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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
Fri Oct 03 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
Fri Jun 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Effect Of Comprehensive Income In Market Value Of Company Importance Of Comprehensive Income In Market Value Of
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The study aims (objective ) to clarify the concept of comprehensive income and its usefulness for users, as the study aims to clarify the relationship between the concept of comprehensive income and market value of the company where the measurement of comprehensive income after accounting for net income and by measuring the unrealized gains or losses in the value of securities available for sale, and measurement the unrealized gains or losses on futures contracts, which are financial derivatives, and measurement the unrealized gains or losses from the settlement of foreign currency translation (conversions), and measurement the impact on the market value of companies and of the present study to rise or fall of return on the stock

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Publication Date
Mon Oct 01 2012
Journal Name
Al–bahith Al–a'alami
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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Publication Date
Tue Dec 01 2015
Journal Name
Journal Of Engineering
Importance of New Use of Concrete in Iraq Analysis of Development And Use of Concrete in Architecture
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Since its invention by the Ancient Romans and later developed during the mid-18th century, the concrete structure and finish, has been considered as the most powerful, practical, economic and constructional material that meets the building’s architectural and aesthetical requirements. By creating unique architectural forms, the pioneer architects used concrete widely to shape up their innovative designs and buildings.

The pre-mixed ultra-high performance concrete which manufactured by Lafarge.

The transparent concrete and cement that allow the light beams to pass through them, introduces remarkable well-lit architectural spaces within the same structural criteria. This product is a recyclable, sustainab

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Publication Date
Fri Oct 03 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Efficacy of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint
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Background: Temporomandibular joint disorders refer to a group of heterogeneous pain and dysfunction conditions involving the masticatory system, reducing life quality of the sufferers. Arthrocentesis is simple and less invasive surgical procedure for the treatment of internal derangement than arthroscopy and better than other conservative procedures such as drugs, occlusal appliances and physiotherapy. The aim of the study was to evaluate the effect of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint for the restoration of its function, reducing pain and preventing further deterioration of the temporomandibular joint dysfunction. Materials and methods: This study was perfo

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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
The role of thclimate in the development of the performance of the administrative bodies of sports clubs
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The role of the climate in the development of the performance of the administrative bodies of sports clubs

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Publication Date
Fri Oct 03 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
Fri Jan 24 2020
Journal Name
Iraqi Journal Of Agricultural Sciences
THE EFFECT OF TERMITES EXTRACT ON INHIBITION OF GROWTH OF SOME PATHOGENIC BACTERIA AND SYNTHESIS OF BIOFILM
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This study was aimed to extract the effective material from the dry nests of termites and detect its antibacterial activity against some pathogenic bacterial isolates and inhibit synthesis of its biofilm. Termites dry nests were collected and the effective material was extracted then the antibacterial activity was detected using the disc diffusion assay. Results were showed that the extract have antibacterial material from the Termites dry nests, this extract showed antibacterial activity against Gram positive bacteria (Staphylococcus aureus) at (21.5mm) and Gram negative bacteria ( Enterobacter sp. and Pseudomonas aeruginosa) at (26 mm and 20 mm) respectively by inhibiting their growth, as well as its effect on biofilm production o

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Publication Date
Mon Oct 01 2018
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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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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.

Design / Approach / Introduction: The research is based on the analytical descriptive approach as a method of study in the field of data collection using a check list and analysis of the data through the use of some statistical treatments.

 Results: The need is to establish a medical waste management in hospitals and follow international standards in all stages of waste management from sorting, collection, transportation and treat

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