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bijps-706
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 Jan 02 2020
Journal Name
Journal Of The College Of Languages (jcl)
Some of the Grammatical Rules of Writing: Zu einigen grammatischen Erscheinungen im Schreiben
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    Language contains various kinds of grammatical rules that are used to express thoughts and feelings. The present paper studies some of the German language grammatical rules as being the most important basics needed to master and develop the art of writing for the German language learners. Writing is one of the productive language learning skills that transform thoughts into a written form. Hence, constant exercising on the use of the language to master the grammatical rules enables German language learners to develop their creative writing skills.

     The present study discusses the importance of grammatical exercises in developing the language learning abilities. The study provides a gener

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Publication Date
Wed Mar 01 2023
Journal Name
Iraqi Journal Of Physics
Geographical Distribution of Landfills in the Outskirts of Baghdad Governorate using the GIS
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The problem of solid waste from domestic, industrial, commercial and medical sources is one of the most important problems facing the local administration in all Iraqi cities. The danger of this problem increases with the rapid increase in the population, changing lifestyles, consumption patterns, limited land suitable for landfill, and high costs of collection and disposal. This research aims to solve these problems by determining the locations of current landfills located in the outskirts of Baghdad Governorate. The ArcGIS program was used, where the sites of the landfills were determined on the map and through the available data about the areas. it was concluded that the existing landfill sites do not meet environmental conditions and

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Publication Date
Mon Dec 05 2022
Journal Name
Baghdad Science Journal
Influence of Optical Fiber Diameters on the Performance of Surface Plasmon Resonance Sensor
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In this research, a sensor for chemical solutions was designed and formed using optical fiber-based on a surface Plasmon resonance technology. A single-mode optical fiber with three different diameters (25, 45 and 65) µm was used, respectively.  The second layer of the low refractive fiber was replaced by gold, which was electrically deposited at 40 µm thickness. For each of the three types of optical fiber, different saline concentrations (different index of refraction) were used to evaluate the performance of the refractive index sensor (chemical sensor) by measuring its sensitivity and resolutions. The highest values we could get for these two parameters were 240mm/RIU, and 6*10-5 RIU respectively, when the diameter of a

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Publication Date
Mon Jan 13 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The evaluation of the role of the information system in reducing tax evasion
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This research attempts to evaluate the role of the information system by highlighting its importance in providing date and information to the tax administration the process of tax accounting for those who are subject to income tax whether they are individuals or companies where the effective information system provides accurate and reliable information in a timely manner.

At the theoretical part of the research, the research approaches the problem of the research represented in that whether the information system, applied in the General Commission for Taxes, is capable of achieving its role in reducing the phenomenon of tax evasion. The existence of a set of things which in the Commission may lead to increase tax evasion by taxpa

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Publication Date
Thu Oct 06 2011
Journal Name
Fes Journal Of Engineering Sciences
Derivation of a New Equation to Obtain the Permeability Coefficient of Clayey Soils
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The main objective of this research is to find the coefficient of permeability (k) of the soil and especially clayey soil by finding the degree of consolidation (rate of consolidation). New modify procedure is proposed by using the odometer (consolidation) device. The ordinary conventional permeability test usually takes a long time by preparing and by testing and this could cause some problems especially if there is a need to do a large number of this test and there were a limited number of technicians and/or apparatus. From this point of view the importance of this research is clear, since the modified procedure will require a time of 25 minute only. Derivation made to produce an equation which could be used to fined the permeabi

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Publication Date
Tue Nov 15 2022
Journal Name
Nasaq Journal
Componential Analysis of Hatred Synonymy in the Lexicons of English and Standard Arabic
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ABSTRACT This paper has a three-pronged objective: offering a unitary set of semantic distinctive features to the analysis of nominal “hatred synonyms” in the lexicon of both English and Standard Arabic (SA), applying it procedurally to test its scope of functionality crosslinguistically, and singling out the closest noun synonymous equivalents among the membership of the two sets in this particular lexical semantic field in both languages. The componential analysis and the matching procedures carried have been functional in identifying ten totally matching equivalents (i.e. at 55.6%), and eight partially matching ones (i.e. at %44.4%). This result shows that while total matching equivalences do exist in the translation of certain Eng

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Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Defects Analysis of Tee-Section Welding Using Friction Stir Welding Process of Aluminum
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Friction stir welding (FSW) of Tee-joints is obtained by inserting a specially designed rotating pin into the clamped blanks, through top plate (skin) to bottom plate (stringer), and then moving it along the joint, limiting the contact between the tool shoulder and the skin. The present work aims to investigate the defects occur for Tee-joint of an Aluminum alloy (Al 5456) with dimensions (180mm x 70mm) for the skin plate, (180mm x 30mm) for stringer plate and thickness of (4mm).
The effects of welding parameters such as rotational speed, linear speed, plunging depth, tool tilting, and die radii of welding fixture on the welding quality of Aluminum Alloy will be studied. Weld defects had been summarized and studied, and then the best

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Publication Date
Wed Mar 15 2023
Journal Name
Bionatura
Calculation of soil pollution indices with elements in residential areas of Baghdad city
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Estimation of elements: Pb, Zn, Mn, Cd, and Cu, which were conducted seasonally from October-2021 till March-2022 in residential areas of Baghdad City using Geoaccumulation index (Igeo), enrichment factor ratios (EF), the factor of contamination (CF), contamination degree (Cd), index of pollution load (PLI) and index of potential ecological risk (Eif). The overall contamination factor in the research area is limited from low contamination with Cu, Mn, and Zn, moderately contaminated to very high contamination with Pb and Cd, while the assessment according to the I-geo index shows categories that vary from a slightly polluted to unpolluted by those examined heavy metals. The pollution load index indicates that the soils in some resi

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Publication Date
Fri Oct 01 2010
Journal Name
Iraqi Journal Of Physics
Analysis of Initiation and Growth of Plasma Channels Within Non-Mixed Dielectric Liquids
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Pre-breakdown phenomenon was investigated within the two, non-mixed dielectric liquids; transformation oil and cresol. Finite element technique was used to follow the initiation and growth of plasma channels (streamer discharge) within pin-plane configuration. That was done for different spacing between the pin-electrode and the liquid-liquid interface. Streamer growth model assumed that, the streamer initiation occurs at the region of the highest value of electric field. Our study shows that the streamer initiates at the tip of the pin and growths toward the other electrode. The study shows, too, that the streamer path controlled by the difference of permittivity of the two liquids and spacing distance of the liquid-liquid interface fro

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Publication Date
Tue Sep 30 2025
Journal Name
Tikrit Journal For Agricultural Sciences
Efficiency of Nano-chitosan and Azotobacter on growth and yield of kohlrabi plant
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The research was conducted in one of the fields of the Department of Plant Production in the desert region (tomato development project) affiliated with the Directorate of Agriculture of the Holy Karbala Governorate for the purpose of studying the effect of spraying the shoots of the Kohlrabi plant (hybrid) with the Nano biopolymer (Chitosan) and the Azotobacter bio inoculum on the roots of the plant seedlings in terms of growth indicators and yield for the autumn agricultural season. 2023-2024 ,The means were compared according to the Duncan multiple ranges test at significant to level of 0.05.with R.C.B.D . The first factor was spraying the shoots with Nano- Chitosan at a concentration of (0, 1, and 2) g L-1, two weeks after transplanting,

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