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 Sep 30 2019
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Development of East Baghdad Oil Field By Clusters of Horizontal Wells
...Show More Authors

There are varieties of reasons lead for drilling horizontal wells rather than verticals. Increasing the recovery of oil, especially from thin or tight reservoir permeability is the most important parameter. East Baghdad oil field considered as a giant field with approximately more than 1billion barrel of a proved reserves accompanying recently to low production rate problems in many of the existing wells.    It is important to say that presence of of  horizontal wells in East Baghdad field especially by converting some of already drilled wells by re-entry drilling horizontal sections may provide one of best solutions for the primary development stage in East Baghdad field which may be followed by drilling new horizont

... Show More
Crossref (3)
Crossref
Publication Date
Tue Jun 01 2021
Journal Name
Al-khwarizmi Engineering Journal
Prediction of Surface Roughness after Turning of Duplex Stainless Steel (DSS)
...Show More Authors

Feed Forward Back Propagation artificial neural network (ANN) model utilizing the MATLAB Neural Network Toolbox is designed for the prediction of surface roughness of Duplex Stainless Steel during orthogonal turning with uncoated carbide insert tool. Turning experiments were performed at various process conditions (feed rate, cutting speed, and cutting depth). Utilizing the Taguchi experimental design method, an optimum ANN architecture with the Levenberg-Marquardt training algorithm was obtained. Parametric research was performed with the optimized ANN architecture to report the impact of every turning parameter on the roughness of the surface. The results suggested that machining at a cutting speed of 355 rpm with a feed rate of 0.07 m

... Show More
View Publication Preview PDF
Scopus (1)
Scopus Crossref
Publication Date
Thu Mar 07 2013
Journal Name
International Journal Of Pharma Sciences
Separation and Purification of Hemolysin from Local Isolate of Serratia marcescens
...Show More Authors

Twenty isolates of Serratia marcescens were isolated from inflammation of the urinary tract (UTI)., These isolates were found to produce hemolysin as indicated by blood agar plates in which the hemolysis of red blood cell indicate a positive result. Isolates were selected according to their hemolysis activity by measuring absorbance of hemoglobin at 405 nm that released from red blood cell. Hemolysin was completely purified using 50-75% saturation of ammonium sulphate followed by ion exchange chromatography with DEAE-cellulose then gel filtration chromatography by sepharose 4B. Accordingly molecular weight for the purified toxin was estimated as 45 KD.

Publication Date
Tue Feb 05 2019
Journal Name
Journal Of The College Of Education For Women
Biography of the Last The formation of the ancient Pharaonic Warrior
...Show More Authors

Cash studies on Biography few self, compared to what feet of analysis and criticism in the other arts as (novel, short story, poetry, theater, painting), however, is a biographical articles in the relatively few Arabic literature as presented in the other Arts, has taken this Art greater opportunity in our literature with his Taha Hussein (days), or (my life) to Ahmed Amin, or Fadwa Toukan (a nice trip, and difficult journey), or Jabra Ibrahim Jabra in the (first well) or (Princess Street), which forms taken from the self point of departure the desire to write a CV to try to familiarize readers with the information possible to the same creator, the remainder (ego) is the axis basis in a CV, gradually, starting from childhood through yout

... Show More
View Publication Preview PDF
Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Purification and Characterization of Endoglucanase from local isolate of Aspergillus flavus
...Show More Authors

Endoglucanase produced from Aspergillus flavus was purified by several steps including precipitation with 25 % ammonium sulphate followed by Ion –exchange chromatography, the obtained specific activity was 377.35 U/ mg protein, with a yield of 51.32 % .This step was followed by gel filtration chromatography (Sepharose -6B), when a value of specific activity was 400 U/ mg protein, with a yield of 48 %. Certain properties of this purified enzyme were investigated, the optimum pH of activity was 7 and the pH of its stability was 4.5, while the temperature stability was 40 °C for 60 min. The enzyme retained 100% of its original activity after incubation at 40 °C for 60 min; the optimum temperature for enzyme activity was 40 °C.

View Publication Preview PDF
Crossref
Publication Date
Sun Mar 06 2011
Journal Name
Baghdad Science Journal
Isochronal Studies of the Structural and Electrical Properties of CdTe Films
...Show More Authors

The paper reports the influence of annealing temperature under vacuum for one hour on the some structural and electrical properties of p-type CdTe thin films were grown at room temperature under high vacuum by using thermal evaporation technique with a mean thickness about 600nm. X-ray diffraction analysis confirms the formation of CdTe cubic phase at all annealing temperature. From investigated the electrical properties of CdTe thin films, the electrical conductivity, the majority carrier concentration, and the Hall mobility were found increase with increasing annealing temperatures.

View Publication Preview PDF
Crossref
Publication Date
Thu Sep 12 2019
Journal Name
Al-kindy College Medical Journal
Association of radiological osteoarthritis of the knee joint with locomotor disability
...Show More Authors

Background:  Knee osteoarthritis (KOA) is a common joint disorder leading to considerable pain and locomotor disability in lower limb function. Locomotor disability, which is difficulty in activities of daily living related to lower limb function, can be the consequence of KOA, so early diagnosis and management may improve quality of life.

Objective: To assess the contribution of radiological osteoarthritis of the knees to disability in the activities of daily living related to lower limb function.

 Methods: One hundred twenty Iraqi KOA patients (104 females and 16 males) who were attending to Rheumatology Unit, Full history was taken and complete clinical exami

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Tue Jan 01 2002
Journal Name
University Of Baghdad
theoretical study of the drift velocity of electron in sf6-n2
...Show More Authors

Publication Date
Thu Jun 30 2016
Journal Name
Al-kindy College Medical Journal
Prevalence Of Energy Drinks Consumption Among Students Of Alkindy Medical College
...Show More Authors

Background: Energy drinks are non alcoholic beverages which contain stimulant drugs chiefly caffeine and marketed as mental and physical stimulators. Consumption of energy drinks is popular practice among college students as they are exposed to academic stress. Caffeine which is the main constituent of energy drinks could become an addictive substance or cause intoxication. Objectives: This study aims to assess the prevalence of energy drinks consumption among medical students of alkindy college of Medicine.Type of the study: A cross sectional study.Methods: It was performed at alkindy medical college on March 2016. A total number of 600 students were contacted to participate in this study. A self administered questionnaire was used to c

... Show More
View Publication Preview PDF
Publication Date
Sun Feb 25 2018
Journal Name
Advances In Bioresearch
Survey of field crickets (Orthoptera, Grylidae) in different regions of Iraq
...Show More Authors