Background: Meclizine hydrochloride (MCZ) is an antihistamine that is used as an antiemetic to prevent and cure nausea and vomiting. Because of its limited water solubility and first-pass metabolism, it exhibits variable absorption. Objective: To formulate and evaluate MCZ as an intranasal in situ gel with increased residence time and permeability. Methods: We made an inclusion complex of MCZ using various cyclodextrins as a complexing agent to help the drug dissolve better. The complexes were studied, and the ones that were better at dissolving were chosen to be used in the creation of an in situ gel with poloxamer 407 (17–20% w/v) and hyaluronic acid (0.25–0.75% w/v). Prepared formulas were subjected to various evaluation tests, and the optimum formula was subjected to an ex vivo permeation study. Results: Hydroxypropyl-cyclodextrin (HP-CD) complexation increased the solubility of MCZ. A prepared complex (10 mg of MCZ) was used for nasal in situ gel preparation. Formula (F3) containing 17% poloxamer 407 and 0.75% hyaluronic acid exhibited favorable characteristics, including optimal gelation temperature (33.33°C), drug content (100.51%), gel strength (35.0 seconds), spreadability (4.2 cm), and 98.52% in vitro drug release over 5 hours in simulated nasal fluid (pH 6.8), and provided considerably high permeability. Conclusions: A mucoadhesive in situ gel formulation of MCZ (HP-β-CD) is a promising nasal formulation for the management of nausea and vomiting.
This study was carried out to prepare and characterize domperidone nanoparticles to enhance solubility and the release rate. Domperidone is practically insoluble in water and has low and an erratic bioavailability range from 13%-17%. The domperidone nanoparticles were prepared by solvent/antisolvent precipitation method at different polymer:drug ratios of 1:1 and 2:1 using different polymers and grades of poly vinyl pyrolidone, hydroxy propyl methyl cellulose and sodium carboxymethyl cellulose as stabilizers. The effect of polymer type, ratio of polymer:drug, solvent:antisolvent ratio, stirring rate and stirring time on the particle size, were investigated and found to have a significant (p? 0.05) effect on particle size. The best formul
... Show MoreFelodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Result
... Show MoreThe present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.
Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses
... Show MoreThe increasing requirement and use of dental implant treatments has rendered dental implantology indispensable in dentistry. The aim of this study is to determine the optimum concentration of calcium silicate to be incorporated into a polyetherketoneketone (PEKK) matrix used as an implant material to enhance the bioactivity and mechanical properties of the composite compared with unmodified PEKK. In this study, different weight percentage (wt%) of micro-calcium silicate (m-CS) is incorporated into PEKK with ethanol as a binder. Subsequently, the mixture is dried in a forced convection oven at 120°C and poured into customized molds to fabricate a bioactive composite via compression molding (310°C, 15 MPa, and 20 min holding time
... Show MoreIn this research four steps of the new derivatives of Naproxen drug have been made which are known as a high medicinal effectiveness; the first step involved converting Naproxen into the corresponding ester (A) by reaction Naproxen with methanol absolute in presence H2SO4. While the second step involved treatment methyl Naproxen ester (A) with hydrazine hydrate 80% in presence of ethanol .The third reaction requires synthesis of Schiff bases (C1-C10) by condensation. of Naproxen hydrazide (B) with many substituted aromatic aldehydes . Finally, the fourth step synthesized new tetrazole derivatives ( D1- D10) by the reaction of the prepared Schiff bases (in the third step) with Sodium azide in THF as a solvent .The prepared compounds wer
... Show MoreThe influence of annealing on quaternary compound Ag0.9Cu0.1InSe2 (ACIS) thin film is considered a striking semiconductor for second-generation solar cells. The film deposited by thermal evaporation with a thickness of about 700 nm at R.T and vacuum annealing at temperatures (373,473) K for 1 hour. It was deposited in a vacuum of 4.5*10-5 Torr on a glass substrate. From XRD and AFM analysis, it is evident that Ag0.9Cu0.1InSe2 films are polycrystalline in nature, having ideal stoichiometric composition. Structural analysis indicated that annealing the films following the deposition resulted in the increasing polycrystalline phase with the preferred orientation along (112) direction. , increasing crystallite size and average grain size
... Show More2(2-Tetrahydropyranylthio) methyl cyclopropyl amines were synthesized from allylmercaptan through several steps. The structures of the intermediates and the final products where confirmed through IR, NMR and elemental analysis, these compounds may be of value in the treatment of diseases where free radicals are implicated in their pathogensis, since the thio and the amino groups of the synthesized compounds may act as free radical scavengers.
This work involves synthesis of amides containing isoxazoline unit starting with
chalcone; 4-[3-(3‾-nitrophenyl)-2-propene- 1-one]-aniline[I]. 4-Aminoacetophenone was
reacted with 3-nitrobenzaldehyde in basic medium giving chalcone [I] by claisen-schemidt
reaction. The chalcone [I] was reacted with hydroxylamine hydrochloride giving isoxazoline
[II] in NaOH basic medium. The amides with structural formula [III]a-h were prepared by the
reaction of amino compounds ; isoxazoline [II] with different acid chlorides in dry pyridine
and using DMF as a solvent at 4
0
C. All the synthesized compounds have been characterized
by melting points , FTIR and
1
HMNR (of compound [III]a) spectroscopy.
Gold nanoparticles AuNPs have proven to be powerful tools in various nanomedicine applications, because of their photo-optical distinctiveness and biocompatibility. Noble metal gold nanoparticles was prepared by pulsed laser ablation method (1064-Nd: YAG with various Laser power from 200 to 800 mJ and 1 Hz frequency) in distil water. The process was characterized using UV-VIS absorption spectroscopy. Morphology and average size of nanoparticles were estimated using AFM and X-ray diffraction (XRD) analysis which show the nature of gold nanoparticles (AuNPs). Antibacterial activity of gold nanoparticles as a function of particles concentration against gram negative bacterium Escherichia coli and gram positive bacterial Staphylococcus aureu
... Show MoreCoumarin derivatives have shown different biological activities, such as antifungal, antibacterial antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr
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