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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
Tue Aug 01 2023
Journal Name
Journal Of Engineering
Impact of Anchored CFRP Composites on the Strengthening of Partially Damaged PC Girders
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This manuscript investigated the effect of anchorage CFRP wrapping sheets, bolts, and laminate interlock on increasing the efficiency of flexural strengthening for the post-tension girder using CFRP composites techniques longitudinal laminates at the soffit for partially damaged loss of about 14.3% from its area of prestressed concrete beams, and the impact on restoring the original flexural capacity of PC girder. Mitigating delamination of the soffit of horizontal laminates (CFRP). The texture of the laminate and anchorages influenced the stress of the laminate carbon fiber, the mode of crack propagation and failure, and consequently, the beam's attitude has been investigated in this manuscript. The experimental findi

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Publication Date
Mon Feb 01 2016
Journal Name
Journal Of Engineering
Valuation of Construction Projects Based on of Quantity Scale by using Expert System
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The subject of an valuation of quality of construction projects is one of the topics which it becomes necessary of the absence of the quantity standards in measuring the control works and the quality valuation standards in constructional projects. In the time being it depends on the experience of the workers which leads to an apparent differences in the valuation.

The idea of this research came to put the standards to evaluate the quality of the projects in a special system depending on quantity scale nor quality specifying in order to prepare an expert system “ Crystal “ to apply this special system to able the engineers to valuate the quality of their projects easily and in more accurate ways.

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Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Assessing the Effect of Using Porcelanite on Compressive Strength of Roller Compacted Concrete
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Roller-Compacted Concrete (RCC) is a zero-slump concrete, with no forms, no reinforcing steel, no finishing and is wet enough to support compaction by vibratory rollers. Because the effectiveness of curing on properties and durability, the primary scope of this research is to study the effect of various curing methods (air curing, emulsified asphalt(flan coat) curing, 7 days water curing and permanent water curing) and different porcelanite (local material used as an Internal Curing agent) replacement percentages (volumetric replacement) of fine aggregate on some properties of RCC and to explore the possibility of introducing more practical RCC for road pavement with minimum requirement of curing. Cubes specimens were sawed from the slab

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Publication Date
Tue Sep 01 2020
Journal Name
Journal Of Engineering
Performance Evaluation of Pump Station of Main Outfall Drain in AL Nassiriyah City
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The Main Outfall drain pumping station in Nassiriyah is an important part in operation  system of the Main Outfall Drain (MOD) where it reduces the water levels in the U/S area of its and converted through Syphon freely under the Euphrates, its consists of several parts: U/S Basin, Station Building which contains 12 pumps, and Head Basin with Syphon, This station suffers from high levels especially in D/S area due to the current situation which is represented by establishing of dyke with pipes on MOD which located at 24 km from D/S of pumping station and Al-Khamisiyah Canal which located at 2.3 km from the U/S of dyke which feeds(Al Hammar Marsh) during drought season, several scenarios were adopted in order to expl

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Publication Date
Thu Feb 01 2024
Journal Name
Journal Of Engineering
Experimental Evaluation of Stability and Rheological Properties of Foam Cement for Oil Wells
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Oilwell cementing operations are crucial for drilling and completion, preserving the well's productive life. However, weak and permeable formations pose a high risk of cement slurry loss, leading to failure. Lightweight cement, like foamed cement, is used to avoid these difficulties. This study is focused on creating a range of foamed slurry densities and examining the effect of gas concentration on their rheological properties. The foaming agent and foam stabilizer are tested, and the optimal concentration is determined to be 2% and 0.12%, respectively, by the weight of the cement.

Furthermore, the construction of samples of foam cement with different densities (0.8, 1.0, 1.2, 1.4, and 1.6) g/cc is performed to f

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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of Engineering
Serviceability of Post-fire RC Rafters with Openings of Different Sizes and Shapes
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This study deals with the serviceability of reinforced concrete solid and perforated rafters with openings of different shapes and sizes based on an experimental study that includes 12 post-fire non-prismatic reinforced concrete beams (solid and perforated). Three groups were formed based on heating temperature (room temperature, 400 °C, and 700 °C), each group consisting of four rafters (solid, rafters with 6 and 8 trapezoidal openings, and rafter with eight circular openings) under static loading. A developed unified calculation technique for deflection and crack widths under static loading at the service stage has been provided, which comprises non-prismatic beams with or without opening exposed to flexure concentra

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Publication Date
Mon Jun 19 2023
Journal Name
Journal Of Engineering
Some Properties of Superplasticized and Retarding Concrete Under Effect of Accelerated Curing Methods
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In recent decades, tremendous success has been achieved in the advancement of chemical admixtures for Portland cement concrete. Most efforts have concentrated on improving the properties of concrete and studying the factors that influence on these properties. Since the compressive strength is considered a valuable property and is invariably a vital element of the structural design, especially high early strength development which can be provide more benefits in concrete production, such as reducing construction time and labor and saving the formwork and energy. As a matter of fact, it is influenced as a most properties of concrete by several factors including water-cement ratio, cement type and curing methods employed.
Because of acce

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Publication Date
Mon Sep 30 2024
Journal Name
Medical Journal Of Babylon
Effectiveness of Deep Breathing Technique on Pain Level of School Children during Catheterization
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Publication Date
Sat Oct 01 2022
Journal Name
Journal Of Engineering
Evaluation of the Physical and Chemical Treatment of Wastewater for the Dairy Industry
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Dairy wastewater generally contains fats, lactose, whey proteins, and nutrients. Casein precipitation causes the effluent to decompose into a dark, strong-smelling sludge. Fluid waste contains soluble organic matter, suspended solids, and gaseous organic matter, which cause undesirable taste and smell, grant tone and turbidity, and advance eutrophication, which plays an essential role in increasing biological oxygen demand (BOD) in water. It also contains detergents and disinfecting agents from the rinses and washing processes, which increase the need for chemical oxygen (COD). One of the characteristics of dairy effluents is their relatively high temperature, high organic contents, and wide pH range, so the discharge of wastewater into

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Publication Date
Tue Sep 01 2020
Journal Name
Heliyon
Extraction, optical properties, and aging studies of natural pigments of various flower plants
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