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 Jul 01 2021
Journal Name
University Of Northampton Pue
Validating a Proposed Data Mining Approach (SLDM) for Motion Wearable Sensors to Detect the Early Signs of Lameness in Sheep
...Show More Authors

View Publication
Publication Date
Tue Jan 01 2013
Journal Name
The Iraqi Journal Of Veterinary Medicine
Detection of methicillin or multidrug resistant Staphylococcus aureus (MRSA) in locally produced raw milk and soft cheese in Baghdad markets.
...Show More Authors

In order to investigate the presence of methicillin or multidrug resistant Staphylococcus aureus in food-chain especially Cows raw milk and white raw soft cheese and its whey, a total of 30 samples were collected randomly from different markets in Baghdad Province during December 2012 till February 2013, in which samples were analyzed by a standard isolation protocols of food microbiology with some modification processing by new, modern and rapid technology tools such as chromogenic medium Baird-Parker agar, Electronic RapIDTM Staph Plus Code Compendium Panel System (ERIC®) Dryspot Staphytect Plus and Penicillin Binding Protein (PBP2') Plus assays; as well as, studying the susceptibility of isolates to different selected antibiotics. The r

... Show More
View Publication
Publication Date
Sun Jun 01 2014
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Internal control and its role in the reform of the tax work: Applied research in the General Commission for Taxes
...Show More Authors

That internal control is particularly important in improvingperformance and tax reform، they play an important role in the regularity ofwork and development and the anti corruption and activating the decisionsand tax legislation، as contained in the organizational plan and the means،procedures and components designed from which to ensure a policy andimplementation plans The research aims to review the reality of the internalcontrol in the General Commission for Taxes and stand on the deficiencies init, with the strengthening of the role of internal control in the GeneralAuthority for taxes based on the laws and regulations and by using modernmeans to work as well as developing the performance of employees in thebody، including helpin

... Show More
View Publication Preview PDF
Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
Bacterial Causes Tonsillitis in Children, Study the Resistance to Antimicrobials and the Effect of Clove Extracts on Selected Isolated Bacteria.
...Show More Authors

In this study Isolated Pathogenic bacteria which causes Tonsillitis in Children with ages between 3-17 years. They are admitted to Central Children Hospital (Al-Karch) and Ebn-Albalady Hospital (Al-Rusafa). 200 cases were collected which include 120 Male and 80 Female. The result of the recent study shows that the isolation percentage was 40% from Male and 35% from Female. In this study Fifty six isolated were Identified, 20 were ?-hemolytic Streptococcus which was Streptococcus pyogenes, formed (36%) from all isolated.6 Pathogenic bacteria were ?- hemolytic Streptococcus which was Streptococcus pneumoniae formed (11%). The number of Moraxella catarrhalis bacteria was 12 formed (21%), the number of Haemophilus influenzae was 1

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Jan 01 2024
Journal Name
Clinical Laboratory
Histopathological Tracing of HPV Genotypes 6 and 11 in Pediatric Patients in Medical City with Chronic Palatine and Pharyngeal Tonsillitis
...Show More Authors

View Publication
Scopus (1)
Scopus Clarivate Crossref
Publication Date
Fri Dec 01 2017
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Settling Accounts of tax According to the unified Tax A Suggested Mechanism for: Application in the general Commission for Taxes
...Show More Authors

Consistent "with the thought of tax talk is unified tax natural evolution for him, as the application leads to the inclusion of tax all branches of income and its sources and through truncated part of this entry through the application of price ascending it, it means the procedures of tax reform. Taxes on total income characterized by giving a clear picture of the total income of the taxpayer and its financial situation and its burden family which allows granting exemptions, downloads, and application of prices that fit this case. This requires reconsideration of the structure of the tax system in force and the transition from a system specific taxes to the tax system on the total income of the integration of income from the rental of re

... Show More
View Publication
Crossref
Publication Date
Fri Sep 30 2022
Journal Name
Journal Of Economics And Administrative Sciences
Choosing the best method for estimating the survival function of inverse Gompertz distribution by using Integral mean squares error (IMSE)
...Show More Authors

In this research , we study the inverse Gompertz distribution (IG) and estimate the  survival function of the distribution , and the survival function was evaluated using three methods (the Maximum likelihood, least squares, and percentiles estimators) and choosing the best method estimation ,as it was found that the best method for estimating the survival function is the squares-least method because it has the lowest IMSE and for all sample sizes

View Publication Preview PDF
Crossref
Publication Date
Thu Oct 01 2020
Journal Name
Biochemical And Cellular Archives
CUT-OFF VALUES OF BLACKCURRANT, LONDON PLANE AND PINE BUDS ON VANCOMYCIN RESISTANT ENTEROCOCCI ISOLATED FROM MASTITIC MILK IN BAGHDAD
...Show More Authors

Generation of new clones of multidrug resistant infectious foci of environmental, zoonotic and reverse zoonotic Enterococcus faecalis & faecium strains from cases of mastitis in cows privileged in Baghdad ecosystem reveal unsafe tricks. Medically important plants Blackcurrant, London Plane and Pine Buds are widely used for resolving these public health threats and hazards as powerful antimicrobial preparations. Totally sixty pooled milk samples were collected from apparently healthy (30 units) and infected (30 units) Cows from different regions of Abu-Ghraib during March until July (2019). Integrated units were checked by California mastitis test and a designed scheme was dependent for recovery of pathogenic Enterococci. Gram staining and c

... Show More
Scopus (4)
Scopus
Publication Date
Wed Jan 28 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Inhibition of bacterial growth around gutta percha cones by different antimicrobial solutions using antibiotic sensitivity test (An in vitro study)
...Show More Authors

Background: Decontamination of gutta percha cones was important factor for success of root canal treatment. The aim of the present in vitro study was to identify and to compare the antimicrobial effect of following disinfection solutions: 0.2% chlorhexidine gluconate, Iodine, tetracycline hydrochloride solution, EDTA & formocresol mixed with zinc oxide eugenol, on E faecalis, E coli and Candida albicans using sensitivity test Materials and Methods: Three types of microorganisms were isolated from infected root canals (E faecalis, E coli and Candida albicans) and cultured on Mueller Hinton agar petri-dishes. Disinfection of gutta percha cones done by immersion in six disinfection solutions (six groups), the groups are: distill water (used a

... Show More
View Publication Preview PDF
Publication Date
Tue Aug 01 2023
Journal Name
Baghdad Science Journal
First record of peregrine shrimp Metapenaeus stebbingi Nobili, 1904 (Crustacea, Decapoda: Penaeidae) in the Iraqi waters, North-West Arabian Gulf
...Show More Authors

One male specimen of the species Metapenaeus stebbingi Nobili, 1904 was first recorded in November 2021 from the Iraqi territorial waters, Northwest of the Arabian Gulf. Therefore, the investigated shrimp species nominally corresponds to the original description of M. stebbing through the main diagnostic features. It must be adopted in the spread and expansion of species, a new record of the area, and a distinctive addition to the species of commercial shrimp within the Iraqi marine waters.

View Publication Preview PDF
Crossref (1)
Crossref