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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
Sat Sep 30 2023
Journal Name
Al–bahith Al–a'alami
The Role of Website Users in the Consumption of Notifications: A Field Study of Websites
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This research seeks to explore the impact of notifications on enhancing user engagement with websites, primarily through user subscriptions and their interaction with notifications on these websites. The significance of this study lies in its implications for crafting compelling headlines that capture users' attention, streamline their access to journalistic content, and align with the objectives and editorial policies of news websites. It sheds light on the factors influencing users' preferences for specific notifications and their engagement with content based on their individual interests, motivations, and the satisfaction derived from such interactions.
The researcher has reached several key findings, inc

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Publication Date
Sat Jun 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
The impact of dimensions of concerning the distribution of daily Iraqi newspapers informing customer loyalty
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Abstract

The study deal with two main variables:- the dimensions of distribution, and the customer loyalty . the researcher has chosen samples of Iraqi newspapers like (AL Sabah, AL Mada, AL Bayna aljdeida newspaper), because this product depends greatly on the consumption of customers so as to achieve the success. After studying the dimensions of these variables ( cost, flixibilty & deliver time ) which concerns the distribution, and for these dimensions ( marketing relationship, customer perception, customer experience, brand, & product quality) which relate to the customer loyalty . the problem has been identified in a number of remarks concerning the extent of awareness that the administration

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Publication Date
Sat Dec 31 2022
Journal Name
Journal Of Economics And Administrative Sciences
Evaluation of the Strategic Performance of the State Board of Antiquities and Heritage/Case Study
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This research aims to the possibility of evaluating the strategic performance of the State Board for Antiquities and Heritage (SBAH) using a balanced scorecard of four criteria (Financial, Customers, Internal Processes, and Learning and Growth). The main challenge was that the State Board use traditional evaluation in measuring employee performance, activities, and projects. Case study and field interviews methodology has been adopted in this research with a sample consisting of the Chairman of the State Board, 6 General Managers, and 7 Department Managers who are involved in evaluating the strategic performance and deciding the suitable answers on the checklists to analyze it ac

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Publication Date
Sun Dec 31 2017
Journal Name
College Of Islamic Sciences
The effect of the significance of the Qur'anic context in the allocation of the year
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Acting on the Holy Qur’an by contemplating its meanings, stopping at its commands and prohibitions, and everything in it that guides us to truth and mercy. The Holy Qur’an includes it for various purposes in one verse, and there is no doubt that this is part of the perfection of this great book, and one of the sciences of the fundamentalists is the indication of the context, and it is a great science of high rank, and it is one of the most important things that lead to the correct understanding of the miraculous and decisive book of God Almighty, and one of the best meanings of the Qur’an It was not from the context of the verses, and from here it can be said that the indication of the context is one of the origins of deriving lega

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Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
The Impact of climatic fluctuations in the production of citrus in the province of Karbala
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The relationship between the elements of the climate and the productivity of citrus (kg
/ tree) in the province of Karbala has been determined through the use of simple correlation
coefficient of Pearson (rp) and (t) test. The result for each of oranges, limes and tangerine had
all shown moral and relevant statistical indications; except for relative humidity, which were
not linked to a moral relationship with productivity of tangerine, oranges and limes.As for the
relationship between climatic factors and yield of bitter orange were all not significant
statistically and very weak.
In order to determine the strength of the correlation between fluctuations in the
climatic elements and fluctuations in the productivi

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Publication Date
Sun Jan 01 2023
Journal Name
Journal Of Advanced Pharmaceutical Technology & Research
Use of factorial design in formulation and evaluation of intrarectal in situ gel of sumatriptan
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Publication Date
Sat Jan 15 2011
Journal Name
International Journal Of Poultry Science
Influence of Source of Oil Added to Diet on Egg Quality Traits of Laying Quail
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This experiment was performed to investigate the influence of different oils in the diets of laying quail on their egg quality characteristics. One hundred and twenty 7-wk old Japanese quails (Coturnix coturnix japonica) were allocated to four groups with three replicates containing 10 quail each (30 quail per each treatment group). They were fed for 13 weeks (including one week of adaptation period) on diets containing 3% oil from different sources, viz. either sunflower (T1), linseed (T2), maize (T3), or fish oil (T4). Inclusion the diet of laying quail with fish oil (T4) and maize oil (T2) resulted in significant increase with respect to egg weight, yolk weight, albumen weight, yolk diameter, yolk height, albumen diameter, albumen height

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Publication Date
Wed Jan 01 2020
Journal Name
2nd International Conference On Materials Engineering & Science (iconmeas 2019)
Modeling of adsorption isotherms of oil content through the electrocoagulation treatment of real oily wastewater
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Publication Date
Thu Jan 01 2015
Journal Name
Iosr Journal Of Applied Chemistry
Purification of G-Protein Coupled Receptor from Membrane Cell of Local Strain of Saccharomyces cerevisiae
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Publication Date
Sun Jan 01 2017
Journal Name
Iraqi Journal Of Agricultural Sciences 47 (1)‏
Effect of irrigation intervals and foliar of salicylic acid on growth and yield of Potato
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