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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 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
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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

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Sat Jun 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Using Some Robust Methods For Handling the Problem of Multicollinearity
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The multiple linear regression model is an important regression model that has attracted many researchers in different fields including applied mathematics, business, medicine, and social sciences , Linear regression models involving a large number of independent variables are poorly performing due to large variation and lead to inaccurate conclusions , One of the most important problems in the regression analysis is the multicollinearity Problem, which is considered one of the most important problems that has become known to many researchers  , As well as their effects on the multiple linear regression model, In addition to multicollinearity, the problem of outliers in data is one of the difficulties in constructing the reg

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Publication Date
Sun Feb 28 2021
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Administrative coordination between the Federal Ministry and the local government and its impact on municipal performance An applied study in the municipalities of Dhi Qar Governorate
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Mon Jan 01 2007
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Therapeutic evaluation of spironolactone and finasteride in the treatment of acne vulgaris
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Tue Mar 28 2017
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Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Antimicrobial Evaluation of New 6 and7 Substituted Derivatives of Coumarin
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A series of benzohydrazide derivatives attached to coumarin moiety at position 6 and 7 have been synthesized. The reaction of coumarin derivatives (coumarin I and II) with p-nitrophenyl hydrazine yield Schiff bases (compound1a and IIa).These Schiff bases were refluxed with benzoyl chloride to give benzohydrazide derivatives of coumarin substituted at its 6 or 7 nucleus position (Ia1 and IIa1).The reaction and the purity of the products were checked by thin layer chromatography (TLC). The structures of the final compounds  and  their intermediates were confirmed by their melting points, infra red spectroscopy, and elemental microanalysis(CHN).

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Publication Date
Sun Mar 01 2020
Journal Name
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Performance Evaluation of Trickling Filter and Extended Aeration of Wastewater Treatment Plants
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In recent decades, there has been increasing interest in wastewater treatment because of its direct impact on the environment and public health. Over time, other forms of treatment have been developed and modified, including extended aeration. This process is included in the suspended growth system. In this paper, a comparative study was conducted between the efficiency of the extended aeration plant and that of the trickling filter plant in removal of BOD and COD.  The method of comparison was done by knowing the value of the pollutant before and after the treatment and then extract the removal ratio of each pollutant within each plant. The results showed that the percentage of removal of BOD in the trickling filte

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Wed Mar 10 2021
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Evaluation of Hemolysis Activity of Zerumbone on RBCs and Brine Shrimp Toxicity
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Zerumbone is a well-known compound having anti-cancer, anti-ulcer, anti-inflammatory and anti-hyperglycemic effects. During its use for the disease treatment, the membrane of erythrocyte can be affected by consumption of this bioactive compound. The current study was the first report of investigation of the hemolytic activities on human erythrocytes and cytotoxic profile of zerumbone. The toxicity of zerumbone on human erythrocytes was determined by in vitro hemolytic assay. Brine shrimp lethality assay was used to evaluate the cytotoxic effect of zerumbone at concentrations 10, 100 and 1000 μg/mL. The human erythrocyte test showed no significant toxicity at low concentrations, whereas hemolytic effect was amplified up to 17.5

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Publication Date
Wed Mar 10 2021
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Evaluation of Hemolysis Activity of Zerumbone on RBCs and Brine Shrimp Toxicity
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Zerumbone is a well-known compound having anti-cancer, anti-ulcer, anti-inflammatory and anti-hyperglycemic effects. During its use for the disease treatment, the membrane of erythrocyte can be affected by consumption of this bioactive compound. The current study was the first report of investigation of the hemolytic activities on human erythrocytes and cytotoxic profile of zerumbone. The toxicity of zerumbone on human erythrocytes was determined by in vitro hemolytic assay. Brine shrimp lethality assay was used to evaluate the cytotoxic effect of zerumbone at concentrations 10, 100 and 1000 μg/mL. The human erythrocyte test showed no significant toxicity at low concentrations, whereas hemolytic effect was amplified up to 17.5 % at

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Publication Date
Sat Apr 23 2022
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Synthesis, and Antimicrobial Evaluation of New hydrazone Derivatives of (2,4-dinitrophenyl) hydrazine
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In this work, novel compounds of hydrazones derived from (2,4-dinitrophenyl) hydrazine were synthesized. Benzamides derivatives and sulfonamides derivatives were prepared from p-amino benzaldehyde. Then these compounds were condensed with (2,4-dinitrophenyl) hydrazine through Imine bond formation to give hydrazones compounds. The compounds were characterized using FT-IR (IR Affinity-1) spectrometer, and 1HNMR analyses. The majority of the compounds have a moderate antimicrobial activity against “Gram-positive bacteria staphylococcus Aureus, and staphylococcus epidermidis, Gram-negative bacteria Escherichia coli, and Klebsiella pneumoniae, and fungi species Candida albicans” using concentrations of 250 µg\ml.

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Publication Date
Fri Jul 01 2022
Journal Name
Iop Conference Series: Earth And Environmental Science
Computer Model Application for Sorting and Grading Citrus Aurantium Using Image Processing and Artificial Neural Network
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