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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
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 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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Thu Jan 31 2019
Journal Name
Journal Of Engineering
Mechanical Properties Enhancement of Conventional Glass Ionomer Cement by Adding Zirconium Oxide Micro and Nanoparticles
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The aim of this work is to enhance the mechanical properties of the glass ionomer cement GIC (dental materials) by adding Zirconium Oxide ZrO2 in both micro and nano particles. GIC were mixed with (3, 5 and 7) wt% of both ZrO2 micro and nanoparticles separately. Compressive strength (CS), biaxial flexural strength (BFS), Vickers Microhardness (VH) and wear rate losses (WR) were investigated. The maximum compression strength was 122.31 MPa with 5 wt. % ZrO2 micro particle, while 3wt% nanoparticles give highest Microhardness and biaxial flexural strength of 88.8 VHN and 35.79 MPa respectively. The minimum wear rate losses were 3.776µg/m with 7 wt. % ZrO2 nanoparticle. GIC-contai

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Publication Date
Fri Jan 01 2021
Journal Name
Ieee Access
Multichannel Optimization With Hybrid Spectral- Entropy Markers for Gender Identification Enhancement of Emotional-Based EEGs
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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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Wed Oct 31 2018
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Comparative study on heat transfer enhancement of nanofluids flow in ribs tube using CFD simulation
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Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Green Engineering
Eco-Friendly Enhancement of Fire Tube Boiler Control in Oil Factory Using Functional Block Diagram
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This research is a continued efforts for a project on the fire tube boiler control for Al Rasheed edible oil factory. The aim is to enhance the control system with new integral control one. A functional blocks diagram (FBD) was built and simulated. With Schneider smart relays, FBD differs than ladder logic programming in which the PID option is active. An extensive work was done to understand the operation sequence, emergency shutdown, and faults causing the trips. A control program was designed to control logical sequence of operation. Furthermore temperature is controlled via cascade control with fuel and air controllers. The temperature controller output is send as remote set point to the fuel controller in a serial cascade manner. The f

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Publication Date
Sat Dec 31 2016
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Investigation of Binary Solvents Performance for Regeneration of Iraqi 15W- 40 Waste Lubricant
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The aim of this study was to investigate the effectiveness of binary solvent for regeneration of spent lubricating oil by extraction-flocculation process. The regeneration was investigated by bench scale experiments by using locally provided solvents (Heavy Naphtha, n-Butanol, and iso-Butanol). Solvents to used oil, mixing time, mixing speed and temperatures were studied as operating parameters. The performance on three estimated depended key parameters, namely the percentage of base oil recovered (Yield), percent of oil loss (POL), and the percent of sludge removal (PSR) were used to evaluate the efficiency of the employed binary solvent on extraction process. The best solvent to solvent ratio for binary system were 30:70 for Heavy Naph

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Publication Date
Tue Jan 17 2012
Journal Name
Journal Of Electron Devices
INVESTIGATION OF OPTICAL PROPERTIES OF THE PbS/CdS THIN FILMS BY THERMAL EVAPORATION
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In this work, we have investigated optical properties of the thermally evaporation PbS/CdS thin films. The optical constant such as (refractive index n, dielectric constant εi,r and Extinction coefficient κ) of the deposition films were obtained from the analysis of the experimental recorded transmittance spectral data. The optical band gap of PbS/CdS films is calculate from (αhυ)1/2 vs. photon energy curve.

Publication Date
Thu Feb 07 2019
Journal Name
Iraqi Journal Of Laser
Investigation of Size-dependent Nonlinearity of Ag Nano-Fluids using Self-defocusing Technique
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In this work, the effect of different particle size on the nonlinear optical properties of silver nanoparticles in de-ionized water was studied. The experimental observation of the far field diffraction patterns by CCD camera in two and three dimensions. The maximum change of nonlinear refractive index and the relative phase shift were calculated. The self-defocusing technique was used with a continuous-wave radiation from DPSS Blue laser .The wavelength is 473 nm with an output power of 270 mW. All the Ag colloids samples containing the sizes 15, 30, 50, and 70 nm of silver nanoparticles used in the study were chemically prepared. It was found that the nonlinear refractive index is a particle size dependent and of the order of 10-7 cm2/

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