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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
Wed Mar 01 2023
Journal Name
Baghdad Science Journal
Sum of Squares of ‘m’ Consecutive Woodall Numbers
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        This paper discusses the Sums of Squares of “m” consecutive Woodall Numbers. These discussions are made from the definition of Woodall numbers. Also learn the comparability of Woodall numbers and other special numbers. An attempt to communicate the formula for the sums of squares of ‘m’ Woodall numbers and its matrix form are discussed. Further, this study expresses some more correlations between Woodall numbers and other special numbers.

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Publication Date
Sun Sep 04 2011
Journal Name
Baghdad Science Journal
Determination of bacterial contamination of milk using fluorometry
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The aim of this paper is to determine the feasibility of using fluorometric methods as an indicator for quality and contamination of milk with E.coli bacteria, and selection the suitable wavelength to be used with laser induced auto fluorescence. Three groups of milk samples were used in this study: Fresh pasteurized milk samples, milk samples containing different concentration of E.coli bacteria which were added artificially, and milk samples that were kept in refrigerator for 3-5 days. Thirteen excitation wavelengths were used to get the emission spectra for all milk samples using spectroflourometer .The results showed that the emission spectra at 275nm excitation wavelength gave a good differentiation between these three groups.

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Publication Date
Fri Dec 30 2011
Journal Name
Al-kindy College Medical Journal
Outcome of surgical treatment of highgrade intramedullary astrocytomas
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Background: Intramedullary astrocytomas
account for about 1% of all CNS tumors and
6–8% of spinal cord tumors. The vast majority
of intramedullary astrocytomas are slowgrowing
lesions.
Objectives: The goal in this study was to
review a series of patients who underwent
surgical removal of intramedullary high-grade
astrocytomas, focusing on the functional
outcome and the effect of multimodality
treatment on the survival of patients with high
grade intramedullary astrocytoma.
Methods: Between June 1999 and June 2004,
22 patients underwent removal of
intramedullary high-grade astrocytomas in four
neurosurgical hospital in Baghdad/ Iraq
(Neurosurgical hospital, Al Shaheed Adnan
Hospital for

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Publication Date
Sat Mar 31 2018
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetics of Thermal Pyrolysis of High-Density Polyethylene
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Thermal pyrolysis kinetics of virgin high-density polyethylene (HDPE) was investigated. Thermal pyrolysis of HDPE was performed using a thermogravimetric analyzer in nitrogen atmosphere under non-isothermal conditions at different heating rates 4, 7, 10 °C/min. First-order decomposition reaction was assumed, and for the kinetic analysis Kissinger-Akahira-Sunose(KAS), Flynn-Wall-Ozawa(FWO) and Coats and Redfern(CR) method were used. The obtained values of  average activation energy by the KAS and FWO methods were equal to137.43 and 141.52 kJ/mol respectively, these values were considered in good agreement, where the  average activation energy value obtained by CR equation methods was slightly different which equal to 153.16 kJ/

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Publication Date
Sun Jan 16 2011
Journal Name
Bayt Alhekma
formations of abstract nouns from groups of goagols
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Abstract The study aimed at reviewing translation theories proposed to address problems in translation studies. To the end, translation theories and their applications were reviewed in different studies with a focus on issues such as critical discourse analysis, cultural specific items and collocation translation.

Publication Date
Thu Nov 01 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Assessment of Factors that Contribute of Lung Cancer
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Abstract A descriptive study to assess of factors that contributes of lung cancer. The study was carried out in Specialized Surgery teaching hospital, Ibin Al- Beetar hospital and Ibin Al- Nafees hospital for the period From January 2004 to October 2004 .The study aimed to assess the factors that contribute to lung cancer and to identify the relationship between the variables of the study with lung cancer. A purposive (non-probability) sample of (70) patients with lung cancer was selected for the study. An assessment form was employed for the purpose of the study. Test- retest reliability was employed through

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Publication Date
Thu Jun 27 2019
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
REVIEW OF OPISTHOGLYPHOUS SNAKES (REPTILIA, OPHIDIA ) OF IRAQ
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Seven species of semi venomous Opisthoglypha snakes (Reptilia, Ophidia) of Iraq are listed with important characteristics in morphology due to geographical and individual variation of species, as well, the confusion in the scales count of Telescopus tessellatus martini (Schmidt, 1939) of Iraq are discussed.

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Publication Date
Wed Sep 01 2021
Journal Name
International Scientific Congress Of Pure, Applied And Technological Sciences (minar Congress)
Evaluation Of Electromagnetic Pollution Of Cellular Mobile Network
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Wireless communications are characterized by their fastest growth in history, as they used ever-evolving and renewed technologies, which have allowed them to spread widely. Every day, communication technology introduces a new invention with features that differ from its predecessor. Bell Laboratories first suggested mobile wireless communication services to the general population in the late 1940s. Still, it wasn't easy at that time to use on a large scale due to its high costs. This paper aims to describe the state of cellular mobile networks; by comparing the sources of electromagnetic pollution caused by these networks, measure the level of power density in some residential areas, and compare them with international standards adopted in

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Publication Date
Sat Dec 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Impact of Electronic commerce In Imposition of taxes
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That the possibility of imposing a tax on electronic commerce is increasing interest in it by governments in developed and developing countries alike, and there is interest in a logical by governments and bodies of taxation, in particular in developing countries erosion potential tax in the tax base resulting from the adoption of e-commerce if not mutation rules and tax legislation, local and international to take into account this important economic developments and how to keep up, said the combination of the taxation system is the only way to increase revenue needed to finance government spending on goods and services needed by society.

The most important conclusions reached by the rese

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Publication Date
Fri Mar 15 2019
Journal Name
Journal Of Baghdad College Of Dentistry
Assessment of Bacterial Contamination of Orthodontic Arch wire
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Background: The microorganisms can impend the life of health care professional and particularly the dental practitioners. They can be transmitted by different ways like airborne and droplet transmission. The current study was carried out to identify whether the arch wires that received from the manufactures are free from microbial contamination and to determine the bacterial species attached to the arch wires. Materials and Methods: This study involved eighty samples, consisted of two types of arch wires (nitinol and stainless-steel) from four companies (3M, G&H, Jiscop, OrthoTechnology). These wires inserted in a plane tube that contains 10 -ml of (Tris [tris(hydroxymethyl)aminomethane] and EDTA (ethylenediaminetetraacetic acid) tri

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