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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 Mar 02 2023
Journal Name
East European Journal Of Physics
Investigation of the Impact of Glass Waste in Reactive Powder Concrete on Attenuation Properties for Bremsstrahlung Ray
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Reactive Powder Concrete (RPC) is one of the most advanced recent high compressive strength concrete. This work explored the effects of using glass waste as a fractional replacement for fine aggregate in reactive powder concrete at levels of 0%, 25%, 50%, and 100%. Linear and mass attenuation coefficients have been calculated as a function of the sample's thickness and bremsstrahlung energy. These coefficients were obtained using energy selective scintillation response to bremsstrahlung having an energy ranging from (0.1-1.1) MeV. In addition, the half-value thickness of the samples prepared has been investigated. It was found that there is a reversal association between the attenuation coefficient and the energy of the bremsstrahlu

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Publication Date
Fri Dec 20 2024
Journal Name
Bulletin Of The Iraq Natural History Museum
INVESTIGATION OF WILD LAND PLANTS OF THE RIPARIAN AREA OF THE DUJAIL RIVER, SALAHALDIN PROVINCE, NORTH OF BAGHDAD, IRAQ
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In the current study, wild land plant specimens were collected during the flowering and fruiting period of these plants in February, April, June, August, and October 2023 from the riparian area of the Dujail River, Salahaldin Province, north of Baghdad, Iraq. Identified and the results showed that the number of these species were: 104 species, belong to 29 plant families, Included 26 dicotyledon families with 76 genera and 96 species. The asteraceae family was the most diverse, with 30 species, followed by Brassicaceae with (12) species. Additionally, there were 13 families represented by only one species in Dujail River which included: Apocynaceae, Berberidaceae, Capparaceae, Caryophyllaceae, Convolvulaceae, Geraniaceae, Lythraceae

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(The role of strategices to manage the human resources in enhancement the process of knowledge management : Field Search in the Ministry of Transportation)
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The aims of the research is to know the role of strategic to manage the human resources in enhancement the process of knowledge management in the Ministry of Transportation , In addition to the effects occurred on outcomes for both the managers and practitioners .

For the purpose of achieving the objectives of the research , the researchers designed a questionnaire that included (40 Points for collecting the primary data from the sample of the research which contained (51) indiviluals. In light of that, the data was to collect and analyzed and hypotheses were tested by using the (SPSS) Program, and a number of statistical techniques was used to attain the goal of the research such as the means ,  Sta

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Thu Oct 01 2009
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Gray-Scale Image Brightness/Contrast Enhancement with Multi-Model Histogram linear Contrast Stretching (MMHLCS) method
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Sat Apr 01 2017
Journal Name
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Transient Stability Enhancement and Critical Clearing Time Improvement for Kurdistan Region Network using Fact Configuration
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The Electrical power system has become vast and more complex, so it is subjected to sudden changes in load levels. Stability is an important concept which determines the stable operation of the power system. Transient stability analysis has become one of the significant studies in the power system to ensure the system stability to withstand a considerable disturbance. The effect of temporary occurrence can lead to malfunction of electronic control equipment. The application of flexible AC transmission systems (FACTS) devices in the transmission system have introduced several changes in the power system. These changes have a significant impact on the power system protection, due to differences inline impedance, line curre

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Thu Nov 02 2023
Journal Name
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Optimum Reinforcement Depth Ratio for Sandy Soil Enhancement to Support Ring Footing Subjected to a Combination of Inclined-Eccentric Load
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This work investigates the impacts of eccentric-inclined load on ring footing performance resting on treated and untreated weak sandy soil, and due to the reduction in the footing carrying capacity due to the combinations of eccentrically-inclined load, the geogrid was used as reinforcement material. Ring radius ratio and reinforcement depth ratio parameters were investigated. Test outcomes showed that the carrying capacity of the footing decreases with the increment in the eccentric-inclined load and footing radius ratio. Furthermore, footing tilt and horizontal displacement increase with increasing the eccentricity and inclination angle, respectively. At the same time, the increment in the horizontal displacement due t

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Experimental investigation on the damping characteristics in dry and saturated sands
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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Investigation Desulfurization Method Using Air and Zinc Oxide/Activated Carbon Composite
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In present work examined the oxidation desulfurization in batch system for model fuels with 2250 ppm sulfur content using air as the oxidant and ZnO/AC composite prepared by thermal co-precipitation method. Different factors were studied such as composite loading 1, 1.5 and 2.5 g, temperature 25 oC, 30 oC and 40 oC and reaction time 30, 45 and 60 minutes. The optimum condition is obtained by using Tauguchi experiential design for oxidation desulfurization of model fuel. the highest percent sulfur removal is about 33 at optimum conditions. The kinetic and effect of internal mass transfer were studied for oxidation desulfurization of model fuel, also an empirical kinetic model was calculated for model fuels

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