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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
Mon Dec 24 2018
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
FAUNISTIC REVIEW OF THE GENUS CHAITOPHORUS KOCH, 1854 (APHIDIDAE, CHAITOPHORINAE, CHAITOPHORINI) WITH NEW RECORD SPECIES FOR IRAQ APHID FAUNA
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    A faunistic review of the genus Chaitophorus Koch, 1854, including four species in Iraq is given; the distribution data of each species and their hosts have been recorded. In this investigation the poplar leaf aphid Ch. populialbae (Boyer de Fonscolombe, 1841) is recorded here for the first time in Iraq on popular trees Populus euphratica Oliv. during the period from November 2016 to April 2017 in Baghdad province.

 

    A brief description for apterous viviparous female of this species is given; and a  key to the species of the genus Chaitophorus is constricted.

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Publication Date
Mon May 31 2021
Journal Name
Journal Of Research In Medical And Dental Science
A Stereomicroscopic Evaluation of Four Endodontic Sealers Penetration into Artificial Lateral Canals Using Gutta-Percha Single Cone Obturation Technique
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A Stereomicroscopic Evaluation of Four Endodontic Sealers Penetration into Artificial Lateral Canals Using Gutta-Percha Single Cone Obturation Technique, Omar Jihad Banawi*, Raghad

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Publication Date
Thu Jan 30 2025
Journal Name
Retos
The effects of the integrative strategy on fostering reflective thinking and imparting basic basketball offensive techniques to female students
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Objective: The objective of this study is to develop instructional materials that teach fundamental basketball skills to female students enrolled in the first year of the College of Physical Education and Sports Sciences for Girls at the University of Baghdad while also encouraging reflective thinking (RT). Research methodology: the researcher chose the experimental methodology with the two equal group's method. Finding the community and choosing the right sample for the study's kind and goals are essential to the accomplishment of any research project. A sample for the primary experiment was picked at random after the researcher confirmed the students' first-year basketball curriculum. This study community consisted of (40) fourth-

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Publication Date
Wed Sep 20 2023
Journal Name
Journal Of Applied And Natural Science
Detection of some virulence genes (esp, agg, gelE, CylA) in Enterococcus faecalis isolated from different clinical cases at Baghdad
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The virulent genes are the key players in the ability of the bacterium to cause disease. The products of such genes that facilitate the successful colonization and survival of the bacterium in or cause damage to the host are pathogenicity determinants. This study aimed to investigate the prevalence of virulence factors (esp, agg, gelE, CylA) in E. faecalis isolated from diverse human clinical collected in Iraqi patient , as well as to assess their ability to form biofilm and to determine their haemolytic and gelatinase activities. Thirty-two isolates of bacteria Enterococcus faecalis were obtained, including 15 isolates (46.87%) of the urine, 6 isolates (18.75%) for each of the stool and uterine secretions, and 5 isolates (15.62%) of the wo

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Publication Date
Wed Jul 01 2015
Journal Name
Drug Design, Development And Therapy
Effect of Clausena excavata Burm. f. (Rutaceae) leaf extract on wound healing and antioxidant activity in rats
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Publication Date
Wed Aug 30 2023
Journal Name
Al-kindy College Medical Journal
The Impact of Osteoporosis on Teeth Decay in relation to Salivary Vitamin D among Menopause in Baghdad city, Iraq
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Background: Osteoporosis is a systemic skeletal disorder that has an impact on general health, dental health and salivary composition. The mineralization of teeth happens simultaneously with that of the skeleton, but if mineral metabolism is disrupted, tooth failures will resemble those that affect bone tissue. Vitamin D plays a key role in bone and tooth mineralization.

Objective: to evaluate the impact of osteoporosis on teeth decay in relation to salivary vitamin D among menopause in Baghdad city.

Subjects and Methods: This study was cross sectional study. The study group consists of

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Publication Date
Wed Mar 30 2022
Journal Name
College Of Islamic Sciences
What the linguists commented on, "I do not know" in the dictionary of Lisan al-Arab, a semantic study
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Absitract

This research was interested in studying the phrase “I don’t know” in the Lisan al-Arab dictionary, and Lisan al-Arab was based on collecting its material from five dictionaries, including: Tahdhib al-Lugha, al-Muqamah, al-Sahih, and the footnotes of Ibn Berri, al-Nihaya and Gharib al-Hadith. The objection to this phrase, and the discussion of its various implications among linguists and the clarification of the closest and most famous content to it according to the data presented to the researcher in his research journey, and to reach this goal, the research division into a preface, five demands and a conclusion and followed the list of sources and references. To define the lexicon of Lisan al-Ar

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Publication Date
Thu Jul 11 2024
Journal Name
الموئتمخر الدولي للعلم والتعليم
SUFFIXAL METHOD FOR FORMING NEW VOCABULARY IN RUSSIAN AND ARARBIAN LANGUAGES AND ITS INFLUENCE ON ACHIEVEMENT OF TRANSLATION ADEQUACY
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Abstract. In this scientific work, we investigate the problem of the practical necessity of achieving the adequacy of translation activities with active translation from Russian into Arabic in various fields of translation. Based on the material of the latest suffix vocabulary, a serious attempt is made to clarify and specify the rules for the development of translator's intuition when translating from Russian into Arabic and vice versa. Based on the material collected by the latest suffix vocabulary, we try to make an attempt to reveal the role of suffix word creation in highlighting the general rules for achieving translation equivalence. The paper examines the process of creating words in multi-family languages, the difference between th

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Publication Date
Sat Jul 01 2017
Journal Name
Energy Procedia
Preparation and Physical Properties of Doped CdBa 2-x Sr x Ca 2 Cu 3 O 8+δ Compound
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Publication Date
Fri Dec 06 2019
Journal Name
Ssociation Of Arab Universities Journal Of Engineering Sciences
Application of Artificial Neural Network and GeographicalInformation System Models to Predict and Evaluate the Quality ofDiyala River Water, Iraq
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This research discusses application Artificial Neural Network (ANN) and Geographical InformationSystem (GIS) models on water quality of Diyala River using Water Quality Index (WQI). Fourteen water parameterswere used for estimating WQI: pH, Temperature, Dissolved Oxygen, Orthophosphate, Nitrate, Calcium, Magnesium,Total Hardness, Sodium, Sulphate, Chloride, Total Dissolved Solids, Electrical Conductivity and Total Alkalinity.These parameters were provided from the Water Resources Ministryfrom seven stations along the river for the period2011 to 2016. The results of WQI analysis revealed that Diyala River is good to poor at the north of Diyala provincewhile it is poor to very polluted at the south of Baghdad City. The selected parameters wer

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