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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
Thu Dec 01 2011
Journal Name
Journal Of Engineering
An Experimental Investigation on Fatigue Properties of AA3003-H14 Aluminum alloy Friction Stir Welds
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AA3003-H14 aluminum alloy plates were welded by friction stir welding and TIG welding.
Fatigue properties of the welded joints were evaluated based on the superior tensile properties for
FSW at 1500 rpm rotational speed and 80 mm/min welding speed. However, there is not much
information available on effect of welding parameters with evolution of fatigue life of friction stir
welds. The present study experimentally analyzed fatigue properties for base, FSW, and TIG welds
of AA 3003-H14 aluminum alloy. Fatigue properties of FSW joints were slightly lower than the
base metal and higher than TIG welding.

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Publication Date
Sat Aug 31 2019
Journal Name
Iraqi Journal Of Physics
Investigation the effect of post deposition thermal treatment on properties P3HT and P3HT:PCBM blend.
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  This work reports the study of heat treatment effect on the structural, morphological, optical and electrical properties of poly [3-hexylthiophene] and its blend with [6,6]-phenyl C61 butyric acid methyl ester ( P3HT:PC61BM). X-ray diffraction (XRD) measurements show that the crystallinity of the films increased with annealing. The evaluation of surface roughness and morphology was investigated using atomic force microscope (AFM), and field emission scanning microscope(FESEM). The optical properties were emphasized a strong optical absorption of P3HT compared with the blend. Hall effect measurement was used to study the electrical properties which revealed there is an increase in the electrical conductivity and Hall mobility of th

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Publication Date
Mon Jul 31 2017
Journal Name
Journal Of Engineering
Experimental and Numerical Investigation of Hyper Composite Plate Structure Under Thermal and Mechanical Loadings
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Publication Date
Thu Apr 01 2021
Journal Name
Journal Of Bridge Engineering
Experimental Investigation of Curved-Soffit RC Bridge Girders Strengthened in Flexure Using CFRP Composites
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Publication Date
Wed Feb 05 2020
Journal Name
Journal Of Physical Education
The Effect of Group Investigation Model on Learning overhead and underarm Pass in Volleyball
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Volleyball is one of the sports that require physical and skill abilities thus many teaching models appeared to teach these abilities like group investigation model. The research aimed at identifying the effect of group investigation model on learning underarm and overhead passing in volleyball. The researchers hypothesized statistical differences between pre and posttests in learning underarm and overhead passing in volleyball as well as differences in posttests of controlling and experimental groups in learning underarm and overhead passing in volleyball. The researcher used the experimental method on (30) second year female students of physical education and sport sciences college/ university of Baghdad. Group investigation model was app

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Publication Date
Tue Oct 01 2024
Journal Name
Journal Of Physics: Conference Series
A comparative Analytical Investigation of Different Geomagnetic Storms During Solar Cycles 23 and 24
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Abstract<p>In this work, the geomagnetic storms that occurred during solar cycles 23 and 24 were classified based on the value of the Disturbance Storm Time index (Dst), which was considered an indicator of the strength of geomagnetic conditions. The special criterion of Dst >-50 nT was adopted in the classification process of the geomagnetic storms based on the minimum daily value of the Dst-index. The number of geomagnetic storms that occurred during the study period was counted according to the adopted criteria, including moderate storms with (Dst >-50 nT), strong storms with (Dst >-100 nT), severe storms with (Dst >-200 nT), and great storms with (Dst >-350 nT). The statistica</p> ... Show More
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Publication Date
Thu Oct 31 2013
Journal Name
Al-khwarizmi Engineering Journal
An Investigation Study of Thinning Distribution in Single Point Incremental Forming Using FEM Analysis
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Single Point Incremental Forming (SPIF) is a forming technique of sheet material based on layered manufacturing principles. The sheet part is locally deformed through horizontal slices. The moving locus of forming tool (called as toolpath) in these slices constructed to the finished part was performed by the CNC technology. The toolpath was created directly from CAD model of final product. The forming tool is a Ball-end forming tool, which was moved along the toolpath while the edges of sheet material were clamped rigidly on fixture.

This paper presented an investigation study of thinning distribution of a conical shapes carried out by incremental forming and the validation of finite element method to evaluate the limits of the p

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Publication Date
Wed Feb 05 2003
Journal Name
. Sc. Conf. Of The College 5th Of Eng. Univ. Of Baghdad 2003
COMPUTATIONAL AND EXPERIMENTAL INVESTIGATION OF THE AERODYNAMIC CHARACTERISTICS FOR A FORWARD SWEPT WING AIRCRAFT
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The aerodynamic characteristics of the forward swept wing aircraft have been studied theoretically and experimentally. Low order panel method with the Dirichlet boundary condition have been used to solve the case of the steady, inviscid and compressible flow. Experimentally, a model was manufactured from wood to carry out the tests. The primary objective of the experimental work was the measurements of the wake dimensions and orientation, velocity defect along the wake and the wake thickness. A blower type low speed (open jet) wind tunnel was used in the experimental work. The mean velocity at the test section was (9.3 m/s) and the Reynolds number based on the mean aerodynamic chord and the mean velocity was (0.46x105). The measurements sho

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Publication Date
Wed May 01 2019
Journal Name
Ieee International Electric Machines & Drives Conference (iemdc)
An Investigation of Short Translator Linear Machines for Use in a Free Piston Engine
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Publication Date
Thu Oct 01 2015
Journal Name
American Research Thoughts
Investigation of some Oral Strategies and their Development to the Iraqi EFL Learners` Performance.
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The present study deals with the effect of teaching oral Communication Strategies on English language learners. The use of oral communication strategies not only solves learners’ communication problems, but also enhances the learner’s interaction in target language, which in turn, improves their oral proficiency .The sample of this study is EFL students in the first stage at the Department of English Language, morning studies, College of Education /Ibn-Rushd .The sample of the study consists of (60) students distributed on experimental group(A) includes (30) students, and (30) students as control group(B). In order to achieve the aim of the study, and to gain a closer idea about the impact of teaching oral Communication Strategies on th

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