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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
Sun Jun 03 2012
Journal Name
Baghdad Science Journal
Approximate Solution of Some Classes of Integral Equations Using Bernstein Polynomials of Two-Variables
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The research aims to find approximate solutions for two dimensions Fredholm linear integral equation. Using the two-variables of the Bernstein polynomials we find a solution to the approximate linear integral equation of the type two dimensions. Two examples have been discussed in detail.

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Publication Date
Mon Nov 08 2021
Journal Name
Caspian Journal Of Environmental Sciences 20 (1),
Evaluate the effect of alcoholic extraction of walnut on gonadal hormones of treated rats
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Publication Date
Thu Mar 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
The Impact of Intellectual trends on the nature of the Economic Structure of Iraq
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The Impact of Intellectual trends on the nature of the Economic Structure of Iraq

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Publication Date
Sat Sep 30 2023
Journal Name
College Of Islamic Sciences
Features of visual formation in the poetry of the poets of the Umayyad era
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Abstract

The Umayyad poets tried to invest all artistic tools in order to achieve a measure of creativity in their texts. The phenomenon of visual composition is breaking the familiar writing system, with the aim of increasing the number of possible connotations. The visual in the Umayyad poetry tries to replace it through expression with the visual image, and its manifestations were manifested by the multiplication of punctuation marks in the body of the poetic text and the tearing of the single poetic line by cutting it into several sentences or repetition.

Keywords: visual formation, poetic writing, Umayyad poetry, recipien

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Publication Date
Sat Mar 30 2002
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Effects of Drying Conditions on the Properties of Dried Particles of Powdered steep Liquor
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Publication Date
Wed Jan 01 2020
Journal Name
Plant Archives
STUDY OF THE EFFECT OF COLD PLASMA ON THE REPRODUCTIVE ENDOCRINOLOGY OF MALE RATS
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Cold atmospheric plasma (CAP) is used widely in medical and biological fields because of non-thermal effected. Direct application of plasma is preferred in medical functions, so, direct application of cold plasma has obtained by the floating electrode dielectric barrier discharge (FE-DBD) system. The purpose of this paper to review the effect of (CAP) on the reproductive hormones (testosterone, LH, E2, progesterone, for male rats. The study appeared that no significant effect on E2 and progesterone hormone for all time of exposure, besides this significant difference in LH hormone (P<0.05) at 15 sec, (P<0.0001) at 30, 90 sec and (P<0.001) at 60 sec of exposure to plasma. Added to that significant difference (P<0.01) at 15, 30, 60 sec and no

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Publication Date
Sun Dec 07 2008
Journal Name
Baghdad Science Journal
The effect of doping ratio of Cu on the structural properties of CdSe Films
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Films of CdSe have been prepared by evaporation technique with thickness 1µm. Doping with Cu was achieved using annealing under argon atmosphere . The Structure properties of these films are investigated by X-ray diffraction analysis. The effect of Cu doping on the orientation , relative intensity, grain size and the lattice constant has been studied. The pure CdSe films have been found consist of amorphous structure with very small peak at (002) plane. The films were polycrystalline for doped CdSe with (1&2wt%) Cu contents and with lattice constant (a=3.741,c=7.096)A°, and it has better crystallinty as the Cu contents increased to (3&5wt%) Cu. The reflections from [(002), (102). (110), (112), and (201)]planes are more prominen

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Publication Date
Wed Jan 02 2019
Journal Name
Journal Of The College Of Languages
The Outcomes of War: A Study of the Character After the Crisis of War
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World War II has brought suffering for all people; it has led people to have a nostalgic feeling. The war has many faces all of them are ugly, like death, separation, loneliness, violence, crime, betrayal, and disconnection and many other meanings. Michael Ondaatje in his novel The English Patient (1992) portrays a picture of the effect of World War II on four different characters; Hana a Canadian nurse, The English patient who is Hungarian, Caravaggio a Canadian-Italitan thief, and Kip an Indian sapper. They live together in one house, share their secrets and memories about World War II. Ondaatje brings them together to reveal their secrets and to heal their wounds of the war experience.

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Publication Date
Wed Jan 02 2019
Journal Name
Journal Of The College Of Languages (jcl)
The Outcomes of War: A Study of the Character After the Crisis of War
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World War II has brought suffering for all people; it has led people to have a nostalgic feeling. The war has many faces all of them are ugly, like death, separation, loneliness, violence, crime, betrayal, and disconnection and many other meanings. Michael Ondaatje in his novel The English Patient (1992) portrays a picture of the effect of World War II on four different characters; Hana a Canadian nurse, The English patient who is Hungarian, Caravaggio a Canadian-Italitan thief, and Kip an Indian sapper. They live together in one house, share their secrets and memories about World War II. Ondaatje brings them together to reveal their secrets and to heal their wounds of the war experience.

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Publication Date
Sun Jun 30 2013
Journal Name
Al-khwarizmi Engineering Journal
Effects of Different Types of Fillers on Dry Wear Characteristics of Carbon-Epoxy Composite
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Experimental investigations had been done in this research to demonstrate the effect of carbon fiber and Ceramic fillers contents on the tribological behaviour of (15% volume fraction) carbon-epoxy composite system under varying volume fraction, load, time and sliding distance. The wear resistance were investigated according to ASTM G99-05standard using pin on disc machine to present the composite tribological behaviour. The influence of three ceramic fillers, granite, perlite and calcium carbonate (CaCO3), on the wear of the carbon fabric reinforced epoxy composites under dry sliding conditions has been investigated. The effect of variants in volume fraction, applied load, time and sliding distance on the wear behaviour of po

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