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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
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Dispersal and Development of Powdery Mildew Disease Caused by Oidiopsis haplophylli on Ornamental Plants (Nasturtium) Tropaeolum majus L. in Baghdad
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This study wass carried out to investigate the incedence of powdery mildew disease on ornamental plants (Nasturtium) Tropaeolum majus L. caused by Oidiopsis haplophylli in some nurseries of Baghdad area and in fields at college of Agriculture /University of Baghdad. This study was conducted in tow succesive seasons of 2011-2012 (April and May). The survey indicated that the Mildew disease existe in the following nurseries (Al-Adhamiya 97.5% ,Palestine street 93.8%, Zayouna 86.0%, and 100% in two fields at college of Agriculture. It has been found that the disease severity was developed in Agriculture college fields successively from 12-4-2011 to 20-5-2011 and from 12-4-2012 to 20-5-2012 (18.0–98.0 % and 22.7–96.0% )for the two sea

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Publication Date
Tue Mar 03 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Root resorption and anti-dentine antibody level in serum and saliva of well-controlled type ? diabetic patients undergoing orthodontic treatment
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Background: Diabetic mellitus type ? is a metabolic disorder of diverse etiological factors, characterized by hyperglycemia resulting from an absolute deficiency of insulin affected childhood and adolescent. Some of these patients seek an orthodontic care .The orthodontist who is treating these medically compromised patients should have a working knowledge of the multitude of medically complex problems. This information will support and enable for delivery of high standards of dental care in general and orthodontic care in particular. The aim of this study was to analyze serum IgG levels and salivary secretory IgA (sIgA) levels in human dentine extract (HDE) before (T0) and 6 months after (T6) orthodontic treatment and to correlate anti-HDE

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Publication Date
Sun Jan 22 2023
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The impact of international Accounting Standard No (21) in reducing tax obstacles : applied research in the General Authority for Taxes .
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               The research aimed to shed light on the impact of international Accounting Standard No (21) on tax obstacles represented by (tax evasion, double taxation) The financial statements of a group of banks operating in the private sector were relied upon to know the impact of the standard on tax obstacles, as well as knowing the amount of amounts, The researcher relied on the method of financial analysis of that data, which was obtained from the website of the Securities Commission, and conducted personal interviews with a number of university professors, chartered accountants, financial experts, banks, and the General Authority for Taxes to benefit from their

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Publication Date
Tue Mar 03 2026
Journal Name
Journal Of Physical Education
A Comparative Study of Mental Alertness Between Inactive and Active Individuals In Baghdad University Students Aged 18 – 22 Years Old
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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Study the Spectral Properties of Coumarine -47 Dissolved in Chloroform: Rafah Abdul Hadi Omer|Mohammed T. Hussian|Lamia Kand Kalif
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The spectral propetties (absorption and fluorescence) of Coumarine-47 laser dye have been studied. This type of laser dye belong the Coumarine family and it has dissolved in chloroform at different concentrations (1x10-5, 5x10-5, and 1x10-4 M) at room temperature. The achieved results have been pointed out to increase in the absorption and fluorescence as the concentration increased which are agreements with Beer – Lambert law. These have been also showed an expansion in the spectral range of absorption and fluorescence with a noticed shift in the direction of longer wavelength (Red-shift) with increasing concentration. The quantum efficiency of the dissolved C47 in chloroform has been computed by using the brevious concentrations

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Publication Date
Wed Aug 10 2016
Journal Name
Fourth International Conference On Genetics And Scientific Environment. Cairo / Arab Republic Of Egypt For The Period From July 23 To 30
Efficacy of Arbuscular mycorrhiza (AM) in inducing non-enzymatic antioxidants in tomato leaves infected with Fusarium oxysporum f. sp. Lycopersici.
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Publication Date
Thu Jul 01 2021
Journal Name
University Of Northampton Pue
Validating a Proposed Data Mining Approach (SLDM) for Motion Wearable Sensors to Detect the Early Signs of Lameness in Sheep
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Publication Date
Tue Jan 01 2013
Journal Name
The Iraqi Journal Of Veterinary Medicine
Detection of methicillin or multidrug resistant Staphylococcus aureus (MRSA) in locally produced raw milk and soft cheese in Baghdad markets.
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In order to investigate the presence of methicillin or multidrug resistant Staphylococcus aureus in food-chain especially Cows raw milk and white raw soft cheese and its whey, a total of 30 samples were collected randomly from different markets in Baghdad Province during December 2012 till February 2013, in which samples were analyzed by a standard isolation protocols of food microbiology with some modification processing by new, modern and rapid technology tools such as chromogenic medium Baird-Parker agar, Electronic RapIDTM Staph Plus Code Compendium Panel System (ERIC®) Dryspot Staphytect Plus and Penicillin Binding Protein (PBP2') Plus assays; as well as, studying the susceptibility of isolates to different selected antibiotics. The r

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Publication Date
Sun Jun 01 2014
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Internal control and its role in the reform of the tax work: Applied research in the General Commission for Taxes
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That internal control is particularly important in improvingperformance and tax reform، they play an important role in the regularity ofwork and development and the anti corruption and activating the decisionsand tax legislation، as contained in the organizational plan and the means،procedures and components designed from which to ensure a policy andimplementation plans The research aims to review the reality of the internalcontrol in the General Commission for Taxes and stand on the deficiencies init, with the strengthening of the role of internal control in the GeneralAuthority for taxes based on the laws and regulations and by using modernmeans to work as well as developing the performance of employees in thebody، including helpin

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Publication Date
Sun Dec 01 2013
Journal Name
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Bacterial Causes Tonsillitis in Children, Study the Resistance to Antimicrobials and the Effect of Clove Extracts on Selected Isolated Bacteria.
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In this study Isolated Pathogenic bacteria which causes Tonsillitis in Children with ages between 3-17 years. They are admitted to Central Children Hospital (Al-Karch) and Ebn-Albalady Hospital (Al-Rusafa). 200 cases were collected which include 120 Male and 80 Female. The result of the recent study shows that the isolation percentage was 40% from Male and 35% from Female. In this study Fifty six isolated were Identified, 20 were ?-hemolytic Streptococcus which was Streptococcus pyogenes, formed (36%) from all isolated.6 Pathogenic bacteria were ?- hemolytic Streptococcus which was Streptococcus pneumoniae formed (11%). The number of Moraxella catarrhalis bacteria was 12 formed (21%), the number of Haemophilus influenzae was 1

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