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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 Feb 01 2024
Journal Name
Journal Of Orthodontic Science
Presurgical management trends and nasoalveolar molding usage for infants with cleft lip and palate in the capital of a developing country
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BACKGROUNDS Nasoalveolar molding (NAM) application is among presurgical management (PSM) techniques used for infants with cleft lip and palate (CLP). It helps to approximate the palatal cleft and to reshape the nasoalveolar complex prior to primary lip repair. This study aimed to explore types of PSM and the dental speciality provision for infants with CLP in Baghdad. The status of NAM usage and surgeons’ perceptions toward NAM usage were assessed. MATERIALS AND METHODS This is a cross-sectional paper-based questionnaire study that collected responses of surgeons perform primary lip and nose repair regarding PSM. The questionnaire was distributed amongst public and private hospitals in Baghdad. Twenty surgeons were enrolled (only those su

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Publication Date
Mon Jul 01 2024
Journal Name
Journal Of The Faculty Of Medicine Baghdad
The Burden of Chronic Obstructive Pulmonary Disease COPD in Stable Patients and its Association with Inflammatory Biomarkers and Body Mass Index
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Background: Chronic obstructive pulmonary disease (COPD) is a progressive airflow limitation that is preventable but not curable. It is associated with persistent symptoms that cause a considerable burden on individual productivity at work, and daily activities, and reduced quality of life, also burdening the healthcare system and society. Objectives: The study aims to measure the burden of COPD on patients in terms of daily activities and work productivity. It also seeks to investigate some inflammatory biomarkers' levels and their correlation with selected outcomes. Patients and Methods: A cross-sectional study on 120 stable COPD patients who were diagnosed and treated according to the GOLD guidelines at Kirkuk General Hospital's

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Publication Date
Tue Jan 08 2019
Journal Name
Iraqi Journal Of Physics
Calculation of the total mass stopping power for electrons in some human body tissues in the energy range 0.01-1000 MeV
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The mass collision energy loss (dE/dX), the mass radiative energy loss (Srad/) and the total mass stopping power of electrons in the energy range of 0.01 MeV up to 1000 MeV has been calculated for Lung, Urea and Skin. The results of the present work for the mass collision stopping power of electrons in Lung, Urea and Skin are in excellent agreement with the standard results given by ESTAR program, where the maximum percentage error between the present calculated values and that of ESTAR program in Lung tissue, Urea and Skin tissue is 0.27%, 0.3% and 0.8% respectively. The mass radiative energy loss of electrons in the same energy range is also calculated using a modified equation, and the results are found to be in very good agreem

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Publication Date
Thu Jun 27 2019
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
MICROFACIES ANALYSIS AND BASIN DEVELOPMENT OF THE CENOMANIAN - EARLY TURONIAN SEQUENCE IN THE RAFAI, NOOR AND HALFAYA OIL FIELDS, SOUTHEASTERN IRAQ
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    The stratigraphic sequence of Cenomanian-Early Turonian is composed of Ahmadi, Rumaila, and Mishrif formations in the Rifai, Noor and Halfaya Oil Fields within the Mesopotamian Zone of Iraq, which is bounded at top and bottom by unconformity surfaces. The microfacies analysis of the study wells assisted the recognition of five main environments (open marine, basinal, shallow open marine, Rudist biostrome, and lagoon); these microfacies were indicative of a normal lateral change facies from shallow water facies to deeper water and open marine sediments.

 

    Ahmadi Formation (Early Cenomanian) is characterized by open marine sediments during the transgressive conditions, and would be

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Ingots Defects under the influence of Solidification and Freezing Conditions. : Farouk Mahdi Mansour|Mustafa A. Rijab Al-Najar|Amera kanan Asfur
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The results of research to reach the conditions that prevents the emergence of primary or secondary voids and achieve worker benefit from molded by almost 100%, which was the situation that cast poured in a mold heated and insulated from all sides to achieve freezing directional full starting from the region remote from the casting and ending then. Has also been compared to the microscopic structure of the resulting castings of various molding conditions, as these conditions have achieved the best sound microscopic structures.

