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
Sat Oct 28 2023
Journal Name
Baghdad Science Journal
Phenol Content and Peroxidase Enzyme Activity in Soybean Infected with Xanthomonas axonopodis pv glycines with the Application of Bacillus subtilis JB12 and Bacillus velezensis ST32
...Show More Authors

Xanthomonas axonopodis pv glycines (Xag) is a pathogen that causes pustule disease in soybeans. Many
techniques for controlling this disease have been widely developed, one of which is the use of biological agents.
Bacillus sp. from the soybean phyllosphere is a biological agent that has the potential to suppress the
development of pustule disease. One of the biological control mechanisms is through biochemical induction
of plant resistance which includes the accumulation of phenols, salicylic acid compounds, and peroxidase
enzymes. Bacillus subtilis JB12 and Bacillus velezensis ST32 are two bacteria isolated from the soybean
phyllosphere which have previously been known to suppress Xag through an anti

... Show More
View Publication Preview PDF
Scopus (3)
Crossref (2)
Scopus Crossref
Publication Date
Sat Dec 30 2023
Journal Name
Basrah Journal Of Surgery
Can Hyaluronic acid gel enhance wound healing faster than Advanced Platelets Rich Fibrin following surgical removal of impacted mandibular third molars? A Randomized Controlled Trial
...Show More Authors

View Publication Preview PDF
Crossref
Publication Date
Sun Dec 06 2009
Journal Name
Baghdad Science Journal
Synthesis and Characterization of (Fe(II),Co(II),Ni(II) and Cu(II)) Complexes with Schiff Base derived from [benzoyl hydrazine] with [benzyl mono oxime]
...Show More Authors

The reaction of [Benzoyl hydrazine] with [Diphenyl mono oxime] and Glacial acetic acid was carried out in methanol gave a new tridentate ligand [Benzoic acid (2- hydroxyimino- 1, 2-diphyneylethylidene) - hydrazide]. This ligand was reacted with some metal ions (Fe(II), Co(II), Ni(II), and Cu(II)) in methanol with (1:1) metal : ligand ratio to give a series of new complexes of the general formula [M(L)Cl2.H2O], where M= Fe(11), Co(11), Ni(11) and Cu(11) . All compounds were characterized by spectroscopic methods (I.R, UV-Vis), elemental microanalysis (C.H.N), atomic absorption, magnetic susceptibility, and conductivity measurements. From the obtained data the proposed molecular structures were suggested for the complexes of Fe (II), Co (II)

... Show More
Publication Date
Wed Mar 02 2022
Journal Name
Journal Of Educational And Psychological Researches
Student Attitudes towards Rooting the Educational Administration Field: A Field Study for Phd Students in the Department of Educational Administration at Umm al-Qura University
...Show More Authors

The study sought to identify the attitudes of PhD students towards establishing the field of educational administration. The study followed the descriptive survey method. The questionnaire was used to collect information from the study community consisting of (95) male and female students in the department of educational administration and Planning. Among the most important results about students ’attitudes towards establishing the educational administration field are the following: 1) identifying the necessity of establishing the educational administration field. 2) Encouraging students to attend seminars and scientific conferences in Islamic rooting. 3) there are no statistically significant differences in the attitudes of doctoral s

... Show More
View Publication Preview PDF
Publication Date
Sun Dec 02 2012
Journal Name
Baghdad Science Journal
Preparation, Study and Theortical Treatment of Co(II) Ni(II) Cu(II) and Zn(II) Schiff Base Coplexes with Sodium [N-(hydroxyl naphtholidine) Glycine imino].
...Show More Authors

Anew Schiff base (NaHL) has been prepared from the reaction between the salt of amino acid glycine with 2-hydroxy naphthaldehyde. By tridentate Schiff base of (ONO), donors were characterized by using U.V and spectrophotometer techniques. Complexes of Co(II) Ni(II) Cu(II) and Zn(II) ion with the ligand have been prepared, these complexes were identified by infrared, electronic spectral data, elemental analysis, magnetic moments, and molar conductivity measurements. It is concluded from the elemental analysis that all the complexes have (1:2) [metal:ligand] molar ratios, octahedral, with the exception to Zn(II) complex which have (1:1)[metal:ligand] molar ratio.

