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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 30 2013
Journal Name
Al-khwarizmi Engineering Journal
Estimation of SNR Including Quantization Error of Multi-Wavelength Lidar Receiver
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 This paper comprises the design and operation of mono-static backscatter lidar station based on a pulsed Nd: YAG laser that operates at multiple wavelengths. The three-color lidar laser transmitter is based on the collinear fundamental 1064 nm, second harmonic 532 nm and a third harmonic 355nm output of a Nd:YAG laser. The most important parameter of lidar especially daytime operations is the signal-to-noise ratio (SNR) which gives some instructions in designing of lidar and it is often limit the effective range. The reason is that noises or interferences always badly affect the measured results. The inversion algorithms have been developed for the study of atmospheric aerosols. Signal-to-noise ratio (SNR) of three-color channel re

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Publication Date
Fri Jun 01 2012
Journal Name
European Journal Of Scientific Research
Occurrence of Cryptosporidium spp among people live in north of Baghdad
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In this study 737 stool specimens were collected from people attending some primary health care centres and hospitals in North of Baghdad, during the period from beginning of April 2009 till the end of March 2010. Different factors were examined to be related with the prevalence of Cryptosporidiosis which were (number of family member, travelling history, source of drinking water and domestic animal present). Significant relations (p≤0.05) were observed between infection rate and the following factor: -Number of family member: The high percentage of Cryptosporidium spp positive cases were seen in families composed of (15-19) and (more than 20) individual which were 28.32% and 16.37% respectively when compared with other family clusters -T

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Publication Date
Fri Jul 01 2022
Journal Name
Journal Of Engineering
Influence of Stone Powder on the Mechanical Properties of Clayey Soil
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In this experimental study, the use of stone powder as a stabilizer to the clayey soil studied. Tests of Atterberg limits, compaction, fall cone (FCT), Laboratory vane shear (LVT), and expansion index (EI) were carried out on soil-stone powder mixtures with fixed ratios of stone powder (0%, 5%, 10%, 15%, and 20%) by the dry weight. Results indicated that the undrained shear strength obtained from FCT and LVT increased at all the admixture ratios, and the expansion index reduced with the increase of the stone powder.

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Publication Date
Sun Jan 13 2019
Journal Name
Iraqi Journal Of Physics
Quantum mechanical study of electronic properties of zigzag nanotubes (9,0) (SWCNTs)
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Quantum calculations on the most stable structure were carried
out for calculating the electronic properties, energies and the charge
density at the Carbon and Hydrogen atoms by Semi-empirical
method (PM3) of zigzag carbon nano tube CNT (9,0) (SWCNTs), at
the equilibrium geometry depending on the pictures of Zigzag
CNT(9,0) which was found to has D3d symmetry point group by
applying for (Gaussian 2003) program. In this work the results
include calculation the relation for axial bonds length, which are the
vertical C-C bonds (annular bonds) in the rings and bonds length
which are in the outer ring that called the circumferential bonds. Also
include a different kind of vibration modes like breathing, puckering

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Publication Date
Tue Nov 08 2022
Journal Name
Aip Conference Proceedings
Prevalence of common skin diseases among outpatients clinic of Baghdad hospital
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Abstract. Healthy skin is an important layer that gives appearance and self-confidence. The skin is affected by internal and external factors that surrounding the body. The problem of skin diseases is considered as one of the widespread diseases. The occurrence of these diseases varies from place to place depending on the nature of climate, the culture of the people, and their economic condition. A cross-sectional study of skin diseases was conducted at the dermatology centre for outpatient clinic of Baghdad hospital. The study is based on 7555 patients of all ages who are attended to this hospital in order to determine the prevalence of skin diseases. The study shows that the most prevalence skin diseases were infectious diseases with

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Publication Date
Wed May 24 2023
Journal Name
College Of Islamic Sciences
Metaphor in the interpretation of the long sea of Ibn Ajiba
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Scientists have delved too much into reality and metaphor, and perhaps a topic of Arabic rhetoric has not received the attention and care of scholars as much as the topic of truth and metaphor. The metaphor opens wide horizons of expression in front of the writer so that he has several means by which he can express the one experience, so his imagination takes off depicting the intelligible as tangible, the seen as audible, and the audible as seen. That image presented by the creative writer.
The first thing to note is that the emergence of metaphor as a rhetorical term was at the hands of the Mu'tazila. Muslims differed about the issue of metaphor in the Holy Qur’an, and the beginning of the dispute was about the verses in which the

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Publication Date
Sun Mar 02 2014
Journal Name
Baghdad Science Journal
Effect of Supplementation Different Level OF Zinc in Boiler Diet, Blood
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Publication Date
Mon Jan 01 2018
Journal Name
Indian Journal Of Public Health Research & Development
Effects of Silver Nanoparticles on Biofilms of <i>Streptococcus</i> Spps
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Today technology using nanoparticle when treatment pathogentic microorganism and we focused on this here. It was found that the species of streptococcus used in present study were sensitive to erythromycin. In present study focusing biofilm formation by Streptococcus spp was evaluated. Species S. mutans was found that highest amount of biofilm compare with the other species. The aim of report effect (SNPs) on ability of biofilm form different species of streptococcus. The anti-biofilm effect of SNPs was in concentration dependent manner. The highest effect of SNP against biofilm formation was found the concentration 160 μg/ml, while the lowest effect was found the lowest used concentration (80 μg/ml) of SNPs. In vivo study revealed that s

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Publication Date
Sat May 01 2021
Journal Name
Key Engineering Materials
The Effect of Temperature Width on Dielectric Constant of Vanadium Dioxide
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A significant influence of temperature width found on the vanadium oxide properties, it plays a major role in highlighting the thermal limits of the three phases (metallic, semiconductor, and dielectric). Two values of the temperature width , and , had taken and studied their effect on both the dielectric constant and its two parts; refractive index, and extinction coefficient, and. It found that: as the temperature width is greater, the more the properties of the three phases for . In addition to increasing the thermal range for phases which can be reached to when , while it's at . Our results have achieved great compatibility with the published results globally. In addition to the effect of both ultraviolet, visible, and infrared

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Publication Date
Fri Sep 30 2022
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetic Study of Transesterification Reaction of Edible Oil Using Heterogenous Catalyst
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   AlPO4 solid acid catalyst was prepared in order to use it in transesterification reaction of edible oil after supporting it with tungsten oxide. The maximum conversion of edible oil was obtained 78.78% at catalyst concentration (5gm.), temperature 70°Ϲ, 30/1 methanol/edible oil molar ratio, and time 5hr. The study of kinetics of the transesterification reaction of edible oil indicates that the reaction has an order of 3/2, while the value of activation energy for  transesterification reaction is 51.367 kJ/mole and frequency factor equal 26219.13(L/ mol.minute).

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