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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 Sep 12 2019
Journal Name
Al-kindy College Medical Journal
Reliability of fine needle aspiration biopsy in diagnosis of breast lump
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Background: breast cancer is commonest cancer globally and the 1st cancer in Iraq among females, its management and prognosis depend on early diagnosis, the traditional method was excisional biopsy which is expensive and invasive leading to delayed diagnosis, FNAB is cheap nom invasive more acceptable to women, Aim of the study: to test the reliability of FNAB in preoperative diagnosis of breast lump.

Methodology: This is a retrospective study of 204 cases, 102 breast cancer cases and 102 benign breast lesions, taken between Jan. 2017 – Nov. 2017. The sample taken from the breast cancer early detection center in  Al-Alwiyaa maternity teaching hospital, during the year 2017

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Publication Date
Sun Mar 13 2011
Journal Name
Baghdad Science Journal
Effect of Manganese Chloride in Histological of Ovaries in Albino mice
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Manganese is considered as one of heavy metals with high toxicity .This element has been used widely in various industries and it is spread with huge quantities in polluted industries areas. As a result the concentrations of this element in the environment have increased and consequently producing acute toxic effects in different tissues and organs of all organisms. A study has been conducted on (30) female of Swiss albino mice, to find out the effect of manganese chloride in histopathological changes of ovaries. The study includes, giving the manganese chloride with concentrations (150, 200 and 250 mg/kg) for (15, 30 and 45 day) for each concentration. The

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Publication Date
Mon Dec 30 2019
Journal Name
College Of Islamic Sciences
His eloquence of Quranic verses in the verses of the Resurrection
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 The research tagged (eloquence of the Qur’anic verses in the resurrection verses) deals with study and analysis of the aesthetics of miracles in the Qur’anic poems centered on the horrors of the Day of Resurrection, and aims to clarify the role of the Qur’anic unique and its impact the miraculousness of the Qur’anic style systems, the accuracy of the unique selection and its wonderful harmony in form and content, voice and meaning, composition And a picture with its context and denomination; based on that, the research was based on the analytical method to reach its goal, and the research plan imposed its division into two preamble and two topics, the first topic dealt with: the rhetoric of the nominal Qur’anic verses in

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Publication Date
Sun Jun 12 2011
Journal Name
Baghdad Science Journal
Effect of additive polyvinyl alcohol polymer on properties of cement – Silica
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Study the effect of additives polymer polyvinyl alcohol (PVA) after solving in water by concentration 10% since represent a standard of PVA solution with added to cement – silica composite of ratio (1:2) with 5%, 10%, 15%, 20%, and 25% respectively to the standard quantity of water which using as a mortar of building. The results are demonstrate increasing on compression resistance with increase of PVA solution until 20%, and decreasing of thermal conductivity which represent a composite are increasing in thermal insulating. The results were recommended decreasing of water absorption with increase of PVA solution ratio as illustrated in this study.

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Publication Date
Sat Oct 01 2022
Journal Name
Al–bahith Al–a'alami
THE IMAGE OF THE IRAQI IN THE MENTALITY OF THE ITALIANS
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Increased interest in the subject of the image because of its great and growing link to the life of the individual and society and its impact on the overall political, economic and cultural conditions. This interest is no longer confined to the images of people or institutions, but has become beyond that to the images of countries and peoples and the impact on bilateral relations between them,

However, we find that the image of the Iraqi abroad remained vague and has not been scientifically recognized and the most that we can generalize are the features of the image of Arabs and Muslims abroad; and assume that the image of the Iraqi applies to them as the Iraqi is in the end an Arab or Muslim.

Based on this, the research

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Publication Date
Tue Sep 01 2009
Journal Name
Al-khwarizmi Engineering Journal
Study Effect of Dezincification on the Fatigue Properties of Brass Alloy
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This research includes a study of dezincification by corrosion from brass alloys in three types of media, which are acidic solution, basic and slat solution in different percentages. The study show the higher dezincification occurs in basic solution which decrease the fatigue properties where the fatigue properties are inversely proportional with dezincification.

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Publication Date
Sat May 16 2009
Journal Name
Journal Of Planner And Development
Quantitative analysis of the economic characteristics of the land transport network
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Highway network could be considered as a function of the developmental level of the region, that it is representing the sensitive nerve of the economic activity and the corner stone for the implementation of development plans and developing the spatial structure. The main theme of this thesis is to show the characteristics of the regional highway network of Anbar and to determine the most important effective spatial characteristics and the dimension of that effect negatively or positively. Further this thesis tries to draw an imagination for the connection between highway network as a spatial phenomenon and the surrounded natural and human variables within the spatial structure of the region. This thesis aiming also to determine the natu

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Publication Date
Mon Dec 31 2012
Journal Name
Al-khwarizmi Engineering Journal
The Effect of Doppler Phenomenon on the Speed of Blood Flow
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This research studying the phenomenon of Doppler (frequency Doppler) as a method through which the direction and speed of the blood cells flows in blood vessels wear measured. This Doppler frequency is relied upon in medicine for measuring the speed of blood flow, because the blood flow is an important concept from the concepts of medicine. It represents the function and efficient of the heart and blood vessels in the body so any defect in this function will appear as a change in the speed of blood flow from the normal value assumed. As this speed changes alot in cases of  disease and morbidity  of the heart, so in order to identify the effect of changing the Doppler frequency on the speed of blood flow and the relationship of

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Publication Date
Fri Dec 01 2023
Journal Name
Political Sciences Journal
Impact of the Rising of China in Restructuring the International System
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It is no secret to everyone that the Arab individual suffers from poor self-awareness and political awareness, which made the state and the importance of its existence and preserving its institutions not among his interests, which made researchers wonder about the possibility of strengthening it and the extent of its impact on the future of building the contemporary Arab state. So, the study attempts to addressing the issue of community awareness and its impact on building the state through a clear intellectual vision that blended what is social and political to define the concept of community awareness and highlight its importance and role as a basic pillar in shaping and building modern Arab countries in the Arab world and ways to enha

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Publication Date
Sat Oct 01 2022
Journal Name
Al–bahith Al–a'alami
Trends of journalists and consumers about the phenomenon of food fraud
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Food comes after air and water in terms of importance in the survival of human beings, In addition, it is the support and strength of health and support, if lost or destroyed man would die or get sick and become a heavy burden on himself and his society. Food, like other sources of life, is subject to various risks and corruption comes from countless sources. Among these dangers is the result of spontaneousness, lack of knowledge or compulsion due to the interaction of variables beyond the will of the producer and the consumer, such as pollution of water, air and environment and their reflection on food consumed by people. However, we can’t deny that some reasons of corruption are intentional and resulting from a planning in advance in

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