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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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Weaponization of outer space from the perspective of international law
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Sun Nov 01 2020
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Potentiality Analysis of Physical Development of International Airports Surrounding Zones
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The areas surrounding Iraqi international airports generally suffer from a lack of interest in their planning in a manner compatible with the airport with the absence of integrated planning between the airport and the city. From here, the search problem appears. It is represented by a lack of interest in the integration of urban planning and airport planning and the lack of a clear policy to deal with the areas surrounding international airports. A desire to achieve the research aims to introduce compatible uses in the vicinity of airports and review the planning and global directions for dealing with the areas surrounding the airports within urban areas. In contrast, the second aspect of the research aims to assess the

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Thu Dec 01 2016
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The role of quality of working life in regulatory alienation
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The goal of this research is to know the quality of working life and its impact on the level of the organizational sense of alienation among a sample of teaching Anbar University in the center of Baghdad. Find and seek to achieve a number of cognitive and practical goals.

Where the quality of work life constitutes one of the main sources to enable organizations of excellence in light of the volatile environment, as is one of alienation regulatory organizations avoid the phenomena that occur because of their negative effects on performance and thus achieve their goals. The most research problem in question the existence of the main deficiencies in the application of the concepts of organiz

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Zinc sulfide(ZnS) thin films of different thickness were deposited on corning glass with the substrate kept at room temperature and high vacuum using thermal evaporation technique.the film properties investigated include their absorbance/transmittance/reflectance spectra,band gap,refractive index,extinction coefficient,complex dielectric constant and thickness.The films were found to exhibt high transmittance(59-98%) ,low absorbance and low reflectance in the visible/near infrared region up to 900 nm..However, the absorbance of the films were found to be high in the ultra violet region with peak around 360 nm.The thickness(using optical interference fringes method) of various films thichness(100,200,300,and 400) nm.The band gap meas

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THE EFFICIENCY OF MICROBIOLOGY IN THE PROCESS OF PESTICIDE BIODEGRADATION
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This study aims at recognizing Pesticides and how the process of pesticides biodegradation by microbiology took place, and the effect of environmental condition on this process. And how the research uncovered the efficiency of microbiology in the biodegradation process of pesticides, as the perfect temperature for the biodegradation process is 40 °C and humidity effect on pesticides efficiency, when high humidity reduces pesticide efficiency and the perfect acidity to increase bacteria efficiency is 7, for the incubation period, it was found during the previous studies that the best incubation period is 5-7 days, in this period the bacteria imprint on pesticides and increase biodegradation of it.

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design of cdte photoconductor detector and study of some electrical
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Been manufacturing detector Altosalih optical pattern contact metal semiconductor through deposition poles of aluminum metal on the chips of crystal cadmium Tleraad (CdTe) with directional [111] and growing with laboratory and annealed at a temperature 80c for 30 minutes and eat Study of some electrical properties nailed and scoutNmadj ??????? copper with non ??????? models to see effect Alichoab well research deals impact Alichoab and frequency detector resistance

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Thu Jun 01 2023
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Thematic characteristics of modern vocabulary of state correspondence in Russian
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Sun Feb 03 2019
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Orphans and Families of Martyrs of Terrorism Expert System-OFMTES
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The increasing number of orphans and their organizations and institutes in our community makes it increasingly important to design and develop an expert system that supports decisions concerning orphans and their families. This system can be used by any orphans organization to facilitate its work.
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Mon Aug 01 2022
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Biannual Journal By Department Of Linguistic And Translation Studies In Bayt Al Hikma
Metaphorical meaning of parts of the human body in Russian
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This article discusses some of the metaphorical use of language units. Here we will define the basic concepts and underline the causes of this phenomenon. Through research it is proven that through the application of names of some body parts achieves the variety of metaphorical meanings.