Preferred Language
Articles
/
bijps-706
Investigation of Solubility Enhancement Approaches of Ticagrelor
...Show More Authors

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).  

 

Scopus Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Thu Nov 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Effect of the professional skepticism characteristics of the auditor on audit qualit
...Show More Authors

The professional skepticism is one of the fundamental concepts necessary for practicing the audit profession, without which the auditor can not reach a reasonable assurance as to the correctness of the evidence and the information obtained by the auditing department. The auditor's possession of the characteristics of professional skepticism and his practice of professional skepticism during the audit process lead to an increase The quality of audit and thus raise the confidence of the financial community in the audit profession again after the exposure of several crises led to the loss of financial society confidence in the audit profession.

The aim of the study is to measure the impact of professional sk

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Sat Jul 01 2023
Journal Name
Industrial Laboratory. Materials Diagnostics
OPTIMIZATION OF PLASMA-ASSISTED DESORPTION/IONIZATIONMASS SPECTROMETRY FOR ANALYSIS OF IBUPROFEN
...Show More Authors

In medical practice, nonsteroidal anti-inflammatory drugs (NSAIDs) are often used to treat osteoarthritis and rheumatoid arthritis. Ibuprofen is a well-known NSAID, analgesic, and antipyretic medication. This chemical is an active ingredient of several oral medications that are offered in tablet, gel pellet, and syrup forms and has higher efficacy, tolerance, and side effect rates than other compounds, including pyrazolone derivatives. We present a unique plasma-assisted desorption/ionization mass spectrometry (PADI-MS) approach for improving pharmaceutically important solids using an ibuprofen tablet as a model solid sample. The goal of the study is to create an innovative mass spectrometric method that could be used for quick and accur

... Show More
Preview PDF
Publication Date
Sat Jun 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Effect of industry specialization of the Iraqi audit firms on audit quality
...Show More Authors

The research aim to measure the impact of the Industry specialization of the auditors on the quality in audit in Iraqi auditing firms, as well as measuring the factors of Industry specialization in the Iraqi audit companies by measuring the market shares of Iraqi audit firms that audit the companies listed on the Iraqi Stock Exchange For 2010 to 2016, by surveying the opinions of (35) Audit firm on the impact of the Industry specialization of auditing firms in audit quality factors, The effect of the variables was revealed through the use of the survey form Distributed to Iraqi audit companies, The industry speci

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
"The role of quality costs in reducing the cost of industrial" products
...Show More Authors

Abstract :-

The aim of the research is to explain the role of quality costs their  importance and their classification, and to clarify the most important tools that help to reduce costs.

In order to achieve the objective of the research and test hypotheses adopted the descriptive approach, as well as the adoption of the analytical approach in the study of applied data has been relied upon in providing data on the financial and production reports of the research sample company, the data were used to study and analyze financial and productivity reports . A number of conclusions have been reached the most important being the following

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Mar 01 2019
Journal Name
Al-khwarizmi Engineering Journal
Large Angle Bending Behavior of Curved Members Using The Method of Characteristics
...Show More Authors

This paper deals with the nonlinear large-angle bending dynamic analysis of curved beams which investigated by modeling wave’s transmission along curved members. The approach depends on the wave propagation in one-dimensional structural element using the method of characteristics. The method of characteristics (MOC) is found to be a suitable method for idealizing the wave propagation inside structural systems. Timoshenko’s beam theory, which includes transverse shear deformation and rotary inertia effects, is adopted in the analysis. Only geometrical non-linearity is considered in this study and the material is assumed to be linearly elastic. Different boundary conditions and loading cases are examined.

From the results obtai

... Show More
View Publication
Publication Date
Sat Oct 01 2022
Journal Name
Al–bahith Al–a'alami
IRAQ BETWEEN A CULTURE OF CIVIL SOCIETY AND A CULTURE OF VIOLENCE
...Show More Authors

The title takes its realistic connotations with its symbols, slogans and historical extensions in Iraq, also, the repercussions of the organic crisis that afflicted it for almost half a century, especially after the abortion of the July 14 Revolution and the spread of the culture of weapons, violence and death that we are living in Iraq nowadays.

The topic is suitable for critical analytical studies carried out by specialists in scientific and academic research centers and cultural institutions because they have an important feasibility at the strategic cultural level in Iraq, the Middle East and the world.

Research in Iraq has fallen to the extreme and is no longer effective, to the extent that it represents a severe cri

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Jul 21 2023
Journal Name
Journal Of Engineering
The Effect Of Curing Types On Compressive Strength Of High Performance Concrete
...Show More Authors

The present investigation considers the effect of curing temperatures (30, 40, and 50˚C) and curing compound method on compressive strength development of high performance concrete, and compares the results with concrete cured at standard conditions and curing temperature (21˚C). The experimental results showed that at early ages, the rate of strength development at high curing temperature is greater than at lower curing temperature, the maximum increasing percentage in compressive strength is 10.83% at 50C˚ compared with 21C˚ in 7days curing age. However, at later ages, the strength achieved at higher curing temperature has been less, and the maximum percentage of reduction has been 5.70% at curing temperature 50C˚ compared with 21

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Wed Nov 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
" The Effect of the Auditor's Experience on the Quality of Internal Audit "
...Show More Authors

The importance of internal audit in the growing demand for services in the public and private economic units, and in the rapid growth of its systems professional, has also been recognition of the importance of internal audit quality and the quality of information provided in a long time, as well as the importance of achieving the greatest possible quality in his work to reduce accounting risks of financial reports misleading or fraudulent, which is one of the important features of the audit.

The internal audit quality are linked with the ability of auditors to detect errors in the financial statements, and their willingness to express an opinion technical neutral and non-aligned based on the results of th

... Show More
View Publication Preview PDF
Crossref (2)
Crossref
Publication Date
Wed Jul 01 2015
Journal Name
Journal Of Engineering
Studying of Some Mechanical Properties of Reactive Powder Concrete Using Local Materials
...Show More Authors

This research aims to investigate and evaluate a reactive powder concrete (RPC) cast using economical materials. Its mechanical properties were investigated and evaluated by studying the effects of using different cement and silica fume contents and locally steel fibers aspect ratios as reinforcement for this concrete. A compressive strength of about 155.2MPa, indirect tensile strength of 16.0MPa, modulus of elasticity of 48.7GPa, flexural strength of 43.5MPa, impact energy of 3294.4kN.m and abrasion loss 0.59%  have been achieved for reinforced RPC contains  910 kg/m3 cement content, silica fume content 185 kg/m3 of cement weight and fiber volume fraction 2%. The water absorption values w

... Show More
View Publication Preview PDF
Publication Date
Sun Apr 30 2017
Journal Name
Journal Of Engineering
Influence of Internal Sulfate Attack on Some Properties of Self Compacted Concrete
...Show More Authors

      Self-compacted concrete (SCC) is a highly flowable concrete, with no segregation which can be spread into place by filling the structures framework and permeate the reinforcement without any compaction or mechanical consolidation ACI 237R-14. One of the most important problems faced by concrete industry in Iraq and Gulf Arab land is deterioration due to internal sulfate attack (ISA) that causes damage of concrete and consequently reduces its compressive strength, increases expansion and may lead to its cracking and destruction. The experimental program was focused to study two ordinary Portland cements with different chemical composition with (5, 10 and 15) % percentage of high reactivity metakaoline (HRM)

... Show More
View Publication Preview PDF