Objective: The present study was aimed to develop a pH-triggered in situ gel for local release of lidocaine hydrochloride (lidocaine HCL) in the buccal cavity to improve the anesthetic effect of this amino amide drug which has very high water solubility. The formulations were introduced to the oral cavity as a spray to improve compliance and for easier administration.Methods: In this work, two grades of carbopol (934 and 940)-based in situ gel spray were designed. The formulations containing lidocaine HCl 5% were prepared by mixing different concentrations of carbopol with xanthan gum. Eight formulations were investigated and evaluated for gelation capacity, spray angle, volume of solution delivered per each actuation, rheological properties, and release kinetic model. Similarity factor (f2) was used for the comparison of dissolution profiles.Results: The prepared formulations undergo gelation after it had been actuated to the buccal cavity as a spray solution. The results showed that, as the concentration of polymer was increased, the release of drug decreased and the viscosity increased for both grades. The spray angle and volume of solution delivered per each actuation varied according to the composition of each formulation. The in situ gel containing 0.3% carbopol 934 and 0.2% xanthan gum regarded as a better candidate which had a good gelation and release property compared to other formulations. Drug release from optimized in situ gel spray followed Korsmeyer–Peppas model and was mediated by Fickian diffusion mechanism.Conclusion: Lidocaine HCl-loaded pH-sensitive in situ gel was successfully developed using carbopol 934 as polymer to be applied to the buccal cavity as spray solution for more effective anesthetic effect and painless treatment.
Five membered heterocyclics derivatives were synthesized in this work by three routes. The first route includes the synthesis of N-benzoic acid 1,2,3,-triazole derivatives (3),(4) by diazotation of methyl-2-amino benzoate and treating the resulted salt (1) with sodium azide and ethyl acetoacetate or acetyl acetone, respectively. In the second route, derivatives of pyrazole (8) pyrazolin-5-one (9), (10) were prepared by the reaction of the salt (1) with some active methylene compounds to give the corresponding hydrazones derivatives (5-7) which then they were treated with hydrazine hydrate. The third route afforded the synthesis of three derivatives (12), (15a), (15b) of thiazolidinone by two different methods. AII compounds were confirmed b
... Show MoreSeveral new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde
... Show MoreGelatin-grafted N- proflavine acryl amide was synthesized through two steps; firstly the Gelatin was grafted with acrylic acid free radically using Ammonium per-sulfate at 60℃, Then it was modified to its corresponding acyl chloride derivation, second step included the substitution with amino group of proflavine, in this research Gelatin was used as a natural nontoxic, water soluble polymer as a drug carrier. The prepared pro drug polymer was characterized by FTIR and 1H-NMR spectroscopies, Controlled drug release was studied in different pH values at 37℃. Many advantages were obtained comparing with other known methods.
New 2-amino thiazole ,oxodiazole, sulphonilamide and diazin derivatives of N-(α-chloro aceto)-3-(tolyl imino)-5-bromo-2-oxo-indole(2) have been synthesized .The preparation process started by the reaction of 5-bromo isatin with P-toluidine in the presence of glacial acetic acid and dimethylformamide(DMF) as a solvent to give 3-(tolyl imino)5-bromo-1H-indole-2-one.(1), Compound (1) with sodium hydride in dimethylformamide(DMF) at 0C0 gave a suspension of the sodium salt of Schiff base derivative and subsequent reaction with monochloroacetylchloride obtained the intermediate compound(2).Compound(2) was reacted with different reagents in four routes.The first route involved direct reaction with substituted 2-aminobenzothiazole u
... Show MoreTwo series of Schiff Bases [VI]n and thiazolidin-4-one derivatives[VII]n were synthesized by many steps starting from cyclization of 4- hydroxyacetophenon with thiourea in iodine to yield 1,3-thiazole compound which was reacted with pentoxy bromide in anhydrous potassium carbonate to converted compound[II] and this reacted with Phenol to yield azo compound[III]. The azo compound reacted with ethyl chloro acetate in basic medium to get a new easter compound[IV] which is converted to their acid hydrazid[V]. The later compound condensation with n-alkoxy benzaldehyde to give new Schiff bases[VI]n . Imine group undergoes addition cyclization with thioglycolic acid to get thiazolidinone compounds[VII]n .Also, two new series of Schiff Bases [XII]n
... Show MoreComplexes of Co(II),Ni(II),Cu(II) and Zn(II) with mixed ligands of phenylalanine (L) and tributylphosphine (TBPh) were prepared in aqueous ethanol with (2:1:1) (M:L:TBPh). The prepared complexes were characterized using flame atomic absorption,(C.H.N)Analysis, FT.IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. In addition biological activity of the phenylalanine and complexes against two selected type of bacteria were also examined. Some of the complexes exhibit good bacterial activities. From the obtained data the octahedral structure was suggested for all prepared complexes.
Copper (I) complex containing folic acid ligand was prepared and characterized on the basis of metal analyses, UV-VIS, FTIR spectroscopies and magnetic susceptibility. The density functional theory (DFT) as molecular modeling calculations was used to determine the donor atoms of folic acid ligand which appear clearly at oxygen atoms binding to hydrogen. Detection of donation sights is supported by theoretical parameters such as geometry, mulliken population, mulliken charge and HOMO-LUMO gap obtained by DFT calculations.
The need for wireless sensing technology has rapidly increased recently, specifically the usage of electromagnetic waves which becoming more required as a source of information. Silicon carbide (SiC) Nano particles has been used in this study, the material under test (MUT) was exposed directly to a microwave field to examine the electromagnetic behavior. The permittivity and permeability were investigated with different filler materials to approach best and optimal electromagnetic absorbing characteristics to assist engineers to monitor structure-based composite for defects evaluation that may occur during operation conditions or through manufacturing process. XRD, FESEM and both complex permittivity and permeability were measured f
... Show MoreABSTRACT. The reaction between benzil and hexamethylenediamine formed a new ligand [L], [(1Z,3Z)-2,3-diphenyl-5,6,7,8,9,10-hexahydro-1,4-diazecine], of the type [N2], was synthesized by the condensation reaction through Schiff base reaction between benzil and hexamethylenediamine. The new Schiff base ligand reacts with Mnп, Niп and Coп metal ions to give the complexes with the general formula: [M(L)Cl2]. The elemental investigations have been used to analyze the ligand and its complexes by CHN, FT-IR, UV-Vis, TLC, mass spectrum, melting point with the study of biological activity to the formed compounds. From the data obtained, the proposed molecular structure adopts square planar structure about the metal ions. The study reveals
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