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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
Thu Jan 01 2026
Journal Name
Lecture Notes In Networks And Systems
The Iraqi Judicial System in Light of the Activation of the Role of the Forensic Accountant: Proposed Strategies and Methods
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Forensic accounting (FA) is an important tool in exposing financial manipulation and corruption within institutions, making the role of FA essential in the Iraqi judicial system (IJS). This role suffers from limited implementation due to the lack of specialized legislation and insufficient awareness of its importance. The role of FA in the IJS can be enhanced by enhancing professional training, amending university curricula to include FA, and developing legislation regulating this field. Furthermore, cooperation between courts and the FA should be strengthened to ensure adequate financial evidence (FE) in judicial cases. For example, the experiences of developed countries, such as the United States and the United Kingdom, demonstrate how FA

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Publication Date
Tue Oct 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
The applicability of green productivity tools: An analytical study in a sample of industrial companies in the province of Nineveh
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                The current research aims to identify the most important green productivity tools GPT and the possibility of applied in industrial companies in general and the companies operating in the province of Nineveh, in particular, as well as the study of some personality characteristics and functional, which is believed to be an impact on the application of these tools in industrial companies. Accordingly, the research community of managers in the company of medicines and medical supplies ready-made clothes _ operating in the province of Nineveh, who are (80) while the manager was subjected to research procedures (49) Director representing (61.25%)

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Publication Date
Thu Dec 01 2022
Journal Name
Baghdad Science Journal
A Green Synthesis of Iron/Copper Nanoparticles as a Catalytic of Fenton-like Reactions for Removal of Orange G Dye
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This research paper studies the use of an environmentally and not expensive method to degrade Orange G dye (OG) from the aqueous solution, where the extract of ficus leaves has been used to fabricate the green bimetallic iron/copper nanoparticles (G-Fe/Cu-NPs). The fabricated G‑Fe/Cu-NPs were characterized utilizing scanning electron microscopy, BET, atomic force microscopy, energy dispersive spectroscopy, Fourier-transform infrared spectroscopy and zeta potential. The rounded and shaped as like spherical nanoparticles were found for G-Fe/Cu‑NPs with the size ranged 32-59 nm and the surface area was 4.452 m2/g. Then the resultant nanoparticles were utilized as a Fenton-like oxidation catalyst. The degradation efficiency of

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Publication Date
Fri Sep 30 2022
Journal Name
College Of Islamic Sciences
The Effectiveness of Combining the Meanings of Grammatical Tools in Understanding the Arabic Sentence A study of Some Linguistic Evidences
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abstract

The grammatical tools (the letters of meanings) are of great importance in understanding the meanings of the Arabic sentences,

This research is a simple attempt to show how our venerable scholars employed the meanings of these tools when they interpreted the linguistic evidence, that is, the grammatical structure largely depends on the tool in forming the meaning within the sentences and employing the meanings of these grammatical tools in explaining the linguistic evidence by clarifying their significance in the contexts of their use and effectiveness. Synthesis of the meanings of grammatical tools is an important tool in understanding the linguistic structure in order to reveal its meaning.

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Publication Date
Tue Aug 01 2017
Journal Name
International Journal Of Science And Research
Effects of Pregabalin Drug on Level of Reproductive Hormones, Sexual Activity, Number and Weight of Offspring in Female Albino Rats
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Abstract: This study was aimed to investigate the effect of two doses of pregabalin (PGB) on hormonal level and sexual activity in female albino rats. Ninety female rats with age (9-10 weeks) and weight (200±20 g) were divided into three major groups of thirty rats. First group was considered as control G1, the second G2 and third G3 groups were exposed to PGB into two doses 150, and 300 mg/kg body weight per day respectively. Each major group was divided into three subgroups (subgroup A, B, and C of each has ten rats), the treatments last for one month for subgroup A, two months for subgroup B, and three months for subgroup C. Five rats from each subgroup were placed separately into two breeding cages with two isolated males and wait

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Publication Date
Tue Dec 01 2020
Journal Name
Journal Of Economics And Administrative Sciences
The Impact of Envy on Workplace Stress A field Study of Faculty Staff at the Technical College of Management-Baghdad
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The research aims to measure the impact of envy on job stress because the topic of envy represents a negative emotion that exists at all organizational levels, which may cause stress in the work environment.

