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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 Sep 01 2023
Journal Name
Iraqi Journal Of Physics
Investigation of Numerical Simulation for Adaptive Optics System
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In this study, the performance of the adaptive optics (AO) system was analyzed through a numerical computer simulation implemented in MATLAB. Making a phase screen involved turning computer-generated random numbers into two-dimensional arrays of phase values on a sample point grid with matching statistics. Von Karman turbulence was created depending on the power spectral density. Several simulated point spread functions (PSFs) and modulation transfer functions (MTFs) for different values of the Fried coherent diameter (ro) were used to show how rough the atmosphere was. To evaluate the effectiveness of the optical system (telescope), the Strehl ratio (S) was computed. The compensation procedure for an AO syst

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Publication Date
Wed Dec 30 2009
Journal Name
Iraqi Journal Of Physics
Electrical Investigation of PSi/Si (n-type) structure
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In this work, porous Silicon structures are formed with photochemical etching process of n-type Silicon(111) wafers of resistivity (0.02.cm) in hydrofluoric acid (HF) of concentration (39%wt) under light source of tungeston halogen lamp of (100 Watt) power. Samples were anodized in a solution of 39%HF and ethanol at 1:1 for 15 minutes. The samples were realized on n-type Si substrates Porous Silicon layers of 100m thickness and 30% of porousity. Frequency dependence of conductivity for Al/PSi/Si/Al sandwich form was studied. A frequency range of 102-106Hz was used allowing an accurate determination of the impedance components. Their electronic transport parameters were determined using complex impedance measurements. These measu

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Publication Date
Sun Dec 01 2019
Journal Name
Al-khwarizmi Engineering Journal
Investigation of Effecting Parameters in a Turning Operation
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        In this study multi objective optimization is utilized to optimize a turning operation to reveal the appropriate level of process features. The goal of this work is to evaluate the optimal combination of cutting parameters like feed, spindle speed, inclination angle and workpiece material to have a best surface quality Taguchi technique L9 mixed orthogonal array, has been adopted to optimize the roughness of surface. Three rods of length around (200 mm) for the three metals are used for this work. Each rod is divided into three parts with 50 mm length. For brass the optimum parametric mix for minimum Ra is A1, B1 and C3, i.e., at tool inclination angle (5), feedrate of 0.01, spindle speed of 120

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Publication Date
Sun Jun 21 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Investigation of Lacidipine as a Nanoemulsions
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Many pharmaceutical molecules have solubility problems that until yet consist a hurdle that restricts their use in the pharmaceutical preparations. Lacidipine (LCDP) is a calcium-channel blocker with low aqueous solubility and bioavailability.

        Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE)  is one of the popular methods that has been used to solve the solubility problems of many drugs. LCDP was formulated as a NE utilizing triacetin as an oil phase, tween 80 and tween 60 as a surfactant and ethanol as a co-surfactant. Nine formulas were prepared, and different tests performed to ensure the stability of the NEs, such as thermodyna

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Publication Date
Thu May 04 2023
Journal Name
Journal Of Communicable Diseases
Enhancement of Swarming and Inhibition of Prodigiosin in Serratia marcescens by Glyceryl Trinitrate
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Introduction:Serratia marcescens is a gram-negative pathogen of many species. Its pathogenicity and survival are linked to its capacity to build biofilms as well as its strong inherent resistance to antimicrobials and cleaning agents. Objectives: To analyse the impact of glyceryl trinitrate (GTN) on the gene expression of QS-related genes (rssB, rsmA,and pigP) of S. marcescens. Methodology: The broth microdilution technique estimated the bactericidal effectiveness of glyceryl trinitrate. The presence of rssB, rsmA,and pigP in S. marcescens isolates was detected using PCR. qRT-PCR was used to assess the effect of GTN on rssB, rsmA,and pigPgene expression. Results: The results demonstrated that GTN has no effect on S. marcesce

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Publication Date
Wed Jan 01 2025
Journal Name
Smart Innovation, Systems And Technologies
The Effect of Two Training Approaches with (Hanging–Heavy) Ropes in Developing Some Physical Abilities and Accuracy of Shooting—In Front of Handball
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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
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
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
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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