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 2004
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
MICROFACIES ANALYSIS OF GHAR FORMATION (WESTERN DESERT OF IRAQ)
...Show More Authors

Ghar Formation outcrop at the Iraqi western desert was studied by microfacies analysis
of (13) thin sections collected from wadi Al-Ratgha ( west of Qaim ) . According to
petrographic com position and organisms content ,rocks were subdivided into (4)
microfacies units :bioclastic wackestone , mudstone , miliolids wackestone , and grainstone
with aggregate grains microfacies .Microfacies units reflect shallow marine environment of
low circulation of very warm water at the middle part . The lower and middle part
interbedded with quite open marine environment below the wave base . The upper part was
deposited at shallow marine environment of low circulation . The main diagenetic processes
were the transformation ( ty

... Show More
View Publication Preview PDF
Publication Date
Thu Dec 16 2021
Journal Name
Journal Of Advance Research In Chemical Sciences
Study of Schiff Bases Complexes of Trimethoprim: A Review
...Show More Authors

Trimethoprim derivative Schiff bases are versatile ligands synthesized with carbonyl groups from the condensation of primary amines (amino acids). Because of their broad range of biological activity, these compounds are very important in the medical and pharmaceutical fields. Biological activities such as antibacterial, antifungal and antitumor activity are often seen. Transition metal complexes derived from biological activity Schiff base ligands have been commonly used.

View Publication Preview PDF
Publication Date
Tue Jun 14 2022
Journal Name
Al-academy
Mechanism of feedback in the theater of the oppressed
...Show More Authors

The art of theater penetrated various scientific and human fields, as well as touching the facts and events surrounding it, and scientific innovations had a wide field, so it adopted feedback in interactive theater performances, especially the theater of the oppressed. Then came the indicators that resulted from the theoretical framework for the formation of the tool by which the research sample is analyzed, and then the chapter concluded with previous studies. As for the third chapter, it involved the research procedures, and through the research tool and the research method, and by selecting the intentional sample, the sample represented by a play (the story of Shahrour) was analyzed. As for the fourth chapter, it included the results

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Dec 30 2018
Journal Name
Journal Of Engineering
Effect of bentonite addition on some properties of porcelain
...Show More Authors

Porcelain is one of the most important ceramic materials with a wide range of traditional and technical applications. Since most mixtures of porcelain have a high sintering temperature, bentonite has been added in this research to improve the characteristics of sintering and burning. The porcelain mixture consisted of the following Iraqi raw materials: 30% wt kaolin, 30 wt% non-plastic clay (grog), 10% wt sodium feldspar, 10 wt% potassium feldspar and 20 wt% flint. After the mechanical mixing process and transfer the powder mixture to the slurry by adding distilled water, then different weight percentage of the sodium bentonite(0, 2.5, 5, 7.5 and 10) wt% was added. The specimens were prepared by using the solid casting m

... Show More
View Publication Preview PDF
Crossref (8)
Crossref
Publication Date
Fri Jan 01 2016
Journal Name
Chemistry And Materials Research
Synthesis of Triazolo and Pyrazolo Derivatives of Quinoline Nucleus
...Show More Authors

New heterocyclic derivatives of quinoline are reported. Reaction of quinoline-2-thiol 4 with hydrazine hydrate gave 2-hydrazionoquinoline 5. Treatment of 5 with CS2 in pyridine afforded 1,2,4-triazolo-[4,3-a]- quinolin-1-2H-thione 6, whereas the reaction of 5 with carboxylic acids namely formic acid or acetic acid, yielded the 1,2,4-triazol-[4,3-a]-quinolin 7 or 5-methyl-1,2,4-triazolo [4,3-a]-quinoline 8 through ring closure. Diazotization of 5 under acidic conditions produced the fused tetrazole compound 9, tetrzolo-[1,5-a]- quinoline. Moreover, treatment of 5 with active methlyene compounds gave two pyrazole derivatives 10 and 11. Azomethines 12a-e were prepared through condensation of 5 with aromatic aldehydes or ketones.

View Publication Preview PDF
Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Effect of Polymers on Permanent Deformation of Flexible Pavement
...Show More Authors

The permanent deformation of flexible pavement represent serious problem in hot climate region. Numerous efforts are devoted to mitigate this distress such as modifying asphalt binder by polymers. The present study demonstrate the effect of utilizing four types of polymers to reduce the permanent deformation, these polymers are Polyethylene Wax (PEW), Styrene Butadiene Rubber (SBR), Ethylene Propylene Dien Monomer (EPDM) and Ethylene Vinyl Acetate (EVA). The prepared mixtures composed of 4.9 % of 40/50 asphalt binder, 12.5 mm nominal aggregate maximum size and limestone dust as filler. The permanent and resilient strains have been recorded when the cylindrical specimens, 101.6 mm in diameter and 203.2 mm in height, tested by repeated loa

... Show More
View Publication Preview PDF
Crossref (2)
Crossref
Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Development of resistance of some klebsiella species isolated locally
...Show More Authors

200 samples collected Adrar of patients with urinary tract infection were investigating the types of bacteria most local isolates showed high resistance to antibiotics penicillin c ??????? Amoxicillin Beracelin

View Publication Preview PDF
Publication Date
Thu Jan 10 2019
Journal Name
Journal Of The College Of Education For Women
Types of parallelism in the poetry of Mahmoud Darwish
...Show More Authors

This research deals with the study of types of parallelism in contemporary Arabic poetry and took the hair Mahmoud Darwish, a model for the study has been the goal of research to clarify the term parallelism and the statement of the most important types, said evidence of that in the poetry of Mahmoud Darwish

View Publication Preview PDF
Publication Date
Fri Nov 09 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Assessment of the Biological Activities of Calendula officials Extracts
...Show More Authors

Objective: To assess two kinds of extraction (aqueous and methanolic) for Calendula officials using flowers, leaves
and stems and studying their antibacterial activity against five different bacteria.
Methodology: Calendula officials were selected to carry out this study. Flowers, leaves and stems were collected from
local markets in Baghdad then dried in shade for 7 days and grinded to fine powder. Aqueous hot extracts for 2hr. at
(100c˚) and alcoholic extracts for 48 hrs at (80c˚) were performed using flowers, leaves and stems then studied
antibacterial effect against five different bacterial genuses by using well diffusion technique.
Results: This study showed that hot aqueous extracts for 2hr. to all parts of Cale

... Show More
View Publication Preview PDF
Publication Date
Wed Jun 20 2012
Journal Name
Journal Of Biotechnology Research Center
Evaluation of toxic effects of two weight reduction pills
...Show More Authors

Abstract his study involved evaluation of side effects of two weight reduction pills that had been widely distributed in the last period. Two weight reduction compounds are studied, Reductil (containing chemical substances) and Chinese’s weight reduction herbs (containing natural substances). Two doses for each compound are used in this research; 5mg/ml and 0.5mg/ml for Reductil, while 30mg/ml and 10mg/ml for Chinese weight reduction herbs. To evaluate the toxic effects of these compounds, the following parameters were determined which include mitotic index (cytogenetic analysis), serum FSH and LH hormones level (follicles stimulation hormone/FSH and lutenising hormone/LH) and histological examination of female mice ovaries. Control group

... Show More