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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
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
Using Index of Compaction in interpreting the distribution and shapes of soil map units of Lower Diyala project.: Using Index of Compaction in interpreting the distribution and shapes of soil map units of Lower Diyala project.
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Abstract
This study was conducted by using soil map of LD7 project to interpret the
distribution and shapes of map units by using the index of compaction as an
index of map unit shape explanation. Where there were wide and varied
ranges of compaction index of map units, where the maximum value was
0.892 for MF9 map unit and the lower value was 0.010 for same map unit.
MF9 has wide range appearance of index of compaction after those indices
were statistically analyzed by using cluster analysis to group the similar
ranges together to ease using their values, so the unit MF9 was considered as
key map unit that appears in the soils of LD7 project which may be used to
expect another map units existence in area of

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Publication Date
Tue Jun 11 2019
Journal Name
Al-kindy College Medical Journal
Effect of HLA-B27 on Development of Psoriatic Arthropathy
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Background: Psoriatic arthritis is a type of arthritis that can often affect some patients who suffer from psoriasis. Approximately 40-50% of individuals with psoriatic arthritis have the HLA-B27 genotype

Objective: To investigate whether we could confirm the role of HLA-B27 alleles and psoriatic arthritis in Iraqi Arab Muslims patients.

Method: A cross sectional case control comparative study included thirty Iraqi Arab Muslims who had psoriatic arthritis that consulted the Dermatological and Rheumatological Department in AL-Kindy Teaching Hospital from November 2014 to June 2015. HLA-genotyping for HLA-B27 were assessed. A control group consisted of fifty-one healthy vol

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Publication Date
Sat May 16 2009
Journal Name
Journal Of Planner And Development
Aesthetic Elements of Urban Townscape of al Nasiriyah City
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the visual and aesthetic characteristics of the city depending on understanding several levels of visual and aesthetic characteristics to the city, starting with the study of the physical characteristics and morphology of the city in general, and urban style to it, and then study of visual composition of the city from the optical components that affect the composition of the image (visual composition) of the city represent by pathways, borders, regions and the specific features as classified by (Kevin Lynch), and then studying the details and the attention of all elements that would confer the beautiful appearance as necessary for the needs of society and the environment in general, for example, interest in the distribution and c

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Publication Date
Tue Aug 20 2019
Journal Name
Political Sciences Journal
The contemporary political history of the State of Zimbabwe
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Abstract: This study aims to identify mainly the experience of development of the state of Zimbabwe. The purpose of this study is to explain African studies in our Arab countries . The approach followed in this study is analytical description using also the comparative method as needed. This research division an introduction ,fourth topics and conclusions .The first dealt with the geographical location of the state of the Zimbabwe and explain of the main cities and a general introduction to the Republic of the state of Zimbabwe . The second section reviewed the historical development since the advent of colonial British colonialism and the declaration of Rhodesia Nyasaland in 1953 . As well as to clarify the position of stats and interna

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Publication Date
Mon Jul 15 2019
Journal Name
Journal Of Pharmaceutical And Biological Sciences
Analysis of genome variation in CEs of meningococcal isolates
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Important points were concluded from this analysis related with the presence of the same variable CEs within multiple isolates with different time points being under the selection and the location of SNPs within the conserved functional pattern of CEs. In the 40 isolates, 9 out of 39 variable CEs conducted with multiple isolates

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Publication Date
Sat Jul 22 2023
Journal Name
Journal Of Engineering
The Impact of Materials’ Technology on Sustainability of Buildings
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The evolution in materials’ technology in the last decades resulted in interesting projects that aimed at preserving the environment and energy and reduce pollution. They have been taken the principles of environmental design as a basis for architectural thought, starting from the early stages of the design process ending in choosing appropriate building materials to achieve sustainable buildings, but these trying are limited in our local environment and there isn’t demanded seriousness. The research problem emerges in the ignorance of the environmental aspect (ecological system) when selecting building materials during design process to achieve sustainable buildings. The aim of this research is revealing the mechanisms of selecting

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Publication Date
Sat Oct 16 2021
Journal Name
Journal Of Advance Research In Chemical Sciences
Study of Schiff Bases Complexes of Trimethoprim: A Review
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Publication Date
Sun Jan 01 2023
Journal Name
8th Engineering And 2nd International Conference For College Of Engineering – University Of Baghdad: Coec8-2021 Proceedings
Overview of seismic performance assessment of reinforced concrete buildings
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Publication Date
Thu Jul 01 2004
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
MICROFACIES ANALYSIS OF GHAR FORMATION (WESTERN DESERT OF IRAQ)
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Ghar Formation outcrop at the Iraqi western desert was studied by microfacies analysis
of (13) thin sections collected from wadi Al-Ratgha ( west of Qaim ) . According to
petrographic com position and organisms content ,rocks were subdivided into (4)
microfacies units :bioclastic wackestone , mudstone , miliolids wackestone , and grainstone
with aggregate grains microfacies .Microfacies units reflect shallow marine environment of
low circulation of very warm water at the middle part . The lower and middle part
interbedded with quite open marine environment below the wave base . The upper part was
deposited at shallow marine environment of low circulation . The main diagenetic processes
were the transformation ( ty

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Publication Date
Fri Jan 05 2024
Journal Name
Al-academy
THE SYSTEM OF SHAPE IN SOME OF PICASSOS CERAMICS
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Picasso ceramics represented illuminated sign in ceramic art and excelled in accord ceramic art dimension aesthetically, and put it in a new prospects, despite the simplicity of the forms turn into a magical images and multiple interpretations.
So the search deliberately to choose purposive (37) samples divided into four groups, as follows: -
A flat shapes / palets or saucers / the vases /modified vases .
benefiting from indicators were spawned from literature ,to analyzing samples within the totals for the identification systems act forming art work`s:-
(1)Picasso's ceramic work product of a deliberate process represented a capacity of technical experience, and formal
(2)The system configuration in the ceramic art works c

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