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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 Oct 15 2023
Journal Name
Revista Bionatura
Estimation of amino acid concentrations in the kidney of albino mice embryo
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Amino acids are the basic building block for peptides and proteins. They are raw materials for generating hormones, purines, pyrimidines and vitamins. Amino acids also provide the body with energy through their carbon structures. The study analyzed the amino acid in the kidneys of the albino mice embryo at 17 and 19 gestation days, using a high-performance liquid chromatography device (HPLC). Samples were obtained after removing them from the embryo and placing them in an ice bath to prevent cell lysis and acid loss. The study found 18 amino acids in the kidneys of the albino mice embryo. They are Asparagine (Asn), Glutamine (Glu), Serine (Ser), Glycine (Gly), Threonine (Thr), Histidine (His), Cysteine (Cys), Alanine (Ala), Proline

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Publication Date
Wed Aug 01 2018
Journal Name
Journal Of Global Pharma Technology
GC/MS analysis of terpenes of Boswellia serrata resin found in Iraq
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Objective: The aim of this work was to detect terpenes other than boswellic acid derivatives in olibanum of Boswellia Serrata found in Iraq. Methods: The olibanum of Boswellia Serrata was macerated in methanol for one day, then filtration. Filter at was concentrated till reddish brown syrupy residue was gained, (3%) potassium hydroxide was added till basification. This basic solution was stirred continuously until a uniform emulsion was formed, then extracted with chloroform in a separatory funnel; the chloroform fraction was analyzed by GC /MS spectrometry. Results: GC /MS analysis reveal the presence of terpenes and non-terpenes constituents. Conclusion: Most of the detected terpenes were sesquiterpenes and the least one was di-terpenes.

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Publication Date
Thu Aug 01 2024
Journal Name
Iop Conference Series: Earth And Environmental Science
Utilization of GIS to Generate a Digital Geotechnical Map of Baghdad City
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Abstract<p>The Geographic Information System (GIS) is considered one of the most prominent programs used to collect, analyze, display, process, and produce geographic information maps for a specific purpose. It is also considered one of the modern database programs. Additionally, we can perform statistical analysis within GIS on predefined data to produce quantitative results. In this study, data was collected from more than 80 engineering projects established in Baghdad City from soil investigation reports for the projects. Geographic information systems were used to produce objective maps showing the variation in the bearing capacity of shallow foundations in the soil of Baghdad Governorate. I</p> ... Show More
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Publication Date
Tue Dec 14 2021
Journal Name
Sustainability
Influence of Iron Filing Waste on the Performance of Warm Mix Asphalt
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Recently, interest in the use of projectiles in research on recycling waste materials for construction applications has grown. Using recycled materials for the construction of asphalt concrete pavement, in the meantime, has become a topic of research due to its significant benefits, such as cost savings and reduced environmental impacts. This study reports on comprehensive experimental research conducted using a typical mechanical milling waste, iron filing waste (IFW), as an alternative fine aggregate for warm mix asphalt (WMA) for pavement wearing surface applications. A type of IFW from a local machine workshop was used to replace the conventional fine aggregate, fine natural sand (FNS), at percentages of 25%, 50% 75%, and 100% b

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Publication Date
Mon Mar 27 2023
Journal Name
Aip Conference Proceedings
Stability of Kongele earth dam against rapid drawdown of water from reservoir
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ABSTRACT In dam construction stages when an earth embankment has retained a reservoir with constant water surface elevation for a long time, seepage conditions within the embankment will be reach a steady state. If it is necessary to drain the reservoir quickly, the pore-water pressures in the embankment may remain relatively high while the stabling effect of the reservoir's weight along the upstream (U/S) side for the embankment has removed. This process is referring to as "Rapid Drawdown" and may be cause instability in the upstream (U/S) face of the embankment. Kongele dam is one of the proposed earth dams to be implement within the current plan in Iraq. The authors study pore water pressure and the effect of rapid drawdown for the dam d

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Publication Date
Tue Feb 05 2019
Journal Name
Journal Of The College Of Education For Women
Ability to solve the problems of high orders for students of University
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It is known that life is as series of variety of difficult problems that individual looks
forward to overcome so as to achieve adaptation and to reach the desired aims .The transition
of the students from the school stage to the stage of the university is actually regarded a
dramatic change where students face when they enter university life that differs from what
they lived in secondary school.
The executive functions are considered the main element that participate in solving the
problems of high orders , because it involves the mental abilities that assist individual to
think and initiative as well as solving problems .
These functions include operational planning and the activated memory and inhibition of
q

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Publication Date
Sun Dec 02 2012
Journal Name
Baghdad Science Journal
Effect of Phoenix dactylifera pollen grains suspension in fertility of male rats.
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This study was conducted to determine the role of Phoenix dactylifera pollen grains suspension in improving reproductive efficiency of white male rats. In thisexperiment 40 adult male rats were divided randomly into five equal groups and by following oral administration:the first group was given Phoenix d. pollen grains suspension with concentration 18 mg/kg body weight daily, the second group was given 54 mg/kg, the third group was given 108 mg/kg and fourth group 216 mg/kg body weight, and the last group which represented a control group administrated distilled water only, the administration continued for 40 consecutive days. The effect of Phoenix d. pollen grains in reproductive efficiency was evaluated depending on some parameters such

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Publication Date
Thu Jan 31 2019
Journal Name
Journal Of The College Of Education For Women
Wordy expressions of integrity and reform in the use of holy Quran
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The aim of this message to monitor this phenomenon throught the Quran , which is the constitution of the Islamic nation and Hariatha as well as to express kasalah integrity , justice honesty , patience , abd pacr .
We feel this vocabulary to hight athical values advocated by the Quran and the need to build commitment to the orthodox society free of corruption that leads ta a disorder of the human society .
The outcome of the study the researcher found that faith to a number of results was most notably the advent of righteusness in the Holy Quran meaning of comprehensive RPR spacious field and breadth Maadenh .

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Publication Date
Fri Oct 01 2010
Journal Name
2010 Ieee Symposium On Industrial Electronics And Applications (isiea)
Effectiveness of the cumulative vs. normal mode of operation for combinatorial testing
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Publication Date
Mon Jan 13 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Role Of The Industrial Bank Of Iraq In Developing The Industrial Sector
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The Industrial Banks in most countries in the world plays an essential and vital role in developing the industrial sector due to its effective importance in the economic and social development. The research aims to study the ability of the Industrial Bank of Iraq to the growth and development of the mixed industrial sector companies through loans granted to them. In addition, the research seeks to study credit policies pursued by the Industrial Bank of Iraq to finance the mixed industrial sector companies. The data of the research has been collected from the financial statements of the Industrial Banks of Iraq  for the period 2007-2011, and by means of questionnaire distributed to a sample of the mixed industrial sector companies in

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