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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
Fri Jun 30 2023
Journal Name
College Of Islamic Sciences
The Role Of Atheism In The Demolition Of Societal Security
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The enemies of religion are still following the approach of undermining the Islamic faith in various ways through the diversity of methods of smear campaigns by raising suspicions to obliterate the Islamic identity and threaten security and stability of social life under the Islamic religion in Islamic societies, as we find that they have employed the doctrine of atheistic thought in order to distance people from the path of truth, distort the features of religion, destabilize psychological security and family stability, and thus destroy societal security by questioning the tolerant faith at times, and by raising suspicions at other times.

Hence, this research came to review the legal duty that requires Islamic scholars to protec

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Publication Date
Thu Jun 29 2017
Journal Name
College Of Islamic Sciences
The prohibition of cheating in the Sunnah of the Prophet
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In The Name of Allah Most Gracious Most Merciful

Cheating is one of the forbidden actions and reprehensible morals that are forbidden by Islamic law, because it involves an assault on rights, whether they are the rights of God Almighty or the rights of God.

people, or self-rights, and because it involves harming others.

Since the Sunnah of the Prophet is the second source of Islamic law, many of the noble hadiths of the Prophet forbid and prohibit cheating.

This study sheds light on it.

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Influence of Laser Irradiation Times on Properties of Porous Silicon
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Porous silicon (P-Si) has been produced in this work by photoelectrochemical (PEC) etching process. The irradiation has been achieved using diode laser of (2 W) power and 810 nm wavelength. The influence of various irradiation times on the properties of P-Si material such as P-Si layer thickness, surface aspect, pore diameter and the thickness of walls between pores as well as porosity and etching rate was investigated by depending on the scanning electron micrograph (SEM) technique and gravimetric measurements.

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Publication Date
Sat Feb 09 2019
Journal Name
Journal Of The College Of Education For Women
A Study of the Problems of Learning and Translating Idioms
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Idioms are a very important part of the English language: you are told that if you want to go far (succeed) you should pull your socks up (make a serious effort to improve your behaviour, the quality of your work, etc.) and use your grey matter (brain).1 Learning and translating idioms have always been very difficult for foreign language learners. The present paper explores some of the reasons why English idiomatic expressions are difficult to learn and translate. It is not the aim of this paper to attempt a comprehensive survey of the vast amount of material that has appeared on idioms in Adams and Kuder (1984), Alexander (1984), Dixon (1983), Kirkpatrick (2001), Langlotz (2006), McCarthy and O'Dell (2002), and Wray (2002), among others

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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Educational And Psychological Researches
Psychological analysis of the drawings of prisoners in the Kurdistan
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The goal of current research to identify the implications of intellectual and psychological drawings of women in prison in Sulaimaniya province through her paint and collected through cooperation with the creativity of the development organization of women in Sulaimaniya, consisted search of five chapters, the first chapter contains the goals of the research and its problem and its significance in addition to its limits and determine the terminology, while the second chapter included the theoretical framework and the literature on the subject of the search, and in the third quarter where he explained the researchers research methodology and procedures, either in the fourth quarter may offer researchers graphics prisoners and then read th

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Publication Date
Wed Jun 30 2010
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetic and Isotherm Modeling of Adsorption of Dyes onto Sawdust
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Sawdust has the ability to adsorb the dyestuff from aqueous solution. It may be useful low cost adsorbent for the treatment of effluents, discharged from textile industries. The effectiveness of sawdust has been tested for the removal of color from the wastewater samples containing two dyes namely Direct Blue (DB) and Vat Yellow (VY). Effect of various parameters such as agitation time, adsorbent dose and initial concentration of each dye has been investigated in the present study. The adsorption of dyes has been tested with various adsorption isotherm models. The Langmuir isotherms model is found to be the most suitable one for the dye adsorption using sawdust and the maximum adsorption capacity is 8.706 mg/g and 6.975 mg/g for DB and V

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Publication Date
Tue Jul 01 2003
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
THE ABDOMINAL NERVE GANGLIA OF SOME CARABIDAE (COLEOPTERA) OF IRAQ
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The abdominal nerve cord of some species of Iraq Carabids has been studied to evaluate
the variation in the number of the abdominal ganglia among the species and to find out
relation of these variations with the classical taxonomy of the family Carabidae into tribes.

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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
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.
The proposed work is designed to manage the Orphans and Families of Martyrs of Terrorism Expert System (OFMTES) by registry all information about all orphans to display mostly orphan deserves bill, data is entered for each orphan, and with each entry a counter is increased according to this input information; the output result represents the score for that orphan. Different orphans have different scores. Coloring is used to know the degree o

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Publication Date
Fri Apr 01 2011
Journal Name
Iraqi Journal Of Community Medicine
Anatomical and Histological Features of Placentae of Different Age Groups
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Methods: 112 placentae samples were investigated during the period from August 2007 to August 2008 under light microscopefor mother aged 15 - 45 years old.Results: It was found that normal placental shapes had no correlation to mother age, while abnormal shapes were found more inyoung age groups. The better placental measured parameters were found in mother age 20-24 years. The percentages ofabnormal umbilical cord insertion were very high compared to other studies. Babies’ gender had a correlation with theplacental thickness; male babies have thicker placentae than females. Male babies have longer umbilical cords with widerdiameter than females. Light microscope picture showed the chorionic villi with isolated fetal blood vessel were hig

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Publication Date
Sat Sep 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Preparation and characterization of oro-dispersible tablets of bromhexine hydrochloride
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