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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 Jan 07 2016
Journal Name
International Journal Of Innovative Research In Science, Engineering And Technology
Effect Of heat Treatment On The Optical Properties Of CuInSe2 Thin Films
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CuInSe2 (CIS)thin films have been prepared by use vacuum thermal evaporation technique, of 750 nm thickness, with rate of deposition 1.8±0.1 nm/sec on glass substrate at room temperature and pressure (10-5) mbar. Heat treatment has been carried out in the range (400-600) K for all samples. The optical properties of the CIS thin films are been studied such as (absorption coefficient, refractive index, extinction coefficient, real and imaginary dielectric constant)by determined using Measurement absorption and transmission spectra. Results showed that through the optical constants we can made to control it is wide applications as an optoelectronic devices and photovoltaic applications.

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Publication Date
Thu Feb 28 2019
Journal Name
Journal Of Engineering
Economic Benefits for the Application of Standards of Sustainability in Construction Projects
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In this research, that been focused on the most important economic benefits expected when applying the three standards of sustainability in construction projects (economic, environmental and social). Fuzzy AHP, a multi-decision decision-making technique for evaluating construction projects. Which when used we get the speed and accuracy in the results. Using this technique will reduce uncertainties decisions significantly (fuzzy environment), that found in most projects .The results of the data analysis showed  that the economic standards take the greatest relative importance (60%) among the three sustainability standards. Therefore, the implementation of any standards need a cost so the economic benefit of any proje

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Publication Date
Sun Jul 01 2018
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
STUDY ON DIVERSITY OF BEES (HYMENOPTERA, APOIDEA) FROM DIFFERENT REGIONS OF IRAQ
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    The fauna of bees (Hymenoptera, Apoidea) from different regions of Iraq is surveyed in this study; there were 16 species, 13 genera that belong to four families which are collected in this investigation.

 

    Also, all the species that are recorded for Iraq in previous investigations are revised; totally there are 110 species, 32 genera belonging to  five families: Apidae, Andernidae, Colletidae, Halictidae and Megachilidae were listed.

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Publication Date
Wed Aug 01 2018
Journal Name
Journal Of Global Pharma Technology
GC/MS analysis of terpenes of Boswellia serrata resin found in Iraq
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Objective: The aim of this work was to detect terpenes other than boswellic acid derivatives in olibanum of Boswellia Serrata found in Iraq. Methods: The olibanum of Boswellia Serrata was macerated in methanol for one day, then filtration. Filter at was concentrated till reddish brown syrupy residue was gained, (3%) potassium hydroxide was added till basification. This basic solution was stirred continuously until a uniform emulsion was formed, then extracted with chloroform in a separatory funnel; the chloroform fraction was analyzed by GC /MS spectrometry. Results: GC /MS analysis reveal the presence of terpenes and non-terpenes constituents. Conclusion: Most of the detected terpenes were sesquiterpenes and the least one was di-terpenes.

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Publication Date
Sun Oct 15 2023
Journal Name
Revista Bionatura
Estimation of amino acid concentrations in the kidney of albino mice embryo
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Amino acids are the basic building block for peptides and proteins. They are raw materials for generating hormones, purines, pyrimidines and vitamins. Amino acids also provide the body with energy through their carbon structures. The study analyzed the amino acid in the kidneys of the albino mice embryo at 17 and 19 gestation days, using a high-performance liquid chromatography device (HPLC). Samples were obtained after removing them from the embryo and placing them in an ice bath to prevent cell lysis and acid loss. The study found 18 amino acids in the kidneys of the albino mice embryo. They are Asparagine (Asn), Glutamine (Glu), Serine (Ser), Glycine (Gly), Threonine (Thr), Histidine (His), Cysteine (Cys), Alanine (Ala), Proline

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
The effects of raddiation on the optical properties of GERMANIUM SELENIDE semiconductor.
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Study was made on the optical properties of Ge2oSe8othinfilms prepared by vac-uum evaporation as radiated by (0,34,69) Gy of 13 ray.The optical band gab Eg and tailing band A.Et were studied in the photon energy range ( 1 to 3)eV. The a-Ge20Se8o film was found to be indirect gap with energy gap of (1.965,1.9 , 1.82) eV at radiated by B ray with absorption doses of (0,34,69)Gy respectively.The Ea and AEt of Ge20Se80 films showed adecrease in E8 and an increase in AEt with radiation. This be-havior may be related to structural defects and dangling bonds.

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Publication Date
Fri Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
"The role of quality costs in reducing the cost of industrial" products
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Abstract :-

The aim of the research is to explain the role of quality costs their  importance and their classification, and to clarify the most important tools that help to reduce costs.

In order to achieve the objective of the research and test hypotheses adopted the descriptive approach, as well as the adoption of the analytical approach in the study of applied data has been relied upon in providing data on the financial and production reports of the research sample company, the data were used to study and analyze financial and productivity reports . A number of conclusions have been reached the most important being the following

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Publication Date
Thu Jan 31 2019
Journal Name
Journal Of The College Of Education For Women
Wordy expressions of integrity and reform in the use of holy Quran
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The aim of this message to monitor this phenomenon throught the Quran , which is the constitution of the Islamic nation and Hariatha as well as to express kasalah integrity , justice honesty , patience , abd pacr .
We feel this vocabulary to hight athical values advocated by the Quran and the need to build commitment to the orthodox society free of corruption that leads ta a disorder of the human society .
The outcome of the study the researcher found that faith to a number of results was most notably the advent of righteusness in the Holy Quran meaning of comprehensive RPR spacious field and breadth Maadenh .

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Publication Date
Tue Sep 30 2008
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
COMPUTATIONAL ANALYSIS OF THE MIXING ZONE IN THE COMBUSTION CHAMBER OF RAMJET
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A theoretical analysis of mixing in the secondary combustion chamber of ramjet is presented. Theoretical investigations were initiated to insight into the flow field of the mixing zone of the ramjet combustor and a computer program to calculate axisymmetric, reacting and inert flow was developed. The mathematical model of the mixing zone of ramjet comprises differential equations for: continuity, momentum, stagnation enthalpy, concentration, turbulence energy and its dissipation rate. The simultaneous solution of these equations by means of a finite-difference solution algorithm yields the values of the variable at all internal grid nodes.
The results showed that increasing air mass flow (0.32 to 0.64 kg/s) increases the development o

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Publication Date
Thu Dec 20 2007
Journal Name
Journal Of Planner And Development
Globalization and the identity of the mental image structure of urban spaces
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This research discusses the subject of identity in the urban environment as it attempts to answer a number of questions that come with the concept of identity. The first of these questions: What is identity? Can a definition or conceptual framework be developed for identity? What about individual, collective, cultural, ethnic, political and regional identity? Is there a definition of identity in the urban environment in particular? If there is a definition of identity, what about social mobility responsible for social change? How can we see identity through this kinetics? Can we assume that identity in the urban environment has a variable structure or is of variable shape with a more stable structure? Can we determine the spatial-tempora

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