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Formulation and Characterization of Isradipine Nanoparticle for Dissolution Enhancement
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Isradipine belong to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is  used in the treatment of hypertension, angina pectoris, in addition to Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, therefore, oral bio-availability will be approximately15 to 24 %.

 

 The aim of this study was to formulate and optimize a stable  nanoparticles of a highly hydrophobic drug, isradipine by anti-solvent microprecipitation Method to achieve the higher in vitro dissolution rate, so that it will be absorbed by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism  and improve drug bioavailability.

 

Twenty one formulas of Isradipine nanoparticles were prepared by antisolvent precipitation method utilizing one of these polymers (Poloxamer 188, PVP-k30, HPMC E5, PVA, Poloxamer 407, and Soluplus) at different drugs: polymer ratios. The polymer type, the drug to polymer ratio, ultrasonication power and the effect of addition of co-stabilizer on the particle size, and polydispersity index (PDI)  were investigated.

 

Among all the prepared nanoparticles formulas, formula (F9) which contain Soluplus as a stabilizer at polymer: drug ratio of (1:0.75) and solvent: antisolvent ratio of (1:9) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 10 times than that of the pure drug. The investigations of the drug–excipients compatibility studies by FTIR and DSC, crystalline state by P-XRD, surface morphology by SEM were done. 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 dissolution rate of Isradipine was significantly increased through particle size reduction to nanosize.

 

 

 

 

 

 

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Publication Date
Wed Nov 01 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization, and Preliminary Evaluation of Antimicrobial activity of Imines derived from Vanillic Acid Conjugated to Heterocyclic
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The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (

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Publication Date
Mon Jan 17 2011
Journal Name
مجلة كلية التربية
Synthesis and Characterization of Complexes of [(N,N- -Bis(2- Hydroxy Ethyl) Glycine] with Some Metal Salts
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Some transition metal ions (Cr +3, Co+2 , Ni+2,Cu+2, Zn+2,Ag + ,Cd+2 ) complexes of [(N, N- - Bis(2- hydroxy ethyl) Glycine] (Bicine) have been synthesized and characterized by FTIR ,UV-Visble spectroscopy, atomic absorption, magnetic susceptibility, conductivity measurements and study of the nature of the complexes formed in ethanolic solution following the moleratio method. From the results obtained the following general formola have been given for the prepared complexes [M m+ (Bicine)n]. XH2O

Publication Date
Wed Nov 01 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization, and Preliminary Evaluation of Antimicrobial activity of Imines derived from Vanillic Acid Conjugated to Heterocyclic
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The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by

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Publication Date
Thu Jan 22 2015
Journal Name
مجلة التربية الاساسية
Synthesis and Characterization of Some New Heterocyclic Compounds Via Unsaturated Ketone with Evaluating of Their biological Activity
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Publication Date
Tue Mar 01 2022
Journal Name
Jordan Journal Of Biological Sciences
Characterization, Biofilm and Plasmid Curing Effect of Silver Nanoparticles Synthesis by Aqueous Extract of Myristica fragrans Seeds
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Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization of New Sulfamethoxazole Derivatives containing β-lactam Ring and Preliminary Evaluation of their Antimicrobial Activity
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Sulfamethoxazole (SMX) is the most significant antibiotic in the sulfonamide family. It was chosen as the representative of this category because of its widespread use. Starting with sulfamethoxazole, a new series of 2-Azetidinone (M1-M6) was synthesized, the structure of these new derivatives was confirmed using spectral methods, starting with the synthesis of Schiff’s bases by reflux of different aromatic benzaldehydes, separately, with Sulfamethoxazole in ethanol with few drops of acetic acid. The final compounds were obtained by ketene-imine synthesis of β-lactam using chloroacetyl chloride. The designed chemicals’ synthesis has been completed successfully. Physical parameters (melting points and Rf values), Fourier transfo

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Publication Date
Sat Jan 01 2011
Journal Name
Carbohydrate Polymers
Synthesis, characterization of acrylamide grafted chitosan and its use in removal of copper(II) ions from water
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Publication Date
Sat Sep 08 2018
Journal Name
International Journal Of Applied Pharmaceutics
PREPARATION AND CHARACTERIZATION OF LAFUTIDINE AS IMMEDIATE RELEASE ORAL STRIP USING DIFFERENT TYPE OF WATER-SOLUBLE POLYMER
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Objective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citri

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Publication Date
Thu Oct 19 2023
Journal Name
Journal Of Optics
Production and characterization of porous silicon via laser-assisted etching as photodetector: effect of different HF concentrations
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Publication Date
Sun Oct 15 2023
Journal Name
Bionatura
Synthesis, Characterization and Evaluation of the Biological Activity of Some New Thiazolidine Derivatives Derived from Schiff bases
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In this research, new compounds were synthesized via the reaction of dichloroacetic acid with two moles of piperidine. The novel acid 1 was converted to its ester 2. Acid hydrizide 3 was prepared by the reaction of hydrazine hydrate with new ester 2, which was later used to prepare derivatives of Schiff bases 4-13. In the last step, Schiff bases and thioglycolic acid were reacted to give thiazolidine derivatives 14-23. All these compounds were diagnosed using melting points, FTIR, 1HNMR and mass spectroscopy. Scheme 1 shows all the synthesized compounds' reaction steps and structures. Keywords: Thiazolidine; Schiff bases; biological activity; piperidine; dichloroacetic acid.

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