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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 Nov 16 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Validity of Hounsfield Units from computed tomographic images of mandibular bone in detection of osteoporosis
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Background: The figure for the clinical application of computed tomography have been increased significantly in oral and maxillofacial field that supply the dentists with sufficient data enables them to play a main role in screening osteoporosis, therefore Hounsfield units of mandibular computed tomography view used as a main indicator to predict general skeleton osteoporosis and fracture risk factor. Material and Methods: Thirty subjects (7 males &23 females) with a mean age of (60.1) years underwent computed tomographic scanning for different diagnostic assessment in head and neck region. The mandibular bone quality of them were determined through Hounsfield units of CT scan images and were correlated with the bone mineral density v

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Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
The Impact of climatic fluctuations in the production of citrus in the province of Karbala
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The relationship between the elements of the climate and the productivity of citrus (kg
/ tree) in the province of Karbala has been determined through the use of simple correlation
coefficient of Pearson (rp) and (t) test. The result for each of oranges, limes and tangerine had
all shown moral and relevant statistical indications; except for relative humidity, which were
not linked to a moral relationship with productivity of tangerine, oranges and limes.As for the
relationship between climatic factors and yield of bitter orange were all not significant
statistically and very weak.
In order to determine the strength of the correlation between fluctuations in the
climatic elements and fluctuations in the productivi

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Publication Date
Tue Dec 26 2023
Journal Name
Proceedings Of Researchfora International Conference, Dubai, Uae
GREEN SYNTHESIS OF SILVER NANOPARTICLES FROM THE ALCOHOLIC EXTRACT OF LEAVES OF HELIANTHEMUM SALICIFOLIUM L
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Publication Date
Wed Mar 30 2022
Journal Name
Journal Of Educational And Psychological Researches
Extension of sense of self According to Cognitive style Of Complexity-Simplicity Among University Students
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The current research aims to identify the level of extension of the sense of self and the cognitive style (complexity - simplification) among university students, as well as the significance of the difference according to gender (males - females), as well as the correlation between the two variables, and in order to verify this, the researcher has constructed The measure of the extension of the sense of self based on the theory of Alport 1961, as the number of its final paragraphs reached (28) paragraphs, and the cognitive style scale (complexity - simplification) prepared by (Abdullah 2017) was adopted, as the scale consisted of (32) paragraphs in its final form. To verify their psychometric properties, and the two tools were applied to

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Publication Date
Tue Feb 01 2022
Journal Name
Academy Of Accounting And Financial Studies Journal
EFFICIENCY OF PERFORMANCE AND COLLECTION OF INCOME TAX -REALISTIC VIEW OF THE GENERAL TAX AUTHORITY
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The process of evaluating and measuring tax performance is critical to support the tax collection process. The comparison of the amount of revenue collection with what is expected and the process of measuring tax performance continuously by the tax administration leads to increase the collection of tax, determine the size of deviations and stand and know the reasons and take the necessary measures to address them to get a better result in the future. According to the different tasks assigned to them, criteria and indicators for measuring the tax performance vary from one organization to another. These are indicators or criteria that measure tax revenue (i.e., amounts). One of the research's main findings was to raise the tax collection leve

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Publication Date
Fri Jan 01 2021
Journal Name
Aip Conference Proceedings
Study of rheological and mechanical properties of bitumen blended with two alpha phases of polyamide
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The effect of D phase polyamide (PA6)on the rheological properties, Young Modulus and the thermal expansion coefficient of two blends groups (bitumen-polyamide) were tested. The first group was for bitumen-PA6 blends and the second group for bitumen blended with polymer resulted from the crystallization of PA6-formic acid solution in water(PAFW).The obtained results proved that adding both types of polyamide has led to a rise in toughness and softening point temperature while the penetration Index approached -3 after adding the polyamide. So, all these changes make bitumen-polyamide blends more suitable for use in hot climate regions. The blends properties were explained according to the reaction that takes place between the polyamide and

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Publication Date
Sat Jan 15 2011
Journal Name
International Journal Of Poultry Science
Influence of Source of Oil Added to Diet on Egg Quality Traits of Laying Quail
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This experiment was performed to investigate the influence of different oils in the diets of laying quail on their egg quality characteristics. One hundred and twenty 7-week-old Japanese quails (Coturnix coturnix japonica) were allocated to four groups with three replicates containing 10 quail each (30 quail per treatment group). They were fed for 13 weeks (including one week of adaptation period) on diets containing 3% oil from different sources, viz., sunflower (T1), linseed (T2), maize (T3), or fish oil (T4). Inclusion of the diet of laying quail with fish oil (T4) and maize oil (T2) resulted in a significant increase with respect to egg weight, yolk weight, albumen weight, yolk diameter, yolk height, albumen diameter, albumen height, sh

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Publication Date
Fri Nov 01 2019
Journal Name
Iop Conference Series: Earth And Environmental Science
The role of low concentrations of some sulfuric antioxidants on the semen characteristics of rams
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Abstract<p>This study aims to investigate the effect of low concentrations of sulfuric antioxidants on sperm of rams. This study was conducted in the field of sheep and goats of the Department of Livestock in the collage of Agricultural Engineering Sciences, University of Baghdad. The semen was collected using the artificial vagina at weekly rate (Pooled semen) and was subjected to different tests and then was divided into seven treatments but different concentrations of cysteine (0.5, 1mM) and glutathione (0.5, 1mM) and taurine (0.5, 1mM).The sample of the semen was diluted with Tris dilution (10: 1). The results showed that the low concentrations of glutathione, cysteine and taurine resulted i</p> ... Show More
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Publication Date
Mon Oct 01 2012
Journal Name
Al–bahith Al–a'alami
Skills of Media Marketing of the Public Relations Staff: (University of Baghdad as a Model)
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Departments and offices of public relations and media in any institution or company is the most important departments that reflect the results of their work negatively or positively on their reputation. This goes beyond the trust and credibility that its internal and external audiences will give it. Where such matter requires the staff, working in these departments and offices, to have communication skills that qualify them to do the role of marketing the communication message. Yet, the communication skills of public relations and media staff vary from person to person depending on the communication position. This skill has two criteria: Achieving the communication goal and the speed in achieving it as a number of skills

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of the Anti-Inflammatory Effect of Pioglitazone in Experimental Models of Inflammation in Rats
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         The antidiabetic thiozolidinediones (TZDs) a class of peroxisome proliferators-activated receptor (PPAR) ligands has recently been the focus of much interest for their possible role in regulation of inflammatory response. The present study was designed to evaluate the anti-inflammatory activity of pioglitazone in experimental models of inflammation in rats. The present study was conducted to evaluate the anti inflammatory effect of TZDs (pioglitazone 3mg/Kg) on acute, sub acute and chronic model of inflammation by using egg-albumin and formalin–induced paw edema in 72 rats, relative to reference drugs Dexamethasone 5mg/Kg and Piroxicam 5mg/Kg. In each inflammation model, 24 rats wer

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