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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 Feb 16 2026
Journal Name
Journal Of Baghdad College Of Dentistry
An Evaluation of the Effectiveness of Coenzyme Q10 Gel in Management of Patients with Chronic Periodontitis (II inter group comparison)
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Background: Anti-oxidants are used as supplements to counteract the over production of free radicals in periodontal disease.Co-Q10 functions as an intercellular antioxidant by acting as a primary scavenger of free radicals (FRs) and reactive oxygen species (ROS), this study aimed to evaluate the effect of intra pocket application of perio Q gel (coenzyme Q10) alone and as adjunct to scaling and root planing on the periodontal clinical parameters in the treatment of patients with chronic periodontitis and compare the better improvement on the clinical periodontal parameters among different treatment modalities at 3 and 6 weeks. Materials and methods: A total of 323 sites with pocket depth (5-8) mm in patients with chronic periodontitis were

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Publication Date
Sun Dec 06 2009
Journal Name
Baghdad Science Journal
Study of properties of electrical conductivity of Tin dioxide thin films treated with Xenon impulse radiation used as Gas sensors
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During of Experimental result of this work , we found that the change of electrical conductivity proprieties of tin dioxide with the change of gas concentration at temperatures 260oC and 360oC after treatment by photons rays have similar character after treatment isothermally. We found that intensive short duration impulse annealing during the fractions of a second leads to crystallization of the films and to the high values of its gas sensitivity.

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Publication Date
Mon Feb 16 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The effect of addition of untreated and oxygen plasma treated polypropylene fibers on some properties of heat cured acrylic resin
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Background: The polymethyl methacrylate is the most reliable material for the construction of complete and partial dentures, despite satisfying esthetic demand itsuffered from having unsatisfactory properties like impact strength and transverse strength. This study was designed to improve the impact strength and transverse strength of heat cure acrylic resin by adding untreated and oxygen plasma treated polypropylene fibers and investigate the effect of this additive on some properties of acrylic resin materials. Materials and methods: Untreated and oxygen plasma treated polypropylene fibers was added to PMMA powder by weight 2.5 %. Specimens were constructed and divided into 5 groups according to the using tests; each group was subdivided

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Publication Date
Mon Feb 13 2023
Journal Name
Journal Of Educational And Psychological Researches
The Effectiveness of the Cooperative Inquiry Strategy in the Achievement and Development of Mathematical Communication Skills of Elementary School Students
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Abstract

This study aims at investigating the effectiveness of the cooperative inquiry strategy in developing the achievement and development of mathematical communication skills of elementary school students. To achieve this aim, the experimental method was utilized. The study sample consisted of an experimental group (n = 34) and a control group (n = 31), which were randomly selected from primary schools. A Teacher's Guide for teaching a unit entitled "Statistics and Graphic Representations" for the sixth elementary graders in the first semester were devised. A (30) multiple-choice item achievement test distributed at the levels of (recall, comprehension, and application), as well as an (18) item mathematical c

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Publication Date
Mon Dec 01 2014
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The effect of promotion means in the developing the activity of financial markets: A case study of Iraqi stock Exchange
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The promotion by its means lead a vital and important role at the level of all organizations, whether (industrial or service) in general, and financial markets in particular. The promotion is earns delved to be as one of the main operations which  market uses it through various means of financial markets and companies which its shares listed in the aim of (finance or investment), with a view to the implementation and financing of public and private projects the one hand, or with a view to achieving profits through investment of speculative or... For other purposes, on the other hand.Accordingly, we find that the set of public and private goals joint between the financial markets and listed companies respectively, will serve the stra

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Publication Date
Wed Jul 01 2015
Journal Name
Political Sciences Journal
Electoral appeals and the separation of organic health In the Constitution of the Republic of Iraq for the year (2005)
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الخلاصة

تعد الانتخابات بمثابة الطريق المؤدي إلى الديمقراطية كونها النمط الأكثر شيوعاً لمشاركة المواطنين في الحياة السياسية للبلدان واختيار ممثليهم في المجالس التشريعية، حيث أن مطلب إجراء انتخابات حرة ونزيهة لم يعد مطلباً داخلياً فحسب بل مطلباً دولياً يصرّ المجتمع الدولي على الوفاء به وهذا يلقي على عاتق كل دولة أن تضع من الضمانات ما يكفل ممارسة هذه الانتخابات ب

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Publication Date
Wed Apr 01 2020
Journal Name
Indian Journal Of Ecology
Effect of Organic, Mineral Fertilizers and Foliar Application of Humic Acid on Growth and Yield of Corn (Zea mays L.)
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Publication Date
Sun Mar 01 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Measurement of the effect of some macroeconomic variable on the phenomenon of unemployment in Iraq For the period 2003-2018
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The aim of this research is analysis the effect of the changes in (GDA, g, inflation) at average and standard economic curriculum in composition of the models, depending on SPSS program in analysis, and according to available date from central bank of Iraq and during the period from 2003 to 2018 and by using OLS and estimate of the equation and the results showed a statistical significance relation in incorporeal level 5% and the R2 value equal  to 92.1 refer to the changes in independent variables explain 92% of changes of unemployment and the independent variables effect are very limit depend on estimated parameters in the model and respectively (0.986,0.229,-0.060), the research recommended necessity to active the inve

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Publication Date
Wed Jun 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
Integrating the role of internal and external audit to ensure the success of the assessment methodSelf-General Authority of Taxation
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المقدمة

تتعامل الجهات الضريبية في مختلف دول العالم بأساليب عديدة لجباية الضرائب من المكلفين بغض النظر عن فئات وأصناف هؤلاء المكلفين،وفي العراق تم اعتماد العديد من الأساليب لجباية الضرائب على امتداد المدد الزمنية المتعاقبة،وكان لأسلوب التقدير الذاتي وهو أحد تلك الأساليب مجالاً للتطبيق خلال مدة زمنية معينة،حيث جرى تطبيق هذا الأسلوب على وحدات اقتصادية معينة، وبالرغم من المساوئ التي قد ترافق تطبيق

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Effect of Proline and Aspirin on Seed Germination and Seedling Growth of Lycopersicon esculentum and Surface Growth of Fusarium oxysporum
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Research was conducted to study the effect of proline and aspirin with 10 and 20 ppm on seed germination and seedling growth of Lycopersicon esculentumand the effect of surface growthof Fusarium oxysporum.The results showed that the proline and aspirin effected significantly to decreased percentage of seed germination, acceleration of germination, promoter indicator, elongation speed of radical and plumule and also the infection percentage of seed decay and surface growth of Fusarium oxysporumwas reduced significantly.