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.
In this rescrch,new mixed ligand Schiff base complexes of Mn(II),Co(II),Ni(II),Cu(II), Cd(II), and Hg(II) are formulated from the Schiff base( L)resulting from o-phathalaldehyde(o-PA) with p-nitroaniline(p-NA)as a primary ligand and anthranilic acid as a subordinate ligand. Diagnosis of prepared Ligand and its complexes is done by spectral methods mass spectrometer;1H -NMR for ligand Schiff base FTIR, UV-Vis, molar conductance, elemental microanalyses, atomic absoption and magnetic susceptibility. The analytical studies for the all new complexes have shown octahedral geometries. The study of organicperformance of ligand Schiff base and its complexes show various activity agansit four type of bactria two gram (+) and two gram (-) .
The reaction of starting materials (L-asCl2):bis[O,O-2,3;O,O-5,6-(chloro(carboxylic) methylidene)]- -L-ascorbic acid] with glycine gives new product bis[O,O-2,3,O,O-5,6-(N,O-di carboxylic methylidene N-glycine)-L-ascorbic acid] (L-as-gly) which is isolated and characterized by, Mass spectrum UV-visible and Fourier transform infrared spectrophotometer (FT-IR) . The reaction of the (L-as-gly) with M+2; Co(II) Ni(II) Cu(II) and Zn(II) has been characterized by FT- IR , Uv-Visible , electrical conductivity, magnetic susceptibility methods and atomic absorption and molar ratio . The analysis showed that the ligand coordinate with metal ions through mono dentate carboxylic resulting in six-coordinated with Co(II) Ni(II) Cu(II) ions while with
... Show MoreOn the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.
Keywords: Coumarin-bas
... Show MoreThe agricultural activity has a great significance in the all four dimensions of sustainable development. Firstly, the economic dimension which it contributes with the GDP, as well as, it is considered as an important source to attract the investment. Secondly, the environmental dimension which also contributes with conserving of the biodiversity, combating the desertification, and increasing the farmlands. Thirdly, for its role in the social dimension to achieve the food security, to eradicate the poverty, and providing jobs. Fourthly, toward the institutional dimension as well it is considered as a source that allows all people to participate effectively, and to exchange of the local and universal experiences and perspectives. For conf
... Show MoreNew, simple and sensitive batch and reverse FIA spectrophotometric methods for the determination of doxycycline hyclate in pure form and in pharmaceutical preparations were proposed. These methods based on oxidative coupling reaction between doxycycline hyclate and 3-methylbenzothiazolinone-2-hydrazone hydrochloride (MBTH) in the presence ammonium ceric sulfate in acidic medium, to form green water-soluble dye that is stable and has a maximum absorbance at 626 nm. A calibration graph shows that a Beer's law is obeyed over the concentration range of 1-80 and 0.5-110 ?g.mL-1 of DCH for the batch and rFIA respectively with detection limit of 0.325 ?g.mL-1 of DCH for r-FIA methods. All different chemicals and physical experimental paramete
... Show MoreBackground: Bisphosphonates are potent inhibitors of osteoclastic bone resorption and widely used for the treatment of osteoporosis, and osteogenesis imperfecta in children. Clinical and experimental studies have demonstrated that Bisphosphonates delay or inhibit tooth eruption. This study tries to focus on the effect of bisphosphonate on teeth development and jaw bones growth. Materials and methods: The present study includes 65 neonatal rats during lactation period from 15 Albino Wister rats mother. Alendronate (one type of Bisphosphonates) was administrated orally (15 mg/kg) into 10 pregnant rats two times a week, while other 5 rats regard as control. Then the neonatal rats sacrificed in I, 6, 11, 16 and 21 days. The lower first molar we
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