabricated. The chamber of this system was includes from two copper coaxial cylinders where the inner one used as a cathode (target) while the outer one used as the anode with Solenoid magnetic coil located on the outer cylinder (anode). The axial profile of magnetic field for various coil current (from 2A to 14 A) are shown. The plasma characteristics in the normal glow discharge region are diagnostics by the 2.2mm diameter Langmuir probe with different length along the cathode and located at different radial positions 1cm and 2cm from the cathode surface. The result of this work shows that, the electron energy distributions at different radial positions along the

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Publication Date
Fri Mar 01 2019
Journal Name
Al-khwarizmi Engineering Journal
The Effect of Additives on The Performance of Hydrostatic Thrust Bearings
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The paper is concerned with, the behavior of the hydrostatic thrust bearings lubricated with liquid-solid lubricants using Einstein viscosity formula, and taking into account the centrifugal force resulting from high speed.  Also studied is the effect of the bearing dimensions on the pressure, flow rate, load capacity, shear stress, power consumption and stiffness.

The theoretical results show an increase in load capacity by (8.3%) in the presence of solid graphite particles with concentration of (16%) by weight as compared with pure oil, with increasing shear stress.  .

In general the performance of hydrostatic thrust bearings improve for load carrying capacity, volume flow rate,

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Publication Date
Mon Aug 01 2016
Journal Name
Journal Of Engineering
Preparation and Characterization of Activated Carbon for Adsorption of Fluoroquinolones Antibiotics
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           In this research, the preparation of a chemically activated carbon from date stones by using electric and microwave assisted K2CO3 activation was studied. The effect of radiation power, radiation time, and impregnation ratio on the yield and Iodine number on the activated carbons was investigated. The activated carbon characterizations were examined by its surface area, pore structure analysis, bulk density, moisture content, ash content, iodine number, FTIR, and scanning electron microscopy (SEM). The adsorption capacity was also studied by adsorption of fluoroquinolones antibiotics, CIP, NOR, and LEVO, by the prepared activated carbon.

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Publication Date
Tue Aug 01 2023
Journal Name
Iop Conference Series: Earth And Environmental Science
Evaluation of the Performance of a Locally Manufactured Palm Service Platform
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Abstract<p>A field experiment was carried out in one of the orchards of Al-Qassim district in Babel Governorate to find out the ability of a locally manufactured platform to serve palm trees by working in flat and uneven orchard land, palm tree heights of 4, 8, and 12 meters, and it performs pollination, pruning and harvesting services. The time of ascent and descent, the palm service, and the palm/hour productivity were measured. A randomized complete block design with three replications used a split split-plot arrangement. The nature of the land (flat or uneven) represented the main plots, the height of the palm trees (4, 8, 12) meters, the sub-plots, and the palm service operations (pollinati</p> ... Show More
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