Solid dispersion (SD) formulation has attracted much attention due to its potential in enhancing dissolution performances of poorly soluble active pharmaceutical ingredients (API). Recently, a review on dissolution performances of SDs classifies the improvement into 3 categories, where 82 % of the studies showed improved bioavailability, 8 % showed reduced bioavailability and 10 % revealed similar bioavailability as compared to pure APIs. This indicates the inconsistent degrees of dissolution improvement of poorly soluble APIs in SD. Although a few factors related to the choice of carriers have been suggested to contribute to the dissolution improvement, however, the underlying factor determining the discrepancy in the degree of dissolution improvement remains in vague. It is hypothesized that the API contributes to the degree of dissolution improvement of SD. Hence, the factor of amorphous solubility advantage of API which leads to the different degrees of dissolution enhancement of SD is investigated in this research. Polyvinylpyrrolidone vinyl acetate (PVPVA)-based SD is prepared with three poorly soluble APIs. Physicochemical properties of SD were characterized using infrared spectroscopy, differential scanning calorimetry (DSC) and X-ray powder diffraction. The dissolution efficiency of each SD was calculated and compared to physical mixture and pure API. Theoretical amorphous solubility advantage for each API was calculated using the thermal properties obtained from DSC. The calculated values were found to be correlating well with the dissolution enhancement of the respective SDs. Hence, this theoretical approach can be utilized as an initial screening tool of API candidates in SD formulation during early pharmaceutical development.
Chronic Kidney Disease (CKD) is a public health problem and many studies support the link between kidney dysfunction and cardiovascular events. Aldosterone has been shown for decades that a plasma aldosterone concentration is elevated in CKD. Whilst, Osteoprotegerin (OPG), after its capacity to protect bone, also osteoprotegerin is elevated in patients with chronic kidney disease (CKD), where it could predict the deterioration of kidney function, cardiovascular, vascular events and all-cause mortality. On the other hand, fibroblast growth factors (FGFs), in patients with CKD, its levels seem to increase progressively as kidney function worsens. The aim of the present study is to assess the correlations between serum osteoprotegerin
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The adsorption ability of Iraqi initiated calcined granulated montmorillonite to adsorb Symmetrical Schiff Base Ligand 4,4’-[hydrazine-1, 2-diylidenebis (methan-1-yl-1-ylidene)) bis (2-methoxyphenol)] derived from condensation reaction of hydrazine hydrate and 4-hydroxy-3-methoxybenzaldehyde, from aqueous solutions has been investigated through columnar method.The ligand (H2L) adsorption found to be dependent on adsorbent dosage, initial concentration and contact time.All columnar experiments were carried out at three different pH values (5.5, 7and 8) using buffer solutions at flow rate of (3 drops/ min.),at room temperature (25±2)°C. The experimental isotherm data were analyzed using Langmuir, Freundlich and Temkin equations. The monol
... Show MoreThe new 4-[(7-chloro-2,1,3-benzoxadiazole)azo]-4,5-diphenyl imidazole (L) have been synthesized and characterized by micro elemental and thermal analyses as well as 1H.NMR, FT-IR, and UV-Vis spectroscopic techniques. (L) acts as a ligand coordinating with some metal ionsV(IV), Fe(III), Co(II), Ni(II), Cu(II), and Zn(II). Structures of the new compounds were characterized by elemental and thermal analyses as well as FT-IR and UV-Vis Spectra. The magnetic properties and electrical conductivities of metal complexes were also determined. Study of the nature of the complexes formed in ethanol following the mole ratio method.. The work also include a theoretical treatment of the formed complexes in the gas phase, this was done using the (hyperch
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The prostaglandins inside inflamed tissues are produced by cyclooxygenase-2 (COX-2), making it an important target for improving anti-inflammatory medications over a long period. Adverse effects have been related to the traditional usage of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of inflammation, mainly centered around gastrointestinal (GI) complications. The current research involves the creation of a virtual library of innovative molecules showing similar drug properties via a structure-based drug design. A library that includes five novel derivatives of Diclofenac was designed. Subsequently, molecular docking through the Glide module and determining the binding free energy implementing the P
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The reaction of 1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one with one equivalent of 4-chlorophenol by coupling reaction afforded (E)-4-((5-chloro-2- hydroxyphenyl)diazenyl)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one. Then azo ligand was characterize using spectroscopic studies ( FTIR,UV-Vis, 1H and 13CNMR, Mass) also micro-elemental analysiz (C.H.N.O). Transition metal chelation with Co(II), Ni(II), Cu(II), and Zn(II) was investigated, revealing 1:2 metal-to-ligand stoichiometry with octahedral geometry. The biological, and industrial application for the azo ligand and it is complexes were evaluated, demonstrating antimicrobial activity against bacterial and fungal strains, with the Zn(II) complex exhibiting superior inhibition. Additionally,
... Show MoreThe syntheses, characterizations and structures of three novel dichloro(bis{2-[1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl-κN3]pyridine-κN})metal(II), [M(L)2Cl2], complexes (metal = Mn, Co and Ni) are presented. In the solid state the molecules are arranged in infinite hydrogen-bonded 3D supramolecular structures, further stabilized by weak intermolecular π…π interactions. The DFT results for all the different spin states and isomers of dichloro(bis{2-[1-phenyl-1H-1,2,3-triazol-4-yl-κN3]pyridine-κN})metal(II) complexes, [M(L1)2Cl2], support experimental measurements, namely that (i) d5 [Mn(L1)2Cl2] is high spin with S = 5/2; (ii) d7 [Co(L1)2Cl2] has a spin state of S = 3/2, (iii) d8 [Ni(L1)2Cl2] has a spin state of S =
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Взгляд на пол как на комплексное социальное отношение означает,что роль женщины в истории следует рассматривать не просто как новый для исторической науки предмет исследования, а как обойденный вниманием ученых вопрос об отношениях между людьми или группами людей.
Женщина играет особую и важную роль в обществе , даже скажут ,что она половина нашего общества ,поэтому она яв
... Show MoreThe present research aimed to study the polymorphisms of the chicken insulin-like growth factor 2 (IGF2) in two commercial broiler breeds (Cobb 500 and Hubbard F-15). In total, 300 avian blood samples were obtained. The genomic DNA was isolated using a fast salt-extraction technique. Moreover, polymerase chain reaction (PCR) was used to amplify 1146 bp fragments of the gene. The amplified fragments were subjected to restriction enzyme digestion using the HinfI endonuclease enzyme, and the digested products were separated on a 2% agarose gel. The findings indicated that there were two alleles, T and C, for the target locus, with frequencies of 73.3% and 26.7%, respectively. Three distinct genotype variations, TT, TC, and CC, were found, with
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