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Preparation and Evaluation of Rebamipide Film using Casting Technique for Local Action
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Abstract

The aim of this study was to prepare rebamipide ocular inserts in order to extend its release on the ocular surface for dry eye treatment. Solubility study was applied to the drug with or without l-arginine using different solvents. Solvent casting technique was used to prepare the inserts; l-arginine was used to solubilize the drug, hydroxypropyl methylcellulose grades (E5 and K15M) and poly ethylene glycol 200 were used as excipients. The inserts were evaluated for their physical and mechanical properties, moisture loss% and absorption %, surface pH, and in-vitro drug release. The use l-arginine exhibited an enhancement of rebamipide solubility in both deionized water and phosphate buffer (pH 7.4) by approximately 250 times and 3 times, respectively. The formulations showed uniform weight and thickness except for F1, and all showed uniform drug content. The absence of plasticizer in F1 caused haziness in its appearance and brittleness of the inserts. F3 which contain hydroxypropyl methylcellulose K15M showed good physical and mechanical properties thus was selected for in vitro release and was compared to the marketed brand Mucosta® suspension eye drop; F3 showed significant enhancement in extending the release of rebamipide compared to the reference marketed brand.

Keywords: Rebamipide, L-arginine, Ocular insert, Solvent casting technique

 

 

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                        ????? ?? ??? ??????? ?? ????? ?????????? ?????? ???? ???? ????? ??????????? ??? ??? ????? ????? ????? ?????. ??? ?????  ??????? ?????? ????? ???????? ? ???? ????? ???????? ?????? ??????. ??????? ????? ??????? ? ???? ?????? ??????? ? ?????? ???????? ?????? ?????? ? ?? ??????? ??????????? ?????? ???? ???????? ?????? (K15M  ? E5 ) ? ?????? ?????? ??????? ?????. ?? ????? ?????? ?????????? ? ?????????? ??????? ? ???? ?????? ??????? ??????? ????? ? ?????? ??????? ? ???? ???? ??????????? ???? ??????? ????? ?????  ????? ??????  ?? ???????. ????? ??????? ?? ???????? ???? ??? ????? ??????? ???????????? ?? ?? ?? ????? ??????? ???????? ? ????? ???????? ?????? (?? ??????????? 7.4 ), ?????? ????? 250 ??? ? ???? ???? ??? ???????. ???????? ????? ??? ? ????? ??????? ???? ??? (F1 ) ? ?? ???????????? ????? ????? ?????? ????????.  ??? ???? ???? ??(F1 ) ??? ??? ?????? ??????? ? ??????. ( F3) ???? ????? ??? ??????????? ?????? ???? ?????????? (M 15 K) ???? ???? ???????? ? ????????? ???? ? ??? ?? ??????? ?????? ??????? ?????? ?????? ?? ??????? ? ??????? ??????? ?????? ? ?? ????? ????? ????? ?????? ???? (????????) ? ?? ???? ?? ??????? F3 ???? ????? ???? ?? ????? ????? ???????????? ?????? ??????? ?????? ?????? ?????.                         

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Publication Date
Sat Sep 25 2021
Journal Name
International Journal Of Drug Delivery Technology
Metal Complexes of Ligand Derived from Amine Compound: Formation, Spectral Characterization, and Biological Evaluation
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A new set of metal complexes by the general formula [M(C)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-chlorophenyl)succinamide] (C) derived from succinyl chloride with 4-Chloroaniline with the transition metal ions Mn(II), Co(II), Ni(II), Hg(II), Cu(II) and Cd(II). Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (C)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (C) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group) and the octahedral composition of these complexes is suggested. The anti-bacterial action of the compounds towards three types of bacteria

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Publication Date
Thu Oct 03 2024
Journal Name
Pharmacia
Synthesis and preliminary antimicrobial evaluation of new 7-amino-4-methyl-coumarin thiazolidinone conjugates
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Abstract As a part of our ongoing project on the design and synthesis of new 4-thiazolidinone derivatives with antimicrobial activity, four new 4-thiazolidinone derivatives carrying bromo, nitro, methyl, and chloro groups on the benzene ring were synthesized by starting with the 7-amino-4-methylcoumarin moiety, linking coumarin with various phenyl isothiocynate to form the thiourea group, and then cyclizing the derivatives, characterized by IR and 1HNMR, and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria and fungi. Overall, 2-(4-methyl-2-oxo-2H-chromen-3-yl)-3-(4-nitrophenyl) thiazolidin-4-one to be the most powerful individuals in the series. Based on the observed data, it can be sta

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Publication Date
Mon May 01 2023
Journal Name
Journal Of Medicinal And Chemical Sciences
Organic Synthesis of Some New Compounds Derived from Furfural and Their Evaluation as Antioxidants
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Heterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep

