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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
Mon Dec 30 2013
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Mass Transfer Enhancement Using Extensions as Turbulence Promoters
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Mass transfer was studied using a rotating cylinder electrode with different lengths of legs acting as turbulence promoters. Two types of rotating cylinder ,made of brass, were examined : an enhanced cylinder one, with four rectangular extensions 10 mm long, 10 mm wide, and 1mm thick, and an enhanced cylinder two with four longitudes 30 mm long,10 mm wide, and 1mm thick. The best performance was obtained for enhanced cylinder two at low rotation speeds while enhanced cylinder one was realized at high rotation speeds. The mass transfer enhancement as compared with a normal rotating cylinder electrode, devoid of promoters, is 53% or 58% higher. The enhancement percentage decreased as rotation speeds increased further, since, seemingly, ful

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Publication Date
Sat Mar 01 2008
Journal Name
Iraqi Journal Of Physics
Adaptive Smoothing Technique for Remotely Sensed Images Enhancement
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Spatial and frequency domain techniques have been adopted in this search. mean
value filter, median filter, gaussian filter. And adaptive technique consists of
duplicated two filters (median and gaussian) to enhance the noisy image. Different
block size of the filter as well as the sholding value have been tried to perform the
enhancement process.

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Publication Date
Tue Aug 01 2017
Journal Name
International Journal Of Greenhouse Gas Control
CO2 geo-storage capacity enhancement via nanofluid priming
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CO2 geo-storage efficiency is strongly influenced by the wettability of the CO2-brine-mineral system. With decreasing water-wetness, both, structural and residual trapping capacities are substantially reduced. This constitutes a serious limitation for CO2 storage particularly in oil-wet formations (which are CO2-wet). To overcome this, we treated CO2-wet calcite surfaces with nanofluids (nanoparticles dispersed in base fluid) and found that the systems turned strongly water-wet state, indicating a significant wettability alteration and thus a drastic improvement in storage potential. We thus conclude that CO2 storage capacity can be significantly enhanced by nanofluid priming.

Publication Date
Sun Jan 01 2023
Journal Name
Proceedings Of International Conference On Data Science And Applications
Very Low Illumination Image Enhancement via Lightness Mapping
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Publication Date
Mon Mar 01 2021
Journal Name
Iop Conference Series: Materials Science And Engineering
Speech Enhancement Algorithm Based on a Hybrid Estimator
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Abstract<p>Speech is the essential way to interact between humans or between human and machine. However, it is always contaminated with different types of environment noise. Therefore, speech enhancement algorithms (SEA) have appeared as a significant approach in speech processing filed to suppress background noise and return back the original speech signal. In this paper, a new efficient two-stage SEA with low distortion is proposed based on minimum mean square error sense. The estimation of clean signal is performed by taking the advantages of Laplacian speech and noise modeling based on orthogonal transform (Discrete Krawtchouk-Tchebichef transform) coefficients distribution. The Discrete Kra</p> ... Show More
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Publication Date
Thu Dec 31 2015
Journal Name
Al-khwarizmi Engineering Journal
Hexapod Robot Static Stability Enhancement using Genetic Algorithm
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Abstract

Hexapod robot is a flexible mechanical robot with six legs. It has the ability to walk over terrain. The hexapod robot look likes the insect so it has the same gaits. These gaits are tripod, wave and ripple gaits. Hexapod robot needs to stay statically stable at all the times during each gait in order not to fall with three or more legs continuously contacts with the ground. The safety static stability walking is called (the stability margin). In this paper, the forward and inverse kinematics are derived for each hexapod’s leg in order to simulate the hexapod robot model walking using MATLAB R2010a for all gaits and the geometry in order to derive the equations of the sub-constraint workspaces for each

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Publication Date
Tue Jan 10 2023
Journal Name
International Journal Of Emerging Technologies In Learning (ijet)
Enhancement the Educational Technology by Using 5G Networks
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With the spread of global markets for modern technical education and the diversity of programs for the requirements of the local and global market for information and communication technology, the universities began to race among themselves to earn their academic reputation. In addition, they want to enhance their technological development by developing IMT systems with integrated technology as the security and fastest response with the speed of providing the required service and sure information and linking it The network and using social networking programs with wireless networks which in turn is a driver of the emerging economies of technical education. All of these facilities opened the way to expand the number of students and s

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Publication Date
Fri Sep 15 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Comparison among pulp capping materials in: calcium ion release, pH change, solubility and water sorption (An in vitro study)
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Background: Calcium hydroxide and calcium-silicate materials used as direct pulp capping materials. The aims of this in vitro study is to compare among these materials in, the calcium ion release and pH change in soaking water after immersion of materials’ specimens in deionized water. Also Solubility and water sorption of materials’ specimens measured after soaking time. Calcium-silicate materials used were Biodentine, TheraCal and MTA Plus. Materials and methods: Four materials used in this study; Urbical lining (as control group), Biodentine, TheraCal and MTA Plus. Ten discs fabricated from each tested material, by using plastic moulds of 9 mm diameter and 1 mm thickness. Each specimen was immersed in 10 ml of d

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Publication Date
Wed Jun 01 2022
Journal Name
Journal Of The College Of Languages (jcl)
Innovative approaches to the development of the lexical composition of the oil and gas industry : Инновационные подходы развития лексического состава нефтегазовой промышленности
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 The present study discusses one of the most relevant and required topics in the recent period during globalization, the modern Russian system of terms for the oil and gas industry as a whole acquired a complete form in the second half of the twentieth century. The period of the late XX - early XXI centuries. marked by cardinal transformations in all areas of the political, economic, social and cultural life of Russia. These changes could not but affect industrial production. Transition to a new vector of development of the Russian economy based on the development of commercial trade, on the change and improvement of the development of industrial enterprises in the context of the implementation of national projects and the introduction

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Enhancement of conversion efficiency of solar cells with different thickness of fluorescent coloring agent
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Different coating layers of fluorescent agent (FCA) on the solar cells were used. An increase of 35% in the energy conversion efficiency of the solar cell have been obtained. This increase is attributed to the reduction ofthe reflected light, eflection spectra show low values at higher thickness which explained the increase ofthe conversion efficiency with increases of layer thickness.

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