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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 Apr 30 2020
Journal Name
Journal Of Economics And Administrative Sciences
Evaluating the quality of municipal services according to the financial budgets for years 2006-2016 Analytical research in Diwaniyah Governorate
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The research aims at determining the main reason for the deterioration of the services and determining the correct method of distributing the funds to the administrative and administrative units. The discrepancy between the size of the financial allocations and the municipal services was the main research problem. Therefore, the researcher identified the gaps in municipal services by the concerned departments and compared them with The percentage of funds obtained through the work of a checklist for each of the directorates concerned. The researcher studied the specific criteria for these services, which were approved by the Ministry of Construction, Housing, Municipalities, and Public Works, and compared them wi

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Publication Date
Sun Jul 03 2016
Journal Name
Journal Of Educational And Psychological Researches
The Impact of the Constructive Scientific Stations Strategy on Achievement and Mind Habits for The Fourth Scientific students in biology
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The study aimed at ideutifying the impact of scieutific skills in strategy and liabits of mind amony stueuts in tenth grade . The study demanded to choose a sampie that coutaiun (42) student of the fourth grade of the secondary school who were dirided into tow groups , the first is experimental studied according to scieutific skill strategy , and the other controlling , studied according to the  usualway . An achievement test  has been taken that adopted  staudard for mind skills as research tools that are applid after ascertaining  sincerity proved at the end of the experiment .The study has reached to the conclusion that there are statistically significant differnces in farour of the experiment group in both

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Publication Date
Mon Jun 05 2023
Journal Name
Al-khwarizmi Engineering Journal
Removal of Malachite Green from Aqueous Solution using Ficus Benjamina Activated Carbon-Nonmetal Oxide synthesized by pyro Carbonic Acid Microwave
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Activated carbon derived from Ficus Binjamina agro-waste synthesized by pyro carbonic acid microwave method and treated with silicon oxide (SiO2) was used to enhance the adsorption capability of the malachite green (MG) dye. Three factors of concentration of dye, time of mixing, and the amount of activated carbon with four levels were used to investigate their effect on the MG removal efficiency. The results show that 0.4 g/L dosage, 80 mg/L dye concentration, and 40 min adsorption duration were found as an optimum conditions for 99.13% removal efficiency. The results also reveal that Freundlich isotherm and the pseudo-second-order kinetic models were the best models to describe the equilibrium adsorption data.

 

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Publication Date
Tue Feb 24 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Immunohistochemical expression of Cyclin D1 and NF-KB p65 in oral lichen planus and oral squamous cell carcinoma (Comparative study)
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Background: Oral Lichen Planus (OLP) is a chronic inflammatory mucosal disease, presenting in various clinical forms WHO had regarded OLP as a precancerous conditions in 1978 because of its potential with cancer. Both antigen-specific and nonspecific mechanisms involved in the pathogenesis of OLP. Oral Squamous Cell Carcinoma (OSCC) is the most common malignant neoplasm of the oral cavity representing more than 94% of oral cancer. It occurs in different sites and has many etiological factors. Cyclin Dl is a proto-oncogene which consider as the key protein in the regulation of cell proliferation and its overexpression led to the occurrence and progression of malignant tumors.NF-KB p65 is a member ofNF-kB family of transcription factors that

