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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 Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Atimicrobial Evaluation of Deuterated Analogues of Metronidazole
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The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met

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Publication Date
Fri Mar 20 2026
Journal Name
Gulf Journal Of Mathematics
New generalization of the class of H-supplemented modules
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Let P be a right R-module, where R is a ring with identity. In the present research, a class of modules is described similar to H-μ-supplemented and μ-lifting modules. A module P is called principally H-μ-supplemented if there is a summand L of P such that pR is μ-equivalent to L for every p in P. Additionally, we present an extension of supplemented modules. A module P is considered to be principally μ-supplemented if, for every p in P, pR has a μ-supplement in P. A number of characteristics of these modules are shown, and it is demonstrated that both the Pμ-H-supplemented and Pμ-supplemented modules include the class of principally μ-lifting modules.

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Publication Date
Sat May 16 2009
Journal Name
Journal Of Planner And Development
Aesthetic Elements of Urban Townscape of al Nasiriyah City
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the visual and aesthetic characteristics of the city depending on understanding several levels of visual and aesthetic characteristics to the city, starting with the study of the physical characteristics and morphology of the city in general, and urban style to it, and then study of visual composition of the city from the optical components that affect the composition of the image (visual composition) of the city represent by pathways, borders, regions and the specific features as classified by (Kevin Lynch), and then studying the details and the attention of all elements that would confer the beautiful appearance as necessary for the needs of society and the environment in general, for example, interest in the distribution and c

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Publication Date
Tue Dec 30 2008
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Study of the Performance of Batch Reactive Distillation Column
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Batch reactive distillation was studied in packed bed column. Esterification of methanol with acetic acid to produce methyl acetate and water with homogenous sulfuric acid as a catalyst was considered. This system was chosen because the reaction is reversible and the boiling point of reactant and products are different.
The reaction was carried out with and without distillation column and shows that the reactive distillation is more efficient from the conventional process (reactor and then separation). The conversion of acetic acid and concentration of methyl acetate increase by (30.43% and 75.14%) respectively at the best condition (reflux ratio 2, feed mole ratio 2 and batch time 90 minute).
The influence of various parameters, s

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Publication Date
Tue Jun 01 2021
Journal Name
Iop Conference Series: Materials Science And Engineering
Hydraulic characteristics of the lower part of Diyala River
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Abstract<p>A one-dimensional hydraulic model was conducted to simulate the flow in Diyala River. The research aims to study the flow capacity along Diyala River and especially concerning on reach of the river within Baqubah City during flood seasons by using HEC-RAS, 5.07 software. Moreover, specifying the hydraulic problems and then the necessary treatments to overcome them were suggested. A 190 km length of the reach of Diyala River was included in this study, starts from Diyala submerged weir to the confluence of Diyala-Tigris River south of Baghdad City. Good agreement resulted between the measured and the simulation results with a determination coefficient (R2) value of 0.84 with Manning Co</p> ... Show More
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Publication Date
Wed Oct 10 2018
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
CHECKLISTS OF DIPLOZOID SPECIES (MONOGENEA) FROM FISHES OF IRAQ
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Surveying 59 references concerning the occurrence of the monogeneans of the family Diplozoidae parasitizing fishes of Iraq showed the occurrence of 15 valid species of this family which included one species of Diplozoon, one species of Eudiplozoon and 13 species of Paradiplozoon. In addition to these species, some unidentified adult and larval (diporpa larvae) specimens of the genus Diplozoon were reported from 12 fish hosts among which four fish species showed no infection with any of the nominated diplozoid species while the others showed mixed diplozoid infections. These diplozoids were reported from 27 fish host species in Iraq. All the diplozoids were recorded from freshwater habitats except one <

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Publication Date
Sun Jun 06 2010
Journal Name
Baghdad Science Journal
The effect of Sunn bug Eurygaster intgriceps infection of wheat on the Capability of bread making
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The present study aims to identifying the effect of Eurygaster integriceps infection on the quality features of the local wheat varity IBA 99. The result revealed significant decrease in the percentage of protein of infected wheat at (4, 5)% compared to sound wheat values for the sound wheat were (10.9%) whereas those for the infected wheat were(9.0, 8.4 )% also the result revealed significant increased in the percentage of ash in the infected wheat flour. The result showed significant decrease in the percentage of wet and dry gluten in the infected wheat by sun bug at the rate of (2, 3, 4, 5)% compared to sound wheat value (27, 9% and 25, 23, 22, 22, 20%) for wet gluten and (8.2, 7.8, 7, 7.2, 6%) for dry glutin . The value of sedimentati

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Publication Date
Sat Sep 01 2018
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The impact of the organizational commitmentIn the job performance of employees of the Iraqi Insurance company
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The research aims at shedding light on the impact of the organizational commitment on the performance of the Iraqi insurance company as a service company that provides many services to customers both internal (individuals working) or external, Whenever the company was able to adopt new concepts to increase the understanding and knowledge of how their attention to individuals working and to provide an appropriate working environment, and to clarify the objectives and strategies for them, and create a sense of their importance, as reflected on job performance in attracting new customers, and build long-term relationships with them . In order to achieve this, the research relied on the questionnaire as a main tool for collecting data and in

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Publication Date
Sat Aug 29 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Comparison of regional bond strength among different types of posts luted with different types of cement
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Background: This in vitro study was carried out to investigate the effect of post space regions (coronal, middle and apical), the effect of post types ( Manually Milled Zirconia post, Prefabricated Fiber post, prefabricated Zirconia post) and the type of cement used (GIC, self-adhesive resin cement) on the bond strength between the posts and root dentin by using push-out test. Material and methods: Forty eight mandibular premolars extracted for orthodontic reasons (single rooted) were instrumented with ProTaper system (hand use) and obturated with gutta percha for ProTaper using AH26® root canal sealer following the manufacturer instructions. After 24 hours, post space was prepared using Zirix and Glassix drills no.3 creating 8 mm dept

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Publication Date
Tue Nov 03 2020
Journal Name
Modern Sport
The effect of using multimedia in learning the skill of passing from the bottom of volleyball
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The aim of the research is to:. Preparation and implementation of special educational units using multimedia to learn the skill of scrolling from below. 2 to recognize the impact of the use of multimedia in learning the skill of scrolling from below. 3 to identify the differences between the tests after the two groups research in learning the skill of passing from the bottom volleyball. The research represented the students of the first stage and the sample of the research was drawn randomly and the number of (50) students were divided into two experimental and control groups and each group (25) students were used standardized tests and conducting pre-tests and the implementation of the main exp

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