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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 May 01 2018
Journal Name
Journal Of Physics: Conference Series
Application of Weyl Module In The Case Of Two Rows
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Publication Date
Wed Dec 15 2021
Journal Name
Journal Of Baghdad College Of Dentistry
Assessment of Coating Zirconium Implant Material with Nanoparticles of Faujasite
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Aim: To evaluate the wettability and microhardness of Zirconium (ZrO2) dental material when coated with different concentrations of Faujasite. Materials and methods: 30 circular disks produced from ZrO2, then each group is classified into 10 control groups, 10 coated groups with 3% Faujasite, and 10 coated groups with 7% faujasite by electro-spun tool to study variable properties in hardness and water contact angle of implant materials. Results: This study stated the high hardness in 7% of faujasite concentration for ZrO2, in addition, the contact angle decreased gradually until reach 0 ᵒ in 7% concentration of faujasite with ZrO2 Conclusion: Water contact angle (WCA) declined till disappeared in (7% wt.) of faujasite coated with the Z

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Publication Date
Wed Dec 30 2020
Journal Name
Al-kindy College Medical Journal
Various types of Alopecia and the options of the treatment
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Alopecia (Baldness) is very usual trouble in current time. It is accompanied by an intensive weakening of the scalp's hair and follows a specific pattern. Hereditary predisposition plays a very important role in alopecia despite not completely understood. Alopecia can be typed to various categories according to etiology, may be due to hereditary factors, autoimmune disease, and drugs or chemicals. There are many options of strategies of treatment according to the type and causes of alopecia. Chemical or synthetic medications apply for the management of hair loss are accompanied by a wide range of undesirable effects. Naturally occurring drugs also play important role in alopecia management with minimal side effects.

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Publication Date
Thu Jul 01 2004
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
MICROFACIE STUDY OF SUBSURFACE SECTION OF BEKHME FORMATION (NORTH IRAQ)
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Bekhme formation, Dernir Dagh well -1 has been divided into two facies units using core
sample slides and depending on sedimentary structures and diagenetic processes .The facies
reflect the environment of the foreslope.This work proves the absence of Bekhme formation
in Dernir Dagh
Well- 1 as a tongue as reported by the Oil Exploration Company. Some species and genera of
bentonic foraminifera were identified. The age of Bekhme formation was estimated
depending on the recognized index fossils to be lower Maastrichtian.

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Publication Date
Sat Jan 01 2022
Journal Name
Aip Conference Proceedings
Study of ground properties of oxygen isotopes using Cosh potential
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Publication Date
Fri Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
Role of ERP In Enhancing the Accuracy of Financial Reporting
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Abstract

Nowadays, the adoption of economic unity on the accuracy of financial reporting is very important. Economic units need accurate financial reporting to be more competitive and to improve the performance. Management can also achieve financial information in real time through the application of ERP systems. This system will facilitate management to access the most up-to-date information such as planning, monitoring and evaluating the business processes of the organization to be more effective.

On the practical side, the Enterprise Resource Planning (ERP) system was applied to the General Company for Vegetable Oils to demonstrate a course in enhancing the accuracy of financial reporting.

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effects of Abuse of Anabolic Androgenic Steroids on Iraqi Athletes
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Anabolic androgenic steroids (AAS) are man-made derivatives of the male sex hormone testosterone, originally designed for therapeutic uses to provide higher anabolic potency with lower androgenic effects. Increasing numbers of young athletes are using these agents illicitly to enhance physical fitness, appearance, and performance despite their numerous side effects and worldwide banning.  Today, their use remains one of the main health problems in sports because of their availability and low price.  The present study focuses on investigating the adverse effects of anabolic androgenic steroid abuse on sex hormones, liver and renal function tests, fasting glucose levels and lipid metabolism in Iraqi male recreational bodybuilders

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Publication Date
Tue Dec 01 2020
Journal Name
Journal Of Economics And Administrative Sciences
The impact of governance on the reputation of the organization
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The current study aims to determine the extent of SOMO's interest in governance and whether this interest is sufficient to be reflected in enhancing its organizational reputation, and the field of research was in the oil marketing company SOMO. (109), (105) questionnaires were distributed, (94) forms and (11) forms were not retrieved, and the valid questionnaires had reached (91). The analytical and descriptive approach was used for the study, and the current research has found a positive impact of government on the reputation of the organization, and this research demonstrated the existence of the proposed relationship and the impact between governance and the reputation of the organization.

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Publication Date
Thu Dec 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
The role of quality of working life in regulatory alienation
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Abstract

The goal of this research is to know the quality of working life and its impact on the level of the organizational sense of alienation among a sample of teaching Anbar University in the center of Baghdad. Find and seek to achieve a number of cognitive and practical goals.

Where the quality of work life constitutes one of the main sources to enable organizations of excellence in light of the volatile environment, as is one of alienation regulatory organizations avoid the phenomena that occur because of their negative effects on performance and thus achieve their goals. The most research problem in question the existence of the main deficiencies in the application of the concepts of organiz

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Publication Date
Thu Dec 01 2011
Journal Name
Journal Of Engineering
The Effect of Shear on the Properties of Rigid PVC
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The rheological and fusion behavior of polyvinyl chloride (PVC) compounds plays a dominant role in
the processing operations and in the development of physical properties in the processed material. A
comprehensive study was made in this work to evaluate the effect of shear and thermal history on stability, mechanical and rheological properties of rigid PVC compounds. Different samples of Rigid Poly vinyl chloride including dry blend powder, granules, and bottles molded from both were examined. A study was also made on recycled RPVC where 25% of reclaimed material was continuously blended with fresh dry blend and processed for 15 cycles. Results showed that compaction of the PVC material took place in the brabender plastograph at co

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