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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 07 2023
Journal Name
Journal Of Educational And Psychological Researches
The Impact of the Sowt Strategy on the Development of Systemic Intelligence among Students of the Ibn Rushd College of Education for the Humanities
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The aim of the current research is to identify the impact of the SWOT strategy on developing systemic intelligence among students of the Ibn Rushd College of Education for Human Sciences University of Baghdad / College of Education Ibn Rushd for Human Sciences. The current research community consists of (8590) male and female students, divided into (7) departments. The current research relied on one of the partial control designs, which is the design of non-random groups: experimental group and a control group with a pre and post-test. As for the research tool, It was represented by Tourmanin’s Systemic Intelligence Scale (2012) of (50) items that measure the eight components of systemic intelligence. The results of the Mann Whitney te

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Tue Jun 30 2020
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
DETECTION OF HEAVY METALS POLLUTION INTYPES OF MILK SAMPLES IN BAGHDAD MARKETS: DETECTION OF HEAVY METALS POLLUTION INTYPES OF MILK SAMPLES IN BAGHDAD MARKETS
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The levels of lead (pb), copper (cu), cobalt (co) and cadmium (cd) were determined in different kinds of milk and the health risks were evaluated. The mean levels were 0.73±0.21, 0.06±0.01, 0.12±0.01 and 0.14±0.01 ppm for these metals respectively. The levels of pb and cu were found to be insignificant differences (p<0.05), whereas the levels of co and cd, were no significant differences (p>0.05). The dry and liquid kinds of milk were different significantly (p<0.05), whereas the original, was no significant differences (p>0.05). The values for all metals were more than one. The metals pb and cd were detected at highest concentrations in most dry and liquid milk samples.

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Publication Date
Thu May 14 2020
Journal Name
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The Impact of the Method of Dealing with the Product of Wars in the Continuity of the Crisis Wars. Beirut city as an Example
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This research investigates the subject of the impact of wars (as a manifestation of crisis) on architecture, and the extent of continuing wars physical and moral results of wars, even after the end of the cause of the crisis. The impact of different rebuilding which exposed to the effects of the war seems different in crisis regions.

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Mon Jun 06 2022
Journal Name
International Journal Of Health Sciences
effect of a training curriculum for the development of some functional variables and the level of achievement in the effectiveness of air rifle shooting
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Mon Feb 04 2019
Journal Name
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The Effect of Using tow Methods of Pronounced and written Feed Back in Academic acquisition of students of technical medicine institute in philosophy curriculum
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Publication Date
Thu Jun 02 2022
Journal Name
Neuroquantology
The effect of the relationship of leptin hormone and live body weight on some chemical characteristics of the blood serum of local laying hens
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The study was conducted out at the Ministry of Agriculture's Poultry Research Station/Animal ResourcesDepartment/Agricultural Research Center. To see how body weight (BW) and leptin hormone (LEP) levels inbreeder blood affect fertility and hatchability. 140 Iraqi local laying chickens (120 females + 20 males) aged 28weeks were used in the study. Following the numbering of The experiment was divided into three periods,each lasting 28 days, during which the breeder's live body weight was recorded and divided into two categories(greater than 1.5 kg and less than 1.5 kg), and blood samples were collected at the end of each period todetermine the concentration of leptin hormone in the breeders' blood. For comparison between mothers'performance,

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Publication Date
Sun Aug 23 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The impact of the capital increase in the rate of return on stock price: Applied in the study of a sample of Iraqi banks
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Publication Date
Tue Aug 01 2023
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COGNITIVE ELEMENTS AND CRITERIA OF THE INFLECTIONAL SYSTEM OF RUSSIAN AND ARABIC LANGUAGUES IN THE PROCCES OF VERBAL COMMUNICATION (COGNUTIVE ANALYSIS OF LANGUAGE STRUCTURE)
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Tue Sep 06 2016
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DETECTION OF IRON AVAILABITITY OF WHEAT FLOUR PRODUCED IN BAGHDAD CITY MILLS: DETECTION OF IRON AVAILABITITY OF WHEAT FLOUR PRODUCED IN BAGHDAD CITY MILLS
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Publication Date
Sat Jul 01 2017
Journal Name
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The Use of Digital Public – Relations in the Work of Iraqi Universities: A Survey Study of the Workers in the Departments of Public Relations
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