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
Tue Jun 01 2021
Journal Name
Journal Of Engineering
A Comparative Study of a Moving Bed Biofilm Reactor and Bio-shaft Technology for a Wastewater Treatment Process: A review
...Show More Authors

In addition to the primary treatment, biological treatment is used to reduce inorganic and organic components in the wastewater. The separation of biomass from treated wastewater is usually important to meet the effluent disposal requirements, so the MBBR system has been one of the most important modern technologies that use plastic tankers to transport biomass with wastewater, which works in pure biofilm, at low concentrations of suspended solids. However, biological treatment has been developed using the active sludge mixing process with MBBR. Turbo4bio was established as a sustainable and cost-effective solution for wastewater treatment plants in the early 1990s and ran on minimal sludge, and is easy to maintain. This

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Jan 18 2017
Journal Name
Effect Of Cutting Angle And Knives Type On Some Operational Characteristics For A Locally Manufactured Palm Pruning Motorized Vibration Cutter‏ Aa Jasim, Mr Abbood, Sm Abbood‏
Effect of Cutting Angle and Knives Type on Some Operational Characteristics for a Locally Manufactured Palm Pruning Motorized Vibration Cutter‏
...Show More Authors

Publication Date
Sun Dec 01 2013
Journal Name
Journal Of Al-nahrain University
Corrosion Inhibition Effects of Some New Synthesized N-Aroyl-N\ -Aryl thiourea Derivatives for Carbon Steel in Sulfuric Acid Media
...Show More Authors

This research includes the synthesis of some new N-Aroyl-N \ -Aryl thiourea derivatives namely: N-benzoyl-N \ -(p-aminophenyl) thiourea (STU1), N-benzoyl-N \ -(thiazole) thiourea (STU2), N-acetyl-N ` -(dibenzyl) thiourea (STU3). The series substituted thiourea derivatives were prepared from reaction of acids with thionyl chloride then treating the resulted with potassium thiocyanate to affored the corresponding N-Aroyl isothiocyanates which direct reaction with primary and secondary aryl amines, The purity of the synthesized compounds were checked by measuring the melting point and Thin Layer Chromatography (TLC) and their structure, were identified by spectral methods [FTIR,1H-NMR and 13C-NMR].These compounds were investigated as a

... Show More
View Publication Preview PDF
Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Gingival microleakage of composite restorations with different bonding protocol in class II cavity treated with chlorhexidine (an in-vitro study)
...Show More Authors

ABSTRACT Background: One of the challenges to use chlorhexidine is its effect on the amount of microleakage after restoration; however, use of the materials with antibacterial properties after tooth preparation and before restoration has been widespread. The objective of this, in-vitro, study was to evaluate the influence of consepsis (chlorhexidine gloconate disinfectant) application on microleakage in class II cavities restored with light cured composite using universal adhesive system; etch and rinse technique –self etch technique. Materials and Methods: Forty class II cavities were prepared on mesial and distal surfaces of 20 non-carious mandibular third molars. The cavities were divided into four groups; (n =10 for each group).

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Mar 28 2023
Journal Name
International Journal Of Dentistry
The Effect of Different Obturation Techniques in Primary Teeth on the Apical Microleakage using Endoflas: A Comparative In Vitro Study
...Show More Authors

Objectives. This study was carried out to quantitatively evaluate and compare the sealing ability of Endoflas by using differentobturation techniques. Materials and Methods. After 42 extracted primary maxillary incisors and canines were decoronated, theircanals were instrumented with K files of size ranging from #15 to #50. In accordance with the obturation technique, the sampleswere divided into three experimental groups, namely, group I: endodontic pressure syringe, group II: modified disposable syringe,and group III: reamer technique, and two control groups. Dye extraction method was used for leakage evaluation. Data wereanalyzed using one-way ANOVA and Dunnett’s T3 post hoc tests. The level of significance was set at p<0:05. Results.

... Show More
View Publication
Crossref (3)
Crossref
Publication Date
Sat Jun 01 2024
Journal Name
Minar International Journal Of Applied Sciences And Technology
PREPARATION, CHARACTERIZATION AND EVALUATE THEIR BIOLOGICAL ACTIVITY OF NEW HETEROCYCLIC COMPOUNDS DERIVED FROM 4-((1-(4-HYDROXYPHENYL) ETHYLIDENE) AMINO) BENZENESULFONAMIDE
...Show More Authors

The research included the preparation of cyclic compounds from thiazoles, imidazoles and oxazepines from the reaction of cyclization starting material that acts Schiff bases, which is a raw material in the formation of cyclic compounds from Schiff's(B1) by reaction of 4- aminobenzenesulfonylamide with 4-hydroxyacetophenone which can used to synthesized two lines. The first introducing the preparation of pyrazoles [B4, B5] from ester [B2], which derived to acid hydrazide[B3] with hydrazine hydrate and final pyrazoles obtained by the reaction with diethylmalonate and acetylacetone. The second including prepared the new 1,3-oxazepine1,5-dione derivatives[B6,B7,B8] from adding different anhydrides to the base[B1] as a seven membered ring ; te

... Show More
View Publication
Crossref
Publication Date
Sat Jan 24 2026
Journal Name
Journal Of Physical Education
The Effect of Proprioceptive Neuromuscular Facilitation Exercises Combined with Superset Pyramid on Maximal Strength in Classic Physique Athletes’ Lower Extremities
...Show More Authors

View Publication
Publication Date
Mon Jan 01 2024
Journal Name
Oncology And Radiotherapy
Comparting study of cytokeratin 18 fragment M65 with CA19-9 and CEA as a biomarker in Iraqi colon cancer patients
...Show More Authors

Scopus
Publication Date
Sun Jan 08 2023
Journal Name
International Journal Of Research In Social Sciences And Humanities
Evaluating Banking Performance According to the European Model of Institutional Excellence: Case Study at United Bank for Investment and Finance1
...Show More Authors

The aim of the research is to identify the impact of the dimensions of the European Excellence Model in evaluating the performance of the bank of the research sample, as well as to interpret which dimensions are more important to the banks of the research sample. Based on the dimensions of this model, the United Bank for Investment and Finance has chosen a research community, and has met with officials of the United Bank for Investment and Finance at various administrative levels to measure the practices of excellence management in the European model, and the analytical approach has been the case study and the construction of the checklist as a tool to collect information. The research has reached the most important results There is a discr

... Show More
View Publication
Publication Date
Wed Dec 13 2017
Journal Name
Al-khwarizmi Engineering Journal
Using Activated Carbon developed from Iraqi Date Palm Seeds as Permeable Reactive Barrier for Remediation of Groundwater Contaminated with Copper
...Show More Authors

The possibility of using activated carbon developed from date palm seeds wastes as a permeable reactive barrier (PRB) to remove copper from polluted shallow groundwater was investigated. The activated carbon has been developed from date palm seeds by dehydrating methods using concentrated sulfuric acid. Batch tests were performed to characterize the equilibrium sorption properties of new activated carbon in copper-containing aqueous solutions, while the sandy soil (aquifer) was assumed to be inert. Under the studied conditions, the Langmuir isotherm model gives a better fit for the sorption data of copper by activated carbon than other models. At a pilot scale, One-dimensional column experiments were performed, and an integrated model ba

... Show More
View Publication Preview PDF