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Dec 06 2009
Journal Name
Baghdad Science Journal
Synthesis and Characterization of (Fe(II),Co(II),Ni(II) and Cu(II)) Complexes with Schiff Base derived from [benzoyl hydrazine] with [benzyl mono oxime]
...Show More Authors

The reaction of [Benzoyl hydrazine] with [Diphenyl mono oxime] and Glacial acetic acid was carried out in methanol gave a new tridentate ligand [Benzoic acid (2-hydroxyimino- 1, 2-diphyneylethylidene) - hydrazide]. This ligand was reacted with some metal ions (Fe(II), Co(II), Ni(II), and Cu(II)) in methanol with (1:1) metal : ligand ratio to give a series of new complexes of the general formula [M(L)Cl2.H2O], where M= Fe(11), Co(11), Ni(11) and Cu(11). All compounds were characterized by spectroscopic methods (I.R, UV-Vis), elemental microanalysis (C.H.N), atomic absorption, magnetic susceptibility, and conductivity measurements. From the obtained data the proposed molecular structures were suggested for the complexes of Fe

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sun Sep 07 2014
Journal Name
Baghdad Science Journal
Comparison the effectiveness of using a magnetic field to control theColi phages isolated from rivulet water with water-treatment using magnetic field added iron filings
...Show More Authors

The present study aimed to use the magnetic field and nanotechnology in the field of water purification, which slots offering high efficiency to the possibility of removing biological contaminants such as viruses and bacteria rather than the use of chemical and physical transactions such as chlorine and bromine, and ultraviolet light and boiling and sedimentation and distillation, ozone and others that have a direct negative impact on human safety and the environment. Where they were investigating the presence in water samples under study Coli phages using Single agar layer method and then treated samples positive for phages to three types of magnetic field fixed as follows (North Pole - South Pole - Bipolar) and compare the re

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Mar 12 2025
Journal Name
The Alarba'een Journal
Analyzing and tracking the data of the millions sized gatherings for the Arba'in visit and proposing alternative ways to relieve congestion using spatial analysis algorithms
...Show More Authors

The city of Karbala is one of the most important holy places for visitors and pilgrims from the Islamic faith, especially through the Arabian visit, when crowds of millions gather to commemorate the martyrdom of Imam Hussein. Offering services and medical treatments during this time is very important, especially when the crowds head to their destination (the holy shrine of Imam Hussein (a.s)). In recent years, the Arba'in visit has witnessed an obvious growth in the number of participants. The biggest challenge is the health risks, and the preventive measures for both organizers and visitors. Researchers identified various challenges and factors to facilitating the Arba'in visit. The purpose of this research is to deal with the religious an

... Show More
View Publication Preview PDF
Publication Date
Thu Jan 09 2020
Journal Name
Plant Archives
Molecular Study of Two Fungi Millerozyma Farinosa and Candida Orthopsilosis by PCR Using Its Gene and Phylogenetic Structuring Tree Isolated from Diabetic Patient in Baghdad
...Show More Authors

Diabetic mellitus is one of the main risk factors of fungal infections because poor glycemic control is associated with a high level of glucose in blood and saliva which could be treated as nutrient to fungi. This study aimed to isolate and identification of pathogenic fungi from diabetic patient. 140 samples were taken from different places of human body from the national center of diabetic patients that related to Mustansiriyah University / college of medicine and Al-yarmuk Hospital in Baghdad. 84 sample (60%) tested positive to fungi and 56 sample (40%) tested negative to fungi. The most frequented fungi isolated have been chosen for molecular identification by PCR (Millerozyma farinosa and Candida orthopsilosis) using specific pri

... Show More
Scopus (1)
Scopus
Publication Date
Fri Jan 01 2021
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Auditor's Evaluation of The Detected Misstatements and Their Reflection on The Administration's Actions is: an Applied Research in the General Company for Grain Processing
...Show More Authors

Some auditors may think that the audit process ends with discovering misstatements and informing management about them, while the discovery of misstatements may be classified by some as the first step in the phase of separating these distortions, as the auditor should collect these misstatements, evaluate them and detail them into misstatements involving errors or misstatements involving fraud Then evaluating it to material or immaterial according to what was stated in the international auditing standards and directing management to amend the essential ones.  The importance of this research lies in identifying the concept of distortions and their types, identifying the method of evaluating distortions into substantial and non-essent

... Show More
View Publication Preview PDF