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
Mon Jun 01 2009
Journal Name
Journal Of Economics And Administrative Sciences
Environmental management system in accordance with the requirements of the international standard (ISO 14004) and its applicability "Case study at Al-Ma'mun plant (vegetable oil)"
...Show More Authors

 The search aims to clarify pollution to negative effects on environment and to an increasing in the dangerous polluted materials that discharged out these factories. To make active procedures in order to limit the environmental pollution.   

 The search problem came from an assumption which has the researched factory is suffering from the lack of applying the international specification      ( ISO 14004 ). The research problem assimilated by these questions:

  1. What is the level or organization in thinking of environmental system according to ISO 14004 .
  2. What are the requirements used in researched factor

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Sep 15 2022
Journal Name
Journal Of Baghdad College Of Dentistry
The effect of sweet and salty taste sensitivity on gin-gival health in relation to salivary serotonin among type1 diabetic patients aged 12-14 years
...Show More Authors

Background: This study was conducted among diabetic persons to assess the sweet and salty taste sensitivity with its effect on gingival health in relation to salivary serotonin levels. Materials and methods: A cross-sectional comparative study design was used. All patients with diabetes aged 12-14 years that attend the Paediatric hospital at Baghdad medical city with specific inclusion criteria were involved in the sample of the present study (patients group 50 patients) compared with non-diabetic persons matched in age and gender of the study sample (control group 70 patients) who were attending dental unit in the college of dentistry/university of Baghdad. A two-alternative forced choice question including each component presented at f

... Show More
View Publication Preview PDF
Scopus (2)
Crossref (2)
Scopus Crossref
Publication Date
Mon Jan 02 2023
Journal Name
Res Militaris
Rehabilitation program for treatment Tennis Elbow (Lateral Epicondylalgia) suffered by the players of Al-Rafidain Sports Club for Tennis League three players in Diyala province
...Show More Authors

Abstract Lateral Epicondylitis (LE) which has been referred to as the Tennis Elbow as well is a lesion affecting common tendinous origins of wrist extensors due to chronic overuse injury that results in damaging common extensor tendons which join forearm extensor muscles to humerus. The aim of the present evidence-based clinical statement is reviewing scientific evidences for efficacy of a variety of the rehabilitation methods, chronic lateral epicondylitis management. It is focused upon treating chronic lateral epicondylitis and the latest developments in physiotherapy area for managing chronic lateral epicondylitis. Due to the fact that primary physical impairments in the LE are decreased is the strength of the grip, fundamentally due to

... Show More
View Publication Preview PDF
Publication Date
Mon Feb 01 2021
Journal Name
Meta Gene
Association analysis of FTO gene polymorphisms rs9939609 and obesity risk among the adults: A systematic review and meta-analysis” Meta Gene (2020) 7–7/100832
...Show More Authors

Background: Obesity typically results from a variety of causes and factors which contribute, genetics included, and style of living choices, and described as excessive body fat accumulation of body fat lead to excessive body, is a chronic disorder that combines pathogenic environmental and genetic factors. So, the current study objective was to investigate the of the FTO gene rs9939609 polymorphism and the obesity risk. Explaining the relationship between fat mass and obesity-associated gene (FTO) rs9939609 polymorphism and obesity in adults. Methods: Identify research exploring the association between the obesity risk and the variation polymorphisms of FTO gene rs9939609. We combined the modified odds ratios (OR) as total groups and subgro

... Show More
View Publication
Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
The Green Regulatory Tapes and Their Reflections on the Job Development - A Study for the Sample of Employees in the Nineveh Directorate for Bridges & Roads
...Show More Authors

The performance of job effectively requires narrowing the meaningful routine activities and attempting employing the job procedures in favor of public welfare through adding the green impact as well as removing them from the red tapes which reflect the firmness of procedures, to enable the job parties to make their job independently, and pushing them to gain priority in the competition layer. This is not attaining easily amidst the regulatory problems expressed by the complication of procedures, the thing which make identifying the problem of the study through the following question:

Should we make the complex of procedures and their firmness a way to adopt the idea of the green regulatory tapes supportin

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Oct 02 2018
Journal Name
Iraqi Journal Of Physics
Nonlinear optical properties of polymer [PMMA] thin films doped with dye lasing compounds, Rhodamine 6G and Acriflavine in chloroform solvent by using dip coating method
...Show More Authors

The fluorescence emission of Rhodamine 6G (R6G) and Acriflavine dyes in PMMA polymer have been studied by changing the irradiation and exposure time of laser light to know the effect of this parameter. It was found that the fluorescence intensity decreases in the polymer samples doped dyes as the exposure time increases and then reaches stabilization at long times, this behavior called photobleaching, which have been shown in liquid phase less than solid phase. Using 2nd harmonic with wavelength 530 nm laser, the photobleaching effect in the two dye-doped polymers different solvent but same was studied. It was observed that photobleaching of by different solution and by using dip spin coating the photobleaching seem in liquid phase

... Show More
View Publication
Crossref (1)
Crossref
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
Wed Sep 15 2021
Journal Name
Al-academy
The concept of stigma and its representations in the Arab theatrical text (The Sultan, Al-Ha'ir play, by choice): نزار شبيب كريم - علاء حاتم محسن
...Show More Authors

The research deals with the concept of stigma as one of the important phenomena that cast a shadow over the nature of the individual, his being and his personality through the inferior view with which he confronts in society, and (Sartors) indicates in this regard that stigma may lead to negative discrimination that leads to many defects, in terms of obtaining On care, poor health, service, and frequent setbacks that can damage self-esteem. The first roots of this phenomenon go back to the Greek civilization and what the Greeks used to burn and cut off some parts of the body and then announce to the nation that the bearer of this sign is a criminal. In addition to the Arab peoples living from setbacks that contributed to the exacerbation

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue May 11 2021
Journal Name
Photonics And Nanostructures - Fundamentals And Applications
The spontaneous emission performance of a quantum emitter coupled to a hybrid plasmonic waveguide with specified output polarization for on-chip plasmonic single-photon source
...Show More Authors

Nowadays, most of the on-chip plasmonic single-photon sources emit an unpolarized stream of single photons that demand a subsequent polarizer stage in a practical quantum cryptography system. In this paper, we numerically demonstrated the coupling of the light emitted from a quantum emitter (QE) at 700 nm wavelength to the propagation mode supported by an on-chip hybrid plasmonic waveguide (HPW) polarization rotator. Our results proved that the light emitted is linearly polarized at 0º, 45º/−45º, and 90º with propagation lengths of 5 μm, 3.3 μm, and 3.9 μm, respectively. Moreover, high power-conversion efficiency was obtained from an applied transverse magnetic (TM) mode (0º-polarization) to a transverse electric (TE) (90º-polari

... Show More
View Publication
Scopus (4)
Crossref (4)
Scopus Clarivate Crossref
Publication Date
Wed Jan 01 2014
Journal Name
Journal Of The College Of Languages (jcl)
COMENTARIO ESTILÍSTICO- LITERARIO DE UN CUENTO DE JOSÉ ANTONIO GRILLO LONGORIA: “EL ALACRÁN Stylistic -Literary analysis of the story Jose Antonio Grillo Longoria: "The Scorpio"
...Show More Authors
 
 
Al  comentar un texto literario no se llega solamente mediante el estudio de su Historia. Ese estudio sería vano, se convertiría en una simple memorización de datos, creo yo.
Comentar un texto supone comprobar las características generales de un movimiento, estilo de un autor... en otras palabras comprender con profundidad el texto literario en s
... Show More
View Publication Preview PDF