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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
Mon May 11 2020
Journal Name
Baghdad Science Journal
The Jacobson Radical of the Endomorphism Semiring of P.Q.- Principal Injective Semimodules
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 In this work, we introduced the Jacobson radical (shortly Rad (Ș)) of the endomorphism semiring Ș =  ( ), provided that  is principal P.Q.- injective semimodule and some related concepts, we studied some properties and added conditions that we needed. The most prominent result is obtained in section three

-If   is a principal self-generator semimodule, then (ȘȘ) = W(Ș).

Subject Classification: 16y60

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Publication Date
Fri Jan 01 2021
Journal Name
Journal Of Economics And Administrative Sciences
The sustainable conflict of globalization And indicators of power rebalancingIn Islamic thought
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 Our research was launched in the study of the sustainable conflict of globalization and the rebalancing of the great powers that have made life on the earth unstable and insecure over the past and present eras, the purpose of which is to pay attention to the waste and instability that human societies are exposed to in different proportions between abstract right and continuous deviation.

The purpose of the study is to show the loss, waste and backwardness in managing and governing societies towards private interests, away from the standards of good institutional governance.

The study’s design was based on two demands, the first on the nature and eternity of

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Publication Date
Thu Nov 01 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Assessment of Nurses Beliefs Toward Reporting of Suspected child abuse in Jordan)
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Abstract Objective: To assess nurses' beliefs toward reporting suspected child abuse. To achieve the objectives of the study a questionnaire of child abuse was used. Methodology:- The sample of the study consist of (224) registered nurses who were employed in general hospitals, pediatric hospitals, National psychiatry and mental illness center, nursing colleges, nursing schools. Data were collected from 20 April 2004 to 20 June 2004.Data were analyzed through the application of descriptive statistical analysis. Percentage frequency and mean and inferential data analysis ANOVA. Results: - The result of t

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Publication Date
Wed May 10 2023
Journal Name
Journal Of Engineering
VARIATION OF SOME WATER QUALITY PARAMETERS OF HUWAIZA MARSH IN SOUTHERN IRAQ
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Huwaiza marsh is considered the largest marsh in the southern part of Iraq. It is located between 31° and 31.75° latitude and extends over the Iraqi-Iranian border; but the largest part lies in Iraq. It is located to the east of Tigris River in Messan and Basra governorates.
In this research, the variation of some water quality parameters at different locations of Huwaiza marsh were studied to find out its efficacy in the treatment of the contamination coming from the wastewater outfall of Kahlaa brokendown sewage treatment plant which lies on the Kahlaa River. This rive is the main feeder of Huwaiza marsh. Ten water quality sampling locations were chosen in this marsh. The water samples were taken during 2009 for three months; Janu

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Publication Date
Wed Feb 05 2020
Journal Name
Political Sciences Journal
The role of the League of Arab States in the Syrian crisis
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Abstract The League of Arab States took many procedures against the Syrian political system, like suspended Syria's membership in the League of Arab States and sent a team of Arab observers headed by Dabi to discuss the situation there and issued some decisions and statements that called the Syrian regime to stop the use of violence and repression against the Syrian opposition.Through these steps, the Arab League has tried to help the Syrian parties to resolve the crisis. However, the role of the league in the Syrian crisis was characterized by weakness in general, and lack of seriousness, which contributed in the aggravation of the situation in Syria, and the intervention of major powers in the internal affairs of Syria.

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
The micronucleated erythrocytes in speeies of Iraqi fish as indieator of dilution
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The micronucleated erythrocytes in fish was used to detect water pollution by genotoxic agents. Fish belonging to different species were collected from three regions from Baghdad during three months (December/2000,January and February/2001 ).The micronucleated erythrocytes was observed in all the specimens. It was concluded that the genotoxic activity' in one region was less than in die other two regions.?

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Publication Date
Thu Oct 01 2020
Journal Name
Biochemical And Cellular Archives
DETECTION OF BACTERIAL INFECTIONS AND THEIR RESISTANCE IN BURN WOUND OF SKIN
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Scopus
Publication Date
Sun Jun 15 2008
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
The prevalence of Schistosomiasis among children of primary Schools in Balad –Rooz
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Balad –Rooz is considered as one of the endemic foci of Schistosomiasisin Iraq.A survey was performed during the first three months of 2002 in fewprimary schools in Balad –Rooz to assess the prevalence among them.

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Crossref
Publication Date
Mon Jan 13 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Role Of The Industrial Bank Of Iraq In Developing The Industrial Sector
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The Industrial Banks in most countries in the world plays an essential and vital role in developing the industrial sector due to its effective importance in the economic and social development. The research aims to study the ability of the Industrial Bank of Iraq to the growth and development of the mixed industrial sector companies through loans granted to them. In addition, the research seeks to study credit policies pursued by the Industrial Bank of Iraq to finance the mixed industrial sector companies. The data of the research has been collected from the financial statements of the Industrial Banks of Iraq  for the period 2007-2011, and by means of questionnaire distributed to a sample of the mixed industrial sector companies in

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Publication Date
Tue Jan 01 2008
Journal Name
Journal Of Alfateh
Study of the current of the MHD generator with modified Bohm diffusion
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generator the metal conductor is replaced by conducting gas plasma.