The Research problem is represented by the lack of perception of most of the faculty staff on the negative effects of envy on their well-being in the Technical College of Management - Baghdad, and what is the impact level of envy on their job stress.

To achieve this, the scale of envy was based on two dimensions (being envied, Envying others), While the job stress scale was based on seven dimensions (workload, conflict role, Family factors, work environment, work relationships

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Publication Date
Sun Jun 30 2013
Journal Name
Al-khwarizmi Engineering Journal
Study on the Effect of the Curvature of Solar Collector on Wind Loading Coefficients and Dynamic Response of Solar Collector
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In the current research, the work concentrated on studying the effect of curvature of solar parabolic trough solar collector on wind loading coefficients and dynamic response of solar collector. The response of collector to the aerodynamic loading was estimated numerically and experimentally. The curvature of most public parabolic trough solar collectors was investigated and compared. The dynamic response of solar collector due to wind loading was investigated by using numerical solution of fluid-structure interaction concept. The experimental work was done to verify the numerical results and shows good agreement with numerical results. The numerical results were obtained by using finite element software package (ANSYS 14). It was found

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Publication Date
Fri Jan 01 2016
Journal Name
Journal Of The Electrochemical Society
Electrochemical Incineration of Oxalic Acid at Manganese Dioxide Rotating Cylinder Anode: Role of Operative Parameters in the Presence of NaCl
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A detailed experimental study was devoted to the anodic oxidation of oxalic acid using manganese dioxide rotating cylinder anode with the objective to evaluate in a systematic way the effect on the oxalic acid oxidation process of several relevant parameters, including the presence of sodium chloride, the current density (J), the rotation speed, the temperature, and the initial concentration of oxalic acid. Thin manganese dioxide film on graphite substrate has been prepared by electrochemical oxidation from MnSO4-H2SO4 electrolyte. The morphology of this electrode was investigated by XRD, SEM, EDS and AFM techniques. The results show that a firm γ-structure of MnO2 film on graphite rod can be obtained successfully. The results indicate tha

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Publication Date
Sat Dec 31 2022
Journal Name
Al-kindy College Medical Journal
Assessment of Serum Level of Protein Carbonyl as a Marker of Protein Oxidation in Patients with Type 2 Diabetes Mellitus
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Background: Diabetes mellitus is a chronic disease with an increasing prevalence worldwide and characterized by an increase in oxidative stress and inflammation. The most important factor that is responsible for oxidative stress and production of reactive oxygen species (ROS) is hyperglycemia. The major targets of ROS are proteins. The most common and widely used biomarker of severe oxidative protein damage is protein carbonyl content.

The study was designed to assess the serum level of protein carbonyl as a marker of protein oxidation in patients with type 2 diabetes mellitus and to evaluate the effect of age, body weight, waist circumference, diabetic control and disease duration on the level

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Publication Date
Sun Feb 01 2015
Journal Name
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Reliability Estimation Of Fuzzy Failure Times Of Free Distribution And It Use To Estimate The Fuzzy Reliability Of Mosul Dam
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The way used to estimate the fuzzy reliability differs according to the nature of the information of failure time which has been dealt in this research.The information of failure times has no probable distribution to explain it , in addition it has fuzzy quality.The research includes fuzzy reliability estimation of three periods ,the first one from 1986 to 2013,the second one from 2013 to 2033 while the third one from 2033 to 2066 .Four failure time have been chosen to identify the membership function of fuzzy trapezoid represented in the pervious years after taking in consideration the estimation of most researchers, proffional    geologists and the technician who is incharge of maintaining of Mosul Dam project. B

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