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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 Feb 01 2019
Journal Name
International Journal Of Mechanical Engineering And Technology (ijmet)
INVESTIGATION THE PROPERTIES OF SILICONE RUBBER BLEND REINFORCED BY NATURAL NANOPARTICLES AND UHMWPE FIBER
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Many faces are exposed to degradation, discoloration, changes in humidity. The primary objective has improved some properties of hybrid nanocomposites materials that used for restoring of the function maxillofacial prosthesis and improving the esthetic. In the present research different lengths chopped and continuous of ultrahigh molecular weight polyethylene (UHMWPE) fiber was added at selected percentage (0.0, 0.2% and 1%) to polymer blend composite (95%SR /5%PMMA: 0.2% Pomegranate Peels Powder (PPP)) for developing the properties of silicone rubber used for the maxillofacial prosthesis applications. Some mechanical and physical properties were done on the all prepared samples. The results showed that all properties have improved when add

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Publication Date
Fri Jan 01 2021
Journal Name
E3s Web Of Conferences
Behavioral Investigation of Reinforced Concrete T-Beams with Distributed Reinforcement in the Tension Flange
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Current design codes and specifications allow for part of the bonded flexure tension reinforcement to be distributed over an effective flange width when the T-beams' flanges are in tension. This study presents an experimental and numerical investigation on the reinforced concrete flanged section's flexural behavior when reinforcement in the tension flange is laterally distributed. To achieve the goals of the study, numerical analysis using the finite element method was conducted on discretized flanged beam models validated via experimentally tested T-beam specimen. Parametric study was performed to investigate the effect of different parameters on the T-beams flexural behavior. The study revealed that a significant reduction in the

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Tue Dec 01 2020
Journal Name
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Investigation of steam jet flash evaporation with solar thermal collectors in water desalination systems
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Tue Jul 29 2025
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Preparation, Characterization, and Photoelectric Properties Investigation of Ag2O Nanoparticles Composited with Reduced Graphene Oxide
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Using an environmentally friendly chemical process, a novel nanocomposite consisting of reduced graphene oxide (rGO) and silver(I) oxide (Ag2O) nanoparticles was successfully synthesized in this work, and its optical properties along with photoelectric performance were investigated. Ag2O is a narrow-bandgap p-type semiconductor with strong visible light response but exhibits poor carrier separation and structural instability during exposure to radiation. In order to overcome shortcomings encountered with Ag2O, rGO was used as a conductive support to produce rGO@Ag2O nanocomposites with improved electronic interactions. Various characterization tests, including energy-dispersive X-ray spectroscopy (EDXS), field emission scanning electron mic

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Mon Dec 01 2025
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Experimental investigation of a solar HDH desalination unit with Pottery tubes in babylon province
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The Humidification-Dehumidification (HDH) desalination technique offers a viable solution for providing freshwater to populations in water-scarce, remote areas. This study experimentally investigates a novel humidifying method by cross airflow over water-wetted pottery tubes, which function as a humidifier, incorporating a thermoelectric cooler to condense water vapor for freshwater production. To optimize freshwater production and thermal efficiency, meticulous design of these components and appropriate operational parameters are selected. Experiments were performed in three environments with differing temperatures and relative humidity levels, while air velocity varied from 1.02 to 1.89 m/s, and thermoelectric cooler voltage ranged from 6

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Publication Date
Fri Sep 30 2022
Journal Name
Iraqi Journal Of Science
Investigation of Ground Density Distributions and Charge Form Factors for 14,16,18,20,22N using Cosh Potential
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     The bound radial wave functions of Cosh potential which are the solutions to the radial part of Schrodinger equation are solved numerically and used to compute the size radii; i.e., the root-mean square proton, neutron, charge and matter radii, ground density distributions and elastic electron scattering charge form factors for nitrogen isotopes 14,16,18,20,22N. The parameters of such potential for the isotopes under study have been opted so as to regenerate the experimental last single nucleon binding energies on Fermi's level and available experimental size radii as well.

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Publication Date
Tue Feb 27 2018
Journal Name
Iraqi Journal Of Laser
Investigation of Densified SiO2 Sol-Gel Thin Films Using Conventional and DPSS Laser Techniques
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The prepared nanostructure SiO2 thin films were densified by two techniques (conventional and Diode Pumped Solid State Laser (DPSS) (532 nm). X-ray diffraction (XRD), Field Emission Scanning electron microscopy (FESEM), and Atomic Force Microscope (AFM) technique were used to analyze the samples. XRD results showed that the structure of SiO2 thin films was amorphous for both Oven and Laser densification. FESEM and AFM images revealed that the shape of nano silica is spherical and the particle size is in nano range. The small particle size of SiO2 thin film densified by DPSS Laser was (26 nm) , while the smallest particle size of SiO2 thin film densified by Oven was (111 nm).

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Publication Date
Wed Feb 22 2023
Journal Name
Iraqi Journal Of Science
A Molecular Investigation of Phytoplasma (Candidatus Phytoplasma) Infecting Arabic Jasmine (Jasminum sambac) in Iraq
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This study was conducted to investigate phytoplasma causing a virescence disease on Arabic jasmine Jasminum sambac based on microscopy and molecular approaches. Samples were collected from symptomatic Arabic jasmine plants grown in nurseries in Baghdad-Iraq. Specimens from infected plants were prepared and Dienes stained for light microscopy examination. Phytoplasma were detected in infected plants by polymerase chain reaction (PCR) using P1/P7 and SecAfor1/SecArev3 Candidatus Phytoplasma specific primer sets. Light microscopy test showed symptomatic Arabic jasmine plants were phytoplasms infected when phloem tissues were stained with a dark blue color. PCR test confirmed the symptomatic plants were phytoplasms infected when SecAfor1/Sec

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Publication Date
Sun Dec 27 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Phytochemical Investigation and Anti-angiogenic Examination of Iraqi Vigna radiata L. Seeds and Sprouts
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Abstract

  The objective of this study was to investigate the phytochemical constituents of two different parts of Vigna radiata (seeds and sprouts), and identify their  anti angiogenic activity .the goal was achieved by Preliminary qualitative phytochemical screening for crude ethanolic extract of two parts of plant

 ; rat aorta anti-angiogenesis assay had been conducted for both extracts .   isolation , separation and purification of some phytochemical constituents that belong to important groups (flavonoids) from  n-butanol fraction extract of Vigna radiata plant had been done in pure form by using preparative thin layer chromatography ( PTLC ) and then

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Publication Date
Sun Jul 09 2023
Journal Name
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An Investigation into Thermal Performance of Mist Water System and The Related Consumption Energy
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Experimental tests were conducted to investigate the thermal performance (cooling effect) of water mist system consisting of 5μm volume median diameter droplets in reducing the heat gain entering a room through the roof and the west wall by reducing the outside surface temperature due to the evaporative cooling effect during the hot dry summer of Baghdad/Iraq. The test period
was Fifty one days during the months May, June, and July 2012. The single test day consists of 16 test hours starting from 8:00 am to 12:00 pm. The results showed a reduction range of 1.71 to 15.5℃ of the roof outside surface temperature and 21.3 to 76.6% reduction in the daily heat flux entering the room through the roof compared with the case of not using w

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