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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 Jan 27 2026
Journal Name
Modern Sport
Determining standard levels to test the strength endurance characteristic of speed for basketball players for juniors aged under (16) years
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Publication Date
Sat Jun 01 2024
Journal Name
Baghdad Science Journal
Carbon Dioxide Availability in Inlands Rivers Is Driven by Dissolved Organic Carbon, Not Warming: A Case Study of Tigris River
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الانهار اصبحت مشبعة بثاني اوكسيد الكربون بشكل عالي وبذلك فهي تلعب دور مهم في كميات الكربون العالمية. لزيادة فهمنا حول مصادر الكربون المتوفرة في النظم البيئية النهرية، تم اجراء هذه الدراسة حول تأثير الكربون العضوي المذاب والحرارة (العوامل الرئيسية لتغير المناخ) كمحركات رئيسية لوفرة ثاني اوكسيد الكربون في الانهار. تم جمع العينات من خمسة واربعون موقع في ثلاثة اجزاء رئيسية لنهر دجلة داخل مدينة بغداد خلال فص

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Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Physics: Conference Series
Laser Irradiation Effect on The Optical Properties of CoO<sub>2</sub>Thin Films deposited via Semi-Computerized Spraying System
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Abstract<p>In this paper deals with the effect laser irradiation on the optical properties of cobalt oxide (CoO<sub>2</sub>) thin films and that was prepared using semi computerized spray pyrolysis technique. The films deposited on glass substrate using such as an ideal value concentration of (0.02)M with a total volume of 100 ml. With substrate temperature was (350 C), spray rate (15 ml/min).The XRD diffraction given polycrystalline nature with Crystal system trigonal (hexagonal axes). The obtained films were irradiated by continuous green laser (532.8 nm) with power 140 mW for different time periods is 10 min,20min and 30min. The result was that the optical properties of cobalt oxide thin films affe</p> ... Show More
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Publication Date
Wed Dec 01 2021
Journal Name
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Antimicrobial Effect of Eco- Friendly Silver Nanoparticles Synthesis by Iraqi Date Palm (Phoenix dactylifera) on Gram-Negative Biofilm-Forming Bacteria
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Date palm silver nanoparticles are a green synthesis method used as antibacterial agents. Today,
there is a considerable interest in it because it is safe, nontoxic, low costly and ecofriendly. Biofilm bacteria
existing in marketed local milk is at highly risk on population health and may be life-threatening as most
biofilm-forming bacteria are multidrug resistance. The goal of current study is to eradicate biofilm-forming
bacteria by alternative treatment green synthesis silver nanoparticles. The biofilm formation by bacterial
isolates was detected by Congo red method. The silver nanoparticles were prepared from date palm
(khestawy) fruit extract. The formed nanoparticles were characterized with UV-Vis

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Publication Date
Wed Jul 05 2017
Journal Name
Https://www.researchgate.net/journal/international-journal-of-science-and-research-ijsr-2319-7064
Evaluation of Water Quality using Bhargava Water Quality Index Method and GIS, Case Study: Euphrates River in Al-Najaf City
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Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
EVALUTION OF OCCUPATIONAL HEALTH AND SAFETY SYSTEM ACCORDING TO ISO 45001 : 2018 Applied Research IN BAGHDAD COMPANY FOR SOFT DRINKS
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Represent a topic occupational safety and health management is one of the priorities of the loading organization in the business environment ,and one of the requirement for the success and its impact on the productivity of workers and their performance in an appropriate working environment .The international responses to the problems that accompany the technological and industrial development of the business environment are the issuance of ISO 45001:2018 aimed at providing an appropriate framework for controlling risks , reducing injuries and work accidents and improving work performance ,after realizing the environmental relationship between safe and sound work with competition .The search’s issue is represented with the exist

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Mon Aug 28 2023
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Estimation of urban land price within holly cities by using integrated GIS-regression models: case study Al-Kufa city- Iraq
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        Urban land price is the primary indicator of land development in urban areas. Land prices in holly cities have rapidly increased due to tourism and religious activities. Public agencies are usually facing challenges in managing land prices in religious areas. Therefore, they require developed models or tools to understand land prices within religious cities. Predicting land prices can efficiently retain future management and develop urban lands within religious cities. This study proposed a new methodology to predict urban land prices within holy cities. The methodology is based on two models, Linear Regression (LR) and Support Vector Regression (SVR), and nine variables (land price, land area,

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Publication Date
Sun Feb 10 2019
Journal Name
Iraqi National Journal Of Nursing Specialties
Effectiveness of Structured Educational Program on Nurses’ Practices Concerning Therapeutic Communication at Cardiac Care Units in Holy Karbala Governorate Hospitals
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Abstract
Objectives: This study aimed to evaluate the effectiveness of an educational program on nurses' practices concerning therapeutic communication.
Methodology: A quasi experimental design was carried out at Karbala Center for Cardiac Diseases and Surgery, Imam Hussein Medical City and Al-Handia General Hospital for period 10th June 2017 to the 15th of August 2018.
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Publication Date
Wed Dec 01 2021
Journal Name
Iraqi Journal Of Physics
Evaluate the Distribution of Heavy Elements that Dissolved in Ground Water Using IDW in AL-Wafa City, Al-Ramadi,Iraq
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Wed Sep 01 2021
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Biochemical and Histological Study of Aminoacylase-1 Purified from Amniotic Fluid in Rats with Oxidative Stress Induced by Lead Acetate
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This work involves separating and studying the aminoacylase-1 (ACY1) of amniotic fluid from healthy pregnant, mainly one peak with higher activity has been isolated by DEAE-Cellulose ion exchange from the proteinous supernatant produced by deposition of proteins using ammonium sulfate  (65%) after dialysis. The purification folds reaching to 19 folds also gave one protein peak when injected into the gel filtration column, a high ACY1 purity was obtained, with 38 folds of purification. It was found that the molecular weight of the isolated ACY1 was up to 46698 Dalton when using gel chromatography technique.The effect of ACY1 isolate was studied on rats with oxidative stress caused by lead acetate(LA) at 40 mg / kg body weight and compare

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