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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 Jun 25 2023
Journal Name
Iraqi Journal Of Agricultural Sciences
BREEDING POTENTIAL OF RICE GENOTYPES IN TWO AGROCLIMATIC CONDITIONS OF SULAIMANI - KURDISTAN REGION - IRAQ
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This study was aimed to investigate the genetic variability of 26 rice genotypes and evaluation at two locations in Sulaimani governorate, Gaba and Chawtan which were completely different in their environmental condition during the season of 2019. The performances of the genotypes were analyzed at both locations as well as the average of both. Simple coefficients of correlation were used to assess the grain yield components and their relationships. Path analysis was used to determine the direct and indirect effects of such components on grain yield plant-1. The genotypes were grouped based on the agro-morphological features using cluster analysis. Almost all of the traits at both locat

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Publication Date
Mon Jun 01 2020
Journal Name
International Journal Of Agricultural And Statistical Sciences
The effect of some herbicides on the companion weed to three cultivars of oats
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A field experiment was carried out to find out the effect of some herbicides(Pallas, Crash, U46) on the companion weed to three cultivars of the oat crop (Shefa, Hamel, and Pimula) and the yield and its components of these cultivars. The results showed the superiority of the two treatments of spraying weed herbicides (T1 and T2 ) by giving the best results, as they recorded the lowest number of weed plants after 30 days of spraying reached 1.44 and 1.67 plant/m2 . Besides, the lowest weed dry weight was 0.11 and 0.00 g/m2, and the highest inhibition percentage in dry weight was 98.44% and 100.0% of the two treatments, respectively. The treatment T2 was also superior by giving the highest control percentage of 93.28% compared to the compari

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Publication Date
Thu Jan 09 2014
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci.
Effect of Thickness on the Electrical Conductivity and Hall Effect Measurements of (CIGS) films
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The influence of different thickness (500, 1000, 1500, and 2000) nm on the electrical conductivity and Hall effect measurements have been investigated on the films of copper indium gallium selenide CuIn1-xGaxSe2 (CIGS) for x= 0.6.The films were produced using thermal evaporation technique on glass substrates at R.T from (CIGS) alloy. The electrical conductivity (σ), the activation energies (Ea1, Ea2), Hall mobility and the carrier concentration are investigated and calculated as function of thickness. All films contain two types of transport mechanisms of free carriers, and increases films thickness was fond to increase the electrical cAnductivity whereas the activation energy (Ea) would vary with films thickness. Hall Effect analysis resu

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Publication Date
Tue Feb 05 2019
Journal Name
Journal Of The College Of Education For Women
Geographical distribution of the potato crop in the district of Abo – Ghraib, 2005- 2011
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Source of energy and protein Field crops considered an important needed for human
beings Due of this fact increases should appear in the quantities of their production in order to
meet the needs of continuous increasing in the population of the glope year after year ;
otherwise, an increase in the gap between the amount of production and consumption will
occur .
This study aims to reveal the geographical distribution of the potato crop in the district
of Abu – Ghraib. For this purpose, a study conducted about the cultivated areas, production
and crop yields per Dunam for period of 7 years lasted from 2005-2011.
The study shows that potato is one of the most important field crops that are grown in
the Abu –

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Publication Date
Sat Mar 01 2008
Journal Name
Iraqi Journal Of Physics
Influence of Gold Concentration on the Main Detection Parameters of Ge-Au Photoconductive Detector
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Ge-Au infrared photoconductive detection was prepared from germanium single crystal which were doped with different gold concentration using thermal evaporation. The spectral resonsivity (Rλ), spectral detectivity (D*) were determined as function of wavelength, also the resistance, conductivity in dark and with illumination to infrared radiation, the gain and relative photo response have been measured with different gold concentration. Remarkable improvements in the photoresponse gain were observed for the highest resistance specimen at the expense of spectral detectivity values.

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Publication Date
Sun Jun 30 2019
Journal Name
Journal Of The College Of Education For Women
The poetry of the sensory image of Ibn Dannir al-Musli poems (B627 H.)
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تُعبّرُ الصُّورةُ الحسَّيةُ في شعرِ ابن دُنَينير الموصليِّ([i]) في بنيتها عن تجربةِ الشاعرِ الوجدانيةِ والذهنيةِ, وأفكارهِ ومشاعرِهِ؛ فيصوغُ بها مَفهومًا جديدًا للواقعِ الماديِّ والمعنويِّ، الذي يتسمُ بالوضوحِ أولاً، وبالقرْبِ من الذهنِ ثانيًا، للربْطِ بين الحواسِّ الإنسانيةِ والمعاني الذهنيةِ، لِتُقَدِّمَ الصُّورةُ الحسيَّةُ إلى ((المتلقي صُورًا مرئيةً، يُعادُ تشكيلُها سياق

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Publication Date
Mon Dec 10 2018
Journal Name
Indian Journal Of Natural Sciences
Verification the Pollution of Tigris River in South of Baghdad using Remote Sensing Techniques
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This paper describes the use of remote sensing techniques in verification of the polluted area in Diyala River and Tigris River and the effected of AL-Rustamiyah wastewater treatment plant, which is located on Diyala River, one of the branches of Tigris River in south of Baghdad. SPOT-5 a French satellite image of Baghdad, Iraq was used with ground resolution of 2.5 m in May 2016. ENVI 5.1 software programming was utilized for Image processing to assess the water pollution of Diyala and Tigris River’s water. Five regions were selected from a study area and then classified using the unsupervised ISODATA method. The results indicated that four classes of water quality which are successful in assessing and mapping water pollution which confi

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Publication Date
Thu Feb 07 2019
Journal Name
Journal Of The College Of Education For Women
Aesthetics third line of the Diversity of his methods in the architecture at Mosques
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The Islamic Arts which include calligraphy and specifically the third line of the greatest
manifestation of Islamic civilization affair, and it was the mosques and mosques and holy
shrines scattered in the city of Baghdad, which had a deep impact in enhancing
communication
This means research study (third line aesthetics diversity of tactics in the architecture of
mosques) It is located in four seasons, which included the first chapter the research problem
represented by asking the following - :
-What are the methods of implementation of the third line in the architecture of mosques ?
And reflected the importance of research in it represents a serious attempt to investigate the
diversity in the organization des

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Publication Date
Sat Feb 02 2019
Journal Name
Journal Of The College Of Education For Women
The Role of Woman In Improving Society: The Role of Woman In Improving Society
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Abstract:
One of the most prominent historical stage feature that is well- known
nowadays in the world is democracy issue. This issue gives man the right to
reflect his concept and notions . It,s the world of freedom , human right and
liberation of women. This leads to the principle of equality between women
and men which is put in the top of liberty and Improvement lists .
Improvement can be defined as a group of means and ways that is
used to direct human work to improve their level of life economically and
socially .
This study contains three sections, the first presents the social state of
women in pre-history period . And the second section presents the theory of
improvement as an important social ph

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Publication Date
Sun Feb 17 2019
Journal Name
Iraqi Journal Of Physics
A study of the solvent effect on the low temperature spectra of benzoanthracene molecules
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been taken at room temperature down to liquid nitrogen temperature (77K). Polar and nonpolar solvents have been used to study the solvent effect on the absorption and fluorescence spectra of solute molecules. Some of the spectroscopic parameters have been determined as functions of solvent polarity and temperature. The results indicate that the band width FWHM increases with increasing the solvent polarity and temperature, while the peak emission cross section decreases with increasing of solvent polarity and decreases with increasing the temperatures. Clear vibrational structure spectra of benzoanthracene molecules have been observed in Nonane and Hexane solvents at 77K.

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