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 Sep 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
The influence of the personal values of the workers in the performance of the work teams
...Show More Authors

The research aims to know the impact of workers values on their performance which is reflected on increasing productivity and improving its quality as well as the organization's progress and success.  Application of this research took place in the General Company Of Electrical Industries; it contained four main pillars; the first involved research methodology، regarding the problem، importance، aim، basic theory، and method of data collection، the second is dedicated to the theoretical framework related to the research basic variables (values and workgroups) the third is assigned to analyze the actual data by using number of statistical methods، such as mathematical medium and standard deviation and also spearman rank

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Dec 30 2020
Journal Name
Biodiversitas Journal Of Biological Diversity
Assessment of some heavy metals in various aquatic plants of Al-Hawizeh Marsh, southern of Iraq
...Show More Authors

Abstract. Al-Abbawy DAH, Al-Thahaibawi BMH, Al-Mayaly IKA, Younis KH. 2021. Assessment of some heavy metals in various aquatic plants of Al-Hawizeh Marsh, southern of Iraq. Biodiversitas 22: 338-345. In order to describe the degree of contamination of aquatic environments in Iraq, heavy metals analysis (Fe, Ni, Cr, Cd, Pb, and Zn) was conducted for six aquatic macrophytes from different locations of Al-Hawizeh Marsh in southern Iraq. The six species were Azolla filiculoides (floating plant), Ceratophyllum demersum, Potamogeton pectinatus, Najas marina (submerged plants), Phragmites australis, and Typha domingensis (emergent plants). The results indicate that cadmium, chromium, and iron concentrations in aquatic plants were above the

... Show More
View Publication
Scopus (14)
Crossref (1)
Scopus Crossref
Publication Date
Sun Sep 02 2012
Journal Name
Baghdad Science Journal
Effect of Replacing Partial of Wheat Flour by Lentil Powder on Quality Properties of Laboratory Bread
...Show More Authors

This investigation was carried out to examine the effect of replacing partial of flour by dried Lentils (Lens culinaris) to white flour in different percentages on the chemical, sensory and storage properties of the Laboratory bread. The results revealed that replacing 0% than wheat flour by lentil powder (1) control was high significan than the replacing 25 and 35% than wheat flour by lentil powder ( 4 and 5) in flavor and chewiness . The results of sensory evaluation showed that replacing 4 were high significan different than that of replacing 1 in external layer colour. Other replacing percentages, however, did not show significant differences of in comparison with control . In regards with chemical analysis of Iron and copper, i

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Sep 30 2015
Journal Name
College Of Islamic Sciences
The impact of the organization of markets, old and new in the holy city of Karbala
...Show More Authors

Any city that has such a market and is organized, organized and established

Mini
And respect
Freedom of expression
Profile.
Conflict resolution and conflict resolution

Political
Which affected the growth of some markets
And religious th
The search for the return of economic and cultural activity and the emigration of some others
Cultural exchange and trade, which in turn
Al-Rifaie
We took the problem that we are experiencing
Menia, the holy city of Karbala in the market organization, has suffered from fierce attacks
Economic and heritage
e
As well as tourism and tourism, as it depends on the abundance of visitors, tourists and residents in terms of needs and motivation
Resource

... Show More
View Publication Preview PDF
Publication Date
Thu Jan 02 2020
Journal Name
Journal Of The College Of Languages (jcl)
A Psychological Reading of The Problem of the Black in John Steinbeck’s Of (Mice and Men)
...Show More Authors

The present paper applies Fanon Psychological reading of the problem of the Black introduced in his book Black Skin White Mask to Crooks, The black Character in John Steinbeck’s  Of Mice and Men. The analysis of this character infers three essential points regarding the artistic achievement of the author. First, he uses a fictional character that offers a psychological interpretation of the black problem of alienation and loneliness in a way that does not disgrace the black. Second, he applies Fanon’s way of showing the various attitudes that the black adopts in contact with the white society. Third, he affirms that the black inferiority complex comes as a result of double proc

... Show More
View Publication Preview PDF
Publication Date
Sat Mar 25 2023
Journal Name
International Journal Of Drug Delivery Technology
Improvement of Entrapment and Ocular Permeability of Ganciclovir Nanostructured Lipid Carriers Using Various Conditions of Preparations
...Show More Authors

Ganciclovir (GCV) is a drug included in BCS-Class III, having high solubility and low permeability. It is a synthetic acyclic nucleoside analog of 2′-deoxyguanosine, considered a potent inhibitor of herpes viruses and cytomegalovirus (CMV) infection. Herpes simplex virus (HSV) infections are very common and are also considered a major cause of corneal blindness. This study intended to advance a pioneering nanostructured lipid carriers (NLCs) system for improving the ocular permeability of GCV. Several procedures were used for the preparation. Cold homogenization, solvent injection, and emulsifi cationultrasonication methods. A mixture of palmitic acid (PA) and oleic acid (OA) as a lipid matrix, cremophore EL, and transcutol HP wer

... Show More
View Publication
Scopus (3)
Scopus Crossref
Publication Date
Sat Jun 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
A field study of the problems of queues at some checkpoints in the city of Baghdad
...Show More Authors

 

Abstract

Due to the momentum of winning in the streets of the city of Baghdad as a result of the large number of checkpoints so felt researcher to conduct a field visit to find out the main reasons that led to this congestion and to find practical solutions to mitigate wastage winning the arrival time citizen to where you want the least possible time.

This research aims to overcome the difficulties experienced by citizens to reach their places of work and reduce waste at the time of service and waiting time as well as reduce the cost of waiting.

Has emerged study a set of conclusions, including the use of model queue (G / G / C) and the mome

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Jun 07 2018
Journal Name
Applied Physics A
Effect of incorporation of conductive fillers on mechanical properties and thermal conductivity of epoxy resin composite
...Show More Authors

View Publication
Crossref (56)
Crossref
Publication Date
Fri Jun 01 2018
Journal Name
Journal Of Cranio-maxillofacial Surgery
Assessment of regional asymmetry of the face before and after surgical correction of unilateral cleft lip
...Show More Authors

View Publication
Scopus (22)
Crossref (22)
Scopus Clarivate Crossref
Publication Date
Mon Dec 31 2012
Journal Name
Al-khwarizmi Engineering Journal
Analysis of the Effects of Aggressive Shot Peening on Fatigue Life of 7075 – T6 Aluminum Alloy
...Show More Authors

 For many years controlled shot peening was considered as a surface treatment. It is now clear that the performance of control shot peening in terms of fatigue depends on the balance between its beneficial (compressive residual stress and work hardening) and beneficial effects (surface hardening).

The overall aim of this paper is to study the effects of aggressive shot peening on fatigue life of 7075 – T6 aluminum alloy. The fatigue life reduction factor (LRF) due to the aggressive shot peening was established and empirical relations were proposed to describe the behavior of LRF, roughness and fatigue life. The benefits of shot peering in terms of fatigue life are dependent on the shot peening time (SPT).

... Show More
View Publication Preview PDF