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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
Wed Apr 01 2015
Journal Name
Al–bahith Al–a'alami
The Educational Role of Children's Programs in Libyan TV An Analytical -Field Study of "Flowers of Life" Program
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Television contributes children the acquisition of knowledge, moral and social values through programs that are offered to them and the extent of the focus on the effective aspects of life in the age of the target stage. The subject of this research aims to know the children programs in Libya television through a comprehensive analytical study of the program entitled “zihur al-hayat” within the broadcast season from April 1, 2004 to June 30, 2004. It also focuses on trying to identify the Libyan television policy in broadcast educational content through the children's programs in the prevailing political and social conditions during the period of study as well as knowing the opinions of the children's sample under study in Al-Baidhaa

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Publication Date
Fri Jan 01 2021
Journal Name
Basra Journal Of Science
Effects of Thicknesses of Two Different Gate Insulators on the Performance of Pentacene Based Organic Field Effect Transistor
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In this paper, a simulation of the electrical performance for Pentacene-based top-contact bottom-gate (TCBG) Organic Field-Effect Transistors (OFET) model with Polymethyl methacrylate (PMMA) and silicon nitride (Si3N4) as gate dielectrics was studied. The effects of gate dielectrics thickness on the device performance were investigated. The thickness of the two gate dielectric materials was in the range of 100-200nm to maintain a large current density and stable performance. MATLAB simulation demonstrated for model simulation results in terms of output and transfer characteristics for drain current and the transconductance. The layer thickness of 200nm may result in gate leakage current points to the requirement of optimizing the t

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Publication Date
Tue Aug 15 2023
Journal Name
Al-academy
The influences of fashion on the design of fabrics and fashion at the time of contemporary social transformations
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The design of fabrics and fashion is manifested by aesthetic advantages betting with the movement of society in its quest to develop as an independent art in itself that is linked to the values and aesthetic concepts of other arts and what appears in them of intellectual systems calling for renewal and modernity. Which brought about a wide change in public taste, as well as a desire for innovation . Which made fashion an interesting aesthetic phenomenon and taste is always subject to change constantly to comply with the social variables that occur in human life, as the fashion that appears in a certain era of time and takes a great distance from spreading as something new and out of the ordinary is in fact the fruit of the development of

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Publication Date
Wed Oct 17 2018
Journal Name
Journal Of Economics And Administrative Sciences
Redesign of Jobs in the Division of Blood Transfusion Services of the Baghdad Health Directorate Rusafa Case Study
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     The purpose of the theme of redesign of jobs one of the topics the task that offers the possibility for individuals to perform several tasks in the organization of health at the same time gain experience and diverse skills and achieve compatibility between the requirements of the most appropriate function and organization  of the hand ,hence, the idea of studying the redesign of jobs of the division of blood transfusion services in the department of health Baghdad Rusafa to change the conventional methods used in the performance of functions ,which are no longer able to meet the needs of patients where blood transfusion is a key  ingredient in health care and equal access to safe blood is needed

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Publication Date
Mon Feb 14 2022
Journal Name
Journal Of Educational And Psychological Researches
Animation Films and Their Impact on the Behavior of Kindergarten Child from the Point of View of Mothers
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The child spends several hours watching animated films, which affect their behavior negatively and positively. This calls parents to monitor what their children are watching, to show them the serious risks of some violent films, and to direct them toward choosing both positive and educational programs that develop their positive behavior. This study aimed to explore the positive and negative effects of watching animation films as well as to identify the role animation films in increasing the cognitive knowledge of kindergarteners. To do this, the descriptive and analytical methods were used. A questionnaire was adopted as a tool for data collection. A scale of (45) items classified into three categories was applied on  the r

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Publication Date
Thu Oct 01 2020
Journal Name
Biochemical & Cellular Archives
RAPID SPECTROPHOTOMETRIC ESTIMATION OF TRACE AMOUNTS OF MEFENAMIC ACID BASED DISPERSIVE LIQUID-LIQUID MICROEXTRACTION OF IN PHARMACEUTICAL PREPARATIONS.
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A dispersive liquid-liquid microextraction combines with UV-V is spectrophotometry for the preconcentration and determination of Mefenamic acid in pharmaceutical preparation was developed and introduced. The proposed method is based on the formation of charge transfer complexation between mefenamic acid and chloranil as an n-electron donor and a p-acceptor, respectively to form a violet chromogen complex measured at 542 nm. The important parameters affecting the efficiency of DLLME were evaluated and optimized. Under the optimum conditions, the calibration graphs of standard and drug, were ranged 0.03-10 µg mL-1. The limits of detection, quantification and Sandell's sensitivity were calculated. Good recoveries of MAF Std. and drug at 0.05,

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Publication Date
Wed Dec 27 2017
Journal Name
Al-khwarizmi Engineering Journal
The Determination of Critical-Sampling Scheme of Preprocessing for Multiwavelets Decomposition as 1st and 2nd Orders of Approximations.
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One of the important differences between multiwavelets and scalar wavelets is that each channel in the filter bank has a vector-valued input and a vector-valued output. A scalar-valued input signal must somehow be converted into a suitable vector-valued signal. This conversion is called preprocessing. Preprocessing is a mapping process which is done by a prefilter. A postfilter just does the opposite.

The most obvious way to get two input rows from a given signal is to repeat the signal. Two rows go into the multifilter bank. This procedure is called “Repeated Row” which introduces oversampling of the data by a factor of 2.

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Effect of Some Herbs on the Level of Some Biochemical Parameters in Blood of Diabetic Patients Type II
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This study included effect of polyherbs mixture treatment of diabetic patients type II for two months. The polyherbs mixture contains Nigella sativa seeds, Boswellia carterri gum, Citrus aurantifolia fruits, Elettaria cardamomum fruits. Also this study included estimation of some biochemical parameters in the serum Diabetes Mellitus (D.M.) patients-type II and knowing the relationship of these parameters with this disease. The parameters are glucose, cholesterol ,High density , Low density lipoproteins( HDL-C, LDL-C) respectively , Triglycerides TG, urea, total protein , albumin , Alkaline phosphatase ALP,Transaminase GOT, GPT enzymes . Take (77) samples of diabetic patients serum type II which included (47) samples for group one: herbs

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Publication Date
Thu Dec 26 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Impact of Social Responsibility on the Financial Performance of Banks: )Applied Research at the Bank of Baghdad)
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The objective of the research is to measure the impact of social responsibility on the financial performance of the Bank of Baghdad for the period from 2014 to 2016 (3 years) through discussing and analyzing the level of practice of the Bank of Baghdad for social responsibility and the impact on their financial performance during the period. To measure the independent variable (CSR), the researcher used the CSR Disclosure Index and relied on the ROA as an indicator to measure the dependent variable (financial performance).The results of the research showed the main hypothesis of the research, which states that the social responsibility of the banks has no significant impact on the financial performance. In relation to the disclosure of s

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Publication Date
Thu Nov 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
((The extent of the obligation of the Federal Board of supreme Audit to apply the INTOSAI 3000 standard))
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Abstract

The research aims to demonstrate the commitment of the Federal Financial Supervisory Bureau to meet the requirements of the International Organization of Supreme Audit Institutions (INTOSAI) 3000, the general and private supervision of performance as the highest supervisory authority in Iraq, which is the only authorized to carry out the process of monitoring the performance of government work and activities. To analyze and present the results of the survey questionnaire prepared for the compliance of the Bureau with the requirements of the general and specific criteria related to the performance control process. The researcher reached a number of conclusions, the most important of which is the commitment of the

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