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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 Mar 01 2021
Journal Name
Iraqi Journal Of Physics
Enhancement CT Scan Image and Study Electronic, Structural and Vibrational Properties of Iobenguane
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This work is divided into two parts first part study electronic structure and vibration properties of the Iobenguane material that is used in CT scan imaging. Iobenguane, or MIBG, is an aralkylguanidine analog of the adrenergic neurotransmitter norepinephrine and a radiopharmaceutical. It acts as a blocking agent for adrenergic neurons. When radiolabeled, it can be used in nuclear medicinal diagnostic techniques as well as in neuroendocrine antineoplastic treatments. The aim of this work is to provide general information about Iobenguane that can be used to obtain results to diagnose the diseases. The second part study image processing techniques, the CT scan image is transformed to frequency domain using the LWT. Two methods of contrast

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Publication Date
Fri Mar 01 2019
Journal Name
Iraqi Journal Of Physics
Enhancement of NO2 gas sensing behavior for ZnS/PPy nanostructure by loading graphene
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The pure ZnS and ZnS-Gr nanocomposite have been prepared
successfully by a novel method using chemical co-precipitation. Also
conductive polymer PPy nanotubes and ZnS-PPy nanocomposite
have been synthesized successfully by chemical route. The effect of
graphene on the characterization of ZnS has been investigated. X-ray
diffraction (XRD) study confirmed the formation of cubic and
hexagonal structure of ZnS-Gr. Dc-conductivity proves that ZnS and
ZnS-Gr have semiconductor behavior. The SEM proved that
formation of PPy nanotubes and the Gr nanosheet. The sensing
properties of ZnS-PPy/ZnS-Gr for NO2 gas was investigated as a
function of operating temperature and time under optimal condition.
The sensitivity,

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Publication Date
Tue Feb 12 2019
Journal Name
Iraqi Journal Of Physics
Investigation of the dielectric properties of Sn – doped PMMA/PVA blends
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Blends of Polymethyl methacrylate (PMMA)/polyvinyl alcohol (PVA) doped with 2% weight percentage of Sn were prepared with different blend ratios using casting technique. The measurements of A.C conductivity σa.c within the frequency range (25kHz – 5MHz) of undoped and Sn doped PMMA/PVA blends obeyed the relationship σ= Aws were the value of s within the range 0 > s > 1. The results showed that σa.c increases with the increase of frequency. The exponent s showed preceding increase with the increase of PVA content for PMMA/PVA blends doped with Sn. The dielectric constant, dielectric loss, A.C electrical conductivity are varied with the concentration of PVA in the blend and frequency of applied electrical field.

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Publication Date
Sun Feb 22 2004
Journal Name
International Conference On Research In Education And Science
Investigation the genome variation of ST-253 of pseudomonas aeruginosa isolates
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The genic variation analysis of Pseudomonas aeruginosa after filtering the spurious variation appeared that 222 variable loci out of 5572 loci were detected. The type of variation analysis revealed that single nucleotide polymorphism was highly significant compared with other types of variation due the fact that the genome variation was achieved on the level of microevolution. Moreover, the proportional effect of functional scheme showed that genes responsible for environmental information were the highest comparable to another scheme. The genes of environmental information processing locate on outer membrane and face the defense strategy of the host therefore change in proteins coded by these genes lead to escape the immune system defense

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Scopus
Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Engineering
Experimental Investigation of the Electro Co-deposition of (Zinc-Nickel) Alloy
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An experimental investigation has been carried out for zinc-nickel (Zn-Ni) electro-deposition using the constant applied current technique. Weight difference approach method was used to determine the cathode current efficiency and deposit thickness. Also, the influence effect of current density on the deposition process, solderability, and porosity of the plating layer in microelectronic applications were examined. The bath temperature effect on nickel composition and the form of the contract was studied using Scanning Electron Microscope (SEM). Moreover, elemental nature of the deposition was analyzed by Energy Dispersive X-Ray (EDX).     

It has been found that the best bath temperature

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Publication Date
Mon Aug 01 2016
Journal Name
Journal Of Engineering
Investigation of Factors Influencing Dispersion of Liquid Hydrocarbons in Porous Media
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An experimental work has been done to study the major factors that affect the axial dispersion of some hydrocarbons during liquid-liquid miscible displacement. Kerosene and gas oil are used as displacing phase while seven liquid hydrocarbons of high purity represent the displaced phase, three of the liquids are aromatics and the rest are of paraffinic base. In conducting the experiments, two packed beds of different porosity and permeability are used as porous media.

The results showed that the displacement process is not a piston flow, breakthrough of displacing fluids are shown before one pore volume has been injected. The processes are stable with no evidence of viscous fingering.

Dispersion model as a

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Publication Date
Wed Dec 01 2021
Journal Name
Chinese Journal Of Physics
Investigation of the thermoelectric properties of one-layer transition metal dichalcogenides
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priorities of materials research due to their promising properties, especially in the field of thermoelectricity. The efficiency or performance of thermoelectric devices is expressed in terms of the thermoelectric figure-of-merit (ZT) – a standard indicator of a material’s thermoelectric properties for use in cooling systems. The evaluation of ZT is principally determined by the thermoelectric characteristics of the nanomaterials. In this paper, a set of investigative computations was performed to study the thermoelectric properties of monolayer TMDCs according to the semiclassical treatment of the Boltzmann transport equation. It was confirmed that the thermoelectric properties of 2D materials can be greatly improved compared with thei

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Publication Date
Fri Mar 31 2017
Journal Name
Al-khwarizmi Engineering Journal
Mechanical Properties Investigation of Composite Material Under Different Parameters Variations
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         The main objective of this research is to design and select a composite plate to be used in fabricating wing skins of light unman air vehicle (UAV). The mechanical properties, weight and cost are the basis criteria of this selection. The fiber volume fraction, fillers and type of fiber with three levels for each were considered to optimize the composite plate selection. Finite element method was used to investigate the stress distribution on the wing at cruise flight condition in addition to estimate the maximum stress. An experiments plan has been designed to get the data on the basis of Taguchi technique. The most effective parameters at the process to be find out by employing L9

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Publication Date
Wed Dec 30 2020
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Experimental Investigation of Moisture Sorption Isotherms for Mefenamic Acid Tablets
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   The moisture sorption isotherms of Mefenamic acid tablets were investigated by measuring the experimental equilibrium moisture content (EMC) using the static method of saturated salt solutions at three temperatures (25, 35, and 45°C) and water activity range from 0.056 to 0.8434. The results showed that EMC increased when relative humidity increased and the sorption capacity decreased, the tablets became less hygroscopic and more stable when the temperature increased at constant water activity. The sorption curves had a sigmoid shape, type II according to Brunauer’s classification. The hysteresis effect was significant along with the whole sorption process. The results were fitted to three models: Oswin, Smith, and Guggen

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Publication Date
Mon Mar 01 2021
Journal Name
Key Engineering Materials
Experimental Investigation of Reinforced Concrete Columns with Steel Embedded Tubes
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This study aimed to investigate the influence of longitudinal steel embedded tubes located at the center of the column cross-section on the behavior of reinforced concrete (RC) columns. The experimental program consisted of 8 testing pin-ended square sectional columns of 150×150 mm, having a total height of 1400 mm, subjected to eccentric load. The considered variables were the steel square tube sizes of 25, 51 and 68 mm side dimensions and the load eccentricity (50 and 150) mm. RC columns were concealed steel tubes with hollow ratios of 3%, 12% and 20% depending on tube sizes used. The experimental results indicated an improvement in the overall behavior of eccentric columns when steel embedded tubes are used. The maximum gain in

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