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Publication Date
Wed Dec 14 2016
Journal Name
Journal Of Baghdad College Of Dentistry
Physical and Histological Evaluation of Coated Implant with Nano ZrO2 after Creation Titania Nanotubes
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Background: Contact between implant material and bones must be strong and fast creation, to fulfill these properties appropriate surface modifications must apply on used implants. In this contribution; double surface modifications are applied on Ti-6Al-4V alloy to accelerate osseointegration. Materials and methods: Anodic process is utilized to create titania nanotubes (TNTs) on the screws made from Ti-6Al-4V alloy. These implants were coated with nano ZrO2 particles. Second modification was annealing anodized screws at 8000C, and implanted in tibiae of nine adult New Zealand white rabbits. Results: Physical and histological consequences of two surface modifications on Ti-6Al-4V alloy screws were studied. Scanning electron microscope (SEM)

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Publication Date
Sun Mar 13 2011
Journal Name
Baghdad Science Journal
Determination and evaluation of principal minerals in Negella sativa by atomic absorption technical methods
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Determination and evaluation of principal minerals in Negella sativa by atomic absorption technical methods were showed, using wet ashing method. This work was done on Negella sativa because of wide using of this plant in many formulations ( in food or medicine ).two types of atomic absorptions were used : first, flame atomic absorption spectroscopy, for minerals of high concentrations such as, Na, Mg, K, Fe, Ca, Li, Ni, Zn, Mn, Cu. Second, flameless atomic absorption spectroscopy, for minerals of low concentrations such as, Al, Si, V, B, Pb, Co, Cd, Cr ,Si, Hg, Sn .The results showed the existence of many minerals in Negella sativa useful to human sanity with acceptable dietary allowance. On other side, the presence of harmful m

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Publication Date
Sat Dec 10 2016
Journal Name
International Journal Of Current Microbiology And Applied Sciences
Synthesis, Characterization and Biological Evaluation of Penicillin Derivatives Complexes with Some Transition Metal Ions
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Publication Date
Fri Jun 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of serum levels Superoxide dismutase in women with polycystic ovarian syndrome and gingivitis
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Background: Polycystic ovary syndrome (PCOS) is the most common endocrine abnormality in women, there is an increasing evidence for an oxidative stress in PCOS that induce genomic and mitochondrial deoxyribonucleic acid damage that leads directly to reduced fertility. The objectives of this study are to assess and compare the periodontal health status by measuring clinical periodontal parameters (PLI, GI and BOP)as well as serum levels of superoxide dismutase at gingivitis ,gingivitis with PCOS and healthy periodontium groups, then correlate between clinical and biochemical parameters. Materials and Methods: 60 females with an age range between (25-40) years old had been tested and divided into3 groups ,the control group consists of (20) f

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Publication Date
Mon Dec 31 2012
Journal Name
Al-khwarizmi Engineering Journal
Evaluation Study of Glass Fiber Reinforced Polyester and Kevlar Reinforced Polyester by Taguchi Method
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     In the present investigation two different types of fiber reinforced polymer composites were prepared by hand lay-up method using three different parameters (curing temperature, pressing load and fiber volume fraction). These composites were prepared from the polyester resin as the matrix material reinforced with glass fibers as first group of samples and mat Kevlar fibers as the second group, both with different volume fractions (4%, 8%, and 12%) of fibers. They were then tested by tensile strength and impact strength. The main objective in this study is to use Taguchi method for predicting the better parameters that give the better tensile and impact strength to the composites, and then preparing composites at

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Publication Date
Sat May 01 2021
Journal Name
Journal Of Physics: Conference Series
Evaluation of Ceruloplasmin ferroxidase activity and lipid profiles in patients with Valvular heart diseases
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Abstract<p>One of the major health problems causing defects or damage to one or more of the four heart valves [aortic, mitral, pulmonary, and tricuspid] is valvular heart disease [VHD]; it occurs due to congenital abnormalities or acquired pathology. It is a defect that results in weak heart valves and is therefore unable to function as precise pathways of the blood. The aim of the current study was to evaluate the ferroxidase activity of ceruloplasmin (Cp) and the lipid profile of valvular heart disease patients in sera. Ninety subjects were included in this study and 60 patients with HDV were divided into two subgroups according to the affected valve: 33 patients with aortic valve disease (AV) and 27 patients</p> ... Show More
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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Design, Synthesis, Characterization and Comparative Cytotoxic Evaluation of bis-(2- mercaptoacetate) gold (III) chloride
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In recent years , the interest in gold (III) species have gained more and more attention for cancer chemotherapy , this was stimulating by the possibility to develop new agents with mode of action and clinical profile different from the established platinum metalodrugs.

With this frame, recently new square planar Au(III)  complexes (Au(L)(L')n); where L=SCH2COO- ; L'=HSCH2COO- had been synthesized with S/O – donor ligands.

In this article and by the aim to replace, one of (L') ligand by anion chloride ligand (which supposedly more relevant for the biodistribution of the compound than for its pharmacodynamic effects), new complex (Au(L')

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