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bijps-413
Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery
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The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of  inflammation and infections in colon).

Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

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Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization of Chlropheniramine maleate– Molecularly Imprinted Polymers and Their Application as Sensors for the Determination of the Drug in Some Pharmaceutical Preparations
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New chlropheniramine maleate (CPM) selective electrochemical membranes were prepared by using chlropheniramine maleate -molecularly imprinted polymers. MIP was prepared by bulk polymerization using 2-hydroxyethyl methacrylate (2-HEMA) as monomer, ethylene glycol dimethacrylate (EGDMA) as a cross-linker and a benzoyl peroxide (BPO) as an initiator at 600C.  Three CPM-MIP electrodes were constructed by using tri-tolyl Phosphate (ToCP), tris (2- ethyl hexyl) Phosphate (TEHP) and tributyl Phosphate (TBP) as plasticizers in PVC matrix.Electrode parameters including slopes, working concentrations ph. The interference effect in the presence of (Na+, Mg+2, Al+3, Glycine, Alanine, Arginine and Phenylalanine) was studied using the separated a

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Publication Date
Mon Jan 01 2018
Journal Name
Journal Of Pharmacy Research
Pulsatile drug delivery system - A review article
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Publication Date
Fri Dec 31 2021
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
SYNTHESIS AND CHARACTERIZATION OF NEW β-LACTAM DERIVATVE FROM SULFADIAZINE DRUG BY MANY STEPS: SYNTHESIS AND CHARACTERIZATION OF NEW β-LACTAM DERIVATVE FROM SULFADIAZINE DRUG BY MANY STEPS
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This research involved synthesis of new β-Lactam derivative from Azo compound[4-amino-N-(pyrimidine-2-yl)-3-(pyrimidine-2-yldiazenyl) benzene sulfonamide] (S1) record previously by many steps. Starting conversion the free amino group in an azo comp. to chloro acetamide derivative(S2), then reacted it with urea to give the oxazole ring  derivative (S3) that which containing free amino group. The condensation reaction between the amino group and P-bromobenzaldehyde to produce Shiff base (B14). Finally staudinger's cyclo addition reaction go run between the Shiff base derivative (B14) and chloro acetyl chloride in the presence of tri ethyl amine (Et3N) as Base catalyst and dioxane a

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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
Sat Jun 30 2012
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Effect of Annealing on the Crystallization of Poly Vinyl Chloride for Drug Delivery System
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Poly vinyl alcohol has been studied for its ability to form crystallites by using annealing method. Semicrystalline films of poly vinyl alcohol (PVA) were prepared by casting 11.5 wt. % and 13 wt. % PVA aqueous solution onto glass slides at annealing temperature range 90 -120°C and duration time 15- 60 minute. This allowed the macromolecules to form crystallites, small regions of folded and compacted chains separated by amorphous regions where single PVA chain may pass through several of these crystallites. Degree of crystallinity of PVA films (hydrogels) was determined by method of density; on the other hand the swelling behavior was conducted by the determination of water uptake, wet degree of crystallinity, gel fraction and solubilit

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Publication Date
Sun Sep 06 2015
Journal Name
Baghdad Science Journal
Methionine as a Spacer between Poly Acrylic acid and Ampicillin
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In this work a novel drug delivery system through modification of poly acrylic acid with Methionine as a spacer between the poly acrylic acid which was converted to its acyl chloride and reacted with Methionine as spacer unit which has been reacted with Ampicillin drug. In vitro drug release study had been conducted successfully in basic medium in pH 7.4 and acidic medium in pH 1.1 at 37?. Due to many problems associated with drug release and, this modification could decrease the side effect of drug. The prepared prodrug polymer was characterized by spectra method [FTIR and 1H?NMR]. Physical properties and intrinsic viscosity of drug polymer were determined. The good results were obtained in the presence of spacer unit with compar

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Publication Date
Fri Jul 01 2022
Journal Name
Journal Of Molecular Structure
Interaction behavior of curcumin encapsulated onto functionalized SBA-15 as an efficient carrier and release in drug delivery
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In this work, mesoporous silica SBA-15 was prepared and functionalized with amine groups (i.e., NH2) to form NH2/SBA-15. The curcumin (CUR) was encapsulated into the surface and pore of NH2/SBA-15 to create CUR@NH2/SBA-15 as an efficient carrier in drug delivery systems (DDSs). The three samples (i.e., SBA-15, NH2/SBA-15, and CUR@NH2/SBA-15) were characterized. The study investigated the effect of the carrier dose, initial CUR concentration, pH, and contact time on the CUR loading efficiency (DLE%) via adsorption. The best DLE% for the SBA-15 and NH2/SBA-15 were found to be 45% and 89.7%, respectively. The Langmuir isotherm had a greater correlation coefficient (R2) of 0.998 for SBA-15. A pseudo-secondorder kinetic model seemed to fit well

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Publication Date
Sun Oct 31 2021
Journal Name
Research Journal Of Pharmacy And Technology
A Review on Film Forming Drug Delivery Systems
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Conventional dosage forms for topical and transdermal drug delivery have several disadvantages related mainly to its poor skin permeation and patient compliance. Many approaches have been developed to improve these dosage forms. Film forming drug delivery systems represents a recent advancement in this field. It provides improved patient compliance with enhanced skin permeation of drugs. In its simplest form, these consist of a polymeric solution, usually in a supersaturated state, in a suitable solvent. A plasticizer is usually added to improve the flexibility and enhance the tensile strength to the film. It is also possible to control and sustain the drug release from the films by controlling the polymeric content, concentration o

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Publication Date
Sat Jun 08 2024
Journal Name
Karbala International Journal Of Modern Science
Designing of Human Serum Albumin Nanoparticles for Drug Delivery: a Potential Use of Anticancer Treatment
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Human serum albumin (HSA) nanoparticles have been widely used as versatile drug delivery systems for improving the efficiency and pharmaceutical properties of drugs. The present study aimed to design HSA nanoparticle encapsulated with the hydrophobic anticancer pyridine derivative (2-((2-([1,1'-biphenyl]-4-yl)imidazo[1,2-a]pyrimidin-3-yl)methylene)hydrazine-1-carbothioamide (BIPHC)). The synthesis of HSA-BIPHC nanoparticles was achieved using a desolvation process. Atomic force microscopy (AFM) analysis showed the average size of HSA-BIPHC nanoparticles was 80.21 nm. The percentages of entrapment efficacy, loading capacity and production yield were 98.11%, 9.77% and 91.29%, respectively. An In vitro release study revealed that HSA-BIPHC nan

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Publication Date
Tue Oct 22 2019
Journal Name
Scientia Pharmaceutica
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc

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