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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
Tue May 23 2023
Journal Name
Journal Of Engineering
Enhancement of the Detection of the TCP SYN Flooding (DDoS) Attack
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The major of DDoS attacks use TCP protocol and the TCP SYN flooding attack is the most common one among them. The SYN Cookie mechanism is used to defend against the TCP SYN flooding attack. It is an effective defense, but it has a disadvantage of high calculations and it doesn’t differentiate spoofed packets from legitimate packets. Therefore, filtering the spoofed packet can effectively enhance the SYN Cookie activity. Hop Count Filtering (HCF) is another mechanism used at the server side to filter spoofed packets. This mechanism has a drawback of being not a perfect and final solution in defending against the TCP SYN flooding attack. An enhanced mechanism of Integrating and combining the SYN Cookie with Hop Count Filtering (HCF) mech

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Publication Date
Wed Dec 30 2015
Journal Name
College Of Islamic Sciences
Investigation Age message
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The research is the realization of a manuscript of Abdul Baqi al-Omari nicknamed (Farouk) relative to Al-Faruq Omar bin al-Khattab (Radha) and (Mosli) relative to the city of Mosul in Iraq and (immediate) to improvisation of poetry immediately lived during the era of the Ottomans. Entitled (Picture written by the whole secret sea embroidered crown literary style genius with wisdom poetry and magical prose Hazrat Abdul Baqi Effendi Omari comforting and congratulated to Sheikh Ali Talabani dear) and the manuscript in two versions, the subject of my brothers, in which congratulations and condolences Sheikh Ali Talabani, an administrative position in the Ottoman Empire, And the importance of the manuscript Baha The twist on the hair of Abdul

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Publication Date
Tue Mar 31 2026
Journal Name
Al-zahraa Journal For Health And Medical Sciences
Molecular Genetics Innovations in Diagnosis of Metabolic Disorders: Integration with Multi-Omics and Computational Approaches (Review Article)
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Inherited metabolic disorders (IMDs) are a diverse group of hereditary abnormalities that leads to a defect in metabolic pathway. Its diagnosis has been transformed by the innovations of molecular genetics and computational biology. Conventionally, diagnosis of IMDs is dependent on clinical findings and biochemical tests. Yet, these methods are limited due to a heterogeneity of such disorders and a large number of genes involved. The main objective of this review is to highlight the role of next-generation sequencing (NGS), including targeted gene panels, whole-exome sequencing (WES), and whole-genome sequencing (WGS), in the diagnosis of IMDs and providing reliable information in identifying genetic causes, and to explore the integrated an

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Publication Date
Thu Jun 01 2017
Journal Name
Process Biochemistry
Microbial levan from Brachybacterium phenoliresistens : Characterization and enhancement of production
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Publication Date
Thu Feb 01 2024
Journal Name
Ain Shams Engineering Journal
Performance enhancement of high degree Charlier polynomials using multithreaded algorithm
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Publication Date
Fri Nov 29 2019
Journal Name
Iraqi Journal Of Physics
Enhancement In Ballistic Performance Of Composite Armor Through Nano Ceramic
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In this study, industrial fiber and polymer mixtures were used for high-speed impact (ballistic) applications where the effects of polymer (epoxy), polymeric
mixture (epoxy + unsaturated polyester), synthetic rubber (polyurethane), Kevlar fiber, polyethylene fiber (ultra High molecular weight) and carbon fiber.
Four successive systems of samples were prepared. the first system component made of (epoxy and 2% graphene and 20 layer of fiber), then ballistic test was
applied, the sample was successful in the test from a distance of 7 m. or more than, by using a pistol personally Glock, Caliber of 9 * 19 mm. The second
system was consisting of (epoxy, 2% graphene, 36 layers of fiber and one layer of hard rubber), it was succeeded

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Publication Date
Sat Mar 19 2022
Journal Name
Al-khwarizmi Engineering Journal
Enhancement of System Security by Using LSB and RSA Algorithms
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A steganography hides information within other information, such as file, message, picture, or video. A cryptography is the science of converting the information from a readable form to an unreadable form for unauthorized person. The main problem in the stenographic system is embedding in cover-data without providing information that would facilitate its removal. In this research, a method for embedding data into images is suggested which employs least significant bit Steganography (LSB) and ciphering (RSA algorithm) to protect the data. System security will be enhanced by this collaboration between steganography and cryptography.

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Publication Date
Mon Mar 27 2017
Journal Name
Optical And Quantum Electronics
Photocurrent enhancement of heat treated CdSe-sensitized titania nanotube photoelectrode
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Publication Date
Fri Jun 20 2025
Journal Name
Bulletin Of The Iraq Natural History Museum
INVESTIGATION OF MACROFUNGI IN THE MIDDLE OF IRAQ
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The study aimed to survey mushroom species from fields among herbs, palm trunks, and trees in central Iraq and to identify them on the basis of morphological and molecular characteristics. As a molecular identification result with polymerase chain reaction six species were recorded (with eight isolates): Agaricus bitorquis (Quéllt) Saccardo. 1887 (SHA14); Candolleomyces candolleanus (Fr.) D. Wächter & Melzer, 2020 (SHA15); Cyclocybe cylindracea (D.C.) Vizzini & Angelini, 2014 (SHA13); Leucoagaricus hesperius Vellinga, 2010 (SHA16); Volvariella sp. (SHA17), and Volvopluteus gloiocephalus (D. C.) Vizzini, Contu & Justo, 2011 (SHA10, SHA101 and SHA12), belonging to four families of Basidiomycetes: Agaricaceae, Pluteaceae,

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Publication Date
Fri Aug 10 2018
Journal Name
In Book: Challenges In Mechanics Of Time-dependent Materials, Volume 2edition: 1stchapter: 12
Experimental Investigation of Segmental Post-tensioned Girders
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