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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
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Isolation and Characterization of Iridoid Glycoside (Gardenoside) Present in the Leaves of Gardenia jasminoides J.Ellis Cultivated in Iraq
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Iridoid glycosides are a group of naturally occurring chemical compounds. They are a large family of compounds biosynthesized by plants, they often have pharmacological effects. The aim of this study is to isolate and identified iridoid glycoside in a newly studied, cultivated in Iraq named Gardenis jasminoides. The medicinal importance of iridoid glycoside, on one hand and absence of phytochemical investigation on leaves of Gardenia on the other hand, acquired this study its importance. Many compounds were isolated from leaves plant part one of these compounds was identified by different chemical analysis like: melting point (MP), thin layer chromatography (TLC), Fourier transforms infrared spectra (FTIR) and high performance l

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Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New 2-amino-5-chlorobenzothiazole Derivatives Containing Different Types of Heterocyclic as Antifungal Activity
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Nine new compounds of 2-amino-5-chlorobenzothiazole derivatives were synthesized. These new compounds were formed through the reaction of 2-amino-5-chlorobenzothiazole 1 with ethyl chloroacetate and KOH, which gave an ester derivative 2, followed by refluxing compound 2 with hydrazine hydrate to afford hydrazide derivative 3. The reaction of compound 3 with CS2 and KOH gave 1,3,4-oxadiazole-2-thiol derivative 4, and then the reaction of compound 2 with thiosemicarbazide to produce compound 5  then treated it with 4%NaOH led to ring closure to provide 1,2,4-triazole-3-thiol derivative

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Publication Date
Wed Jun 26 2019
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical Sciences
Synthesis, Characterization Antimicrobial Activities Studies Of Mixed-Ligand Complexes Of Curcumin And Anthranilic Acid With Bivalent Metals Chlorides
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Publication Date
Sat Oct 01 2022
Journal Name
Inorganic Chemistry Communications
Synthesis, characterization, and bioactivity of several metal complexes of (4-Amino-N-(5-methyl-isaxazol-3-yl)-benzenesulfonamide)
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Publication Date
Fri Jun 28 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Synthesis, Characterization, Molecular Docking, ADMET Study, and Antimicrobial Evaluation of New Mannich Bases of Isatin–Thiazole Imine Bases
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Background: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted o

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Publication Date
Sun Feb 01 2026
Journal Name
Journal Of Molecular Structure
Biosynthesis, characterization, antimicrobial and adsorbent effects of γ-aluminum oxide-NPs using aqueous extract of boswellia carterii resin
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γ-Al2O3–NPs were synthesized by a green synthesis process based on Boswellia carterii resin extract and aluminum sulphate in an alkaline medium. Boswellia carterii resin extract is a significant reducing and stabilizing agent for synthesizing γ-Al2O3–NPs.Several techniques, including Fourier–transform infrared (FT-IR), UV–visible spectroscopy, x-ray diffraction, electron microscopy (XRD), energy dispersive x-ray (EDX), scanning electron microscopy (SEM), Transmission electron microscopy (TEM), and atomic force microscopy (AFM), were utilized to investigate the final product. XRD and SEM confirmed a plate-like crystalline structure with an average size of 17.5 nm. FT-IR analysis identified aluminum oxide stretching vibrations (655,

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Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Bioactivity Study of Few Metal Complexes of Curcumin with 2-(1H-Benzimidazol-2-yl) Aniline
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We have synthesized many metal (II) complexes using curcumin L1 as the major ligand and 2-(1H-Benzimidazol-2-yl) aniline L2 as a supporting ligand. The complexes were characterized by spectroscopy methods such as; molar conductivity, elements microanalysis, Fourier-transform spectroscopy (FT-IR), UV-vis, and mass spectroscopy. Both curcumin ligands and L2 were found to be capable of binding to M(II) and metal ions via their two N atoms, according to the data. The formula for the complexes is the same. [M (L1)(L2)H2OCl], where M is Ni(II), Co(II), Cu(II), Cd(II), and Hg(II) (II). Octahedral complexes are proposed for the prepared compounds. The bio-actives suggested that the complexes are effective against bacteria and fungus on a mi

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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Medicinal And Chemical Sciences
Synthesis and Characterization with Antimicrobial Studies of mixed Curcumin Schiff Base–L-dopa with Divalent Cations Complexes
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In the present article, mixed ligand metal (II) complexes have been synthesized with Schiff base (1E, 5Z, 6E)-1,7 bis (4-hydroxy-3- methoxyphenyl)-5-(3-hydroxyphenyl) imino) hepta-1,6-dien-3-one derived from Curcumin and 3-aminophenol as primary ligand and L-dopa as a secondary ligand. The Schiff base act as bidentate and arrange to the metals through the azomethine (C=N) nitrogen and (C=O) oxygen atom. The mode of bonding of the Schiff base has been affirmed on the infrared by the UV-Visible, 1H, and 13C NMR spectroscopic techniques. The magnetic susceptibility and the UV-Vis data of the complexes propose octahedral geometry around the central metal ion. The information appears that the complexes have the structure of [L-M-(L-dopa)] system

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Publication Date
Wed Jan 17 2018
Journal Name
Journal Of Engineering And Applied Sciences
PREPARATION, CHARACTERIZATION AND THERMAL ANALYSIS OF POLYMERIC BLEND NANOCOMPOSITES BASED ON PVA-PVPPEGDOPED WITH ZINC OXIDE NANOPARTICLES
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Publication Date
Thu Jun 08 2017
Journal Name
International Journal Of Applied Chemistry
Synthesis and characterization of some New Oxazepine Compounds Containing 1,3,4-Thiadiazole Ring Derived form D-Erythroascorbic Acid
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This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in dry pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [2-amino-5-mercapato-1,3,4-thiadiazole] was prepared through the reaction of thiosemicarbazide with carbon disulphide (CS2) in entity of anhydrous (Na2CO3) in (abs. ethanol ). Compound (VI) [2-(5-mercapto-1,3,4-thiadiaz

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