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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
Tue Jan 01 2002
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Variation of digital dermatoglyphics in females of northern Iraq
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The digital dermatoglyphics were studied in 120 females derived from northern region of Iraq (60 Arabs and 60 Kurds). Two kinds of analyses were perfomed : Quantitative and Qualtative. The unilateral and bilateral analyses for dermal ridge counts in each digital and the overall did not reveal any significant difference when t-test was used. A high correlation coefficients were revealed in this study between homologous and adjacent digits, moreover, significant differences were revealed between Arabian and Kurdish samples in both analyses when Fisher Z transform test was used, but the significant differences in the bilateral analysis exceed the ones in the unilateral. This indicates the importance of the former analysis in detecting the vari

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Publication Date
Wed May 25 2016
Journal Name
International Journal Of Current Microbiology And Applied Sciences
Parasitoid insects of Agromyza Fallen (Diptera: Agromyzidae)of Iraq
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Publication Date
Wed Sep 30 2020
Journal Name
College Of Islamic Sciences
Saba is a semantic study of examples of pronouns
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which is much useful in the Arabic Language generally in the Holly Quran especially. It is the pronoun  I have taken in the semantic aspect from it and I have done on the surra sabba which varities  the semantical pronoun in it among the pronoun of the speaker the conscience of the addressee the absent  such the the siprat pronoun that comes in it with the explanation for its importance and its work and this is the subject of the first unit which I advanced it from the concept of the pronoun Linguistically and convention. After that I have lighten in some meanings which I have done in the surrat as a semantic , magnification , proud, reprimand and others which I ended my research I have reached the results from it

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Publication Date
Tue Jun 20 2023
Journal Name
Baghdad Science Journal
Determination of Molecular Weight and Viscosity of Irradiated Polystyrene
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The varied applications of polystyrene in various fields of life led to examining the cause of radiation influence on some rheological behavior of commercial Polystyrene (PS) solution in the chloroform (CHCl3) solvent. Polystyrene grains shape samples were irradiated using the radioactive element Cesium- 137 with (9 µci) activity for 10, 20, and 30 minutes. The viscosity of the polymer solution depends on the concentration and size (i.e. molecular weight) of the dissolved polymer. Experimental data showed that the radiation dose affected the value of viscosity (shear, relative, specific, and reduced). The viscosity value significantly reduced at 10 min radiation dose and when increasing the dose, the viscosity value increased

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Development of resistance of some klebsiella species isolated locally
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200 samples collected Adrar of patients with urinary tract infection were investigating the types of bacteria most local isolates showed high resistance to antibiotics penicillin c ??????? Amoxicillin Beracelin

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Publication Date
Fri Nov 09 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Assessment of the Biological Activities of Calendula officials Extracts
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Objective: To assess two kinds of extraction (aqueous and methanolic) for Calendula officials using flowers, leaves
and stems and studying their antibacterial activity against five different bacteria.
Methodology: Calendula officials were selected to carry out this study. Flowers, leaves and stems were collected from
local markets in Baghdad then dried in shade for 7 days and grinded to fine powder. Aqueous hot extracts for 2hr. at
(100c˚) and alcoholic extracts for 48 hrs at (80c˚) were performed using flowers, leaves and stems then studied
antibacterial effect against five different bacterial genuses by using well diffusion technique.
Results: This study showed that hot aqueous extracts for 2hr. to all parts of Cale

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Publication Date
Wed Jun 20 2012
Journal Name
Journal Of Biotechnology Research Center
Evaluation of toxic effects of two weight reduction pills
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Abstract his study involved evaluation of side effects of two weight reduction pills that had been widely distributed in the last period. Two weight reduction compounds are studied, Reductil (containing chemical substances) and Chinese’s weight reduction herbs (containing natural substances). Two doses for each compound are used in this research; 5mg/ml and 0.5mg/ml for Reductil, while 30mg/ml and 10mg/ml for Chinese weight reduction herbs. To evaluate the toxic effects of these compounds, the following parameters were determined which include mitotic index (cytogenetic analysis), serum FSH and LH hormones level (follicles stimulation hormone/FSH and lutenising hormone/LH) and histological examination of female mice ovaries. Control group

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Publication Date
Fri Dec 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
Transparency of government performance to the state of iraq
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The most important recommendations of this research are:-

1.The benefit of the other countries experiences about the transparency of the government performance, without depending on the transparency that imitating the other experiences; that may not fit with the Iraqi government units.

2.The Ministry of Finance has to prepare the citizen guidebook about the government performance which is considered an essential document, it should be simple and available for all the parties of relation; and for not specialized citizen for the purpose of simplifying the understanding of government performance details.

3.The benefit of the government units websites of inte

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Publication Date
Sun Oct 01 2023
Journal Name
International Science And Technology Journal
Impact of Concentration of Cow MANURE ON Biogas Production
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In Libya, there are multiple sources of pollution, one of which is animal waste. The anaerobic digestion (AD) of organic wastes to produce biogas has the advantage of producing valuable, renewable energy while reducing the environmental impact of these wastes. Cowmanure have the potential to produce biogas due to their high organic content. This study aimed to study different concentrations for the feedstock (1:1 and 2:1 cow manure: water v/v) to monitor which one gives higher biogas production. A plastic tank with a capacity of 72 liters and a feedstock volume of 60 liters was used to create a pilot scale. The biogas was analyzed using a GC device at the end of the experiment in the Zawiya Oil Refining Company. The result indicated that th

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Publication Date
Fri Apr 01 2016
Journal Name
Al–bahith Al–a'alami
Priorities Media Richness of Users of Iraqi Electronic Newspapers
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The electronic press is one of the distinctive media due to its unique features such as instant publishing and interactivity, uses multimedia, the use of hypertext, the personalization of media content, getting echo of the media messages provision of electronic archive of previous numbers of the newspaper.
The richness theory means that media are different depending on its wealth aspects which distinguish it from other media. The aspects of wealth here represent the features that characterize online press and constitute factors of media richness.

The researcher studies the properties of Iraqi media richness of their users. The researcher uses a field study to get the goals of the research and tests the hypotheses of media ric

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