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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
Sun May 01 2016
Journal Name
Journal Of Engineering
Encoding of QC-LDPC Codes of Rank Deficient Parity Matrix
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The encoding of long low density parity check (LDPC) codes presents a challenge compared to its decoding. The Quasi Cyclic (QC) LDPC codes offer the advantage for reducing the complexity for both encoding and decoding due to its QC structure. Most QC-LDPC codes have rank deficient parity matrix and this introduces extra complexity over the codes with full rank parity matrix. In this paper an encoding scheme of QC-LDPC codes is presented that is suitable for codes with full rank parity matrix and rank deficient parity matrx. The extra effort required by the codes with rank deficient parity matrix over the codes of full rank parity matrix is investigated.

 

 

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Publication Date
Sat Jun 30 2018
Journal Name
College Of Islamic Sciences
Location and level of ambition At the University of Sulaimaniyah
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The study of the concept of the location of control and the level of ambition of important topics and represent a large area in the educational and psychological sciences, which gives importance to this study at the present time, is the complex and difficult conditions experienced by the Kurdish man, all age groups or social segments, and because of the changes It increases the rate of stress and hardship, which in turn raises the rate of psychological and physical disorder to prevent a healthy individual's compatibility, which has a fundamental impact on their personality, leading to a defect in some important organs of the personality.
   The research aimed to identify the location of control among students of the Uni

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Publication Date
Sat Jan 01 2011
Journal Name
Journal Of Engineering
ORGANOCLAY FOR ADSORPTION OF BINARY SYSTEM OF POLLUTANTS FROM WASTEWATER
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single and binary competitive sorption of phenol and p-nitrophenol onto clay modified with
quaternary ammonium (Hexadecyltrimethyl ammonium ) was investigated to obtain the
adsorption isotherms constants for each solutes. The modified clay was prepared from
blending of local bentonite with quaternary ammonium . The organoclay was characterized
by cation exchange capacity. and surface area. The results show that paranitrophenol is
being adsorbed faster than phenol . The experimental data for each solute was fitted well with
the Freundlich isotherm model for single solute and with the combination of Freundlich-
Langmuier model for binary system .

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Publication Date
Thu Jan 31 2019
Journal Name
Journal Of Engineering
Experimental Study of Solar Still Under Influence of Various Conditions
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In the present work, experimental tests was done to explain the effect of insulation and water level on the yield output. Linear basin, single slope solar still used to do this purpose. The test was done from May to August 2017 in Mosul City-Iraq (Latitude: Longitude: Elevation: 200 m, and  South-East face). Experimental results showed that the yield output of the still increased by 20.785% and 19.864% in case of using thermal insulation at 4cm and 5cm respectively, also the yield output decrease by 15.134% as the water level increase from 4 to 5cm, with the presence of insulation and 14.147% without it. It has been conclude that the insulation and water level play important role in the process of passive

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Publication Date
Tue Jul 01 2003
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
THE ABDOMINAL NERVE GANGLIA OF SOME CARABIDAE (COLEOPTERA) OF IRAQ
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The abdominal nerve cord of some species of Iraq Carabids has been studied to evaluate
the variation in the number of the abdominal ganglia among the species and to find out
relation of these variations with the classical taxonomy of the family Carabidae into tribes.

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Publication Date
Fri Jun 01 2007
Journal Name
Al-khwarizmi Engineering Journal
Effect of the Mechanical and Thermal Stresses of Rotating Blades
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         Rotating blades are the important parts in gas turbines. Hence, an accurate mathematical estimation (F.E.M) of the stresses and deformations characteristics was required in the design applications to avoid failure. In recent year’s there are researchers interest in the effect of temperature on solid bodies has greatly increased, The main of this study investigated the thermal and rotational effects.  So, the thermal stresses due to high pressure and temperature are studies, also determine the steady state stresses and deformations of rotating blades due to mechanical effect. Many parameters such as thickness and centre of rotating are investigated in this paper. The

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Publication Date
Sun Jan 08 2023
Journal Name
Journal Of Planner And Development
Analysis of Walking Accessibility of Community Park in Duhok City
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Research studies show that urban green spaces promote physical activity, the health of urban residents, and psychological well-being. Taking the community park in Duhok city as the research object, the spatial service area in terms of accessibility of to the Community Park under the mode of pedestrian transportation is analyzed by using the network analysis service area function of the geographic information system (GIS). The results show that under the walking mode in the research area, Parks are concentrated in the north and south of the city, but community parks are few in disadvantaged neighborhoods. In addition, there is a significant disparity between the number of community parks and the number of communities. Only 11 communities

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Publication Date
Wed Dec 30 2015
Journal Name
College Of Islamic Sciences
Methodology of the concept of sovereignty in contemporary Islamic thought
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The methodology of the concept of sovereignty in contemporary Islamic thought

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
The Effect Of Thickness on The Optical Properties Of ZnS
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Zinc sulfide(ZnS) thin films of different thickness were deposited on corning glass with the substrate kept at room temperature and high vacuum using thermal evaporation technique.the film properties investigated include their absorbance/transmittance/reflectance spectra,band gap,refractive index,extinction coefficient,complex dielectric constant and thickness.The films were found to exhibt high transmittance(59-98%) ,low absorbance and low reflectance in the visible/near infrared region up to 900 nm..However, the absorbance of the films were found to be high in the ultra violet region with peak around 360 nm.The thickness(using optical interference fringes method) of various films thichness(100,200,300,and 400) nm.The band gap meas

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Publication Date
Wed Jul 01 2015
Journal Name
Political Sciences Journal
Factors affecting the future of Iraq's production of crude oil
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As the major role of oil sector in financing and development of Iraqi economy this study tried to research on the factors which influencing the future of oil production in Iraq and for that study addressed the hypothesis (the production and export of crude oil in Iraq , influenced by many factors divided into internal and external factors this factors shared the effect varies in the size of their participation and runs from different sectors economic , political and social , in order to test the study hypothesis study addressed the subject of three axes(an overview of the history and facts of crude oil production in Iraq and factors internal Affecting the future of oil production in Iraq and external factors affecting the future

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