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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 Apr 04 2010
Journal Name
Journal Of Educational And Psychological Researches
Translation & Adaptation of(Patterns) & (Assembly) Scales of The Flanagan Aptitude Classification Tests (FACT)
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The Flanagan Aptitude Classification Tests (FACT) assesses aptitudes that are important for successful performance of particular job-related tasks. An individual's aptitude can then be matched to the job tasks. The FACT helps to determine the tasks in which a person has proficiency. Each test measures a specific skill that is important for particular occupations. The FACT battery is designed to provide measures of an individual's aptitude for each of 16 job elements.

The FACT consists of 16 tests used to measure aptitudes that are important for the successful performance of many occupational tasks. The tests provide a broad basis for predicting success in various occupational fields. All are paper and pen

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Publication Date
Thu Dec 01 2011
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
ISOLATION AND IDENTIFICATION OF INTESTINAL PARASITES FROM VEGETABLES FROM DIFFERENT MARKETS OF IRAQ.
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This investigation was designed to determine the occurrence of intestinal parasites in fresh
vegetables(Apium graveolense, Lepidium aucheri and Allium porrum), from different markets
as a primary effort in Iraq. Eight genera and species of intestinal parasites appear in
vegetables, they were as follow: Echinococcus sp. 50%,Oxyuris equi 45%,Habronema sp.
45%,Parascaris equroum 31.6%,Strongyloides westrei 30%,Toxocara sp. 18.3%,Ascaris
lumbricoides 11.6% and Hymenolepis sp. 8.3% .The scarcity of fresh water has meant that
urban gardeners are increasingly irrigating their plots with wastewater. This poses a threat to
public health in addition of roaming dogs in open farms. All studied areas showed high rates
of eggs

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Publication Date
Wed Nov 07 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Assessment of Factors Associated with Prehospital Delay of Patients with Acute Myocardial Infarction
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Objective(s): to assess the factors which are associated with the prolonged prehospital delay of patients with
acute myocardial infarction.
Methodology: A descriptive study was conducted at the Coronary Care unit (CCU) in Al-Yarmok Teaching
Hospital, Ibn AL-Nafis Hospital for Cardiovascular Diseases, AL-Kadumia Teaching Hospital, Baghdad Teaching
Hospital, and AL-Kindy Teaching Hospital during the period of the study from February 2
nd
, 2009 to October 30th
,
2009. A random sample of (160) paƟent who were admiƩed to the hospitals were selected one by one. A
questionnaire was constructed for the purpose of the study, which is comprised of four parts that include (1)
sociodemographic data; (2) prehospital d

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Publication Date
Tue Aug 15 2023
Journal Name
Al-academy
Usage of the visual elements in the interior designing of indoor swimming pools
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The research specializes in (Usage of the visual elements in the interior designing of indoor swimming pools), the research seeks to provide a study that contributes to providing scientific and knowledge material, as a reference for researchers, students of interior design and architecture, and companies constructing indoor swimming pools.
The objective research is to detect the actual state of the interior design of the indoor swimming pools, and recognize the most important standards and techniques used in its design to provide appropriate design solutions if needed also Proposing a development proposals for the interior design of indoor swimming pools, the theoretical framework of this study, included two sections, The first one ta

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Publication Date
Mon Mar 15 2021
Journal Name
Egyptian Journal Of Chemistry
Synthesis and Characterization of some Tetrazole Derivatives and Evaluation of their Biological Activity
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Publication Date
Thu Aug 28 2025
Journal Name
Tikrit Journal Of Engineering Sciences
Influence of High Temperatures on the Mechanical Properties of GFRP Pultruded Sections- Review
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The application of pultruded (GFRP) composite has become increasingly prominent in civil infrastructure projects. This study provides a comprehensive analysis of experimental and numerical studies conducted on the mechanical characteristics of (GFRP) composites across various temperature conditions, encompassing ambient and fire scenarios. The compilation comprises over 100 scholarly articles that examine the mechanical behavior of (GFRP) materials, specifically emphasizing their tensile and compressive strengths, showed the mechanical properties of (GFRP) materials are commonly compromised when exposed to high temperatures that approach or surpass the resin's glass transition temperature (Tg). In contrast, temperatures that are low

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Publication Date
Sun Mar 05 2017
Journal Name
Baghdad Science Journal
Studying the effective of conductor polymer substrate on the electrical properties of semiconductors
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This research includes depositionof thin film of semiconductor, CdSe by vaccum evaporation on conductor polymers substrate to the poly aniline where, the polymer deposition on the glass substrats by polymerization oxidation tests polymeric films and studied the structural and optical properties through it,s IR and UV-Vis , XRD addition to thin film CdSe, on of the glass substrate and on the substrate of polymer poly-aniline and when XRD tests was observed to improve the properties of synthetic tests as well as the semiconductor Hall effect proved to improve the electrical properties significantly

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Publication Date
Mon Dec 11 2017
Journal Name
Al-khwarizmi Engineering Journal
Improvement of Mechanical and Rheological Properties of Natural Rubber for Anti-Vibration Applications
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Abstract  

This research aims to study and improve the passivating specifications of rubber resistant to  vibration. In this paper, seven different rubber recipes were prepared based on mixtures of natural rubber(NR)  as an essential part in addition to the synthetic rubber (IIR, BRcis, SBR, CR)with different rates. Mechanical tests such as tensile strength, hardness, friction, resistance to compression, fatigue and creep testing in addition to the rheological test were performed. Furthermore, scanning electron microscopy (SEM)test was used to examine the structure morphology of rubber. After studying and analyzing the results, we found that, recipe containing (BRcis) of 40% from th

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Publication Date
Wed Apr 01 2015
Journal Name
Journal Of Educational And Psychological Researches
The Effect of Enrichment Programs on the Performance of Gifted Students in KSA
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       The current study aimed at identifying the impact of each of the full and part time summer enrichment programs on the performance of gifted students. Moreover, it aimed to study the difference between the full and part time programs on the performance of gifted students. The study sample consisted of (115) students from the full time programs and (137) students from the part time programs, they have been randomly selected from the gifted students participating in the full and part time summer enrichment programs. The researcher used the scale of student performance. The results indicated that there were statistically significant differences between the averages of the pre and post applications of the

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Publication Date
Tue Jun 05 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and characterization of timed drug delivery system of sumatriptan using natural polymers
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Pulsatile drug delivery systems are time-controlled dosage forms which are designed to release the active pharmaceutical ingredient after a predetermined lag time to synchronize the disease circadian rhythm. A migraine shows circadian rhythm with a marked increase in attacks between 6 a.m. and 8 a.m.

Sumatriptan is a selective agonist at serotonin (5-Hydroxy tryptamine1  (5-HT1))receptors, is an effective treatment for acute migraine attacks.

The aim of this work is to prepare time-controlled press-coated tablet with a lag time of 5.45 hrs.

Six formulas of fast dissolving core tablets and three formulas of press-coated tablets were prepared by using direct compression method using different variables to prepa

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