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Publication Date
Mon Mar 08 2021
Journal Name
Journal Of Physics: Conference Series
Design and Implementation of a Moving Robot Equipped with an Arm and an FPGA to Deliver Objects between Two Positions
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Abstract<p>In this paper a system is designed and implemented using a Field Programmable Gate Array (FPGA) to move objects from a pick up location to a delivery location. This transportation of objects is done via a vehicle equipped with a robot arm and an FPGA. The path between the two locations is followed by recognizing a black line between them. The black line is sensed by Infrared sensors (IR) located on the front and on the back of the vehicle. The Robot was successfully implemented by programming the Field Programmable Gate Array with the designed system that was described as a state diagram and the robot operated properly.</p>
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Publication Date
Sat Jan 02 2021
Journal Name
Journal Of The College Of Languages (jcl)
Methods of computer word formation in the modern Russian language: Способы словообразования в сфере компьютерных неологизмов в современном русском языке
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This paper discusses the study of computer Russian language neologisms. Problems of studying computer terminology are constantly aggravated by the processes of computer technology that is introduced to all walks of life. The study identifies ways of word formation: the origin of the computer terms and the possibility of their usage in Russian language. The Internet is considered a worldwide tool of communication used extensively by students, housewives and professionals as well The Internet is a heterogeneous environment consisting of various hardware and software configurations that need to be configured to support the languages used. The development of Internet content and services is essential for expanding Internet usage. Some of the

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Publication Date
Fri Dec 30 2022
Journal Name
Voprosy Istorii
Changing the agricultural map of Diyala Governorate for the years (1980, 1990, 2000, 2010, 2020) using GIS and remote sensing
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Abstract. Geographical and remote sensing, which gave a picture of the change in the area of agricultural land in the study area for selected years (1980, 1990, 2000, 2010, 2020). In particular and Iraq in general, as this led to a reduction in the areas of agricultural lands and in return an increase in arid lands and their desertifica- tion and the loss of their productive value, which as a result leads to the migration of the population, the change of land sex, the failure to achieve food security and dependence on the import of the food basket.

Publication Date
Mon Apr 01 2024
Journal Name
Iop Conference Series: Earth And Environmental Science
Studying some of the optimal conditionals for the best bacterial isolates from soil and its effects on their growth rates
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Abstract<p>The current study aimed to use some bacterial isolates from the local soil of Baghdad city by study the effects of temperature, pH and incubation period on the growth rates of isolated bacteria and choose the optimal conditions for their diversity and for understanding bacterial growth and their requirements for survival and proliferation. This information can be applied to obtain their high growth rate for use in various fields such as agriculture, medicine and environmental sciences in the future. And it used to assess the degree of variation in across bacteria species in pH, temperature and incubation period. A number of local bacterial isolates as <italic>Enterobacter cloacae</italic></p> ... Show More
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Publication Date
Wed Aug 11 2021
Journal Name
Neuroquantology
Measuring the Pollution Level with Uranium and Radon in the Soil of Some Areas Inside Baghdad University Campus-AL-Jadiriyah
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In present study, the technique was used, including nuclear track detector type (CR-39), for appreciative concentrations uranium and radon in soil samples from Baghdad University Campus-AL-Jadiriyah utilizing a prolonged -term with a solid-state nuclear path sensor, a technique for charged particles has been developed., the radon concentrations, effective dose rate and uranium concentrations have measured in soil samples. Eight various venues from soil Baghdad University Campus have appointed. The results indicated variant values about uranium and radon concentrations, the average value for radon gas, effective dose rate and uranium concentrations was found to be 281.59 Bq/cm3, 7.09 mSv/y and 0.01 Bq/mm-2 respectively. All results a

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Publication Date
Sun Feb 10 2019
Journal Name
Journal Of The College Of Education For Women
The Female Characters In The Pre-Raphaelite Novel: M.E. Braddon’s Lady Audley’s Secret (An Extracted Research of Master Degree Letter)
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Victorian age is known as a time of perpetual change. It is a time of new industrialization, increased urbanization and new technology. Therefore, one of the strongest undercurrents of this is the position of women. Woman at that time was viewed as “an angel in the house” especially this who belongs to the upper-middle class. She is described in such term because she spends much time in her domestic domain. Therefore, she should be passive, obedient and dependent. Despite the Victorian society contains several classes; women are defined under two labels: the angel and the demon or the whore. The angel woman can be any woman from the lower middle class to the aristocracy, while the whore refers to any working class woman. The differen

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