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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 10 2021
Journal Name
Baghdad Science Journal
Serum Protein Profile Of Iraqi Hydatidosis Patients with Different Sites of Infection
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Blood samples of One hundred and twenty patients from different hospitals in Baghdad infected with hydatidosis in different sites of the body (Liver, Lung, multiorgans and kidney) were collected for this study. On the other hand, 30 healthy individuals were included as a control group. This study was conducted to evaluate the effect of this disease on the serum protein profile of the patients using electrophoresis. The results revealed four different protein banding patterns with difference in number of bands and their molecular weights in comparison to the control group, and these differences depended on the site of infection. However the data showed a presence of the same band in all patients with different site of infection.

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Publication Date
Sun Sep 30 2018
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetic Study of Hydroisomerization of n-Decane using Pt/SAPO-11 catalysts
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The hydroisomerization of n-decane was studied on SAPO-11 catalyst. Catalyst of 0.25wt.%Pt/SAPO-11 was prepared locally and used in the present work. The hydroconversion performed in a continuous fixed-bed laboratory reaction unit. Experiments of n-decane isomerization were performed in a temperature range of 200 to 275°C,LHSV range of 0.5-2 h-1, and hydrogen to decane mole ratio of 2.1-8.2. The results show that the n-decane conversion increases with increasing temperature and  decreasing LHSV , the maximum conversion 56.77 % was achieved at temperature 275°C and LHSV of 0.5 h-1. The kinetic of n-decane isomerization was also studied and the reaction was first order. The kinetic analysis also showed that the activation energy eq

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Publication Date
Fri Nov 09 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Knowledge of Prenatal Care Nurses toward Management of Toxoplasmosis in Pregnant Women
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Objective: This study aims to assess the level of nurse's knowledge regarding toxoplasmosis management
in pregnant women.
Methodology: A descriptive analytic study was carried out from January 2012 to March 2012. A sample of
(70)nurses who provide prenatal care to pregnant women at primary health care centers of AL-Adala,ALHindia,AL-Askary,AL-Jamea,AL-Ansar
and AL-Salam in AL-Najaf city. The questionnaire was self-completed
and included questions on sociodemographic characteristics and toxoplasmosis aspects.
Results: The findings of the study indicated that (44.3%) of nurses have moderate level of knowledge.
(32.9%) of nurses was with age ranging from 31-36 years. (74.3%) were male. (52.9%) were secondary
graduate

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Publication Date
Sun Jan 02 2022
Journal Name
Journal Of The College Of Languages (jcl)
The Effect of Genderism on the Process and the Product of Translation
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    Many studies have been made and still concerning the field of translation. Since the mid-90's a considerable amount of researches has tackled the problem of gender and its effect on the process and the product of translation. Simon (1996, p 508) points out that when comparing women and men as translators and writers through history, women seem to be the weaker side. This paves the way to feminist movements which produce prominent studies concerning gender as a concept and translator's gender as practice on the quality and the accuracy of the translation.           

     Flotow (in Meschia, 2012, p 1-4) outlines several issues that can be

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Publication Date
Sat Dec 02 2017
Journal Name
Al-khwarizmi Engineering Journal
Improvement of Microhardness and Corrosion Resistance of Stainless Steel by Nanocomposite Coating
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Abstract

 

Stainless steel (AISI 304) has good electrical and thermal conductivities, good corrosion resistance at ambient temperature, apart from these it is cheap and abundantly available; but has good mechanical properties such as hardness. To improve the  hardness and corrosion resistance of stainless steel its surface can be modified by developing nanocomposite coatings applied on its surface. The main objective of this paper is to study effect of electroco-deposition method on microhardness and corrosion resistance of stainless steel, and to analyze effect of nanoparticles (Al2O3, ZrO2 , and SiC)  on properties of composite coatings. I

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Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Modeling of Electron and Lattice Temperature Distribution Through Lifetime of Plasma Plume
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When employing shorter (sub picosecond) laser pulses, in ablation kinetics the features appear which can no longer be described in the context of the conventional thermal model. Meanwhile, the ablation of materials with the aid of ultra-short (sub picosecond) laser pulses is applied for micromechanical processing. Physical mechanisms and theoretical models of laser ablation are discussed. Typical associated phenomena are qualitatively regarded and methods for studying them quantitatively are considered. Calculated results relevant to ablation kinetics for a number of substances are presented and compared with experimental data. Ultra-short laser ablation with two-temperature model was quantitatively investigated. A two-temperature model

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Publication Date
Mon Aug 29 2016
Journal Name
World Journal Of Experimental Biosciences (issn: 2313-3937)
Effect of lead on biofilm formation by environmental isolates of Bacillus spp.
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Biofilm formation is one of the biggest challenges of scientists. Role of heavy metals in forming biofilm is not clear enough. Here, the effect of lead on biofilm formation by Bacillus spp. isolated from soil in terms of biofilm formation and remove was studied. In present study, 10 isolates of Bacillus spp were isolated from soil. The ability of all isolates to form biofilm was evaluated. The effect of lead on biofilm formation was studied by adding lead (pb) before forming biofilm. In another experiment the lead was added after biofilm formation to study the effect of lead on biofilm remove. The current study, showed the ability of all studied isolates to form biofilm. Maximum biofilm formation by Bacillus spp isolate number 8 (B8) follow

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Publication Date
Tue Aug 20 2019
Journal Name
Political Sciences Journal
"Khurasan statehood" : new centralization of ISIS and limits of incursion and development
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Abstract This study aims to discover the ways that adopted by extremism to expand to new geographical areas, in order to spread out its ideology, which led to create new geo-strategic zone, aims to recognize ISIS’s strategy to move towards new geographic locations and the motivations behind these transformations, the study also analyses all aspects of this strategy, the group’s relationship with other terrorist groups in these areas and limits of the competition between them. The study also highlights the factors that have led ISIS to move to new geographical areas and its techniques to control them.

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Publication Date
Thu Jun 13 2019
Journal Name
Al–bahith Al–a'alami
The role of radio advertising in promoting purchasing decisions of Iraqi citizens
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This research aims to identify the role of radio advertising in promoting purchasing decisions of Iraqi audiences, especially that the placement of the announcement through the Iraqi radio stations dealt with a little of Iraqi researchers, and the goal of the research to know the extent of public exposure to the radio advertising through Iraqi radio and patterns of exposure,disclosure of the reasons for public hearing of the radio advertisement, identifying the most important factors influencing the decision to buy in the radio advertisement, this research is descriptive in terms of type as the researcher used the survey method,questionnaire and scale for data and information collection, the sample was selected according to the purp

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Publication Date
Wed Apr 02 2025
Journal Name
University Of Thi-qar Journal
Production of Thermostable Bioflocculant from Bacillus subtilis and Optimization of Flocculation Conditions
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Bacteria strain H7, which produces flocculating substances, was isolated from the soil of corn field at the College of Agriculture in Abu-Ghrib/Iraq, and identified as Bacillus subtilis by its biochemical /physiological characteristics. The biochemical analysis of the partially purified bioflocculant revealed that it was a proteoglycan composed of 93.2 % carbohydrate and 6.1 % protein. The effects of bioflocculant dosage, temperature, pH, and different salts on the flocculation activity were evaluated. The maximum flocculation activity was observed at an optimum bioflocculant dosage of 0.2 mL /10 mL (49.6%). The bioflocculant had strong thermal stability within the range of 30-80 °C, and the flocculating activity was over 50 %. The biofloc

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