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
Sun Jun 30 2013
Journal Name
Al-kindy College Medical Journal
Huge Chondrosarcoma of Shoulder
...Show More Authors

Background: Chondrosarcoma is the second most frequent primary malignant tumor of bone. It is considered relatively an uncommon tumor. Generally it is not common for chondrosarcoma to attend huge size; however, one type was described as mesenchymal chondrosarcoma of low grade cartilaginous cells, with female predominance which can grow to exceptionally large size. Case Presentation: We report a case of Chondrosarcoma, in 30 years old woman of 4 years duration, with a huge mass (weighted 16 Kg) and roughly measured 40x30 x20cm, around the right shoulderInvestigations: Repeated MRI of the shoulder and trunk revealed a clear plane of cleavage between the tumor mass and the chest and abdominal walls and absence of invasion of the abdomen. Ul

... Show More
View Publication Preview PDF
Publication Date
Sun Dec 31 2000
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Preparation of Tartaric Acid
...Show More Authors

View Publication Preview PDF
Publication Date
Sun Sep 01 2013
Journal Name
Chemical Engineering Science
Evaporation dynamics of microbubbles
...Show More Authors

View Publication
Scopus (56)
Crossref (56)
Scopus Clarivate Crossref
Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation of Rifampicin Suspension
...Show More Authors

     

Rifampicin is the drug of choice in treatment of tuberculosis. Also, it is effective in treatment of various bacterial infections.This study was carried out to prepare a stable suspension for rifampicin through preparation of different formulas of rifampicin aqueous suspension either as ready to use or as granular powder to be reconstituted.The selected formula (A) was evaluated and compared with commercial brand of rifampicin (Rifactine®) as a reference through measuring their dissolution rates and other physical properties.The results indicated that the selected formula had better dissolution rate compared with the reference suspension and the rheogram showed that the selected formula was less

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sat Jun 30 2012
Journal Name
Al-kindy College Medical Journal
Management of Chronic Osteomylitis
...Show More Authors

Background : Bone infections is one of the most challenging orthopaedic complications, with considerable morbidity. There is significant impact on the life of the patients; socially, financially, physically, and mentally and it could be a limb-threatening complication. Osteomyelitis is a bone infection usually caused by bacteria, including mycobacteria, but mainly Staphylococcus aureus which is the most commonly responsible bacteria . Aim of study: To evaluate our management policy of chronic osteomylitis (C.O.M).
Methods : 32 patients presented with different types &forms of chronic osteomyelitis in many sites of long & flat bones such as tibia , femur, ,humerus ,iliac bones and knee joint , which are not response to previous

... Show More
View Publication Preview PDF
Publication Date
Thu Sep 30 2021
Journal Name
College Of Islamic Sciences
Augustine’s theory of knowledge
...Show More Authors

The issue of epistemology is one of the theological issues that were and still is a relentless pursuit of knowledge, knowing the true knowledge of certainty. Therefore, it formed a main focus because of its great importance expressing the deep desire of the human soul to explore the self and reality and answer all the questions that it may raise. Knowledge is the highest function. For man to exist.

Therefore, the establishment of epistemology was general in knowledge, a characteristic that was distinguished, as it is an ancient and renewed subject that is still being raised and raised, although there are many methods of treating it and sacred solutions to it. To finally prove its potentia

... Show More
View Publication Preview PDF
Publication Date
Sun Apr 02 2017
Journal Name
Journal Of Educational And Psychological Researches
Philosophical origins of psychology
...Show More Authors

Since the beginning of Philosophical thinking, philosophers had interested in matters that related to psychology. Greek philosophy had sought different psychological cases such as knowledge, thought, sense, and cognition. Plato classified cognitive processes and distinguished between intelligence, emotions, and desires. As Aristotle believed that soul is the essence of human beings that characterize it from other creatures. Regarding the European philosophy, Descartes linked the optics field to psychology that comprises theories about visual perception. Then, john Watson who interested in behaviorism, he believes that the interpretation of behavior will be materialistic. However, the evolutionary view had great effect on psychology that

... Show More
View Publication Preview PDF
Publication Date
Tue Jan 16 2018
Journal Name
International Journal Of Science And Research (ijsr)
The Effect of Woods' Strategy on Achieving of Second Grade Students in Physics
...Show More Authors

: The aim of this research is to investigate the impact of Woods ' strategy in collecting second graders average for physics. To achieve the objective researcher coined the following hypothesis: there was no statistically significant difference at a level (0.05) between the average grades of the experimental group students studying physics as Woods and strategy between the average control group students who are studying the same article in the regular way. Test collection. Search sample amounted to (83) students and (42) students for the experimental group, and (41) students for the control group. Students were subjected to test experiment is composed of (30) after the completion of the experiment. And use appropriate statistical methods re

... Show More
Publication Date
Thu Dec 01 2016
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
MORPHOLOGICAL AND HISTOCHEMICAL STUDY OF HARDERIAN GLAND OF DOMESTIC PIGEON (COLUMBA LIVIA DOMESTICA)
...Show More Authors

    The aim of this work is to study the histological and histochemical structure of the Harderian gland in indigenous pigeons. Samples were obtained from 10 males and 10 females of adult healthy pigeons. Hematoxylin and eosin, Alcian blue (pH 2.5), periodic acid-Schiff and promo phenol blue, stains were used for paraffin section examination. The gland was teardrop like in shape, light brown to pink in color, capsulated with thin connective tissue. It was multilobular compound acinotubular in structure and lined by columnar epithelial cells. Lymphocyte, plasma cells and plasma cells with Russell bodies were present underneath the epithelia of central collecting duct and around the secretory unite. Histochemically; the

... Show More
View Publication Preview PDF
Publication Date
Sun Feb 03 2019
Journal Name
Iraqi Journal Of Physics
Effect of CuI concentration on structural and optical properties of PVA: CuI nanocomposites
...Show More Authors

The nanocomposite on the base of synthesis Copper iodide
nanoparticles and polyvinyl alcohol (PVA/CuI) with different
concentration of CuI were obtained using casting technique.
PVA/CuI polymer composite samples have been prepared and
subjected to characterizations using FTIR spectroscopy, The FTIR
spectral analysis shows remarkable variation of the absorption peak
positions with increasing CuI concentration. The obtained results by
X-ray diffraction indicated the formation of cubic CuI particles. The
effects of CuI concentrations on the optical properties of the PVA
films were studied in the region of wavelength, (190-1100) nm.
From the derivation of Tauc's relation it was found that the direct
allowed t

... Show More
View Publication Preview PDF
Crossref (1)
Crossref