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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
Fri Dec 31 2021
Journal Name
Iraqi Journal Of Laser
Experimental Study to The Effect of Applying Stressing Force on Etched Polarization Maintaining Fiber as Hybrid Fabry-Perot /Mach-Zehnder inline fiber interferometer
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Abstract: The increased interest in developing new photonic devices that can support high data rates, high sensitivity and fast processing capabilities for all optical communications, motivates a pre stage pulse compressor research. The pre-stage research was based on cascading single mode fiber and polarization maintaining fiber to get pulse compression with compression factor of 1.105. The demand for obtaining more précised photonic devices; this work experimentally studied the behavior of Polarization maintaining fiber PMF that is sandwiched between two cascaded singe mode fiber SMF and fiber Bragg gratings FBG. Therefore; the introduced interferometer performed hybrid interference of both Mach-Zehnder

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Sat Sep 01 2007
Journal Name
Al-khwarizmi Engineering Journal
Free Convective Heat Transfer with Different Sections Lengths Placed at the Exit of a Vertical Circular Tube subjected to a Constant Heat Flux
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A free convective heat transfer from the inside surface of a uniformly heated vertical circular tube has been experimentally investigated under a constant wall heat flux boundary condition for laminar air flow in the ranges of RaL from 6.9108 to 5109. The effect of the different sections (restrictions) lengths placed at the exit of the heated tube on the surface temperature distribution, the local and average heat transfer coefficients were examined. The experimental apparatus consists of aluminum circular tube with 900 mm length and 30 mm inside diameter (L/D=30). The exit sections (restrictions) were included circular tubes having the same inside diameter as the heated tube but with different lengths of

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Thu Oct 29 2020
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Toxicological Research
Liver functions in combined models of the gentamicin induced nephrotoxicity and metabolic syndrome induced by high fat or fructose diets: a comparative study
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Mon Oct 01 2018
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Journal Of Educational And Psychological Researches
The instrumental support search strategies and avoid coping to psychological stressors and their relationship to the cognitive motivation of Al-Anbar University students.
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the Current research aims to identify the psychological stressors coping strategies and their relationship to the cognitive motivation among Al-Anbar University students through the following hypotheses: 1) no statistically significant differences at a level (0.05) among the sample according to the instrumental support strategy depending on the variable type and specialization, 2) No statistically significant differences at a level (0.05) among the sample in regard of coping avoiding strategy depending on the variable type and specialization, 3) There is no statistically significant difference at a level (0.05) in cognitive motivation level among Al-Anbar University students, 4) No statistically significant differences at a level (0.05)

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Tue Oct 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
The impact of Innovation in offering the banking services in achieving competitive advantage for banks ( An applied study in the Iraqi private Banks )
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Fri Jan 01 2021
Journal Name
Revista Iberoamericana De PsicologÍa Del Ejercicio Y El Deporte
SPECIAL EXERCISES IN THE HIERARCHICAL OPPOSING TRAINING METHOD AND ITS EFFECT ON DEVELOPING PHYSICAL ABILITIES AND ACCURACY OF SOCCER SCORING FOR ADVANCED PLAYERS
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Sat May 01 2021
Journal Name
Journal Of Engineering
Impact of the Weir Slit Location, the Flow Intensity and the Bed Sand on the Scouring Area and Depth at the Dam Upstream
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A total of 48 experiments were conducted to investigate the impact of slit weir dimensions and locations on the maximum scour depth and scour area created upstream. The slit weir model was a 110 mm slit opening, and it was installed at the end of the working section in a laboratory flume. The flume was 10.0 m long, 30 cm wide, 30 cm deep, and almost middle. It includes a 2 m working section with a mobile bed with 110 mm in thickness. In the mobile bed, two types of nonuniform sand (with a geometric standard deviation of 1.58 and 1.6) were tested separately. The weir dimensions and location were changed with flow rates. Then dimensions of the slit weir were changed from 60 x 110 mm to 60 x 70 mm (width x height), while th

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Fri Jun 30 2023
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The International Tinnitus Journal
Adenoidectomy and Endoscopic Myringotomy with and without ventilation tube insertion for Treatment of Otitis Media with Effusion in 6-12 years old Children
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Publication Date
Fri Jan 01 2010
Journal Name
Journal Of The College Of Languages (jcl)
Die Dimensionen der Kurzgeschichte”Steh auf, steh doch auf“ The Dimension of short story (wake, Wake) 1958 by the German writer, Heinrich Böll.
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In dieser Kurzgeschichte werden die Züge der Trümmerliteratur präzis dargestellt. Die wurde von Heinrich Böll im Jahr 1958 geschrieben. In der vorliegenden Arbeit konzentriere ich mich auf vielfältige Stoffe in Bezug auf die Lage nach dem Zweiten Weltkrieg. So gab ich dieser Arbeit einen besonderen Titel, der die Dimensionen dieser Kurzgeschichte heißt. Ich meine hier, die profunde Interpretation dieses Werkes, denn ich fand zwar hinter einigen Wörtern eine ganze Geschichte, die uns der Erzähler dadurch zeigen wollte.

So teilte ich diese Wörter (Grab, Schatten, Last, Schrei) als Dimensionen, von denen diese Arbeit umgekreist wird.

Diese Arbeit besteht aus vier Kapiteln, die aufeinander aufgebaut sind. Im ersten K

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Publication Date
Mon Dec 28 2020
Journal Name
Journal Of Physical Education
The Effect of Self Scheduling Strategy Using Competitive Style in Learning Short and Long Passes in Handball for 2nd Grade Secondary School Students
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The research aimed at designing teaching sessions using the self-scheduling strategy with a competitive style in learning handball as well as identifying differences between pre and post tests in both groups in learning short and long passes in handball. The researchers used the experimental method on 2nd-grade secondary school students. The researchers concluded using the self-scheduling strategy due to its positive effect on learning short and long handball passes in handball. Finally, the researchers recommended applying strategies and styles in teaching different school levels as well as making similar studies using teaching strategies and styles for learning handball skills in students.

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