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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
Thu Jun 30 2022
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EFFECT OF INJECTED DIFFERENT CONCENTRATIONS OF ALCOHOLIC EXTRACT OF Moringa oleifera LEAVES POWDER IN HATCHING EGGS OF ADVANCED AGE OF BROILER BREEDERS ON PRODUCTIVE PERFORMANCE AND CARCASSES OF BROILER CHICKENS: EFFECT OF INJECTED DIFFERENT CONCENTRATIONS OF ALCOHOLIC EXTRACT OF Moringa oleifera LEAVES POWDER IN HATCHING EGGS OF ADVANCED AGE OF BROILER BREEDERS ON PRODUCTIVE PERFORMANCE AND CARCASSES OF BROILER CHICKENS
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This experiment was conducted to study the effect of injecting hatching eggs into a flock of broiler aged mothers with different concentrations of the alcoholic extract of Moringa oleifera powder on productive performance of broilers during the period of rearing of 35 days. The study included two experiments for a period at 2/10/2021 to 28/11/2021, where eggs were injected into the Mustafa Poultry Hatchery/ Wasit Governorate- Aziziyah District. A 400 hatching eggs of 308 Ross  mothers of modern broilers used at age  of 48  week, eggs of average weight  66 ± 1 g/egg were collected in same day then stored for two days. A quarter of treatments were randomly distributed with 100 eggs for each treatment.

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Publication Date
Fri Mar 15 2019
Journal Name
Journal Of The College Of Education For Women
The Philosophy of Beauty of Hegel
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Hegel's book entitled"The science of Beauty" is a serious attempt to establish a foundationfor this science. Hegel decided from the beginning, that his research is limited to artistic beauty more than natural beauty. He regards artistic beauty above the natural beauty as the former is the product of the soul.

            Everything that comes from the soul is superior to what is found in nature and the worst idea that penetrates human's thoughtbetter  than any  product of the nature. Man turned to art as a means of his awareness of his superior soul and his interests. All nations poured  their highest outputs of their  perceptions in the product of art.

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Wed Jan 01 2014
Journal Name
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A statistical study was made to know the characteristics of Decametric (DAM) emission emitted from Jupiter's planet. These characteristics are the sporadic nature, time, type and the frequency. Period of 11 years was taken to study the first and year 2004 was taken to study the others. Data were provided from Radio Jove project, which gave information about the observer's location, date, time, type and the frequency. The results indicated that the DAM emission was sporadic, the time was between (00:01-05:31) hour, it was found that (Io-B) is the largest number, as compared with others , a large number emission occurred at frequency range (20-21) MHz. The results were compared with results of Radio Jove software, which indicated that the DAM

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Study of Stability of Personal Dosimeter
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Publication Date
Sun Jan 11 2026
Journal Name
Journal Of The Iraqi University
The experience of providing selective broadcasting of information in the library of the Institute of Management / Rusafa
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The selective information broadcasting service is one of the important services in libraries and information centers, as it is the link between the source and the beneficiary and between related sources, as it links similar sources through keywords and then sends them to beneficiaries, which contributes to reducing the time and effort spent by beneficiaries in obtaining sources or information. Therefore, the application of this service is an important matter and gives a positive indicator in the progress of the library towards the integration of its services. From this standpoint, this research came to answer some questions, including: 1. What are the outlets for beneficiaries (the research community) in obtaining information sources? 2. Wh

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Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Development of methods of treatment of medical waste in the hospitals of Baghdad health Department / (Rusafa survey)
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Purpose: To contribute to the development of an appropriate program for the management of medical waste based on clear-cut principles in order to reach the overall goal of improving the public health and environment of the population in our country.

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Mon Oct 01 2012
Journal Name
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Semantic Confusion of the Term in Cultural Pages for Students of College of Arts (University of Baghdad)
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The research is exposed to an important issue, related to communication obstacles that prevent the media message contained in cultural topics published in local newspapers to reach the hands of the readers; or related to lack of awareness of aspects of that media message, Because it contains immersed vocabulary in elitism where, sometime, the average reader of the newspaper of medium-sized educated, and even the academic reader are unable to decode it and understand its significance.

After determining the problem of the study and the tools that the researcher wants to use to accomplish his research, a sample of students of college of Arts at the University of Baghdad was selected. As they are clo

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Fri Jun 01 2012
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Publication Date
Sun Feb 03 2019
Journal Name
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The role of thclimate in the development of the performance of the administrative bodies of sports clubs
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