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 May 28 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Shear bond strength of stainless steel brackets bonded to porcelain surface treated with 1.23% acidulated phosphate fluoride gel compared to hydro fluoric acid with silane coupling agent (In vitro comparative study)
...Show More Authors

Background: With the increasing demands for adult orthodontics, a growing need arises to bond attachments to porcelain surfaces. Optimal adhesion to porcelain surface should allow orthodontic treatment without bond failure but not jeopardize porcelain integrity after debonding.The present study was carried out to compare the shear bond strength of metal bracket bonded to porcelain surface prepared by two mechanical treatments and by using different etching systems (Hydrofluoric acid 9% and acidulated phosphate fluoride 1.23%). Materials and Methods: The samples were comprised of 60 models (28mm *15mm*28mm) of metal fused to porcelain (feldspathic porcelain). They were divided as the following: group I (control): the porcelain surface left u

... Show More
View Publication Preview PDF
Publication Date
Tue Jan 02 2018
Journal Name
Journal Of Educational And Psychological Researches
Psychological social conflict and its relation with family parental style for adolescences from the intermediate stage student at governmental Hail school, in the light of economical levels and sex variables .KSA
...Show More Authors

The current research attempts to examine the relationship between social-psychological conflict and their relation to family upbringing approaches among the adolescents of intermediate stage according to sex and economical level. To do this, the researcher prepared a questionnaire to measure social-psychological conflict that consisted of (32) item divided on four dimensions, and also she prepared a questionnaire to measure family upbringing approaches which composed of (28) item divided on four dimensions. The sample was (260) male and female student from intermediate stage chosen randomly. The results revealed that there were significant differences between social-psychological conflict which went to male, there was a negative correlat

... Show More
View Publication Preview PDF
Publication Date
Sun Jun 01 2008
Journal Name
Baghdad Science Journal
Synthesis and characterization of VO(II), Cr(III),Mn(II), Fe(II),Zn(II),Cd(II),Hg(II) and UO2(VI) complexes with ligands containing (ONO) and (ON) donor set atoms
...Show More Authors

A new Schiff base o-hydroxybenzylidene-1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-on (HL) ,have been prepared and characterization.(HL) has been used as a chelating ligand to prepare a number of metal complexes VO(II) ,Cr(III) ,Mn(II),Fe(II),Hg(II) and UO2(II) .and mixed ligands complexes have been prepared between o-hydroxybenzylidene-1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-on and 8- hydroxy quinoline with VO(II),Zn(II),Cd(II), Hg(II) and UO2(II) the prepared complexes were isolated and characterized by (FT-IR)and (UV-Vis) spectroscopy. Elemental analysis (C.H.N) Chloride contents, Flame atomic absorption technique. in addition to magnetic susceptibility and conductivity measurement. Molar ratio measurement in solution gave comparabl

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Tue Jun 07 2022
Journal Name
Egyptian Journal Of Chemistry
Structural, characterization and biological activity of new ligand N-(pyrimidin-2-yl carbamothioyl) acetamide and its complexes with (VO(II), Mn (II), Cu (II), Zn (II), Cd (II) and Hg (II)
...Show More Authors

New ligand of N-(pyrimidin-2-yl carbamothioyl)acetamide was synthesized and its complexes with (VO(II), Mn (II), Cu (II), Zn (II), Cd (II) and Hg (II) are formed with confirmation of their structures on the bases of spectroscopic analyses. Antimicrobial activity of new complexes are studied against Gram positive S. aureus and Gram negative E. coli, Proteus, Pseudomonas. The octahedral geometrical structures are proved depending on the outcomes from the preceding procedures

View Publication
Clarivate Crossref
Publication Date
Tue Dec 13 2022
Journal Name
Dental Hypotheses
Comparative Evaluation of Marginal Microleakage Between Bulk-Fill, Preheated Bulk-Fill, and Bulk-Fill Flowable Composite Resins Above and Below Cemento-Enamel Junction Using Micro-Computed Tomography: An In Vitro Study
...Show More Authors

Objective: The aim of this study was to compare the marginal microleakage between bulk-fill, preheated bulk-fill, and bulk-fill flowable composite resins above and below cemento-enamel junction (CEJ) using micro-computed tomography. Methods: Sixty freshly extracted premolar teeth were prepared with a slot shaped cavities of a total of 120 Class II: 3mm (bucco-lingual), 2mm (mesio-distal) with mesial-gingival margin located 1mm coronal to CEJ, and distal gingival margin located 1mm apical to the CEJ. The samples were randomly divided into two main groups according to the restorative material (Tetric EvoCeram and 3M Filtek), and each group was further sub-divided into three subgroups according to the consistency (bulk fill, preheated bulk fil

... Show More
View Publication
Scopus (11)
Crossref (7)
Scopus Clarivate Crossref
Publication Date
Sun Jan 01 2023
Journal Name
Results In Chemistry
Synthesis and characterization of (E)-4-(((4-(5-mercapto-1, 3, 4-oxadiazol-2-yl) phenyl) amino) methyl)-2-methoxyphenol as a novel corrosion inhibitor for mild-steel in acidic medium
...Show More Authors

View Publication
Scopus (26)
Crossref (27)
Scopus Clarivate Crossref
Publication Date
Sun Jan 01 2017
Journal Name
Journal Of Cosmetics, Dermatological Sciences And Applications
Topical 40% <i>Loranthus europaeus</i> Ointment as an Alternative Medicine in the Treatment of Acute Cutaneous Leishmaniasis versus Topical 25% Podophyllin Solution
...Show More Authors

View Publication
Crossref (3)
Crossref
Publication Date
Wed Aug 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Prepare a plan for the Total Productive Maintenance in the light of the concurrent engineering A Field Study in AL-Askandria General Company Machanical Industries and AL-Musaib Electric Power Station
...Show More Authors

           Strives Total Productive Maintenance  to increase the overall effectiveness of the equipment through the early involvement in the design and manufacture of equipment productivity. It also operates in an environment of simultaneous engineering work on the synchronization of activities to take advantage of early information by maintenance engineers, design, operation, and that helps to reduce the faults and facilitate future maintenance tasks.

    Has adopted a search in the theoretical concept of the total maintenance productivity and concurrent engineering activities carried out during which the conjunction a

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sun Apr 30 2017
Journal Name
Journal Of Engineering
Experimental Study on Heat Transfer and Friction Factor Characteristics of Single Layer Graphene Based DI-water Nanofluid in a Circular Tube under Laminar Flow and Different Heat Fluxes as Boundary Conditions
...Show More Authors

An experimental study was performed to estimate the forced convection heat transfer performance and the pressure drop of a single layer graphene (GNPs) based DI-water nanofluid in a circular tube under a laminar flow and a uniform heat flux boundary conditions. The viscosity and thermal conductivity of nanofluid at weight concentrations of (0.1 to 1 wt%) were measured. The effects of the velocity of flow, heat flux and nanoparticle weight concentrations on the  enhancement of the heat transfer are examined. The Nusselt number of the GNPs nanofluid was enhanced as the heat flux and the velocity of flow rate  increased, and the maximum Nusselt number  ratio (Nu nanofluid/ Nu base fluid)   and thermal performance factor

... Show More
View Publication Preview PDF
Publication Date
Fri Dec 01 2023
Journal Name
Case Studies In Chemical And Environmental Engineering
Removal of copper from a simulated wastewater by electromembrane extraction technique using a novel electrolytic cell provided with a flat polypropylene membrane infused with 1-octanol and DEHP as a carrier
...Show More Authors

View Publication
Scopus (8)
Crossref (9)
Scopus Crossref