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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 Mar 01 2019
Journal Name
Al-khwarizmi Engineering Journal
The Effect of Micro and Nano Material on Critical Heat Flux (CHF) Enhancement
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The Nano materials play a very important role in the heat transfer enhancement. An experimental investigation has been done to understand the behaviors of nano and micro materials on critical heat flux. Pool boiling experiments have used for several concentrations of nano and micro particles on a 0.4 mm diameter nickel chrome (Ni-Cr) wire heater which is heated electrically at atmospheric pressure. Zinc oxide(ZnO) and silica(SiO2) were used as a nano and micro fluids with concentrations (0.01,0.05,0.1,0.3,0.5,1 g/L), a marked enhancement in CHF have been shown in the results for nano and micro fluids for different concentrations compared to distilled water. The deposition of the nano particles on the heater surface was the rea

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Publication Date
Thu Oct 31 2013
Journal Name
Al-khwarizmi Engineering Journal
Enhancement of a Power System Transient Stability Using Static Synchronous Series Compensator SSSC
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Static Synchronous Series Compensator (SSSC) is a well known device for effectively regulating the active power flow in a power system. In this paper, the SSSC linearized power flow equations are incorporated into Newton-Raphson algorithm in a MATLAB written program to investigate the control of active poweer flow and the transient stability of a five bus and a thirty bus IEEE test systems, during abnormal conduction (three phase fault near buses). A comparison of the results obtained for the base case without SSSC and with it to investigate the effectiveness of the device on both of the active power flow and the transient stability.

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Publication Date
Wed Jun 14 2023
Journal Name
Al-academy
Functional enhancement and its reflection on industrial product systems
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The research tagged (functional enhancement and its reflection on industrial product systems) focused on the possibility of enhancing industrial products in terms of form and functionality in a way that they are able to meet the needs of the user through the impact of technology and modern technologies on the functional enhancement of industrial products and their effectiveness in achieving formal and functional design variables, and producing products Industrial products are highly efficient and durable in order to improve them in order to meet the needs of the user, the transfer of technology between life forms and industrial products is desirable because the functional enhancement processes that occurred in general on industrial produ

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Publication Date
Mon Jan 09 2023
Journal Name
2023 15th International Conference On Developments In Esystems Engineering (dese)
Deep Learning-Based Speech Enhancement Algorithm Using Charlier Transform
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Publication Date
Wed Nov 06 2024
Journal Name
2024 17th International Conference On Development In Esystem Engineering (dese)
Speech Enhancement Algorithm using Deep Learning and Hahn Polynomials
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Mon Apr 16 2018
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Cooperativity enhancement in buckled-dome microcavities with omnidirectional claddings
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Publication Date
Sat Dec 31 2022
Journal Name
Mathematical Modelling Of Engineering Problems
Investigation of Energy Efficient Clustering Algorithms in WSNs: A Review
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In recent years, Wireless Sensor Networks (WSNs) are attracting more attention in many fields as they are extensively used in a wide range of applications, such as environment monitoring, the Internet of Things, industrial operation control, electric distribution, and the oil industry. One of the major concerns in these networks is the limited energy sources. Clustering and routing algorithms represent one of the critical issues that directly contribute to power consumption in WSNs. Therefore, optimization techniques and routing protocols for such networks have to be studied and developed. This paper focuses on the most recent studies and algorithms that handle energy-efficiency clustering and routing in WSNs. In addition, the prime

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Publication Date
Thu May 01 2025
Journal Name
Journal Of Engineering
Transient Response Investigation of Cross-Ply Plates Using Refined Theory
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Response of cross-ply plates subjected to transient load is obtained using five variables refined plate theory, and four variables plate theory. Equations of motion are derived through the principleof virtual work. Navier series used for simply supported laminated plates. The results of this work are presented for different parameters, such as the ply number, thickness, and modulus ratio with mechanical load (sinusoidal and step pulses), which are compared with those obtained using high-order shear plate theory. Five variables of refined plate theory give results that are considerably different from the four variables of refined plate theory and higher-order theory. The obtained results from the four variables theory have the same behavior

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Publication Date
Wed Jan 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Numerical Investigation of Drag Reduction Techniques in a Car Model
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Abstract<p>Reducing the drag force has become one of the most important concerns in the automotive industry. This study concentrated on reducing drag through use of some external modifications of passive flow control, such as vortex generators, rear under body diffuser slices and a rear wing spoiler. The study was performed at inlet velocity (V=10,20,30,40 m/s) which correspond to an incompressible car model length Reynolds numbers (Re=2.62×10<sup>5</sup>, 5.23×10<sup>5</sup>, 7.85×10<sup>5</sup> and 10.46×10<sup>5</sup>), respectively and we studied their effect on the drag force. We also present a theoretical study finite volume method (FVM) of solvi</p> ... Show More
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Publication Date
Fri Jan 01 2021
Journal Name
Chemical Industry And Chemical Engineering Quarterly
Electrochemical harvesting of microalgae꞉ Parametric and cost-effectivity comparative investigation
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The cost of microalgae harvesting constitutes a heavy burden on the commercialization of biofuel production. The present study addressed this problem through economic and parametric comparison of electrochemical harvesting using a sacrificial electrode (aluminum) and a nonsacrificial electrode (graphite). The harvesting efficiency, power consumption, and operation cost were collected as objective variables as a function of applied current and initial pH of the solution. The results indicated that high harvesting efficiency obtained by using aluminum anode is achieved in short electrolysis time. That harvesting efficiency can be enhanced by increasing the applied current or the electrolysis time for both electrode materials, where 98

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