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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
The Role of the School Garden, and its Importance in the school Building - A field study in the social school service
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This research concerns the fact of the school garden and how can we tackle this issue. The research starts with a question forwarded to those who are interested in the ministry of education matters; the question is that how is the extent of interest in the school garden project? And how it is activated in the Iraqi Educational Institution program? In addition, the analysis reveals the importance of the school garden since we, as teachers and students, suffer from seeing the view of the trashes, the wastes of school furniture, the stinking water and the weeds and how it is accumulated in the back yard of the school. To add fuel to the fire, the increase in number of the students; year after year. This increase leads to adding more classes

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Publication Date
Wed Jan 01 2020
Journal Name
Iraqi National Journal Of Nursing Specialties
Effectiveness of Health Educational Program on Nurses’ Knowledge About Communication Skills with Children at Welfare Children Teaching Hospital in Baghdad City
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Background: Therapeutic communication is the basis of interactive relationships among nursing team and their children: that affords opportunities to establish rapport, understand the client’s experience, formulate individualized or client interventions and optimize health care resources.

Objectives: The main aim of the study is to determine the Effectiveness of Education Program on Nurses’ Knowledge about Communication Skills with Children.

Methodology: A quasi-experimental study was conducted in Children Welfare Teaching Hospitals from 7th, October 2018 to the 20th, May 2019. The program and instruments have been constructed by the researcher for the purpose of the study. A non- prob

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Publication Date
Wed Jan 01 2020
Journal Name
Periodicals Of Engineering And Natural Sciences (pen)
Estimating the reliability function of the asymmetrical hybrid parallel-series system: Applied study at the state company for vegetable oils industry
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The research studied and analyzed the hybrid parallel-series systems of asymmetrical components by applying different experiments of simulations used to estimate the reliability function of those systems through the use of the maximum likelihood method as well as the Bayes standard method via both symmetrical and asymmetrical loss functions following Rayleigh distribution and Informative Prior distribution. The simulation experiments included different sizes of samples and default parameters which were then compared with one another depending on Square Error averages. Following that was the application of Bayes standard method by the Entropy Loss function that proved successful throughout the experimental side in finding the reliability fun

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Publication Date
Sat Nov 01 2014
Journal Name
Journal Of Next Generation Information Technology
The effect of the smoothing filter on an image encrypted by the blowfish algorithm then hiding it in a BMP image
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order to increase the level of security, as this system encrypts the secret image before sending it through the internet to the recipient (by the Blowfish method). As The Blowfish method is known for its efficient security; nevertheless, the encrypting time is long. In this research we try to apply the smoothing filter on the secret image which decreases its size and consequently the encrypting and decrypting time are decreased. The secret image is hidden after encrypting it into another image called the cover image, by the use of one of these two methods" Two-LSB" or" Hiding most bits in blue pixels". Eventually we compare the results of the two methods to determine which one is better to be used according to the PSNR measurs

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Publication Date
Wed Sep 01 2021
Journal Name
Iraqi Journal Of Physics
Study the Effect of Graphene on the Contact Angle, Water Absorption and Thermal Stability ( TGA ,DSC) for Blend (Epoxy & Repcoat ZR)
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In this study, polymeric coating was developed by incorporating nano graphene in the polymer blend with applications to oil storage tanks. The oil storage tanks samples were brought from the oil Pipeline Company / Doura refinery in Baghdad. The coating polymer was formed with a blend (epoxy resin and repcoat ZR). The proportion of mixing the mixture was 3:1:1 epoxy resin 21.06 gm: repcoat ZR 10.53 gm: hardener 10.53 gm. The blend/graphene was prepared using in stui-polymerization method with different weight percentage 1, 3, 5, and 7 wt % added to blend. The resulting solution was put in a glass tube on a magnetic stirrer for one hour at a temperature of 40 °C. The result of contact angle and wate

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