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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
Fri Nov 05 2021
Journal Name
Review Of International Geographical Education Online
Measuring The Efficiency of The Departments of The College of Administration and Economics / University of Baghdad Using the Method of Data Envelopment Analysis (DEA), A Comparative Study
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Publication Date
Fri Jan 01 2021
Journal Name
Review Of International Geographical Education Online
Measuring The Efficiency of The Departments of The College of Administration and Economics / University of Baghdad Using the Method of Data Envelopment Analysis (DEA), A Comparative Study
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The research aims at the possibility of measuring the technical and scale efficiency (SE) of the departments of the College of Administration and Economics at the University of Baghdad for a period lasting 8 years, from the academic year 2013-2014 to 2018-2019 using the method of Applied Data Analysis with an input and output orientation to maintain the distinguished competitive position and try to identify weaknesses in performance and address them. Nevertheless, the research problem lies in diagnosing the most acceptable specializations in the labor market and determining the reasons for students’ reluctance to enter some departments. Furthermore, the (Win4DEAp) program was used to measure technical and scale efficiency (SE) and rely on

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Publication Date
Sun Jan 16 2011
Journal Name
Bayt Alhekma
formations of abstract nouns from groups of goagols
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Abstract The study aimed at reviewing translation theories proposed to address problems in translation studies. To the end, translation theories and their applications were reviewed in different studies with a focus on issues such as critical discourse analysis, cultural specific items and collocation translation.

Publication Date
Sat Mar 31 2018
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetics of Thermal Pyrolysis of High-Density Polyethylene
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Thermal pyrolysis kinetics of virgin high-density polyethylene (HDPE) was investigated. Thermal pyrolysis of HDPE was performed using a thermogravimetric analyzer in nitrogen atmosphere under non-isothermal conditions at different heating rates 4, 7, 10 °C/min. First-order decomposition reaction was assumed, and for the kinetic analysis Kissinger-Akahira-Sunose(KAS), Flynn-Wall-Ozawa(FWO) and Coats and Redfern(CR) method were used. The obtained values of  average activation energy by the KAS and FWO methods were equal to137.43 and 141.52 kJ/mol respectively, these values were considered in good agreement, where the  average activation energy value obtained by CR equation methods was slightly different which equal to 153.16 kJ/

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Publication Date
Fri Dec 30 2011
Journal Name
Al-kindy College Medical Journal
Outcome of surgical treatment of highgrade intramedullary astrocytomas
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Background: Intramedullary astrocytomas
account for about 1% of all CNS tumors and
6–8% of spinal cord tumors. The vast majority
of intramedullary astrocytomas are slowgrowing
lesions.
Objectives: The goal in this study was to
review a series of patients who underwent
surgical removal of intramedullary high-grade
astrocytomas, focusing on the functional
outcome and the effect of multimodality
treatment on the survival of patients with high
grade intramedullary astrocytoma.
Methods: Between June 1999 and June 2004,
22 patients underwent removal of
intramedullary high-grade astrocytomas in four
neurosurgical hospital in Baghdad/ Iraq
(Neurosurgical hospital, Al Shaheed Adnan
Hospital for

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Publication Date
Sat Jun 02 2018
Journal Name
Iosr Journal Of Applied Physics (iosr-jap)
Measurement of Radioactivity inMarsh Sediments of South Iraq
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Publication Date
Wed Mar 01 2023
Journal Name
Baghdad Science Journal
Sum of Squares of ‘n’ Consecutive Carol Numbers
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The discussion in this paper gives several theorems and lemmas on the Sums of Squares of  consecutive Carol Numbers. These theorems are proved by using the definition of carol numbers and mathematical induction method. Here the matrix form and the recursive form of sum of squares of  consecutive Carol numbers is also given. The properties of the Carol numbers are also derived.

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Publication Date
Thu Aug 27 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Clinical importance of gingival biotype (Review of literature)
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This review discusses the gingival biotypes, their characteristics, analysis based on the measurement of the dentopapillary complex. Also discuss their response to inflammation, surgery, and ridge healing after tooth extraction, their influence in the behavior of the peri-implant tissue

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Publication Date
Thu Jun 27 2019
Journal Name
Bulletin Of The Iraq Natural History Museum
REVIEW OF OPISTHOGLYPHOUS SNAKES (REPTILIA, OPHIDIA ) OF IRAQ
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Seven species of semi venomous Opisthoglypha snakes (Reptilia, Ophidia) of Iraq are listed with important characteristics in morphology due to geographical and individual variation of species, as well, the confusion in the scales count of Telescopus tessellatus martini (Schmidt, 1939) of Iraq are discussed.

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Publication Date
Sun Jun 07 2009
Journal Name
Baghdad Science Journal
Spectrophotometry of Saliva of Oral Squamous CellCarcinoma Patients
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Back ground: Spectral analyses of solutions have long been applied to various body fluids for the purpose of clinical study as well as research .Human saliva can be easily obtained by non invasive .In this study typical spectra (for UV and IR) of saliva of oral cancer Squamous cell carcinoma patients were determined under average conditions and evaluated in relation to the spectra of normal specimens. Materials and Methods: Seventeen patients of oral cancer Squamous cell carcinoma and seventeen age matched healthy subject were included in this study .Chewing - Stimulated Saliva was collected in plastic test tube and stored at -20° C. Bach of saliva samples were used for UV and IR measurements. Results: Many differences between the IR spect

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