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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 Jun 01 2007
Journal Name
Al-khwarizmi Engineering Journal
Investigation of heat transfer phenomena and flow behavior around electronic chip
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Computational study of three-dimensional laminar and turbulent flows around electronic chip (heat source) located on a printed circuit board are presented. Computational field involves the solution of elliptic partial differential equations for conservation of mass, momentum, energy, turbulent energy, and its dissipation rate in finite volume form. The k-ε turbulent model was used with the wall function concept near the walls to treat of turbulence effects. The SIMPLE algorithm was selected in this work. The chip is cooled by an external flow of air. The goals of this investigation are to investigate the heat transfer phenomena of electronic chip located in enclosure and how we arrive to optimum level for cooling of this chip. These par

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Publication Date
Mon Jan 01 2024
Journal Name
Journal Of Engineering
Experimental Investigation about the Effects of Blockage on Upstream Box Culverts
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This experimental study focuses on scouring in box culvert inlets under steady-state conditions and at different percentages of blockage ranging from 0% to 65%, and also looks at the hydraulics of water in the culvert. The investigation shows that the blockage of the culverts has influenced the scouring pattern at the blocked culverts' entrances. Ten experiments were carried out at the laboratory to see how blockage impacts the scouring pattern upstream of a box culvert during steady flow. Both partially blocked and unblocked cases were implemented in this study. The experimental tests were done until the equilibrium scour occurred, which took about 3.5 hours of water flow to reach equilibrium conditions.  The results r

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Publication Date
Thu May 18 2023
Journal Name
Journal Of Engineering
Experimental and Theoretical Investigation of Noise Effect in Centrifugal Fan Impeller
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In this work a study was made in centrifugal fan blower to investigate the effect of impeller blade design on sound pressure level (SPL). Shroud and unshroud impeller of nine blades are used. The sound generation from flow inside the test rig at different positions was displayed by using spectral analyzer. The experiments were carried out in anechoic chamber with small holes in its walls, under ambient condition about (25-27) C ° to avoid the effect of temperature on the sound pressure level. The results showed that (SPL) decreased with the increase of distance from the source about (3-4)dB when distance varied about (0.8-1.06)m, and the (SPL) decreased with the decrease of velocity about (8-12)dB when velocity varied between (13000-260

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Publication Date
Wed Jun 15 2022
Journal Name
Malaysian Journal Of Science
INVESTIGATION OF FAST NEURON ATTENUATION COEFFICIENTS FOR SOME IRAQI BUILDING MATERIALS
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This research aims to improve the radiation shielding properties of polymer-based materials by mixing PVC with locally available building materials. Specifically, two key parameters of fast neutron attenuation (removal cross-section and half-value layer) were studied for composite materials comprising PVC reinforced with common building materials (cement, sand, gypsum and marble) in different proportions (10%, 30% and 50% by weight). To assess their effectiveness as protection against fast neutrons, the macroscopic neutron cross-section was calculated for each composite. Results show that neutron cross-section values are significantly affected by the reinforcement ratios, and that the composite material PVC + 50% gypsum is an effect

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
An Investigation Release and Rheological Properties of Miconazole Nitrate from Emulgel
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         In this study miconazole nitrate was formulated as topically applied emulgel; different formulas were prepared using sodium carboxymethylcellulose (SCMC) and carboxypolymethylene (carbomer 941) as gelling agents. The influence of type of gelling agent and concentration of both oil phase and emulsifying agent on drug release was studied and compared with commercially available miconazole nitrate cream (Mecozalen®). The results of in vitro release showed that SCMC emulgel bases gave better release than carbomer 941 bases and the release of drug increase from both bases as a function of increasing the concentration of emulisifying agent. The oil phase had retardation effect when

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Publication Date
Wed Oct 02 2013
Journal Name
International Journal Of Advanced Research In Computer Science And Software Engineering
Investigation over Efficient Broadcasting Mechanism in MANET
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Mobile ad hoc network is nothing but the temporary network which is having the collection of mobile nodes. Routing and broadcasting are major operations of MANET network. The major operation in ad hoc mobile network is the broadcasting which sometime results to storm problem of the broadcast if the forwarding mechanism is not properly designated. Thus the challenges in the MANET are to reduce the broadcasting redundancy and under high transmission error rate provides high delivery ratio. Hence in our proposed research, we are introducing and investigating the new mechanism of broadcasting called Dual Covered Broadcast. This method takes the broadcast redundancy advantage order to improve packet delivery ratio especially under environments w

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Publication Date
Fri Jul 21 2023
Journal Name
Journal Of Engineering
DESIGN OF A VARIABLE GAIN NONLINEAR FUZZY CONTROLLER AND PERFORMANCE ENHANCEMENT DUE TO GAIN VARIATION
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In this paper, variable gain nonlinear PD and PI fuzzy logic controllers are designed and the effect of the variable gain characteristic of these controllers is analyzed to show its contribution in enhancing the performance of the closed loop system over a conventional linear PID controller. Simulation results and time domain performance characteristics show how these fuzzy controllers outperform the conventional PID controller when used to control a nonlinear plant and a plant that has time delay.

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Publication Date
Sun Jan 01 2023
Journal Name
Technologies And Materials For Renewable Energy, Environment And Sustainability: Tmrees22fr
A theoretical enhancement of electronic transfer dynamics in the D35CPDT dye donor to 𝑻𝒊𝑶𝟐 acceptor
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Publication Date
Sun Jan 01 2012
Journal Name
Journal Of Engineering
DESIGN OF A VARIABLE GAIN NONLINEAR FUZZY CONTROLLER AND PERFORMANCE ENHANCEMENT DUE TO GAIN VARIATION
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In this paper, variable gain nonlinear PD and PI fuzzy logic controllers are designed and the effect of the variable gain characteristic of these controllers is analyzed to show its contribution in enhancing the performance of the closed loop system over a conventional linear PID controller. Simulation results and time domain performance characteristics show how these fuzzy controllers outperform the conventional PID controller when used to control a nonlinear plant and a plant that has time delay.

Publication Date
Sun Jun 01 2025
Journal Name
Cleaner Waste Systems
Performance enhancement of natural asphalt using waste-derived modifiers: Sugarcane molasses and waste engine oil
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The growing demand for sustainable and high-performance asphalt binders has prompted the exploration of waste-derived modifiers. This study investigates the performance enhancement of Natural Asphalt (NA) using Sugarcane Molasses (SM) and Waste Engine Oil (WEO). The modified blends were prepared by partially replacing 50 % NA with varying proportions of SM and WEO ranging from 10 % to 40 % of the total weight of NA. Comprehensive testing was conducted, including penetration, softening point, ductility, viscosity, Bending Beam Rheometer (BBR), Multiple Stress Creep Recovery (MSCR), Energy Dispersive X-ray Spectroscopy (EDX), Fourier Transform Infrared (FTIR) spectroscopy, and Scanning Electron Microscopy (SEM). The results demonstrated that

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