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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 15 2023
Journal Name
Oncology And Radiotherapy
Synthesis, spectroscopic characterization, molecular docking, antioxidant and anticancer studies of some metal complexes from tetraazamacrocyclic Schiff base ligand
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Five novel nickel, iron, cobalt, copper, and mercury complexes were synthesized from tetraazamacrocyclic Schiff base ligand (L), which were derived from 3-(4-(dimethyl amino) benzylidene) pentane-2,4-dione and 1,2- diaminocyclohexane in a 2:2 molar ratio. Many physico-chemical and spectroscopic techniques, including melting point, 1HNMR, 13CNMR, elemental analysis, molar conductance, magnetic susceptibility, UV-Vis, FT-IR, and thermogravimetric analysis (TGA), were used to characterize the Schiff base ligand and all metal complexes. The octahedral geometry of all the complexes [MLCl2] is confirmed by spectroscopic analyses. All substances' biological properties, such as their in vitro antioxidant activity or level of free radical scavenging

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Publication Date
Wed Jun 03 2015
Journal Name
Baghdad
Synthesis, characterization and Antibacterial of 2, 3 Dihydrobenzo Thiazole -2- Carboxylic acid complexes with some selected Metal ions.
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Publication Date
Thu Aug 28 2014
Journal Name
Iraqi National Journal Of Chemistry The Editorial Board
The New C-2,C-3 Substituted Heterocyclic Derivatives of L-Ascorbic acid: Synthesis, Characterization, and Bacterial Activity
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New Schiff bases derivatives [IV]a-e is prepared via condensation of Derythroascorbic acid with p-substituted aldehydes in dry benzene. To obtain these derivatives, the 5,6-O-isopropylidene-L-ascorbic acid[I] was chosen as starting material, compound prepared from the reaction of L-ascorbic acid as starting material. Compound[I] was prepared from the reaction of L-ascorbic acid with dry acetone in the presence of hydrogen chloride. The esterification of hydroxyl groups at C-2 and C-3 positions with excess ofethyl α –chloroacetate in the presence of sodium acetate produce acorresebonding ester [II] , which was condensed with hydrazine hydrate to give new hydrazide [III] . The new Schiff bases [IV]a-e were synthesized by reaction of acid h

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Publication Date
Fri Sep 01 2023
Journal Name
International Journal Of Biological Macromolecules
Optimization and characterization of carrageenan/gelatin-based nanogel containing ginger essential oil enriched electrospun ethyl cellulose/casein nanofibers
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Publication Date
Wed Jul 01 2015
Journal Name
Advanced Powder Technology
Characterization of nano-silica prepared from local silica sand and its application in cement mortar using optimization technique
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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Global Pharma Technology
Preparation, Characterization and Biological Activity of New Derivatives of 3-Cyclic Oxazepine, 3-Cyclic Lactam and 3- Aminomethyl Imidazo (1, 2-a) Benzthiazol
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In this work a series of fourteen new compounds were synthesized. Compound [1] was formed from the reaction of 2-aminobenzothiazole and p-bromophenacyl bromide. Aldehyde group [2] was obtained from the reaction of compound [1] with pocl3 in presence of DMF and CHCl3 .After that shiff bases have been synthesized from the reaction of compound [2] with different aromatic amine to give new shiff bases [3- 5]. These new shiff bases have been reduced to their corresponding amine [6-8] by means of sodium borohydride. Then reaction of shiff bases [3-5] with phenyl isocyanate gives 3-cyclic lactam derivatives [9-11]. 3-cyclic Oxazepine derivatives [12-14] were obtained by reaction of shiff bases [3-5] with succinic anhydride. These new formed co

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Publication Date
Thu Mar 25 1993
Journal Name
كلية العلوم. / جامعة بغداد
ISOLATION AND CHARACTERIZATION OF EXTREMELY HALOPHILIC BACTERIA FROM SADDAM RIVER REGIONS AND THE RULE OF MEMBRANE PROTEINS IN THE RESISTANCE TO HIGH SALINITY
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This study included isolation and characterization of extremely halophilic bacteria from Al-Massab Al-Aam region in South of Iraq Fifty isolates were identified by using numerical taxonomy 40 strains belonged to the genus Halobacterium which inclucted Hb. halobium Hb. cutirubrum Hb. salinarium Hb. saccharovorum Hb. valismortis and Hb. volcanii. Ten strains belonged to the genus Halococcus which included Hc. morrhuae Hc. saccharolyticus. Growth curves were sensitive mutants determined for wild type and salt Generation time in logarthmic phase was measured and found to be (10.37 2hr 7 0.59) for Hb. salinarium / 18 (6.490 hr 0.24) for Hb. cutirubrum / 32, (6.700 hr + 0.488) for Hb. valismortis / 20, (11.243 hr + 0.96) for Hb. volcanii / 7. (7

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Publication Date
Wed Feb 01 2023
Journal Name
Baghdad Science Journal
Synthesis, characterization and bioactivity Study from azo – ligand derived frommethyl-2-amino benzoatewith some metal ions
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A Ligand (ECA) methyl 2-((1-cyano-2-ethoxy-2-oxoethyl)diazenyl)benzoate with metals of (Co2+, Ni2+, Cu2+) were prepared and characterization using H-NMR, atomic absorption spectroscopy, ultra violet (UV) visible, magnetic moments measurements, bioactivity, and Molar conductivity measurements in soluble ethanol. Complexes have been prepared using a general formula which was suggested as [M (ECA)2] Cl2, where M = (Cobalt(II), Nickel(II) and Copper(II), the geometry shape of the complexes is octahedral.

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Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Synthesis, Characterization and Antibacterial Activity of 1,4-di[ aminomethylene carboxyl] phenylene (H2L) and its Complexes Co(II), Cu (II), Zn(II) and Cd (II)
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Publication Date
Tue Jan 15 2008
Journal Name
Journal Of Kerbala University
Synthesis and Characterization of New Ligand type N2O2 and its complexes with (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) ions
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The [2-hydroxy-1, 2-diphynel-ethanone oxime] was reacted with 1, 2-dichloroethan to give the new ligand [H2L]. this ligand was reacted with some metal ions (Co (II), Ni (II), Cu (II), Zn (II) and Cd (II) in methanol as a solvent to give a series of new (1: 1) complexes of the general formula [M (HL)] Cl,(where: M= Co (II), Ni (II), Cu (II), Zn (II) and Cd (II)) are isolated All compounds have been characterized by spectroscopic methods [IR, UV-Vis] atomic absorption. Chloride content along with conductivity measurements. From the above data the proposed molecular structure for (Co, Cu, Ni, Zn and Cd) complexes adopting a tetrahedral structure