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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 Mar 01 2009
Journal Name
Baghdad Science Journal
Effect of leaves Extracts of Duranta repens on growth and activity of some types of Pathogenic Bacteria and Some types of Fungi
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A study were conducted to examinate the effect of organic and aqueous (Hot, Cold) Extracts from leaves of Duranta repens on the growth and activities of the following types of Bacteria:- Staphylococcus aureus,Streptococcus pyogens ,Escherichia coli,Klebsilla pneumonia, in addition to the yeast Candida albicans and the fungi Aspergullis niger ,Aspergulls flavus.The result showed that gram Positive Bacteria is more sensitive to the extracts than gram negative bacteria with Minimum inhibitory concentration (MIC) value (50,25,50,100)% and Minimum Bactericidal Concentration (MBC) value (100,50,200,100)% for all types Bacteria respectively . The most active extract against A.niger ,A,flavus was cold and hot aqueous extract from the leaves with d

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Publication Date
Mon Jun 30 2025
Journal Name
مجلة القادسية للقانون والعلوم السياسية
Insurance of Unlawful Risks: Towards a Reinterpretation of Public Policy in Light of the Protection of Innocent Victims and Freedom of Contract
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The issue of insurance against unlawful risks raises a jurisprudential and judicial debate between two opposing trends: the first considers coverage of these risks invalid due to their impact on public order or morals, while the second—which this research analyses—calls for the possibility of covering these risks in specific circumstances, based on contractual considerations in accordance with the principle that the contract is the law of the contracting parties, and based on the obligation to compensate the harmed third party—the victim—who has no connection to the unlawful act. In this context, our research highlights that contractual considerations can justify coverage of some unlawful risks, provided that the goal is to achieve

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Publication Date
Sun May 08 2011
Journal Name
Journal Of Planner And Development
The use of GIS in the analysis of existing condition of spatial distribution of wire communications network in the city of Baghdad
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The increasing efficiency of the telecommunications network in the city contributes to the increase in spatial interaction between activities (to influence and mutual influence) This study is based on the idea that the upgrading of telephone services provided to citizens are done exclusively through the growth and development of all levels of the service using advanced technologies to know the problems and appropriate solutions in short time and less cost. Thus, crystallized the objectives of the study which was built for the importance of GIS in the planning of services in general, and infrastructure services, in particular, including telephone services, which is represent a point of contact between individuals on the one hand a

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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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Publication Date
Wed Jan 01 2014
Journal Name
Al- Mustansiriyah Journal Science
Characteristics of Decametric Emission of Jupiter
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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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Publication Date
Sun Dec 06 2009
Journal Name
Baghdad Science Journal
Study of Stability of Personal Dosimeter
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The study is carried out by using personal dosimeters (film badge). The films are irradiated to absorbed dose of range (0.01-10000 rad). The calibration curves are drawn by using the ordinary method taking into account the filtration effects in three regions (D (Pb/Sn),D(Du),D(300). The calibration films are stored in ambient condition. It is found that the optical density increases, which is attributed to the photodegradation of the films may induce localized states in the energy gap causing increasing in optical absorption, but optical density decreases, which attributed to the photodegradation of the films may cause some cracks at the film surface during the first month, whereas at the rest months we see clear stability in optical d

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Publication Date
Tue Nov 11 2025
Journal Name
Journal Of Baghdad College Of Dentistry
The Effect of LED Light on Depth of Cure and Microhardness of Three Types of Bulkfill Composite
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Background: To evaluate the ISO depth of cure of bulkfill composites and depth of cure which determined by Vickers microhardness test. Materials and Methods: Bulkfill resin composite specimens (n=150) were prepared of three bulkfill composite materials (TetricEvo Ceram, Quixfil and SDR) and light cured by Flash max p3 for 3, 10, 20 seconds and by wood pecker for 10, 20 seconds respectively, a mold was filled with one of the three bulkfill composites and light cured. The specimens removed from the mold and scraped by plastic spatula and the remaining length (absolute length) was measured which represent the ISO depth of cure. After that the specimens were returned into the mold and a microhardness indentation device applied on the specimen

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Publication Date
Tue Nov 11 2025
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
Mon Oct 01 2018
Journal Name
Journal Of Educational And Psychological Researches
The Effect of PDEODE Strategy on the Acquisition of Historical Concepts of First Class of Intermediate Students
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The research aims to find out the effect of PEDODE Strategy on the acquisition of historical concepts of First Intermediate Grade. To achieve this goal, the researcher has put forward this zero hypothesis: There is no statistically significant difference at the level of (05,0) between the mean of the students' marks in the experimental group who study the history subject using PEDODE strategy and that of the students' marks in the control group who study the subject according to the traditional method in the post-testing on the acquisition of historical concepts. The sample of the study consists of (62 female-students) of First Intermediate Grade in the Directorate of Baghdad Education/ Karkh2nd for the academic year 2016-2017. The sampl

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