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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
Wed Jun 01 2022
Journal Name
Baghdad Science Journal
Design and Performance Investigation of a Solar- Powered Biological Greywater Treatment System in the Iraqi Climate
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            The increase in population resulted in an increase in the consumption of water. The present work investigates the performance of a recycling solar- powered greywater treatment system for the purposes of irrigation, used to reduce the amount of waste grey water and reduce electricity consumption and reduce the costs of constructing large scale water treatment plants. The system consumes about 3814W per hour and provides water treatment about 1.4 m3 per day. The proposed system is designed to    residential, office and governmental buildings application. Tests are conducted in an office building at the Ministry of Science and Technology site in Baghdad. Laboratorial water samples testing analyses are co

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Publication Date
Sun Jun 03 2018
Journal Name
Baghdad Science Journal
Triterpenoid Saponins Investigation and Pharmacological (Cytotoxic and Antioxidant) Properties of Bacopa monnieri L. Cultivated in Iraq
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Bacopa monnieri L. (Scrophulariaceae), synoname is Herpestis monniera that provides bioactive compounds, especially triterpenoid saponins (Bacosides) which exhibits an important biological activities, like hypothyroidism, anticonvulsant, memory enhancing and antistress. Because there are no researches about B. monnieri L. plant that grow in Iraq, and there active compounds especially triterpenoid saponin (TS), and there effects. This study was detected the presence of (TS) in, and examined the cytotoxic and the antioxidant activity of these compounds in vitro. The study was included the extraction and identification of TS from the whole parts of B. monnieri L. by using three methods, and the best yield was analyzed by High Performance Liqui

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Publication Date
Sun Oct 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Investigation The Biological Activity of Some New Alkenes Based on Thiazoldin-4-one Compounds
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This work has been done to prepare a series of new alkene compounds derived from 4-thiozolidinones by substituting different aldehydes, P-acetamido-phenol, and 2-mercapto-benzoimidazole, which were used as starting materials to form ester [I]a,b and then make hydrazides [II]a,b, which were used to prepare 1, 3, and 4-oxadiazoles [III]a,b, which were then used for prepared Schiff bases [IV]a-f, The next step was the synthesis of 4-thiazoldinone derivatives [V]a-f  from Schiff bases. The final step was the synthesis of alkenes [VII]a-f, the prepared derivatives were identified with spectral methods (FT-IR, 1H-NMR, mass, and CHNS). The antibacterial activity of the prepared derivatives was evaluated against four types of bacteria, pos

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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization and Investigation Liquid Crystalline, Properties of 1, 2, 3-triazole Derivatives via Cycloaddition Reaction
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The new of compounds synthesized by sequence reactions starting from a reaction of 3-phenylenediamine or 4-phenylenediamine with chloroacetyl chloride to produce the compounds [I]a,b, then the compounds[I]a,b reacted with sodium azide to yield compounds[II]a,b that reacted 1,3-dipolarcycloaddition reaction with acrylic acid to give compounds [III]a,b these compounds reacted with methanol led to ester compounds[IV]a,b then reacted with hydrazine to give acid hydrazide [V]a,b . Finally compounds [V]a,b reacted with aromatic aldehydes to product shiff bases derivatives. The compounds characterized by mp. , IR, 1HNMR in addition to mass spectroscopy for some of them the liquid crystals properties were studied by using polarized optical microsco

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Publication Date
Wed Mar 03 2021
Journal Name
Innovative Infrastructure Solutions
Experimental investigation of a new sustainable approach for recycling waste styrofoam food containers in lightweight concrete
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Publication Date
Sat Jan 01 2022
Journal Name
Technologies And Materials For Renewable Energy, Environment And Sustainability: Tmrees21gr
Theoretical investigation of charge transfer at N3 sensitized molecule dye contact with TiO2 and ZnO semiconductor
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(3) (PDF) Theoretical investigation of charge transfer at N3 sensitized molecule dye contact with TiO2 and ZnO semiconductor. Available from: https://www.researchgate.net/publication/362773606_Theoretical_investigation_of_charge_transfer_at_N3_sensitized_molecule_dye_contact_with_TiO2_and_ZnO_semiconductor [accessed May 01 2023].

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Publication Date
Fri Dec 07 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Phytochemical Investigation of Corchorus olitorius L. Leaves Cultivated in Iraq and it’s In Vitro Antiviral Activity
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The aim of our study was to investigate the antiviral activity of the Corchorus olitorius family Tiliaceae cultivated in Iraq against measles virus, and to demonstrate an overview about chemical constituents and pharmacological activity of Corchorus olitorius L.

About150 gm Leaves of Corchorus. olitorius were defatted by maceration in hexane for 24 hrs. The defatted plant materials were subjected for extraction after filtration using Soxhlet apparatus, with aqueous methanol 85% as a solvent extraction for 24 hours, the extract was filtered, and the solvent was evaporated under reduced pressure using a rotary evaporator to get a dry extract of about 12 gm. About 4 gm from the residue was suspended in 100

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Publication Date
Mon Feb 14 2022
Journal Name
Journal Of Educational And Psychological Researches
An Investigation of the Relationship between Writing Achievement and Writing Strategy Use by Secondary School Students
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Basically, this study aims to identify the extent to which Iraqi secondary school students use writing strategies and how proficiency level and students gender could affect writing strategy use. The study also examines the relationship between writing achievement and writing strategy use among Iraqi secondary school students. For this purpose, 140 Iraqi secondary school students were selected randomly from six different schools. Petric and Czarl’s questionnaire (2003) was adopted in the study as an instrument to collect the needed data. A software of SPSS used to analyze the collected data. The findings revealed that secondary school students appeared as low users of writing strategies; low proficient students do not show a sta

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Publication Date
Fri Dec 15 2023
Journal Name
Iraqi Journal Of Laser
D-shape Optical Fiber Development and Enhancement as a Refractive Indices Sensor Using Surface Plasmon Resonance
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This article showcases the development and utilization of a side-polished fiber optic sensor that can identify altered refractive index levels within a glucose solution through the investigation of the surface Plasmon resonance (SPR) effect. The aim was to enhance efficiency by means of the placement of a 50 nm-thick layer of gold at the D-shape fiber sensing area. The detector was fabricated by utilizing a silica optical fiber (SOF), which underwent a cladding stripping process that resulted in three distinct lengths, followed by a polishing method to remove a portion of the fiber diameter and produce a cross-sectional D-shape. During experimentation with glucose solution, the side-polished fiber optic sensor revealed an adept detection

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Publication Date
Mon Jun 19 2023
Journal Name
Journal Of Engineering
Compound Heat Transfer Enhancement in Dimpled and Sinusoidal Metal Solar Wall Ducts Fitted with Wired Inserts
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An improved Metal Solar Wall (MSW) with integrated thermal energy storage is presented in this research. The proposed MSW makes use of two, combined, enhanced heat transfer methods. One of the methods is characterized by filling the tested ducts with a commercially available copper Wired Inserts (WI), while the other one uses dimpled or sinusoidal shaped duct walls instead of plane walls. Ducts having square or semi-circular cross sectional areas are tested in this work.
A developed numerical model for simulating the transported thermal energy in MSW is solved by finite difference method. The model is described by system of three governing energy equations. An experimental test rig has been built and six new duct configurations have b

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